Faculty of Pharmacy, Integral University, Lucknow, India.
Drug Dev Ind Pharm. 2013 Jan;39(1):1-19. doi: 10.3109/03639045.2012.660949. Epub 2012 Feb 29.
The oral delivery of hydrophobic drug presents a major challenge because of the low aqueous solubility of such compounds. Self-emulsifying/microemulsifying drug delivery system (SEDDS/SMEDDS), which are isotropic mixtures of oils, surfactants, solvents and co-solvents/surfactants, can be used for the design of formulations in order to improve the oral absorption of highly lipophilic drug compounds. The efficiency of oral absorption of said drug from such type of formulation depends on many formulation-related parameters, such as surfactant concentration, oil/surfactant ratio, polarity of the emulsion, droplet size and charge, all of which in essence determine the self-emulsification ability. Thus, only very specific pharmaceutical excipient combinations will lead to efficient self-emulsifying systems. With the growing interest in this field, there is an increasing need for guidelines in excipient selection to obtain effective delivery system with improved bioavailability. The aim of this review is to present the recent approaches in selecting the most appropriate lipid system(s); methods for its characterization and role of various excipients for improved delivery of dosage form.
由于这些化合物的水溶性低，因此经口递送疏水性药物是一项重大挑战。自乳化/微乳化药物递送系统（SEDDS/SMEDDS）是油、表面活性剂、溶剂和共溶剂/表面活性剂的各向同性混合物，可用于设计制剂，以提高高度亲脂性药物化合物的口服吸收。此类制剂中药物的口服吸收效率取决于许多与制剂相关的参数，例如表面活性剂浓度、油/表面活性剂比、乳液的极性、液滴大小和电荷，所有这些参数本质上都决定了自乳化能力。因此，只有非常特定的药物赋形剂组合才能导致有效的自乳化系统。随着对该领域的兴趣日益增加，人们越来越需要在赋形剂选择方面的指南，以获得具有改善生物利用度的有效递送系统。本综述的目的是介绍选择最合适的脂质系统的最新方法；其特征化方法以及各种赋形剂在改善剂型递送上的作用。
