Nattha Kaewnopparat - Academia.edu (original) (raw)
Papers by Nattha Kaewnopparat
The objective of this study was to develop vaginal suppository containing lactobacillus. Four kin... more The objective of this study was to develop vaginal suppository containing lactobacillus. Four kinds of vaginal suppositories containing Lactobacillus paracasei HL32 were formulated: 1) a conventional suppository with Witepsol H-15 as a base, 2) a conventional suppository with mixed polyethylene glycols (PEGs) as a base, 3) a hollow-type suppository with Witepsol H-15 as a base and 4) a hollow-type suppository with mixed PEGs as a base. The release studies demonstrated that the hollow-type suppository with mixed PEGs as the base gave the highest release of L. paracasei HL32 and was microbiological stable after storage at 2- 8°C over the period of 3 months.
Solid dispersions (SD) of curcuminpolyvinylpyrrolidone in the ratio of 1:2, 1:4, 1:5, 1:6, and 1:... more Solid dispersions (SD) of curcuminpolyvinylpyrrolidone in the ratio of 1:2, 1:4, 1:5, 1:6, and 1:8 were prepared in an attempt to increase the solubility and dissolution. Solubility, dissolution, powder X-ray diffraction (XRD), differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR) of solid dispersions, physical mixtures (PM) and curcumin were evaluated. Both solubility and dissolution of curcumin solid dispersions were significantly greater than those observed for physical mixtures and intact curcumin. The powder X-ray diffractograms indicated that the amorphous curcumin was obtained from all solid dispersions. It was found that the optimum weight ratio for curcumin:PVP K-30 is 1:6. The 1:6 solid dispersion still in the amorphous from after storage at ambient temperature for 2 years and the dissolution profile did not significantly different from freshly prepared.
Food Chemistry, 2022
Curcuminoids are known to exert diverse pharmacological effects and used in some pharmaceutical f... more Curcuminoids are known to exert diverse pharmacological effects and used in some pharmaceutical formulations. This study describes the preparation, characterization, and enhancement in the solubility and anticancer activity of a curcuminoids-rich extract (CRE) using a ternary inclusion complex system. CRE containing 88.9% w/w curcuminoids was prepared using a 'green' microwave extraction coupled with fractionation on a column of hydrophobic adsorbent resin. The ternary complex consisting of CRE, hydroxylpropyl-β-cyclodextrin and polyvinylpyrrolidone K30 was prepared using the solvent evaporation method and thoroughly characterized using Fourier-transform infrared spectroscopy, powder X-ray diffractograms, differential scanning calorimetry and scanning electron microscopy. The ternary complex of CRE improved the water-solubility of curcuminoids (up to 70.3 µg/mL) as well as the dissolution rate when compared to those of CRE (0 µg/mL). In addition, the ternary complex exhibited significantly stronger anticancer activity against human lung adenocarcinoma (A-549), human cervical adenocarcinoma (HeLa) and human colon adenocarcinoma (HT-29) cell lines than CRE.
International journal of pharmaceutical compounding, 2018
Vetiveria zizanioides (vetiver) contains viscous volatile oil, which has the ability to repel mos... more Vetiveria zizanioides (vetiver) contains viscous volatile oil, which has the ability to repel mosquitoes similar to citronella oil, a well-known mosquito repellent in tropical countries, like Thailand. The objectives of the current study were to formulate the stable oil-in-water vetiver oil lotions using Simulgel FL as a liquid emulsifier, to investigate the physicochemical properties of the prepared lotions and to evaluate the in vitro release characteristics of the stable vetiver oil lotions. In this work, the concentrations of Simulgel FL ranged from 1% to 3% weight in weight, whereas the concentrations of vetiver oil were varied: 2.5%, 5%, and 10% weight in weight. The suitable concentration of Simulgel FL was found to be 3% weight in weight. For comparison purposes, oil-in-water citronella oil lotions (10% weightin- weight citronella oil) were also prepared with similar ingredients. A mixture of vetiver oil and citronella oil (1:1 by weight) was also used as an active ingredien...
Excessive and daily inhalation of talcum, a main ingredient of face powders, causes pulmonary tal... more Excessive and daily inhalation of talcum, a main ingredient of face powders, causes pulmonary talcosis, which has led to the replacement of talcum with safer natural ingredients. RiceSorb®, or Oryza sativa starch from Japanese rice, was used as an alternative owing to its nontoxic and excellent oil absorption capacity. The objectives of the present work were to formulate loose face powders from RiceSorb® and to investigate the physicochemical properties of the prepared formulations. Five formulations of loose face powders were prepared by varying the ratios between talcum and RiceSorb®: 4:0 (FT0), 3:1 (FT1), 1:1 (FT2), 1:3 (FT3), and 0:4 (FT4). The physicochemical properties were evaluated mainly based on USP 41 and NF 36 such as morphology by using a scanning electron microscope, bulk density, flow property (angle of repose), moisture content (MC), and pH. The stability of the formulations were also performed at ambient temperature and 45°C for 2 months. The formulations had pH 6.9...
MATTER: International Journal of Science and Technology, 2019
The fruit pulp extracts of Tamarindus indica have been reported to possess several biological act... more The fruit pulp extracts of Tamarindus indica have been reported to possess several biological activities, especially antioxidant property which is suitable for cosmetic application. Therefore, the aims of this study were to formulate the tamarind fruit pulp extract loaded lotions (o/w emulsions), and to assess the antioxidant activity of tamarind fruit pulp extract loaded lotions. Initially, tamarind fruit pulp extracts were prepared by a solvent extraction method. The solvents used were water or a mixture of water and ethanol (water: ethanol= 1:1). Afterwards, the obtained tamarind fruit pulp extracts were subjected to lyophilization process. The tamarind fruit pulp extracts were tested for antioxidant activity by 2, 2-diphenyl-1-picrylhydrazyl (DPPH) assay to determine suitable concentrations of the extracts to be incorporated into the lotions, which were 2 and 4%w/w in the current study. Apart from the basic ingredients of the oil phase and water phase, ViscOptima SE (2%w/w) was selected as an emulsifier and a thickener of the formulations. The tamarind fruit pulp extract loaded lotions were characterized for physicochemical property and antioxidant potential. The freshly prepared tamarind fruit pulp extract loaded lotions were light brown with homogeneity and no phase separation was observed after centrifugation at 3,000 rpm for 30 min. They had weak acidic pH (4.4-5.1), considered acceptable for skin application. The loaded formulations (F1, 2%w/w) and F2, 4%w/w)) exhibited significantly higher conductivity values than that of the unloaded formulation (F0) (p<0.05). The formulations behaved as pseudoplastic flows with low viscosity. The DPPH measurement revealed that the formulations F1 and F2 had potential antioxidant activity. In conclusion, topical o/w lotions containing tamarind fruit pulp extract were successfully prepared. They had substantial antioxidant activities. As a result, tamarind fruit pulp extract loaded lotions displayed a potential use in cosmetic formulations, especially antiaging products.
International Journal of Pharmaceutics, 1999
Solid dispersions of piroxicam were prepared with polyvinylpyrrolidone (PVP) K-17 PF and PVP K-90... more Solid dispersions of piroxicam were prepared with polyvinylpyrrolidone (PVP) K-17 PF and PVP K-90 by solvent method. The physical state and drug:PVP interaction of solid dispersions and physical mixtures were characterized by X-ray diffraction, Fourier transform infrared (FTIR) spectroscopy and differential scanning calorimetry (DSC). FTIR analysis demonstrated the presence of intermolecular hydrogen bonding between piroxicam and PVP in solid dispersions. These interactions reflected the changes in crystalline structures of piroxicam. The amorphousness within the PVP moeity might be predicted in piroxicam dispersions by the disappearance of N-H or O-H peak of piroxicam. Dissolution studies indicated a significant increase in dissolution of piroxicam when dispersed in PVP. The better results were obtained with the lower molecular weight PVP K-17 than with higher molecular weight PVP K-90. The non-amorphous solid dispersions in PVP K-17 showed almost equally fast dissolution rates to amorphous dispersions in PVP K-90. The mechanism of dissolution of solid dispersion in PVP K-90 is predominantly diffusion-controlled due to the very high viscosity of PVP K-90. Dissolution was maximum with the amorphous solid dispersions containing drug:PVP K-17 1:5 and 1:6 which showed a 40-fold increase in dissolution in 5 min as compared with pure drug.
AIMS Microbiology, 2017
Encapsulation may protect viable probiotic cells. This study aims at the evaluation of a bambara ... more Encapsulation may protect viable probiotic cells. This study aims at the evaluation of a bambara groundnut protein isolate (BGPI)-alginate matrix designed for encapsulating a probiotic Lactobacillus rhamnosus GG. The response surface methodology was employed to gain the optimal concentrations of BGPI and alginate on encapsulation efficiency and survival of encapsulated cells. The capsules were prepared at the optimal combination by the traditional extrusion method composed of 8.66% w/v BGPI and 1.85% w/v alginate. The encapsulation efficiency was 97.24%, whereas the survival rates in an acidic condition and after the freeze-drying process were 95.56% and 95.20%, respectively-higher than those using either BGPI or alginate as the encapsulating agent individually. The designed capsules increased the probiotic L. rhamnosus GG survival relative to free cells in a simulated gastric fluid by 5.00 log cfu/ml after 3 h and in a simulated intestinal fluid by 8.06 log cfu/ml after 4 h. The shelf-life studies of the capsules over 6 months at 4 °C and 30 °C indicated that the remaining number of viable cells in a BGPI-alginate capsule was significantly higher than that of free cells in both temperatures. It was demonstrated that the BGPI-alginate capsule could be utilized as a new probiotic carrier for enhanced gastrointestinal transit and storage applied in food and/or pharmaceutical products.
International Journal of Food Science & Technology, 2016
Four legume water extracts, that is bambara groundnut, soya bean, red kidney bean and black bean ... more Four legume water extracts, that is bambara groundnut, soya bean, red kidney bean and black bean as well as skim milk, were examined for their effectiveness in protecting Lactobacillus rhamnosus GG and Lactobacillus fermentum SK5 during the freeze-drying and storage. Bambara groundnut water extract (BGWE) showed promising cryoprotective activity that was comparable to skim milk. BGWE and skim milk at 2-10% w/v and 5-20% w/v individually produced survival rates for both strains of 87-88%. To further optimise the synergistic cryoprotective medium, response surface methodology was employed. The optimal combination was 4.93% w/v BGWE and 11.68% w/v skim milk for L. rhamnosus GG and 5.17% w/v BGWE and 11.36% w/v skim milk for L. fermentum SK5 with survival rates of 95.17% and 94.36%, respectively. The storage life of freeze-dried cells of both probiotics at 4°C and 30°C for 6 months was markedly improved when they were produced with these optimal combinations.
Journal of Drug Delivery Science and Technology, 2011
Tramadol rectal gel preparations were developed using poloxamer or hydroxyethylcellulose as a gel... more Tramadol rectal gel preparations were developed using poloxamer or hydroxyethylcellulose as a gel base. The tramadol rectal gel using poloxamer has a gel point at 36 °C and was more bioadhesive (65.5 ± 2.4 x 10 2 dyne/cm 2) to the rectal mucous membrane than was the gel with the hydroxyethylcellulose base (37.4 ± 2.2 x 10 2 dyne/cm 2) with the gel strength of 87 ± 2 and 70 ± 2 s, respectively. All rectal gel formulations were colorless, clear, viscous liquid with a pH range of 6.65-7.13. In an in vitro release study, the release profiles of the drug from both rectal gels were similar and the cumulative amount of drug release was about 97 and 98 % in 5 h for the mucoadhesive gel and thermoreversible gel, respectively. Analysis of the release kinetics revealed that the drug might be released from the rectal gels by non-Fickian diffusion. In an in vivo analgesic study, administration of tramadol (0.25, 0.5, and 1.0 mg) rectal gel using poloxamer as the gel base, exerted a marked increase in the latency of the nociceptive response in mice. Similar results were also observed when using hydroxyethylcellulose as the base. These results indicated that tramadol rectal gels prepared using poloxamer or hydroxyethylcellulose as a gel base showed a complete release of the drug from the bases, as well as prolonging the latency of a nociceptive response in experimental animals.
Human vagina represents a dynamic ecosystem dominated by certain species of Lactobacillus. This m... more Human vagina represents a dynamic ecosystem dominated by certain species of Lactobacillus. This microorganism restricts the growth of pathogens by using properties of steric exclusion and inhibitory substance production. Serious complications including bacterial vaginosis and vaginal cancer are often determined in women with reduced numbers of lactobacilli. Local application of Lactobacillus is consequently promising to keep the vagina colonized by this strain, which consequently reduces the infections. In the present work, two vaginal formulations, e.g. effervescent tablet and PEG-based suppository, containing Lactobacillus were prepared. The hollow type PEG-based suppository was satisfied according to physical and biological characterizations. The lactobacilli inoculated had released from the formulation within 30 minutes. More than 90% of the bacteria released were viable and remained demonstrating good adherence to HeLa cells. Moreover, the abilities on bacteriocin and H 2 O 2 productions were not deteriorated by the suppository manipulation. ©All right reserved.
International journal of pharmaceutical compounding
The objective of this study was to develop a rapid-release diazepam suppository. Four kinds of di... more The objective of this study was to develop a rapid-release diazepam suppository. Four kinds of diazepam suppositories were formulated: (1) a conventional suppository with Witepsol H-15 as a base, (2) a conventional suppository with mixed polyethylene glycols as a base, (3) a hollow-type suppository with Witepsol H-15 as a base that contained diazepam solution in its cavity and (4) a hollow-type suppository with Witepsol H-15 as a base that contained diazepam powder in its cavity. The result of the differential scanning calorimetry thermograms indicated that diazepam dissolved in Witepsol base had a strong affinity to the lipophiic base while diazepam dispersed in polyethylene glycol base was still in the crystalline form. The release study of prepared suppositories showed that the release of diazepam from suppository 1 and suppository 4 was very slow. The diazepam released from suppository 2 after 5 minutes was about 30%. The diazepam released from suppository 3 after 5 minutes was ...
Die Pharmazie, 2001
The stabilities of X-ray amorphous solid dispersions of piroxicam and polyvinylpyrrolidone (PVP) ... more The stabilities of X-ray amorphous solid dispersions of piroxicam and polyvinylpyrrolidone (PVP) K-17 and PVP K-30 (1:5 and 1:4), respectively, were investigated after storage for 12 months. X-ray diffraction showed that in the aged solid dispersions piroxicam remained in the amorphous state. Fourier transform infrared (FTIR) spectroscopy indicated that the interactions between drug and PVP in aged solid dispersions are similar to those in freshly prepared samples. The dissolution rates of the X-ray amorphous solid dispersions during storage for 12 months at 45 degrees C and ambient temperature were examined. Very minor decreases in dissolution rates of aged solid dispersions were found which might be due to the coarsening of the particles. Dissolutions of these amorphous solid dispersions after aging for 12 months still showed an about 40-fold increase in dissolution in 5 min compared to pure drug.
Asian Biomedicine, 2011
Background: Tramadol is a centrally acting analgesic drug. Rectal administration of tramadol is u... more Background: Tramadol is a centrally acting analgesic drug. Rectal administration of tramadol is useful in the treatment of post-operative pain or malignant pain in cases where it cannot be administered orally. In Thailand, tramadol is available only as a capsule for oral use and as a solution for injection. Objective: Develop tramadol hydrochloride rectal suppositories and rectal gel preparations. Methods: Tramadol rectal suppository and rectal gel were prepared. Physicochemical properties (viscosity, gel strength, mucoadhesive force) and the in vitro release of tramadol hydrochloride were investigated from different bases (Witepsol H15, polyethylene glycol, poloxamer, and hydroxyethylcellulose). The analgesic activity of rectal tramadol hydrochloride using the hot plate test was evaluated in rats. Results: Tramadol hydrochloride rectal gel using poloxamer was more mucoadhesive to the rectal mucous membrane than was the gel with the hydroxyethylcellulose base. Tramadol hydrochloride...
Journal of Natural Medicines, 2014
The in vivo wound healing potential of a standardized pomegranate rind extract (SPRE) and its maj... more The in vivo wound healing potential of a standardized pomegranate rind extract (SPRE) and its major antioxidant constituent, ellagic acid (EA, 13 %, w/w), were investigated in three rat dermal wound models. It was found that both SPRE (5 and 2.5 %) and its equivalent amount of EA (0.65 and 0.325 %) increased the tensile strength of the incision wound by a maximum of 35.43 and 31.82 %, respectively. SPRE at 5 and 2.5 % accelerated wound contraction of the excision wound and the burn wound, while EA was effective only at 0.65 % in these two wound models. Further assays revealed that SPRE enhanced the synthesis of collagen by a maximum of 21.83 mg/g and inhibited neutrophil infiltration dose-dependently, while EA was not effective in increasing collagen accumulation and its inhibitory effect on neutrophil infiltration was milder. These results indicated that SPRE is a promising phytopharmaceutical effective in facilitating the healing of wounds and is superior to its marker compound EA.
Prodrug of non-steroidal anti-inflammatory drugs (NSAIDs) or NSAIDs linked with guaiacol have bee... more Prodrug of non-steroidal anti-inflammatory drugs (NSAIDs) or NSAIDs linked with guaiacol have been reported to suppress gastrointestinal (GI) toxicity or induce GI protective effect. In this study, mefenamic-guaiacol ester was synthesized and its physicochemical properties, stability, and transport across Caco-2 monolayers were investigated. Methods. Synthesis of the ester was carried out using mefenamic acid, guaiacol, N, NЈ-dimethylaminopyridine, and N, NЈdicyclohexylcarbodiimide. The hydrolysis of the ester was investigated in aqueous buffer solutions pH 1-12 as well as in Caco-2 homogenate, human plasma, and porcine liver esterase. Caco-2 cell monolayers were utilized for transport studies. Due to the high lipophilicity of the ester with a calculated logP of 6.15, bovine serum albumin (BSA, 4%) was included in the receiver compartment to obtain a good in vitro-in vivo correlation. Permeation of the ester was assessed with or without the exposure of cells to PMSF, an inhibitor of esterase. Results. The ester was stable at a wide pH range from 1-10. However, it was hydrolyzed by enzymes from porcine liver esterase and Caco-2 homogenate. With the PMSF exposure on the apical (AP) side and in the presence of 4% BSA on the basolateral (BL) side, the transported amount of the ester from AP-to-BL direction was 14.63% after 3 hr with a lag time of 23 min. The Papp for the ester was 4.72 × 10 −6 cm s −1. Conclusion. The results from hydrolysis studies indicate that this ester is a prodrug. The Papp value suggests the moderate absorption characteristic of the compound. The accumulation of this highly lipophilic ester in Caco-2 cells is reduced in the presence of BSA.
Anaerobe, 2013
A lactobacillus strain isolated from a vaginal tract of a healthy woman was examined in vitro for... more A lactobacillus strain isolated from a vaginal tract of a healthy woman was examined in vitro for its probiotic potential. This strain, identified as Lactobacillus fermentum SK5, was able to survive at pH 3e4 and 0.1e0.2% bile, and unaffected by pepsin (3 g l À1) and pancreatin (1 g l À1), but was susceptible to all tested antibiotics except metronidazole. L. fermentum SK5 had an antimicrobial potential against gastrointestinal pathogenic Escherichia coli and vaginal pathogenic Gardnerella vaginalis. The effective substance was suspected to be a bacteriocin-like compound with a molecular weight of more than 10 kDa, but hydrogen peroxide was also detected. Further studies revealed that L. fermentum SK5 had good autoaggregation characteristic and a high surface hydrophobicity that enhanced its adhesion ability to epithelial cells and for biofilm formation. This lactobacillus showed coaggregation with E. coli and G. vaginalis to affect their adhesion and colonization. The adhesion of L. fermentum SK5 to HeLa, HT-29 and Caco-2 cells and its inhibition of E. coli and G. vaginalis adherence to these cells were demonstrated. These incidences provided evidence of the possible colonization of L. fermentum SK5 that would prevent binding and growth of E. coli and G. vaginalis onto intestinal and vaginal epithelial cells. On the basis of the ability of L. fermentum SK5 to inhibit pathogenic microorganisms through coaggregation and antimicrobial substances, it is likely that this lactobacillus strain could be a potential probiotic candidate for beneficial use in protecting against gastrointestinal and vaginal microbial infections.
Phytotherapy Research, 2013
The present study evaluated the topical anti-inflammatory potential of a standardized pomegranate... more The present study evaluated the topical anti-inflammatory potential of a standardized pomegranate rind extracts (SPRE) in parallel with its marker compound ellagic acid (EA, 13% w/w) against a mouse model of contact dermatitis. In the phenol-induced mouse ear edema, topical application of SPRE (5, 2.5, and 1 mg/ear) and EA (0.65, 0.325, and 0.13 mg/ear, equivalent to its content in SPRE) dose-dependently reduced the ear edema with the maximal inhibition of 79.12% and 73.63%, respectively. Triamcinolone (0.1 mg/ear) and diclofenac (1 mg/ear) as reference drugs inhibited the edema by 73.63% and 37.91%. Myeloperoxidase (MPO) activity in the mouse ear was also decreased by SPRE and EA up to 69.68% and 68.79%, respectively. Triamcinolone and diclofenac decreased the MPO activity by 76.66% and 80.14% similarly. The results indicated that topical application of SPRE and EA is promising for use in the treatment of inflammatory skin disorders.
The objective of this study was to develop vaginal suppository containing lactobacillus. Four kin... more The objective of this study was to develop vaginal suppository containing lactobacillus. Four kinds of vaginal suppositories containing Lactobacillus paracasei HL32 were formulated: 1) a conventional suppository with Witepsol H-15 as a base, 2) a conventional suppository with mixed polyethylene glycols (PEGs) as a base, 3) a hollow-type suppository with Witepsol H-15 as a base and 4) a hollow-type suppository with mixed PEGs as a base. The release studies demonstrated that the hollow-type suppository with mixed PEGs as the base gave the highest release of L. paracasei HL32 and was microbiological stable after storage at 2- 8°C over the period of 3 months.
Solid dispersions (SD) of curcuminpolyvinylpyrrolidone in the ratio of 1:2, 1:4, 1:5, 1:6, and 1:... more Solid dispersions (SD) of curcuminpolyvinylpyrrolidone in the ratio of 1:2, 1:4, 1:5, 1:6, and 1:8 were prepared in an attempt to increase the solubility and dissolution. Solubility, dissolution, powder X-ray diffraction (XRD), differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR) of solid dispersions, physical mixtures (PM) and curcumin were evaluated. Both solubility and dissolution of curcumin solid dispersions were significantly greater than those observed for physical mixtures and intact curcumin. The powder X-ray diffractograms indicated that the amorphous curcumin was obtained from all solid dispersions. It was found that the optimum weight ratio for curcumin:PVP K-30 is 1:6. The 1:6 solid dispersion still in the amorphous from after storage at ambient temperature for 2 years and the dissolution profile did not significantly different from freshly prepared.
Food Chemistry, 2022
Curcuminoids are known to exert diverse pharmacological effects and used in some pharmaceutical f... more Curcuminoids are known to exert diverse pharmacological effects and used in some pharmaceutical formulations. This study describes the preparation, characterization, and enhancement in the solubility and anticancer activity of a curcuminoids-rich extract (CRE) using a ternary inclusion complex system. CRE containing 88.9% w/w curcuminoids was prepared using a 'green' microwave extraction coupled with fractionation on a column of hydrophobic adsorbent resin. The ternary complex consisting of CRE, hydroxylpropyl-β-cyclodextrin and polyvinylpyrrolidone K30 was prepared using the solvent evaporation method and thoroughly characterized using Fourier-transform infrared spectroscopy, powder X-ray diffractograms, differential scanning calorimetry and scanning electron microscopy. The ternary complex of CRE improved the water-solubility of curcuminoids (up to 70.3 µg/mL) as well as the dissolution rate when compared to those of CRE (0 µg/mL). In addition, the ternary complex exhibited significantly stronger anticancer activity against human lung adenocarcinoma (A-549), human cervical adenocarcinoma (HeLa) and human colon adenocarcinoma (HT-29) cell lines than CRE.
International journal of pharmaceutical compounding, 2018
Vetiveria zizanioides (vetiver) contains viscous volatile oil, which has the ability to repel mos... more Vetiveria zizanioides (vetiver) contains viscous volatile oil, which has the ability to repel mosquitoes similar to citronella oil, a well-known mosquito repellent in tropical countries, like Thailand. The objectives of the current study were to formulate the stable oil-in-water vetiver oil lotions using Simulgel FL as a liquid emulsifier, to investigate the physicochemical properties of the prepared lotions and to evaluate the in vitro release characteristics of the stable vetiver oil lotions. In this work, the concentrations of Simulgel FL ranged from 1% to 3% weight in weight, whereas the concentrations of vetiver oil were varied: 2.5%, 5%, and 10% weight in weight. The suitable concentration of Simulgel FL was found to be 3% weight in weight. For comparison purposes, oil-in-water citronella oil lotions (10% weightin- weight citronella oil) were also prepared with similar ingredients. A mixture of vetiver oil and citronella oil (1:1 by weight) was also used as an active ingredien...
Excessive and daily inhalation of talcum, a main ingredient of face powders, causes pulmonary tal... more Excessive and daily inhalation of talcum, a main ingredient of face powders, causes pulmonary talcosis, which has led to the replacement of talcum with safer natural ingredients. RiceSorb®, or Oryza sativa starch from Japanese rice, was used as an alternative owing to its nontoxic and excellent oil absorption capacity. The objectives of the present work were to formulate loose face powders from RiceSorb® and to investigate the physicochemical properties of the prepared formulations. Five formulations of loose face powders were prepared by varying the ratios between talcum and RiceSorb®: 4:0 (FT0), 3:1 (FT1), 1:1 (FT2), 1:3 (FT3), and 0:4 (FT4). The physicochemical properties were evaluated mainly based on USP 41 and NF 36 such as morphology by using a scanning electron microscope, bulk density, flow property (angle of repose), moisture content (MC), and pH. The stability of the formulations were also performed at ambient temperature and 45°C for 2 months. The formulations had pH 6.9...
MATTER: International Journal of Science and Technology, 2019
The fruit pulp extracts of Tamarindus indica have been reported to possess several biological act... more The fruit pulp extracts of Tamarindus indica have been reported to possess several biological activities, especially antioxidant property which is suitable for cosmetic application. Therefore, the aims of this study were to formulate the tamarind fruit pulp extract loaded lotions (o/w emulsions), and to assess the antioxidant activity of tamarind fruit pulp extract loaded lotions. Initially, tamarind fruit pulp extracts were prepared by a solvent extraction method. The solvents used were water or a mixture of water and ethanol (water: ethanol= 1:1). Afterwards, the obtained tamarind fruit pulp extracts were subjected to lyophilization process. The tamarind fruit pulp extracts were tested for antioxidant activity by 2, 2-diphenyl-1-picrylhydrazyl (DPPH) assay to determine suitable concentrations of the extracts to be incorporated into the lotions, which were 2 and 4%w/w in the current study. Apart from the basic ingredients of the oil phase and water phase, ViscOptima SE (2%w/w) was selected as an emulsifier and a thickener of the formulations. The tamarind fruit pulp extract loaded lotions were characterized for physicochemical property and antioxidant potential. The freshly prepared tamarind fruit pulp extract loaded lotions were light brown with homogeneity and no phase separation was observed after centrifugation at 3,000 rpm for 30 min. They had weak acidic pH (4.4-5.1), considered acceptable for skin application. The loaded formulations (F1, 2%w/w) and F2, 4%w/w)) exhibited significantly higher conductivity values than that of the unloaded formulation (F0) (p<0.05). The formulations behaved as pseudoplastic flows with low viscosity. The DPPH measurement revealed that the formulations F1 and F2 had potential antioxidant activity. In conclusion, topical o/w lotions containing tamarind fruit pulp extract were successfully prepared. They had substantial antioxidant activities. As a result, tamarind fruit pulp extract loaded lotions displayed a potential use in cosmetic formulations, especially antiaging products.
International Journal of Pharmaceutics, 1999
Solid dispersions of piroxicam were prepared with polyvinylpyrrolidone (PVP) K-17 PF and PVP K-90... more Solid dispersions of piroxicam were prepared with polyvinylpyrrolidone (PVP) K-17 PF and PVP K-90 by solvent method. The physical state and drug:PVP interaction of solid dispersions and physical mixtures were characterized by X-ray diffraction, Fourier transform infrared (FTIR) spectroscopy and differential scanning calorimetry (DSC). FTIR analysis demonstrated the presence of intermolecular hydrogen bonding between piroxicam and PVP in solid dispersions. These interactions reflected the changes in crystalline structures of piroxicam. The amorphousness within the PVP moeity might be predicted in piroxicam dispersions by the disappearance of N-H or O-H peak of piroxicam. Dissolution studies indicated a significant increase in dissolution of piroxicam when dispersed in PVP. The better results were obtained with the lower molecular weight PVP K-17 than with higher molecular weight PVP K-90. The non-amorphous solid dispersions in PVP K-17 showed almost equally fast dissolution rates to amorphous dispersions in PVP K-90. The mechanism of dissolution of solid dispersion in PVP K-90 is predominantly diffusion-controlled due to the very high viscosity of PVP K-90. Dissolution was maximum with the amorphous solid dispersions containing drug:PVP K-17 1:5 and 1:6 which showed a 40-fold increase in dissolution in 5 min as compared with pure drug.
AIMS Microbiology, 2017
Encapsulation may protect viable probiotic cells. This study aims at the evaluation of a bambara ... more Encapsulation may protect viable probiotic cells. This study aims at the evaluation of a bambara groundnut protein isolate (BGPI)-alginate matrix designed for encapsulating a probiotic Lactobacillus rhamnosus GG. The response surface methodology was employed to gain the optimal concentrations of BGPI and alginate on encapsulation efficiency and survival of encapsulated cells. The capsules were prepared at the optimal combination by the traditional extrusion method composed of 8.66% w/v BGPI and 1.85% w/v alginate. The encapsulation efficiency was 97.24%, whereas the survival rates in an acidic condition and after the freeze-drying process were 95.56% and 95.20%, respectively-higher than those using either BGPI or alginate as the encapsulating agent individually. The designed capsules increased the probiotic L. rhamnosus GG survival relative to free cells in a simulated gastric fluid by 5.00 log cfu/ml after 3 h and in a simulated intestinal fluid by 8.06 log cfu/ml after 4 h. The shelf-life studies of the capsules over 6 months at 4 °C and 30 °C indicated that the remaining number of viable cells in a BGPI-alginate capsule was significantly higher than that of free cells in both temperatures. It was demonstrated that the BGPI-alginate capsule could be utilized as a new probiotic carrier for enhanced gastrointestinal transit and storage applied in food and/or pharmaceutical products.
International Journal of Food Science & Technology, 2016
Four legume water extracts, that is bambara groundnut, soya bean, red kidney bean and black bean ... more Four legume water extracts, that is bambara groundnut, soya bean, red kidney bean and black bean as well as skim milk, were examined for their effectiveness in protecting Lactobacillus rhamnosus GG and Lactobacillus fermentum SK5 during the freeze-drying and storage. Bambara groundnut water extract (BGWE) showed promising cryoprotective activity that was comparable to skim milk. BGWE and skim milk at 2-10% w/v and 5-20% w/v individually produced survival rates for both strains of 87-88%. To further optimise the synergistic cryoprotective medium, response surface methodology was employed. The optimal combination was 4.93% w/v BGWE and 11.68% w/v skim milk for L. rhamnosus GG and 5.17% w/v BGWE and 11.36% w/v skim milk for L. fermentum SK5 with survival rates of 95.17% and 94.36%, respectively. The storage life of freeze-dried cells of both probiotics at 4°C and 30°C for 6 months was markedly improved when they were produced with these optimal combinations.
Journal of Drug Delivery Science and Technology, 2011
Tramadol rectal gel preparations were developed using poloxamer or hydroxyethylcellulose as a gel... more Tramadol rectal gel preparations were developed using poloxamer or hydroxyethylcellulose as a gel base. The tramadol rectal gel using poloxamer has a gel point at 36 °C and was more bioadhesive (65.5 ± 2.4 x 10 2 dyne/cm 2) to the rectal mucous membrane than was the gel with the hydroxyethylcellulose base (37.4 ± 2.2 x 10 2 dyne/cm 2) with the gel strength of 87 ± 2 and 70 ± 2 s, respectively. All rectal gel formulations were colorless, clear, viscous liquid with a pH range of 6.65-7.13. In an in vitro release study, the release profiles of the drug from both rectal gels were similar and the cumulative amount of drug release was about 97 and 98 % in 5 h for the mucoadhesive gel and thermoreversible gel, respectively. Analysis of the release kinetics revealed that the drug might be released from the rectal gels by non-Fickian diffusion. In an in vivo analgesic study, administration of tramadol (0.25, 0.5, and 1.0 mg) rectal gel using poloxamer as the gel base, exerted a marked increase in the latency of the nociceptive response in mice. Similar results were also observed when using hydroxyethylcellulose as the base. These results indicated that tramadol rectal gels prepared using poloxamer or hydroxyethylcellulose as a gel base showed a complete release of the drug from the bases, as well as prolonging the latency of a nociceptive response in experimental animals.
Human vagina represents a dynamic ecosystem dominated by certain species of Lactobacillus. This m... more Human vagina represents a dynamic ecosystem dominated by certain species of Lactobacillus. This microorganism restricts the growth of pathogens by using properties of steric exclusion and inhibitory substance production. Serious complications including bacterial vaginosis and vaginal cancer are often determined in women with reduced numbers of lactobacilli. Local application of Lactobacillus is consequently promising to keep the vagina colonized by this strain, which consequently reduces the infections. In the present work, two vaginal formulations, e.g. effervescent tablet and PEG-based suppository, containing Lactobacillus were prepared. The hollow type PEG-based suppository was satisfied according to physical and biological characterizations. The lactobacilli inoculated had released from the formulation within 30 minutes. More than 90% of the bacteria released were viable and remained demonstrating good adherence to HeLa cells. Moreover, the abilities on bacteriocin and H 2 O 2 productions were not deteriorated by the suppository manipulation. ©All right reserved.
International journal of pharmaceutical compounding
The objective of this study was to develop a rapid-release diazepam suppository. Four kinds of di... more The objective of this study was to develop a rapid-release diazepam suppository. Four kinds of diazepam suppositories were formulated: (1) a conventional suppository with Witepsol H-15 as a base, (2) a conventional suppository with mixed polyethylene glycols as a base, (3) a hollow-type suppository with Witepsol H-15 as a base that contained diazepam solution in its cavity and (4) a hollow-type suppository with Witepsol H-15 as a base that contained diazepam powder in its cavity. The result of the differential scanning calorimetry thermograms indicated that diazepam dissolved in Witepsol base had a strong affinity to the lipophiic base while diazepam dispersed in polyethylene glycol base was still in the crystalline form. The release study of prepared suppositories showed that the release of diazepam from suppository 1 and suppository 4 was very slow. The diazepam released from suppository 2 after 5 minutes was about 30%. The diazepam released from suppository 3 after 5 minutes was ...
Die Pharmazie, 2001
The stabilities of X-ray amorphous solid dispersions of piroxicam and polyvinylpyrrolidone (PVP) ... more The stabilities of X-ray amorphous solid dispersions of piroxicam and polyvinylpyrrolidone (PVP) K-17 and PVP K-30 (1:5 and 1:4), respectively, were investigated after storage for 12 months. X-ray diffraction showed that in the aged solid dispersions piroxicam remained in the amorphous state. Fourier transform infrared (FTIR) spectroscopy indicated that the interactions between drug and PVP in aged solid dispersions are similar to those in freshly prepared samples. The dissolution rates of the X-ray amorphous solid dispersions during storage for 12 months at 45 degrees C and ambient temperature were examined. Very minor decreases in dissolution rates of aged solid dispersions were found which might be due to the coarsening of the particles. Dissolutions of these amorphous solid dispersions after aging for 12 months still showed an about 40-fold increase in dissolution in 5 min compared to pure drug.
Asian Biomedicine, 2011
Background: Tramadol is a centrally acting analgesic drug. Rectal administration of tramadol is u... more Background: Tramadol is a centrally acting analgesic drug. Rectal administration of tramadol is useful in the treatment of post-operative pain or malignant pain in cases where it cannot be administered orally. In Thailand, tramadol is available only as a capsule for oral use and as a solution for injection. Objective: Develop tramadol hydrochloride rectal suppositories and rectal gel preparations. Methods: Tramadol rectal suppository and rectal gel were prepared. Physicochemical properties (viscosity, gel strength, mucoadhesive force) and the in vitro release of tramadol hydrochloride were investigated from different bases (Witepsol H15, polyethylene glycol, poloxamer, and hydroxyethylcellulose). The analgesic activity of rectal tramadol hydrochloride using the hot plate test was evaluated in rats. Results: Tramadol hydrochloride rectal gel using poloxamer was more mucoadhesive to the rectal mucous membrane than was the gel with the hydroxyethylcellulose base. Tramadol hydrochloride...
Journal of Natural Medicines, 2014
The in vivo wound healing potential of a standardized pomegranate rind extract (SPRE) and its maj... more The in vivo wound healing potential of a standardized pomegranate rind extract (SPRE) and its major antioxidant constituent, ellagic acid (EA, 13 %, w/w), were investigated in three rat dermal wound models. It was found that both SPRE (5 and 2.5 %) and its equivalent amount of EA (0.65 and 0.325 %) increased the tensile strength of the incision wound by a maximum of 35.43 and 31.82 %, respectively. SPRE at 5 and 2.5 % accelerated wound contraction of the excision wound and the burn wound, while EA was effective only at 0.65 % in these two wound models. Further assays revealed that SPRE enhanced the synthesis of collagen by a maximum of 21.83 mg/g and inhibited neutrophil infiltration dose-dependently, while EA was not effective in increasing collagen accumulation and its inhibitory effect on neutrophil infiltration was milder. These results indicated that SPRE is a promising phytopharmaceutical effective in facilitating the healing of wounds and is superior to its marker compound EA.
Prodrug of non-steroidal anti-inflammatory drugs (NSAIDs) or NSAIDs linked with guaiacol have bee... more Prodrug of non-steroidal anti-inflammatory drugs (NSAIDs) or NSAIDs linked with guaiacol have been reported to suppress gastrointestinal (GI) toxicity or induce GI protective effect. In this study, mefenamic-guaiacol ester was synthesized and its physicochemical properties, stability, and transport across Caco-2 monolayers were investigated. Methods. Synthesis of the ester was carried out using mefenamic acid, guaiacol, N, NЈ-dimethylaminopyridine, and N, NЈdicyclohexylcarbodiimide. The hydrolysis of the ester was investigated in aqueous buffer solutions pH 1-12 as well as in Caco-2 homogenate, human plasma, and porcine liver esterase. Caco-2 cell monolayers were utilized for transport studies. Due to the high lipophilicity of the ester with a calculated logP of 6.15, bovine serum albumin (BSA, 4%) was included in the receiver compartment to obtain a good in vitro-in vivo correlation. Permeation of the ester was assessed with or without the exposure of cells to PMSF, an inhibitor of esterase. Results. The ester was stable at a wide pH range from 1-10. However, it was hydrolyzed by enzymes from porcine liver esterase and Caco-2 homogenate. With the PMSF exposure on the apical (AP) side and in the presence of 4% BSA on the basolateral (BL) side, the transported amount of the ester from AP-to-BL direction was 14.63% after 3 hr with a lag time of 23 min. The Papp for the ester was 4.72 × 10 −6 cm s −1. Conclusion. The results from hydrolysis studies indicate that this ester is a prodrug. The Papp value suggests the moderate absorption characteristic of the compound. The accumulation of this highly lipophilic ester in Caco-2 cells is reduced in the presence of BSA.
Anaerobe, 2013
A lactobacillus strain isolated from a vaginal tract of a healthy woman was examined in vitro for... more A lactobacillus strain isolated from a vaginal tract of a healthy woman was examined in vitro for its probiotic potential. This strain, identified as Lactobacillus fermentum SK5, was able to survive at pH 3e4 and 0.1e0.2% bile, and unaffected by pepsin (3 g l À1) and pancreatin (1 g l À1), but was susceptible to all tested antibiotics except metronidazole. L. fermentum SK5 had an antimicrobial potential against gastrointestinal pathogenic Escherichia coli and vaginal pathogenic Gardnerella vaginalis. The effective substance was suspected to be a bacteriocin-like compound with a molecular weight of more than 10 kDa, but hydrogen peroxide was also detected. Further studies revealed that L. fermentum SK5 had good autoaggregation characteristic and a high surface hydrophobicity that enhanced its adhesion ability to epithelial cells and for biofilm formation. This lactobacillus showed coaggregation with E. coli and G. vaginalis to affect their adhesion and colonization. The adhesion of L. fermentum SK5 to HeLa, HT-29 and Caco-2 cells and its inhibition of E. coli and G. vaginalis adherence to these cells were demonstrated. These incidences provided evidence of the possible colonization of L. fermentum SK5 that would prevent binding and growth of E. coli and G. vaginalis onto intestinal and vaginal epithelial cells. On the basis of the ability of L. fermentum SK5 to inhibit pathogenic microorganisms through coaggregation and antimicrobial substances, it is likely that this lactobacillus strain could be a potential probiotic candidate for beneficial use in protecting against gastrointestinal and vaginal microbial infections.
Phytotherapy Research, 2013
The present study evaluated the topical anti-inflammatory potential of a standardized pomegranate... more The present study evaluated the topical anti-inflammatory potential of a standardized pomegranate rind extracts (SPRE) in parallel with its marker compound ellagic acid (EA, 13% w/w) against a mouse model of contact dermatitis. In the phenol-induced mouse ear edema, topical application of SPRE (5, 2.5, and 1 mg/ear) and EA (0.65, 0.325, and 0.13 mg/ear, equivalent to its content in SPRE) dose-dependently reduced the ear edema with the maximal inhibition of 79.12% and 73.63%, respectively. Triamcinolone (0.1 mg/ear) and diclofenac (1 mg/ear) as reference drugs inhibited the edema by 73.63% and 37.91%. Myeloperoxidase (MPO) activity in the mouse ear was also decreased by SPRE and EA up to 69.68% and 68.79%, respectively. Triamcinolone and diclofenac decreased the MPO activity by 76.66% and 80.14% similarly. The results indicated that topical application of SPRE and EA is promising for use in the treatment of inflammatory skin disorders.