Kumar Mukesh, Singh Dilpreet, Bedi Neena
Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar, Punjab 143005, India.
Ther Deliv. 2019 Jan;10(1):21-36. doi: 10.4155/tde-2018-0053.
The current investigation is focused on solid self-microemulsifying drug-delivery systems (S-SMEDDS) of mefenamic acid (MFA) for improving pharmacodynamic activity. Methodology & results: Solubility assessment in various lipid excipients and optimization of pseudoternary plots were carried out for development of liquid SMEDDS. The optimized liquid SMEDD formulation was spray dried to solid dosage form and observed with enhanced amorphization or molecular dispersion of MFA in S-SMEDDS, as evident from x-ray diffractometry and differential scanning calorimetry studies. Enhanced in vitro dissolution rate of optimized formulation was observed, resulting in multifold enhancement in absorption profile of MFA, as compared with pure drug and marketed product. These studies further substantiate the dose reduction in SMEDDS by gaining equivalent therapeutic profile with marketed product. Enhanced analgesic and anti-inflammatory activity was observed with S-SMEDD formulations in acetic acid-induced writhings and carrageenan-induced paw edema models, respectively.
The optimized S-SMEDD formulation holds great promise for enhancement of its physiochemical and biological attributes.
当前研究聚焦于甲芬那酸（MFA）的固体自微乳化药物递送系统（S-SMEDDS），以提高其药效学活性。方法与结果：为开发液体自微乳化药物递送系统（SMEDDS），对多种脂质辅料中的溶解度进行了评估，并对伪三元相图进行了优化。将优化后的液体SMEDDS制剂喷雾干燥成固体剂型，通过X射线衍射和差示扫描量热法研究发现，MFA在S-SMEDDS中呈现出增强的非晶化或分子分散状态。观察到优化制剂的体外溶出速率提高，与纯药物和市售产品相比，MFA的吸收情况得到了数倍增强。这些研究进一步证实，通过获得与市售产品相当的治疗效果，SMEDDS可实现剂量降低。在醋酸诱导扭体模型和角叉菜胶诱导足跖肿胀模型中，分别观察到S-SMEDDS制剂具有增强的镇痛和抗炎活性。
优化后的S-SMEDDS制剂在改善其理化和生物学特性方面具有巨大潜力。
