Studying the Effect of Different Gelling Agent on the Preparation and Characterization of Metronidazole as Topical Emulgel (original) (raw)
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Development and evaluation of Metronidazole containing topical gel using different gelling agents
Asian Journal of Pharmacy and Pharmacology
Among the all bacteriostatic substance metronidazole is an important active substance that has been used for antibiotic and antiprotozoal medication. It is used for the treatment of pelvic inflammatory disease, endocarditic, dracunculiasis, giardiasis, trichomoniasis, amebiasis, and most important in bacterial vaginitis. According to World Health Organisation's list of essential medicines metronidazole is most effective and safe medicine for human health system with few common side effects such as nausea, metallic taste, loss of appetite and headaches when taken it orally (Yellanki et al., 2010). An attempt has been made, in the present work, to develop antibacterial gels of Metronidazole, using a bland of
Formulation and Characterization of Micro Sponge Loaded Topical Gel Preparation of Metronidazole
2017
Key Words Metronidazole topical gel, Micro sponge formulation, Over-the-counter (OTC) Permeation enhancer Micro-sponge containing Metronidazole as active constituent with four different formulations by changing the proportions of drug (Metronidazole), polymer (ethyl cellulose), emulsifier (Poly vinyl alcohol) were obtained successfully using emulsion solvent diffusion method. Metronidazole topical gel is used in the treatment of fungating tumours, rosacea. The drug was chosen because unavailable micro sponge dosage forms in the market in order to decrease the skin irritation by preventing excess accumulation of drug on epidermis. The size of the micro sponges can be varied, usually from 5-300 μm in diameter, depending upon the degree of smoothness or after-feel required for the end formula. The micro sponge system can also avoid unnecessary accumulation of ingredients within the epidermis and the dermis. Potentially, they can reduce considerably the irritation of effective drugs wit...
CHEMICAL & PHARMACEUTICAL BULLETIN, 2012
The aim of this study was to prepare a topical water-in-oil type microemulsion containing metronidazole and to compare its effectiveness with a commercial gel product in the treatment of rosacea. A pseudoternary phase diagram (K m 2 : 1) was constructed using lecithin/butanol/isopropyl myristate/water. The microemulsion was chosen from the microemulsion region in the phase diagram. The formulation was a water-in-oil type microemulsion (droplet size: 11.6 nm, viscosity: 457.3 mPa•s, conductivity: 1.5 µs/cm, turbidity: 6.89 NTU) and the addition of the metronidazole did not alter the properties of the system. The release experiment showed that the release rate of metronidazole from the commercial gel product was higher than that of the microemulsion. Stability experiments showed that the metronidazole microemulsion remained stable for at least 6 months; none of the characteristic properties of the microemulsion had changed, the system retained its clarity and there was no sign that crystallization of metronidazole has occurred. Microemulsion was compared to a gel product in a randomized, double-blind, baseline-controlled, split-face clinical trial for the treatment of patients. After the 6-week treatment period there was a statistically significant difference in reduction of the main symptoms of rosacea. Of the patients treated with the microemulsion, 17% experienced complete relief from inflammatory lesions, and 50% from erythema. The microemulsion resulted in complete relief in 38% of the patients with telangiectasia while the commercial product did not provide any relief of telangiectasia symptoms. In conclusion, the microemulsion containing metronidazole was found to be more effective in reducing the symptoms of rosacea compared to the commercial gel product.
International journal of Pharmacy and Pharmaceutical Sciences, 2015
The aim of the research work is to formulate emulgel of Meloxicam for topical application. Methods: The method used for preparation of microemulsion was water titration method with Oleic acid as oil phase, Tween 20 as surfactant and PEG 400 as co-surfactant and its concentrations were fixed based on Pseudoternary phase diagrams. The optimized emulsion formulation was incorporated into the gel matrix that is Carbopol981 NF and Carbopol 974 P NF. Results: The prepared emulsions were characterized for globule size, drug content, zeta potential and the emulgel for physical appearance, drug content, pH, viscosity, spreadability, extrudability and in vitro drug release studies. The optimized emulsion formulations E1 and F1 showed globule size of 176 nm and 128 nm respectively and the emulgel formulation M2F1 with 1.5% Carbopol 981 and optimized F1 emulsion formulation showed in vitro drug release of 89.934% at the end of 8 h. The optimized formulation showed no skin irritation when compared with standard irritant 0.8% of Formalin. The optimized formulation showed better anti-inflammatory effect when compared with marketed formulation. Conclusion: Meloxicam was proven to be a suitable candidate for formulating emulgel for topical delivery to achieve better patient compliance.
In Vitro Drug Release Studies of Metronidazole Topical Formulations Through Cellulose Membrane
The East and Central African Journal of Pharmaceutical Sciences, 2012
The present work reports on the mucoadhesive and mechanical properties of the water-soluble gum obtained from Entandophragma angolense when incorporated in oral tablets. Flat-faced chlorpheniramine maleate tablets containing the gum were formulated. The potential for chemical interaction between the gum and drug was evaluated by UV spectroscopy. The mucoadhesive, mechanical and release properties of the tablets were evaluated. The rates of water uptake and erosion were determined for the tablets. The detachment time for the tablets increased from 78.71 ± 0.43 to 84.28 ± 0.75 min, and from 33.57 ± 0.48 to 79.27 ± 4.7 min as the amount of gum per tablet was increased from 2.5 to 10.0% w/w, respectively. The drug release time for all tablets increased with binder concentration. UV spectroscopy suggested the absence of chemical interactions. The novel natural gum compared favourably with established mucoadhesive polymers namely hydroxypropylcellulose and gelatin. The mucoadhesive, mecha...
A Review on Formulation Development and Evaluation of Novel Topical Emulgel (An Overview)
International journal of pharmaceutical sciences review and research, 2022
Over the last decade the treatment of illness has been accomplished by administering drug to human body via various routes namely oral, sublingual, rectal, parental etc. Many advantages of gels a major limitation is in the delivery of hydrophobic drugs. So to overcome this limitation an emulsion based approach is being used so that even a hydrophobic therapeutic moiety can enjoy the unique properties of gels. The topical drug delivery system is generally used where these systems of drug administration fails or in local skin infection like fungal infection. Topical drug delivery can be defined as the application of a drug containing formulation to the skin to directly treat cutaneous disorder. The combination of hydrophilic cornified cells in hydrophobic intercellular material provides a barrier to both hydrophilic and hydrophobic substances. Within the major group of semisolid preparations, the use of transparent gels has expanded both in cosmetics and in pharmaceutical preparations. Polymer can function as emulsifiers and thickeners because the gelling capacity of these compounds allows the formulation of stable emulsions and creams by decreasing surface and interfacial tension and at the same time increasing the viscosity of the aqueous phase. These Emulgel are having major advantages on novel vesicular systems as well as on conventional systems in various aspects. Various permeation enhancers can potentiate the effect, so Emulgel can be used as better topical drug delivery systems over present systems.
Formulation And Evaluation Of Emulgel Of An Antifungal Drug For Topical Drug Delivery
Journal of Pharmaceutical Negative Results, 2022
Topical drug delivery system improved bioavailability, reduced side effects, more uniform plasma levels, longer duration of action, resulting in a reduction in dosing frequency and improve therapy due to plasma levels up to the end of the dosing interval compared to a decline in plasma levels with conventional oral dosage form. Emulgel are generally used where the other systems of drug administration fails to directly treat cutaneous disorders such as fungal infections, acne, psoriasis etc. Materials and methods: Fluconazole emulgel was optimized based on Design-Expert® software using central composite design (CCD) making Fourteen formulations using jojoba oil and liquid paraffin, Methylparaben, Propylparaben and Triethanolamine. Results and Discussions:-The spreadability test range find from 8.9 g.cm/min to 14.87 g.cm/min for the formulations F1 and F14, respectively. Formulations having low amount of jojoba oil and liquid paraffin had the high spreadability index. As the viscosity of the gel increased, the release of the drug was expected to be slower. Complete drug release (100%) was achieved at the 3rd hr for the formulations F1, F8, F7 and F14 released more than 80 % of the drug and in vitro results showed that an emulgel formulation can be a potential candidate for the delivery of fluconazole for the skin disease, with better in vitro physical, using jojoba oil and liquid paraffin as drug carriers. SEM analysis of emulgel shows the uniform structure of emulgel formulation.
Vehicle influence on in vitro release of metronidazole: role of w/o/w multiple emulsion
International Journal of Pharmaceutics, 1994
Few studies have been made on the topical administration of w/o/w multiple emulsions, although their advantages in the controlled release by oral and parenteral administration have already been shown. The objective of this study was to compare the in vitro release of a hydrosoluble molecule (metronidazole) from w/o/w multiple, w/o and o/w emulsions. In order to avoid any influence of the formulation, all emulsions were prepared according to the same formula. The microscopic aspect, conductivity values and rheological parameters confirmed that three emulsion types were obtained. Metronidazole release was studied on synthetic membranes and on rat skin biopsies. When the synthetic membrane offered negligible resistance to passage of the drug (cellulose membrane), metronidazole release from the w/o/w emulsion was slightly slower compared with the o/w emulsion, while much slower release was observed with the w/o emulsion. When the synthetic membrane was rate-controlling diffusion (silicone), the difference between the emulsions was decreased, although the rank order remained the same. In the case of skin, the absorption of metronidazole is similar from w/o/w and o/w emulsions, however, it is faster from these two emulsions than from the w/o emulsion.
Journal of Pharmacy & Bioresources
The rationale for this study was to increase the absorption of model drug metronidazole by formulating an organogel using detarium oil in place of conventional oils used in drug formulation such as liquid paraffin. The organogels were prepared by fluid-filled mechanism using metronidazole as the model drug. The drug-surfactant mixtures were dissolved in oil followed by the addition of water which led to the formation of organogels at specific compositions. The formulations were analyzed by microscopy, rheology, in vitro drug release and X-ray diffraction (XRD). Microscopic studies revealed the gels contained clusters of water-filled spherical structures. FTIR study showed compatibility of components of the organogels. DSC result showed all the organogels released heat during formation. The viscosity of the organogels showed an elastic flow followed by a non-elastic phase. The cumulative percentagerelease of metronidazole was found to be between 63% and 85% at the end of 10 h, with O...
REVIEW ON EMULGEL FORMULATIONS WITH NON-STEROIDAL ANTI-INFLAMMATORY DRUGS FOR TOPICAL ADMINISTRATION
Pharma Science Monitor, 2017
The review was carried out to discuss in detail about theemulgel formulations for the non steroidal anti-inflammatory drugs. In emulgel is a novel dosage form for topical delivery of various drugs. It is applying into the skin as semisolid preparation and it contact with the epidermis of skin. The mainadvantage of using topical delivery isbypass the first pass metabolism, shelf medicated, improve patient compliance, more selective to a specific site, incorporation of hydrophobic drugs, better loading capacity, enhanced stability, production probability and low preparation cost and Controlled release in comparison to other drugdelivery systems. The formation of emulgel depends on oil phase, aqueous phase, emulsifiers, polymers and the permeation enhancers used in the formulations. The review was focused on types, advantages, disadvantages of emulgel, constituents, preparation method and various characterization studies of emulgels, mechanism of NSAIDs, various marketed NSAIDs emulgel formulations and current research on NSAIDs emulgel.