Mwangi Alex N, Njogu Peter M, Maru Shital M, Njuguna Nicholas M, Njaria Paul M, Kiriiri Geoffrey K, Mathenge Agnes W
Department of Pharmaceutics and Pharmacy Practice, University of Nairobi, P.O. Box 19676-00202, Nairobi, Kenya.
Department of Pharmaceutical Chemistry, University of Nairobi, P.O. Box 19676-00202, Nairobi, Kenya.
Saudi Pharm J. 2021 Apr;29(4):351-360. doi: 10.1016/j.jsps.2021.03.005. Epub 2021 Mar 23.
The study designed, formulated and evaluated meloxicam emulgels as a potential alternative topical treatment option for rheumatism.
A 3 factorial design was employed to formulate nine preliminary meloxicam emulgels (Formulations F1 - F9). The influences of carbopol-934 and menthol as gelling agent and drug release enhancer, respectively, were correlated with four pharmaceutical properties of the formulated emulgels namely viscosity, spreadability, and cumulative drug release at one hour and at eight hours. Using the generated data and applying the Design Expert® modelling software, two optimized meloxicam emulgels (Formulations F10 and F11) were designed, formulated and evaluated. In vivo anti-inflammatory efficacy was conducted using carrageenan-induced rat paw oedema method. Drug release kinetics was modelled using DDSolver® dissolution software.
All formulations were homogenous with no observable grittiness or phase separation. The optimized Formulations F10 and F11 had pH 6.5 and 6.4, viscosity of 23656 and 24524 mPa.s, spreadability of 9.9 and 9.5 cm, and drug content of 90.4% and 92.9%, respectively, all within optimal values. The cumulative percentage of drug released was 21.0% and 22.9% after one hour and 50.1% and 55.8% after eight hours for Formulations F10 and F11, respectively. Drug release kinetics exhibited Fickian diffusion best described by Korsmeyer-Peppas model. Paw volume inhibition by Formulation F11 at two and three hours after carrageenan injection was statistically significant ( < 0.05).
The optimized meloxicam emulgels had high pharmaceutical quality and were pharmacologically active. Further optimization could potentially provide a safe and efficacious alternative treatment option for rheumatism.
本研究设计、制备并评估美洛昔康乳胶剂，作为一种潜在的风湿性疾病局部替代治疗选择。
采用三因素设计制备九种初步的美洛昔康乳胶剂（制剂F1 - F9）。分别考察卡波姆-934和薄荷醇作为凝胶剂和药物释放增强剂对所制备乳胶剂的四种药学性质（即粘度、铺展性以及1小时和8小时的累积药物释放量）的影响。利用所得数据并应用Design Expert®建模软件，设计、制备并评估了两种优化的美洛昔康乳胶剂（制剂F10和F11）。采用角叉菜胶诱导的大鼠足爪肿胀法进行体内抗炎疗效研究。使用DDSolver®溶出软件对药物释放动力学进行建模。
所有制剂均均匀，无明显砂粒感或相分离。优化后的制剂F10和F11的pH值分别为6.5和6.4，粘度分别为23656和24524 mPa·s，铺展性分别为9.9和9.5 cm，药物含量分别为90.4%和92.9%，均在最佳值范围内。制剂F10和F11在1小时后的药物累积释放百分比分别为21.0%和22.9%，8小时后分别为50.1%和55.8%。药物释放动力学表现为符合Korsmeyer-Peppas模型的菲克扩散。角叉菜胶注射后2小时和3小时，制剂F11对足爪体积的抑制作用具有统计学意义（P < 0.05）。
优化后的美洛昔康乳胶剂具有较高的药学质量且具有药理活性。进一步优化可能为风湿性疾病提供一种安全有效的替代治疗选择。
