Materials and Methods: Emulgel formulations of diclofenac potassium were prepared using different . subjected to various evaluation parameters such as drug. Emulgels have been extensively covered as a promising drug delivery system for the administration of lipophilic drugs. This work was. Formulation and Evaluation of Luliconazole Emulgel for. Topical Drug Delivery. Dhobale Shankar,* Shelke Gajanan, Jadhav Suresh, Gaikwad.
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Aceclofenac is a non-steroidal anti-inflammatory drug used for pain relief and inflammation in certain joint disorders. In this study, polymer-based emulgel formulation of aceclofenac with a microemulsion base was developed and assessed for its anti-inflammatory activity.
FORMULATION AND EVALUATION OF TERBINAFINE HYDROCHLORIDE FILM FORMING EMULGEL
Microemulsion of aceclofenac was formulated with various polymers and optimized. The optimized formulation was subjected to gelling, resulting in formulation of an emulgel. The resulting emulgel was optimized for desired pharmaceutical characteristics and later evaluated for anti-inflammatory effect in rats, comparing against the standard most popular marketed anti-inflammatory emulggel formulation.
The resultant microemulsion and emulgel both exhibited the desired drug release in-vitro and ex-vivo. The in vivo anti-inflammatory activity of topical aceclofenac emulgel on carrageenan induced paw edema model showed a time dependent response in reduction of inflammation showing the highest inhibition of The activity produced by the formulated emulgel for,ulation at par with the most marketed emulgel formulation.
Thus, the microemulsion base improved evaluztion solubility of the drug and the emulgel formulation enhanced the delivery in a sustained manner.
Formulation and Evaluation of Tioconazole Emulgel for Topical Drug Delivery System
Hence, the formulation strategy for aceclofenac and thereby, an efficient drug delivery led to an effective anti-inflammatory activity. Aceclofenac is a non-steroidal anti-inflammatory drug NSAID glycolic formulwtion of diclofenac, used for certain joint disorders.
It has a better tolerability profile as well as a better analgesic activity in comparison with diclofenac. Hence, developing formulation strategies for aceclofenac is particularly imperative 12.
Currently, the marketed formulation contains a tablet and a gel. However, side effects such as gastric ulcerogenicity, flatulence, indigestion and nausea, limit the utility of oral aceclofenac 1. Hence, the topical route would be one of the ideal alternatives to enhance local delivery, bypassing these side effects.
Compared with ointments and creams, gelsprovide a better feel are greaseless and easily washable. Additionally, a gel formulation aids in faster drug release in comparison to other semisolids 2.
However, a prominent drawback in formulating gels is difficulty in delivery of hydrophobic drug. To overcome this limitation, emulgel, a novel drug delivery has emerged which is a combination of gel and emulsion, where the presence of gelling agent in the water phase converts a classical emulsion into a gel. It combines dual release pattern of both gel and emulsion providing better therapeutic action and sustained release 34. Microemulsion-based formulations have an advantage of improved solubility and have reported to enhance drug permeation, owing to reduced surface tension and particle size 56.
Microemulsions are thermodynamically stable and enhance drug permeation and release. Hence, a microemulsion of Aceclofenac was formulated, which was later formed into an emulgel. Data regarding formulation of microemulsion-based emulgel of aceclofenac are limited and none of the previously published studies present a comparison of the aceclofenac emulgel with the currently marketed, most popular anti-inflammatory emulgel, diclofenac.
Thus, the study was conducted to develop novel microemulsion-based emulgel formulations of aceclofenac, a poorly water soluble drug and evaluate its anti-inflammatory activity. The current study focused on the development and optimization of an emulgel formulation of aceclofenac and evaluation of its anti-inflammatory activity against the standard, most preferred marketed Diclofenac emulgel in experimental animals.
The study was commenced after the relevant approvals from the concerned authorities as well as the animal ethics committee. The animal studies were conducted in the animal house, under appropriate care and precautions. The total duration of this study was approximately 5 months considering conceptualization to completion of animal studies.
The study was initiated in December, and completed in May, Polysorbate 80, isopropyl myristate, was procured from Molychem Mumbai, India and Loba chemie pvt limited, Mumbai, Indiarespectively. All other chemicals and solvents were of analytical reagent grade.
Saturation solubility of aceclofenac in various oils, surfactants, co-surfactants was determined by saturation solubility method. Based on the results of this study, pseudo ternary phase diagram was fromulation using the Tridraw software, to calculate the surfactant and co-surfactant ratio Smix.
After a number of trials, microemulsion of aceclofenac was optimized with:. Oil was mixed in the Smix for around 10 min on a magnetic stirrer. Aceclofenac was added to it in small parts until the drug completely dissolved in the solution.
The optimized quantity of distilled water was then added drop by drop in the solution with constant stirring at 50rpm on a magnetic stirrer. Different concentrations of carbopol were taken for trials and the optimum emulgel formulation was selected Table 1 and Fig. Evaluation of microemulsion 4 – 7 Appearance and pH: The test substance was diluted in 1: Forkulation size and zeta potential: The particle size and zeta potential of the microemulsion was evaluated using nano zeta sizer.
In vitro diffusion studies: Rmulgel vitro diffusion studies were done with the help of modified Franz diffusion cell Sumati sales corporation, Mumbai, India. Microemulsion containing 15 mg of aceclofenac was evenly applied onto the surface of dialysis membrane along with aceclofenac suspension in water for comparison. The dialysis membrane was attached between the donor and the receptor chamber of diffusion cell.
The receptor chamber was filled with freshly prepared phosphate buffer pH 6. The receptor formulstion was stirred by magnetic stirrer. The aliquots 1 mL were collected at time intervals of 1 h up to 8 h.
Samples were analyzed for drug content by UV-Vis spectrophotometer after appropriate dilutions. Cumulative corrections were made to obtain the total amount of ane release at each time interval. Evaluation of emulgel 7 – 11 Optimization: F1 and F2 with 0. Hence, F3 with 1. These studies were conducted in the same way as that described for microemulsion, but by using the emulgel in the place of microemulsion.
Ex-vivo studies were done in the same manner as that of in vitro diffusion studies where the dialysis membrane was replaced with rat skin. The average cumulative amount of drug permeated per unit surface area of the skin was plotted versus time.
Aceclofenac content in emulgel was measured by dissolving known 0. Absorbance was measured after suitable dilution at nm using UV-Vis spectrophotometer.
Formulation and evaluation of Cyclosporin A emulgel for ocular delivery.
The protocol designed for animal studies was compliant with the CPCSEA guidelines and was approved by the institutional animal ethics committee. Ethics committee approval number: Skin irritation test patch test 7 – A set of nine rats was used in the study.
The emulgel was applied on the properly shaven skin of rat. Undesirable skin changes, i. Anti-inflammatory studies by carrageenan induced paw edema model: A total of 6 rats were used in each group, for placebo, marketed gel and aceclofenac formulated emulgel, amounting to 18 rats in total.
The anti-inflammatory activity of aceclofenac emulgel was evaluated using carrageenan induced paw edema in rats by a method described by Gerald et al. Female wistar rats weighing g were divided into three groups. Group I was diseased control, group II received dose of 25 mg of aceclofenac emulgel whereas group III evaluatkon marketed eevaluation emulgel.
Edema was induced in rats using 0. The swelling in the paw of each rat was measured by plethysmometer by volume displacement method at baseline and every h till the 6th h Percentage inflammation was calculated as under:.
Anti-inflammatory studies by croton oil induced ear edema: The anti-inflammatory activity of aceclofenac emulgel was evaluated using croton oil induced ear edema against acute inflammation. Wistar rats g were divided randomly into three groups. Group I was taken as disease control. Group II received aceclofenac emulgel equivalent to 2.
The inflammation in the ear of each rat was noted using Vernier caliper at 1st, 2nd, 3rd and 4th h of treatment. The percentage change in inflammation was calculated by the same formula as mentioned above.
The solubility of aceclofenac in different oils, surfactants and co-surfactants was determined since it is the most important criteria for microemulsion preparation Table 2. The solubilization capability of aceclofenac in different oils, surfactant and co surfactant was shown in the Table 1.
Isopropyl myristate showed best solubility amongst all the oils, polysorbate 80 showed two times better solubility than other surfactants and Ethanol showed the 5 times better solubility amongst co-surfactants. Based on the results of solubility studies, Isopropyl myristate, Polysorbate 80 and Ethanol were chosen as oil, surfactant and co-surfactant, respectively.
Pseudo ternary phase diagram was constructed by varying Polysorbate 80 and ethanol in 1: The microemulsion region obtained in 1: The particle size of 1: Ethanol was chosen for further studies. The microemulsion which had highest amount of drug solubility and water uptake in the pseudo ternary phase diagram was chosen for trials on microemulsion.
A formulation yielding clear and transparent appearance and the one not cracking when observed for 24 h was selected for further studies. Evaluation of microemulsion Appearance and Ph: The aceclofenac microemulsion was transparent yellow colored solution with a pH of 5. The microemulsion when diluted in 1: Particle size and Zeta potential analysis: The particle size of the microemulsion was found to be The drug release was found to be Formulation, development and evaluation of emulgel: