a Department of Pharmaceutics , NIPER Ahmedabad , C/o B.V. Patel PERD Centre , Ahmedabad , Gujarat , India.
Drug Deliv. 2015;22(6):675-90. doi: 10.3109/10717544.2014.896058. Epub 2014 Mar 27.
Self-microemulsifying drug delivery system (SMEDDS) has emerged as a vital strategy to formulate poor water soluble compounds for bioavailability enhancement. However, certain limitations are associated with SMEDDS formulations which include in vivo drug precipitation, formulation handling issues, limited lymphatic uptake, lack of predictive in vitro tests and oxidation of unsaturated fatty acids. These limitations restrict their potential usage. Inclusion of polymers or precipitation inhibitors within lipid based formulations helps to maintain drug supersaturation after dispersion. This, thereby, improves the bioavailability and reduces the variability on exposure. Also, formulating solid SMEDDS helps to overcome liquid handling and stability problems. Usage of medium chain triglycerides (MCT) and suitable antioxidants to minimize oxidation of unsaturated fatty acids are few of the steps to overcome the limitations associated with SMEDDS. The review discussed here, in detail, the limitations of SMEDDS and suitable measures that can be taken to overcome them.
自微乳药物传递系统（SMEDDS）已成为将水溶性差的化合物制成制剂以提高生物利用度的重要策略。然而，SMEDDS 制剂存在一些局限性，包括体内药物沉淀、制剂处理问题、有限的淋巴摄取、缺乏预测性的体外试验和不饱和脂肪酸的氧化。这些限制限制了它们的潜在用途。在基于脂质的制剂中加入聚合物或沉淀抑制剂有助于在分散后保持药物的过饱和状态。这进而提高了生物利用度并降低了暴露的变异性。此外，将 SMEDDS 制成固体形式有助于克服液体处理和稳定性问题。使用中链甘油三酯（MCT）和合适的抗氧化剂来最小化不饱和脂肪酸的氧化是克服 SMEDDS 相关限制的几种方法。本文详细讨论了 SMEDDS 的局限性以及可以采取的克服这些局限性的适当措施。
