Formulation, development and characterization of ibuprofen microemulgel for arthritis

M. H. T. Bhatti, Sarim Sohail, M. U. Aslam, Hana Ather, T. Hussain, Muhammad Kashif
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Abstract

Objective: Microemulgel is composed of aqueous phase, lipophilic phase, along with surfactant and co-surfactant, a suitable gelling agent is also incorporated. The drug Ibuprofen is non-steroidal anti-inflammatory drug. Its oral administration associated with many GIT, hepatic and renal problems. The main objective of the study was to formulate a stable topical microemulgel of ibuprofen in order to achieve the highest bioavailability with least side effects. Method: Pseudo ternary phase diagram was constructed in order to get the suitable concentrations of lipophilic phase, surfactant and co-surfactant. Phase titration method was used to prepare microemulsion, with surfactant and co-surfactant in a ratio of 2:1 respectively, along with gelling agent to form microemulgel. Formulations were evaluated to check appearance, pH, flowability, particle size, drug content, spreadability, drug release and skin irritation. Results: The globule size of microemulsion was 400 nm and zeta potential was -14 mV showing acceptable stability. Formulated emulgel showed good physical characteristics, suitable pH of 6.4 for skin. The drug content was 98.474%. The stability study showed that the ibuprofen was stable in phosphate buffer pH of 6.8. The carbopol 940 as a gelling agent showed high release rate values. The release rate of the optimized formulation, F1 was 94% and it followed Korsmeyer Peppas model (n=0.467). Conclusion: The prepared formulation was cost-effective because of promising highest bioavailability. The results suggest the potential use of developed microemulgel is mainly for topical delivery of ibuprofen, ensuring the safe use.
关节炎用布洛芬微凝胶的制备、研制及表征
目的:制备由水相、亲脂相、表面活性剂和助表面活性剂组成的微乳液,并加入合适的胶凝剂。布洛芬是一种非甾体抗炎药。它的口服与许多胃肠道、肝脏和肾脏问题有关。本研究的主要目的是制备一种稳定的局部布洛芬微凝胶,以达到最高的生物利用度和最小的副作用。方法:构建拟三元相图,确定亲脂相、表面活性剂和助表面活性剂的适宜浓度。采用相滴定法制备微乳液,表面活性剂和助表面活性剂分别以2:1的比例与胶凝剂形成微乳液。对配方进行外观、pH、流动性、粒径、药物含量、涂抹性、药物释放和皮肤刺激性等评价。结果:微乳液粒径为400 nm, zeta电位为-14 mV,稳定性良好。所配制的乳液具有良好的物理特性,pH值为6.4,适合皮肤使用。药品含量为98.474%。稳定性研究表明,布洛芬在pH为6.8的磷酸盐缓冲液中稳定。卡波波尔940作为胶凝剂具有较高的释放速率值。优化后的配方释放率F1为94%,符合Korsmeyer Peppas模型(n=0.467)。结论:该制剂具有较高的生物利用度,具有较好的成本效益。结果表明,所研制的微凝胶的潜在用途主要是局部给药,确保布洛芬的安全使用。
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