Formulation and evaluation of topical piroxicam microemulgel for arthritis

Mehreen Sattar, Somia Sarfraz, Uzma Liaquat, Iqra Shoukat, B. Ahmad, T. Hussain
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Abstract

Background: Piroxicam is an anti-inflammatory, analgesic, and antipyretic drug. Piroxicam is widely used in the management of chronic pain. The objective of this work was to develop and analyze topical Piroxicam microemulgel to improve drug solubility, enhance permeation, reduce GIT side effects reduce the frequency of the drug. Method: The Piroxicam microemulgel was prepared by drawing the pseudo ternary phase picture and water titration procedure. Formulation was prepared by using isopropyl myristate as an oil, Tween 80 as an surfactant, n-butanol as Co-surfactant and water. It was converted to gel by using 1% Carbopol 940 and few drops of ethanolamine. The prepared formulation was characterized for thermodynamic stability, pH, droplet size, viscosity, FTIR,DSC, electrical conductivity, dye solubility drug content, and in-vitro release using a Franz diffusion cell. Result: Microemulgel formulation was thermodynamically stable on visual inspection after being treated with a freeze-thaw cycle and centrifugation. pH of formulation was 6.5. The mean droplet size for ME gel was 100±0.472nm. The viscosity of the microemulgel was 90.4±0.01 cps which showed Newtonian flow. FTIR and DSC studies showed that microemulgel was compatible with its excipients. Electrical conductivity and dye solubility testing confirmed that the microemulgel was O/W. Piroxicam microemulsion gel showed 89.89% drug content and the release rate of piroxicam was 98±8.63% after 48h. It followed the Korsmeyer Pappas model which means it was a hydrogel-based system. Conclusion: Microemulsion gel formulation obtained remarkably inflated skin retention for piroxicam over the piroxicam gel. It might act as a promising vehicle for the topical delivery of poor water-soluble drugs.
局部吡罗昔康微凝胶治疗关节炎的配方及评价
背景:吡罗昔康是一种抗炎、镇痛和解热的药物。吡罗昔康广泛用于慢性疼痛的治疗。本工作的目的是开发和分析吡罗昔康外用微凝胶,以提高药物溶解度,增强渗透,减少GIT副作用,减少给药频率。方法:采用拟三元相图和水滴定法制备吡罗昔康微乳。以肉豆肉酸异丙酯为油,吐温80为表面活性剂,正丁醇为助表面活性剂,水为原料制备配方。用1%卡波波尔940和少量乙醇胺将其转化为凝胶。采用Franz扩散池对制备的制剂进行热力学稳定性、pH、液滴大小、粘度、FTIR、DSC、电导率、染料溶解度、药物含量和体外释放度的表征。结果:微乳制剂经冻融循环和离心处理后,目测热稳定性良好。配方pH为6.5。ME凝胶的平均滴度为100±0.472nm。微乳液的粘度为90.4±0.01 cps,为牛顿流体。FTIR和DSC研究表明,微乳与配形剂具有良好的相容性。电导率和染料溶解度测试证实微乳为O/W。吡罗昔康微乳凝胶药含量为89.89%,48h后吡罗昔康释放率为98±8.63%。它遵循科斯迈耶·帕帕斯模型,这意味着它是一个基于水凝胶的系统。结论:微乳凝胶制剂比吡罗西康凝胶具有明显的皮肤保留率。它可能作为一种有前途的载体,局部递送水溶性差的药物。
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