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Papers by rehab yusif

Research paper thumbnail of Wound Healing Efficacy of Rosuvastatin Transethosomal Gel, I Optimal Optimization, Histological and In Vivo Evaluation

Pharmaceutics

This study aimed to make a formulation and statistical optimization of transethosomal formulation... more This study aimed to make a formulation and statistical optimization of transethosomal formulations of rosuvastatin (ROS) to enhance its topical wound healing efficiency. Design-Expert® software was used to employ I optimal design. The formulation variables in the study were surfactant concentration (%w/v), ethanol concentration (%w/v) and surfactant type (span 60 or tween 80), while the dependent responses were entrapment efficiency percent (EE%), vesicle size (VS) and zeta potential (ZP). The numerical optimization process employed by the design expert software resulted in an optimum formula composed of 0.819439 (%w/v) span 60, 40 (%w/v) ethanol and 100 mg lecithin with a desirability of 0.745. It showed a predicted EE% value of 66.5517 vs. 277.703 nm and a ZP of −33. When it was prepared and validated, it showed less than a 5% deviation from the predicted values. The optimum formula was subjected to further characterizations, such as DSC, XRD, TEM, in vitro release, the effect of ...

Research paper thumbnail of Brain Targeting of Quetiapine Fumarate via Intranasal Delivery of Loaded Lipospheres: Fabrication, In-Vitro Evaluation, Optimization, and In-Vivo Assessment

Pharmaceuticals

A liposphere system for intranasal delivery of quetiapine fumarate (QTF) was created to assess th... more A liposphere system for intranasal delivery of quetiapine fumarate (QTF) was created to assess the potential for enhanced drug delivery. We investigated the effects of particle size, entrapment effectiveness, poly dispersibility index, and pluronic incorporation percentage on these variables. The optimal formula was examined using a TEM, and investigations into DSC, XRD, and FTIR were made. Optimized liposphere formulation in vitro dissolution investigation with a mean diameter of 294.4 ± 18.2 nm revealed about 80% drug release in 6 h. The intranasal injection of QTF-loaded lipospheres showed a shorter Tmax compared to that of intranasal and oral suspension, per the findings of an in vivo tissue distribution investigation in Wistar mice. Lipospheres were able to achieve higher drug transport efficiency (DTE %) and direct nose-to-brain drug transfer (DTP %). A potentially effective method for delivering QTF to specific brain regions is the liposphere system.

Research paper thumbnail of Central Composite Optimization of Glycerosomes for the Enhanced Oral Bioavailability and Brain Delivery of Quetiapine Fumarate

Pharmaceuticals

This study aimed to formulate and statistically optimize glycerosomal formulations of Quetiapine ... more This study aimed to formulate and statistically optimize glycerosomal formulations of Quetiapine fumarate (QTF) to increase its oral bioavailability and enhance its brain delivery. The study was designed using a Central composite rotatable design using Design-Expert® software. The independent variables in the study were glycerol % w/v and cholesterol % w/v, while the dependent variables were vesicle size (VS), zeta potential (ZP), and entrapment efficiency percent (EE%). The numerical optimization process resulted in an optimum formula composed of 29.645 (w/v%) glycerol, 0.8 (w/v%) cholesterol, and 5 (w/v%) lecithin. It showed a vesicle size of 290.4 nm, zeta potential of −34.58, and entrapment efficiency of 80.85%. The optimum formula was further characterized for DSC, XRD, TEM, in-vitro release, the effect of aging, and pharmacokinetic study. DSC thermogram confirmed the compatibility of the drug with the ingredients. XRD revealed the encapsulation of the drug in the glycerosomal ...

Research paper thumbnail of Formulation and In-Vivo Study of Ketoprofen Tablets Prepared Using Chitosan Interpolymer Complexes

Bulletin of Pharmaceutical Sciences. Assiut, 2012

The application of interpolymer complexes (IPCs) for oral controlled drug delivery systems was te... more The application of interpolymer complexes (IPCs) for oral controlled drug delivery systems was tested between chitosan and various anionic polymers viz sodium alginate, sodium carboxymethylcellulose and pectin. The prepared IPCs were investigated using Fourier transform infra-red spectroscopy and differential scanning calorimetry. Ketoprofen tablets were prepared using the polymers alone, physical mixtures of chitosan with sodium alginate, sodium carboxymethylcellulose or pectin in different ratios; 1:3, 1:1 and 3:1, and the corresponding IPCs. In-vitro release studies were carried out in two dissolution media; 0.1 N HCl of pH 1.2 and phosphate buffer of pH 7.4. It was found that, chitosan-sod. carboxymethylcellulose IPC tablets showed more controlled drug release compared to that containing chitosan-sodium alginate and chitosanpectin IPCs. The dissolution rate from tablets prepared using physical mixtures of polymers were found to be dependant on the interaction between chitosan and each of the anionic polymers in the physical mixtures, their ratios and pH of the dissolution medium. Tablets prepared using chitosan-sod. carboxymethylcellulose physical mixture 1:1 and chitosan-sod. carboxymethylcellulose IPC were selected for the in-vivo study using albino rabbits. The results showed a lower peak plasma concentration and marked controlled release effect of drug in tablets containing the physical mixture compared to that of the IPC and the control tablets.

Research paper thumbnail of Polymeric micelles for potentiated antiulcer and anticancer activities of naringin

International journal of nanomedicine, 2018

Naringin is one of the most interesting phytopharmaceuticals that has been widely investigated fo... more Naringin is one of the most interesting phytopharmaceuticals that has been widely investigated for various biological actions. Yet, its low water solubility, limited permeability, and suboptimal bioavailability limited its use. Therefore, in this study, polymeric micelles of naringin based on pluronic F68 (PF68) were developed, fully characterized, and optimized. The optimized formula was investigated regarding in vitro release, storage stability, and in vitro cytotoxicity vs different cell lines. Also, cytoprotection against ethanol-induced ulcer in rats and antitumor activity against Ehrlich ascites carcinoma in mice were investigated. Nanoscopic and nearly spherical 1:50 micelles with the mean diameter of 74.80±6.56 nm and narrow size distribution were obtained. These micelles showed the highest entrapment efficiency (EE%; 96.14±2.29). The micelles exhibited prolonged release up to 48 vs 10 h for free naringin. The stability of micelles was confirmed by insignificant changes in d...

Research paper thumbnail of Enhanced in vitro cytotoxicity and anti-tumor activity of vorinostat-loaded pluronic micelles with prolonged release and reduced hepatic and renal toxicities

European Journal of Pharmaceutical Sciences, 2017

Enhanced in vitro cytotoxicity and anti-tumor activity of vorinostat-loaded pluronic micelles wit... more Enhanced in vitro cytotoxicity and anti-tumor activity of vorinostat-loaded pluronic micelles with prolonged release and reduced hepatic and renal toxicities, (2016),

Research paper thumbnail of Investigation and Evaluation of an in Situ Interpolymer Complex of Carbopol with Polyvinylpyrrolidone as a Matrix for Gastroretentive Tablets of Ranitidine Hydrochloride

Chemical & pharmaceutical bulletin, 2016

Carbopol (CP) is a biocompatible bioadhesive polymer used as a matrix for gastroretentive (GR) ta... more Carbopol (CP) is a biocompatible bioadhesive polymer used as a matrix for gastroretentive (GR) tablets, however, its rapid hydration shortens its bioadhesion and floating when incorporated in effervescent formulae. The interpolymer complexation of CP with polyvinylpyrrolidone (PVP) significantly reduced the excessive hydration of CP, prolonging floating and maintaining the mucoadhesiveness. In early attempts, a lengthy process was followed to prepare such an interpolymer complex. In this study, an in situ interpolymer complexation between CP and two grades of PVP (K25 and K90) in 0.1 N HCl was investigated and characterized by Fourier transform infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC). Hence, directly compressed GR tablets of different combinations of PVP and CP with sodium bicarbonate (SB) as an effervescent agent were examined for prolonged gastroretention and sustained release of ranitidine hydrochloride (RHCl) as a model drug. Tablets were evalua...

Research paper thumbnail of Gastroretentive Matrix Tablets of Boswellia Oleogum Resin: Preparation, Optimization, In Vitro Evaluation, and Cytoprotective Effect on Indomethacin-Induced Gastric Ulcer in Rabbits

AAPS PharmSciTech, 2015

Currently available anti-ulcer drugs suffer from serious side effects which limited their uses an... more Currently available anti-ulcer drugs suffer from serious side effects which limited their uses and prompted the need to search for a safe and efficient new anti-ulcer agent. Boswellia gum resin (BR) emerged as a safe, efficient, natural, and economic potential cytoprotective agent. Thus, it is of medical importance to develop gastroretentive (GR) formulations of BR to enhance its bioavailability and antiulcer efficacy. Early attempts involved the use of organic solvents and non-applicability to large-scale production. In this study, different tablet formulations were prepared by simple direct compression combining floating and bioadhesion mechanisms employing hydroxypropyl methylcellulose (HPMC), sodium carboxymethyl cellulose (SCMC), pectin (PC), and/or carbopol (CP) as bioadhesive polymers and sodium bicarbonate (SB) as a gas former. The prepared tablets were subjected for assessment of swelling, floating, bioadhesion, and drug release in 0.1 N HCl. The optimized GR formulation was examined for its protective effect on the gastric ulcer induced by indomethacin in albino rabbits compared with lactose tablets. The obtained results disclosed that swelling, floating, bioadhesion, and drug release of the GR tablets of BR depend mainly on the nature of the matrix and the ratio of polymer combinations. Moreover, a combination of SCMC-CP in a ratio of 2:1 (SCP21) exhibited desirable floating, bioadhesion, swelling, and extended drug release. Also, a 6-h pretreatment with SCP21 tablets decreased the severity of inflammation and number of bleeding spots among ulcer-induced rabbits in comparison to those treated with lactose tablets.

Research paper thumbnail of Formulation and In-Vivo Study of Diltiazem Hydrochloride Tablets Prepared Using Interpolymer Complexes

British Journal of Pharmaceutical Research, 2012

Aim: To investigate interpolymer complexes (IPCs) formation between carbopol and cationic polymer... more Aim: To investigate interpolymer complexes (IPCs) formation between carbopol and cationic polymers such as chitosan and Eudragit E for oral controlled drug delivery systems. Methodology: The prepared IPCs were investigated using Fourier transform infra-red spectroscopy (FT-IR) and differential scanning calorimetry (DSC). Chitosan-carbopol and Eudragit E-carbopol IPCs loaded with diltiazem hydrochloride (DTZ HCl) with different drug:polymer ratios were also prepared. Diltiazem hydrochloride tablets were prepared using polymers alone, physical mixtures of chitosan or Eudragit E with carbopol and the corresponding drug loaded IPCs. In-vitro release studies were carried out in two dissolution media; 0.1 NHCl of pH 1.2 and phosphate buffer of pH 7.4. Results: The dissolution rate of DTZ HCl from the prepared tablets were found to be dependant on the interaction between chitosan or Eudragit E with carbopol in the physical mixture, drug:polymer ratio and pH of the dissolution medium. Tablets prepared using chitosan-carbopol IPC, Eudragit E-carbopol IPC, and Eudragit Ecarbopol physical mixture of drug:polymer ratio 1:5 were selected for the in-vivo study using rabbits. The results showed a lower peak plasma concentration and marked prolonged release effect of tablets containing Eudragit E-carbopol IPC and the corresponding physical mixture compared to that of commercial Altiazem tablets. Conclusion: Tablets containing Eudragit E-carbopol or chitosan-carbopol physical mixtures showed prolonged drug release compared to that containing the corresponding IPCs, Furthermore, Eudragit E-carbopol matrix tablets showed slower drug release than that of chitosan-carbopol.

Research paper thumbnail of Some variables affecting the characteristics of Eudragit E-sodium alginate polyelectrolyte complex as a tablet matrix for diltiazem hydrochloride

Acta Pharmaceutica, 2014

Eudragit E (EE)-sodium alginate (SA) polyelectrolyte complexes (PECs) were prepared at pH 4 and 5... more Eudragit E (EE)-sodium alginate (SA) polyelectrolyte complexes (PECs) were prepared at pH 4 and 5.8 using sodium alginate of high (SAH) and low viscosity (SAL). The optimum EE-SA complexation mass ratio was determined using viscosity measurements. Interactions between EE and SA in PECs were characterized by Fourier transform infra-red spectroscopy (FT-IR) and differential scanning calorimetry (DSC). Diltiazem hydrochloride (DTZ HCl) tablets were prepared using the prepared EE-SA PECs and their physical mixtures at different ratios as matrices. Tablets were evaluated for swelling characteristics and in vitro drug release. Tablets containing EE-SAH physical mixtures of ratios (1.5:1 and 1:3) as matrices were effective in achieving sustained release of DTZ HCl, where the percent drug released was significantly (p < 0.05) decreased compared to that from tablets either containing the same ratios of EE-SAL physical mixtures or the preformed EE- -SAH and EE-SAL PECs.

Research paper thumbnail of Potential Use of Niosomal Hydrogel as an Ocular Delivery System for Atenolol

Biological and Pharmaceutical Bulletin, 2014

Niosomes have been reported as possible approach to improve the low corneal penetration and bioav... more Niosomes have been reported as possible approach to improve the low corneal penetration and bioavailability characteristics for many drugs. The purpose of this study was to prepare and characterize an effective ocular niosomal hydrogel containing 0.5% (w/v) atenolol which is β1 adrenoceptor blocker for treatment of glaucoma. Thin film hydration method was used for the preparation of niosomes using Span 60 and cholesterol at different molar ratios. Niosomes were characterized using laser diffraction particle size analyzer, transmission electron microscopy, and differential scanning calorimetry. The results showed that higher entrapment efficiency (80.7% 1.2) was obtained from niosomes prepared using Span 60/cholesterol at a 2 : 1 molar ratio. Stability study revealed that a fairly high retention of atenolol inside vesicles (83.1% 2.35) up to a period of 3 months at 4°C. It was found that niosomal hydrogel formulation using carbopol 934P significantly exhibited sustained in vitro release of the drug compared with free drug solution and other polymeric hydrogels. The intraocular pressure (IOP) lowering activity of selected atenolol formulations was determined and compared with that of atenolol solution. It is worth noting that niosomal hydrogel formulation was found to show the most significant prolonged decrease in IOP, suggesting that niosomal hydrogel could be a promising delivery system for atenolol.

Research paper thumbnail of Wound Healing Efficacy of Rosuvastatin Transethosomal Gel, I Optimal Optimization, Histological and In Vivo Evaluation

Pharmaceutics

This study aimed to make a formulation and statistical optimization of transethosomal formulation... more This study aimed to make a formulation and statistical optimization of transethosomal formulations of rosuvastatin (ROS) to enhance its topical wound healing efficiency. Design-Expert® software was used to employ I optimal design. The formulation variables in the study were surfactant concentration (%w/v), ethanol concentration (%w/v) and surfactant type (span 60 or tween 80), while the dependent responses were entrapment efficiency percent (EE%), vesicle size (VS) and zeta potential (ZP). The numerical optimization process employed by the design expert software resulted in an optimum formula composed of 0.819439 (%w/v) span 60, 40 (%w/v) ethanol and 100 mg lecithin with a desirability of 0.745. It showed a predicted EE% value of 66.5517 vs. 277.703 nm and a ZP of −33. When it was prepared and validated, it showed less than a 5% deviation from the predicted values. The optimum formula was subjected to further characterizations, such as DSC, XRD, TEM, in vitro release, the effect of ...

Research paper thumbnail of Brain Targeting of Quetiapine Fumarate via Intranasal Delivery of Loaded Lipospheres: Fabrication, In-Vitro Evaluation, Optimization, and In-Vivo Assessment

Pharmaceuticals

A liposphere system for intranasal delivery of quetiapine fumarate (QTF) was created to assess th... more A liposphere system for intranasal delivery of quetiapine fumarate (QTF) was created to assess the potential for enhanced drug delivery. We investigated the effects of particle size, entrapment effectiveness, poly dispersibility index, and pluronic incorporation percentage on these variables. The optimal formula was examined using a TEM, and investigations into DSC, XRD, and FTIR were made. Optimized liposphere formulation in vitro dissolution investigation with a mean diameter of 294.4 ± 18.2 nm revealed about 80% drug release in 6 h. The intranasal injection of QTF-loaded lipospheres showed a shorter Tmax compared to that of intranasal and oral suspension, per the findings of an in vivo tissue distribution investigation in Wistar mice. Lipospheres were able to achieve higher drug transport efficiency (DTE %) and direct nose-to-brain drug transfer (DTP %). A potentially effective method for delivering QTF to specific brain regions is the liposphere system.

Research paper thumbnail of Central Composite Optimization of Glycerosomes for the Enhanced Oral Bioavailability and Brain Delivery of Quetiapine Fumarate

Pharmaceuticals

This study aimed to formulate and statistically optimize glycerosomal formulations of Quetiapine ... more This study aimed to formulate and statistically optimize glycerosomal formulations of Quetiapine fumarate (QTF) to increase its oral bioavailability and enhance its brain delivery. The study was designed using a Central composite rotatable design using Design-Expert® software. The independent variables in the study were glycerol % w/v and cholesterol % w/v, while the dependent variables were vesicle size (VS), zeta potential (ZP), and entrapment efficiency percent (EE%). The numerical optimization process resulted in an optimum formula composed of 29.645 (w/v%) glycerol, 0.8 (w/v%) cholesterol, and 5 (w/v%) lecithin. It showed a vesicle size of 290.4 nm, zeta potential of −34.58, and entrapment efficiency of 80.85%. The optimum formula was further characterized for DSC, XRD, TEM, in-vitro release, the effect of aging, and pharmacokinetic study. DSC thermogram confirmed the compatibility of the drug with the ingredients. XRD revealed the encapsulation of the drug in the glycerosomal ...

Research paper thumbnail of Formulation and In-Vivo Study of Ketoprofen Tablets Prepared Using Chitosan Interpolymer Complexes

Bulletin of Pharmaceutical Sciences. Assiut, 2012

The application of interpolymer complexes (IPCs) for oral controlled drug delivery systems was te... more The application of interpolymer complexes (IPCs) for oral controlled drug delivery systems was tested between chitosan and various anionic polymers viz sodium alginate, sodium carboxymethylcellulose and pectin. The prepared IPCs were investigated using Fourier transform infra-red spectroscopy and differential scanning calorimetry. Ketoprofen tablets were prepared using the polymers alone, physical mixtures of chitosan with sodium alginate, sodium carboxymethylcellulose or pectin in different ratios; 1:3, 1:1 and 3:1, and the corresponding IPCs. In-vitro release studies were carried out in two dissolution media; 0.1 N HCl of pH 1.2 and phosphate buffer of pH 7.4. It was found that, chitosan-sod. carboxymethylcellulose IPC tablets showed more controlled drug release compared to that containing chitosan-sodium alginate and chitosanpectin IPCs. The dissolution rate from tablets prepared using physical mixtures of polymers were found to be dependant on the interaction between chitosan and each of the anionic polymers in the physical mixtures, their ratios and pH of the dissolution medium. Tablets prepared using chitosan-sod. carboxymethylcellulose physical mixture 1:1 and chitosan-sod. carboxymethylcellulose IPC were selected for the in-vivo study using albino rabbits. The results showed a lower peak plasma concentration and marked controlled release effect of drug in tablets containing the physical mixture compared to that of the IPC and the control tablets.

Research paper thumbnail of Polymeric micelles for potentiated antiulcer and anticancer activities of naringin

International journal of nanomedicine, 2018

Naringin is one of the most interesting phytopharmaceuticals that has been widely investigated fo... more Naringin is one of the most interesting phytopharmaceuticals that has been widely investigated for various biological actions. Yet, its low water solubility, limited permeability, and suboptimal bioavailability limited its use. Therefore, in this study, polymeric micelles of naringin based on pluronic F68 (PF68) were developed, fully characterized, and optimized. The optimized formula was investigated regarding in vitro release, storage stability, and in vitro cytotoxicity vs different cell lines. Also, cytoprotection against ethanol-induced ulcer in rats and antitumor activity against Ehrlich ascites carcinoma in mice were investigated. Nanoscopic and nearly spherical 1:50 micelles with the mean diameter of 74.80±6.56 nm and narrow size distribution were obtained. These micelles showed the highest entrapment efficiency (EE%; 96.14±2.29). The micelles exhibited prolonged release up to 48 vs 10 h for free naringin. The stability of micelles was confirmed by insignificant changes in d...

Research paper thumbnail of Enhanced in vitro cytotoxicity and anti-tumor activity of vorinostat-loaded pluronic micelles with prolonged release and reduced hepatic and renal toxicities

European Journal of Pharmaceutical Sciences, 2017

Enhanced in vitro cytotoxicity and anti-tumor activity of vorinostat-loaded pluronic micelles wit... more Enhanced in vitro cytotoxicity and anti-tumor activity of vorinostat-loaded pluronic micelles with prolonged release and reduced hepatic and renal toxicities, (2016),

Research paper thumbnail of Investigation and Evaluation of an in Situ Interpolymer Complex of Carbopol with Polyvinylpyrrolidone as a Matrix for Gastroretentive Tablets of Ranitidine Hydrochloride

Chemical & pharmaceutical bulletin, 2016

Carbopol (CP) is a biocompatible bioadhesive polymer used as a matrix for gastroretentive (GR) ta... more Carbopol (CP) is a biocompatible bioadhesive polymer used as a matrix for gastroretentive (GR) tablets, however, its rapid hydration shortens its bioadhesion and floating when incorporated in effervescent formulae. The interpolymer complexation of CP with polyvinylpyrrolidone (PVP) significantly reduced the excessive hydration of CP, prolonging floating and maintaining the mucoadhesiveness. In early attempts, a lengthy process was followed to prepare such an interpolymer complex. In this study, an in situ interpolymer complexation between CP and two grades of PVP (K25 and K90) in 0.1 N HCl was investigated and characterized by Fourier transform infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC). Hence, directly compressed GR tablets of different combinations of PVP and CP with sodium bicarbonate (SB) as an effervescent agent were examined for prolonged gastroretention and sustained release of ranitidine hydrochloride (RHCl) as a model drug. Tablets were evalua...

Research paper thumbnail of Gastroretentive Matrix Tablets of Boswellia Oleogum Resin: Preparation, Optimization, In Vitro Evaluation, and Cytoprotective Effect on Indomethacin-Induced Gastric Ulcer in Rabbits

AAPS PharmSciTech, 2015

Currently available anti-ulcer drugs suffer from serious side effects which limited their uses an... more Currently available anti-ulcer drugs suffer from serious side effects which limited their uses and prompted the need to search for a safe and efficient new anti-ulcer agent. Boswellia gum resin (BR) emerged as a safe, efficient, natural, and economic potential cytoprotective agent. Thus, it is of medical importance to develop gastroretentive (GR) formulations of BR to enhance its bioavailability and antiulcer efficacy. Early attempts involved the use of organic solvents and non-applicability to large-scale production. In this study, different tablet formulations were prepared by simple direct compression combining floating and bioadhesion mechanisms employing hydroxypropyl methylcellulose (HPMC), sodium carboxymethyl cellulose (SCMC), pectin (PC), and/or carbopol (CP) as bioadhesive polymers and sodium bicarbonate (SB) as a gas former. The prepared tablets were subjected for assessment of swelling, floating, bioadhesion, and drug release in 0.1 N HCl. The optimized GR formulation was examined for its protective effect on the gastric ulcer induced by indomethacin in albino rabbits compared with lactose tablets. The obtained results disclosed that swelling, floating, bioadhesion, and drug release of the GR tablets of BR depend mainly on the nature of the matrix and the ratio of polymer combinations. Moreover, a combination of SCMC-CP in a ratio of 2:1 (SCP21) exhibited desirable floating, bioadhesion, swelling, and extended drug release. Also, a 6-h pretreatment with SCP21 tablets decreased the severity of inflammation and number of bleeding spots among ulcer-induced rabbits in comparison to those treated with lactose tablets.

Research paper thumbnail of Formulation and In-Vivo Study of Diltiazem Hydrochloride Tablets Prepared Using Interpolymer Complexes

British Journal of Pharmaceutical Research, 2012

Aim: To investigate interpolymer complexes (IPCs) formation between carbopol and cationic polymer... more Aim: To investigate interpolymer complexes (IPCs) formation between carbopol and cationic polymers such as chitosan and Eudragit E for oral controlled drug delivery systems. Methodology: The prepared IPCs were investigated using Fourier transform infra-red spectroscopy (FT-IR) and differential scanning calorimetry (DSC). Chitosan-carbopol and Eudragit E-carbopol IPCs loaded with diltiazem hydrochloride (DTZ HCl) with different drug:polymer ratios were also prepared. Diltiazem hydrochloride tablets were prepared using polymers alone, physical mixtures of chitosan or Eudragit E with carbopol and the corresponding drug loaded IPCs. In-vitro release studies were carried out in two dissolution media; 0.1 NHCl of pH 1.2 and phosphate buffer of pH 7.4. Results: The dissolution rate of DTZ HCl from the prepared tablets were found to be dependant on the interaction between chitosan or Eudragit E with carbopol in the physical mixture, drug:polymer ratio and pH of the dissolution medium. Tablets prepared using chitosan-carbopol IPC, Eudragit E-carbopol IPC, and Eudragit Ecarbopol physical mixture of drug:polymer ratio 1:5 were selected for the in-vivo study using rabbits. The results showed a lower peak plasma concentration and marked prolonged release effect of tablets containing Eudragit E-carbopol IPC and the corresponding physical mixture compared to that of commercial Altiazem tablets. Conclusion: Tablets containing Eudragit E-carbopol or chitosan-carbopol physical mixtures showed prolonged drug release compared to that containing the corresponding IPCs, Furthermore, Eudragit E-carbopol matrix tablets showed slower drug release than that of chitosan-carbopol.

Research paper thumbnail of Some variables affecting the characteristics of Eudragit E-sodium alginate polyelectrolyte complex as a tablet matrix for diltiazem hydrochloride

Acta Pharmaceutica, 2014

Eudragit E (EE)-sodium alginate (SA) polyelectrolyte complexes (PECs) were prepared at pH 4 and 5... more Eudragit E (EE)-sodium alginate (SA) polyelectrolyte complexes (PECs) were prepared at pH 4 and 5.8 using sodium alginate of high (SAH) and low viscosity (SAL). The optimum EE-SA complexation mass ratio was determined using viscosity measurements. Interactions between EE and SA in PECs were characterized by Fourier transform infra-red spectroscopy (FT-IR) and differential scanning calorimetry (DSC). Diltiazem hydrochloride (DTZ HCl) tablets were prepared using the prepared EE-SA PECs and their physical mixtures at different ratios as matrices. Tablets were evaluated for swelling characteristics and in vitro drug release. Tablets containing EE-SAH physical mixtures of ratios (1.5:1 and 1:3) as matrices were effective in achieving sustained release of DTZ HCl, where the percent drug released was significantly (p < 0.05) decreased compared to that from tablets either containing the same ratios of EE-SAL physical mixtures or the preformed EE- -SAH and EE-SAL PECs.

Research paper thumbnail of Potential Use of Niosomal Hydrogel as an Ocular Delivery System for Atenolol

Biological and Pharmaceutical Bulletin, 2014

Niosomes have been reported as possible approach to improve the low corneal penetration and bioav... more Niosomes have been reported as possible approach to improve the low corneal penetration and bioavailability characteristics for many drugs. The purpose of this study was to prepare and characterize an effective ocular niosomal hydrogel containing 0.5% (w/v) atenolol which is β1 adrenoceptor blocker for treatment of glaucoma. Thin film hydration method was used for the preparation of niosomes using Span 60 and cholesterol at different molar ratios. Niosomes were characterized using laser diffraction particle size analyzer, transmission electron microscopy, and differential scanning calorimetry. The results showed that higher entrapment efficiency (80.7% 1.2) was obtained from niosomes prepared using Span 60/cholesterol at a 2 : 1 molar ratio. Stability study revealed that a fairly high retention of atenolol inside vesicles (83.1% 2.35) up to a period of 3 months at 4°C. It was found that niosomal hydrogel formulation using carbopol 934P significantly exhibited sustained in vitro release of the drug compared with free drug solution and other polymeric hydrogels. The intraocular pressure (IOP) lowering activity of selected atenolol formulations was determined and compared with that of atenolol solution. It is worth noting that niosomal hydrogel formulation was found to show the most significant prolonged decrease in IOP, suggesting that niosomal hydrogel could be a promising delivery system for atenolol.