Nikumbh Kishor V, Sevankar Shailesh G, Patil Moreshwar P
Department of Pharmaceutics, MET's Institute of Pharmacy, Bhujbal Knowledge City , Adgaon, Nashik , India.
Drug Deliv. 2015;22(4):509-15. doi: 10.3109/10717544.2013.859186. Epub 2013 Nov 25.
Anti-inflammatory agents are widely used to relieve inflammation caused by various factors.
This study was initiated with the intention to deliver low aqueous soluble ketoprofen to enhance its solubility by developing microemulsion system as a template and then incorporating it into gel phase.
Initially ketoprofen was solubilized into microemulsion preparation made up of clove oil, Tween 20 and propylene glycol as oil phase, surfactant and co-surfactant respectively, then it was incorporated into different concentration of gelling phase using gelling agents namely Carbopol 940, Carbopol 934 and hydroxypropyl methyl cellulose K(4)M (HPMC K(4)M). Formulated emulgels were evaluated for their physical appearance, pH, rheological properties, globule size, extrudability, drug content, spreadability, bioadhesion strength, in vitro and ex vivo drug release, skin irritation test and anti-inflammatory activity.
Microemulsion had shown globule size 396 nm, pH 6-6.7, viscosity 29.4 cps and zeta potential -12 mV indicating good stability. Formulated emulgels showed good physical appearance, skin acceptable pH 6-6.9, non-Newtonian shear thinning system, drug content 99.28 ± 0.16%, bioadhesion strength 48.4 gram force, globule size 473 nm, spreadability 22.96 gm.cm/s, good extrudability, in vitro release, ex vivo release did not showed any irritation reaction and possess a good anti-inflammatory activity.
Selected batch showed enhanced drug release (92.42 ± 4.66%) as compared to marketed gel (65.94 ± 3.30). Similarly ex vivo release of formulation showed 72.22% release through mice skin compared with marketed gel. Formulations followed Korsmeyer-Peppas diffusion kinetic model. It was observed from the results that the formulated emulgel can provide promising delivery of ketoprofen.
抗炎剂被广泛用于缓解由各种因素引起的炎症。
本研究旨在通过开发微乳系统作为模板来提高低水溶性酮洛芬的溶解度，然后将其制成凝胶剂。
首先将酮洛芬溶解于由丁香油、吐温20和丙二醇分别作为油相、表面活性剂和助表面活性剂组成的微乳制剂中，然后使用卡波姆940、卡波姆934和羟丙基甲基纤维素K（4）M（HPMC K（4）M）等凝胶剂将其掺入不同浓度的凝胶相中。对所制备的乳化凝胶进行外观、pH值、流变学性质、球粒大小、挤出性、药物含量、铺展性、生物黏附强度、体外和离体药物释放、皮肤刺激性试验及抗炎活性等方面的评价。
微乳的球粒大小为396nm，pH值为6 - 6.7，粘度为29.4cps，ζ电位为 - 12mV，表明具有良好的稳定性。所制备的乳化凝胶外观良好，皮肤可接受的pH值为6 - 6.9，为非牛顿剪切变稀系统，药物含量为99.28±0.16%，生物黏附强度为48.4克力，球粒大小为473nm，铺展性为22.96gm.cm/s，挤出性良好，体外释放、离体释放均未显示任何刺激反应，且具有良好的抗炎活性。
与市售凝胶（65.94±3.30）相比，所选批次显示出更高的药物释放率（92.42±4.66%）。同样，该制剂的离体释放显示，通过小鼠皮肤的释放率为72.22%，而市售凝胶为[此处原文未提及市售凝胶离体释放的对比数据]。制剂遵循Korsmeyer-Peppas扩散动力学模型。从结果可以看出，所制备的乳化凝胶可为酮洛芬提供有前景的给药方式。
