基于微乳的萘丁美酮透皮给药用于治疗关节炎的研究进展
Development of Microemulsion Based Nabumetone Transdermal Delivery for Treatment of Arthritis.
作者信息
Jagdale Swati C, Deore Gokul K, Chabukswar Anuruddha R
机构信息
Department of Pharmaceutics, MAEER`s Maharashtra Institute of Pharmacy, MIT Campus, Kothrud, Pune, (MS), 411038, India.
出版信息
Recent Pat Drug Deliv Formul. 2018;12(2):130-149. doi: 10.2174/1872211312666180227091059.
BACKGROUND
Nabumetone is biopharmaceutics classification system (BCS) class II drug, widely used in the treatment of osteoarthritis and rheumatoid arthritis. The most frequently reported adverse reactions for the drug involve disturbance in gastrointestinal tract, diarrhea, dyspepsia and abdominal pain. Microemulgel has advantages of microemulsion for improving solubility for hydrophobic drug. Patent literature had shown that the work for drug has been carried on spray chilling, enteric coated tablet, and topical formulation which gave an idea for present research work for the development of transdermal delivery.
OBJECTIVE
The objective of the present research work was to optimize transdermal microemulgel delivery for Nabumetone for the treatment of arthritis.
METHODS
Oil, surfactant and co-surfactant were selected based on solubility study of the drug. Gelling agents used were Carbopol 934 and HPMC K100M. Optimization was carried out using 32 factorial design. Characterization and evaluation were carried out for microemulsion and microemulsion based gel.
RESULTS
Field emission-scanning electron microscopy (FE-SEM) study of the microemulsion revealed globules of 50-200 nm size. Zeta potential -9.50 mV indicated good stability of microemulsion. Globule size measured by dynamic light scattering (zetasizer) was 160nm. Design expert gave optimized batch as F7 which contain 0.2% w/w drug, 4.3% w/w liquid paraffin, 0.71% w/w tween 80, 0.35% w/w propylene glycol, 0.124% w/w Carbopol 934, 0.187% w/w HPMC K100M and 11.68% w/w water. In-vitro diffusion study for F7 batch showed 99.16±2.10 % drug release through egg membrane and 99.15±2.73% drug release in ex-vivo study.
CONCLUSION
Nabumetone microemulgel exhibiting good in-vitro and ex-vivo controlled drug release was optimized.
背景
萘丁美酮是生物药剂学分类系统（BCS）II类药物，广泛用于治疗骨关节炎和类风湿性关节炎。该药物最常报告的不良反应包括胃肠道紊乱、腹泻、消化不良和腹痛。微乳凝胶具有微乳液改善疏水药物溶解度的优点。专利文献表明，针对该药物开展了喷雾冷冻、肠溶包衣片和局部制剂等方面的研究工作，这为本研究开发透皮给药制剂提供了思路。
目的
本研究工作的目的是优化萘丁美酮透皮微乳凝胶制剂用于治疗关节炎。
方法
基于药物的溶解度研究选择油相、表面活性剂和助表面活性剂。使用的胶凝剂为卡波姆934和羟丙甲纤维素K100M。采用32析因设计进行优化。对微乳液和基于微乳液的凝胶进行表征和评价。
结果
微乳液的场发射扫描电子显微镜（FE-SEM）研究显示球粒大小为50 - 200 nm。ζ电位为-9.50 mV表明微乳液具有良好的稳定性。通过动态光散射（粒度分析仪）测量的球粒大小为160nm。Design Expert软件给出的优化批次为F7，其含有0.2% w/w的药物、4.3% w/w的液体石蜡、0.71% w/w的吐温80、0.35% w/w的丙二醇、0.124% w/w的卡波姆934、0.187% w/w的羟丙甲纤维素K100M和11.68% w/w的水。F7批次的体外扩散研究表明，通过卵膜的药物释放率为99.16±2.10%，体外研究中的药物释放率为99.15±2.73%。
结论
优化得到了体外和体内均具有良好控释效果的萘丁美酮微乳凝胶。
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