Singh Bhupinder, Beg Sarwar, Khurana Rajneet Kaur, Sandhu Premjeet Singh, Kaur Ravinder, Katare Om Parkash
University Institute of Pharmaceutical Sciences, UGC Centre of Advanced Studies, Panjab University, Chandigarh 160 014, India; UGC Centre of Excellence in Applications of Nanomaterials, Nanoparticles & Nanocomposites (Biomedical Sciences).
University Institute of Pharmaceutical Sciences, UGC Centre of Advanced Studies, Panjab University, Chandigarh 160 014, India.
Crit Rev Ther Drug Carrier Syst. 2014;31(2):121-85. doi: 10.1615/critrevtherdrugcarriersyst.2014008502.
One of the biggest challenges confronting the contemporary drug delivery science today is to improve on the oral bioavailability of a vast number of drugs exhibiting poor and inconsistent gastrointestinal absorption. Self-emulsifying drug delivery systems (SEDDS) have been proved as highly useful technological innovations to surmount such bioavailability hiccups by virtue of their diminutive globule size, higher solubilization tendency for hydro-phobic drugs, robust formulation advantages, and easier scalability in the industrial milieu. Besides, these systems are also known to inhibit the P-glycoprotein (P-gp) efflux, reduce metabolism by gut Cytochrome P-450 enzymes, and circumnavigate the hepatic first-pass effect, facilitating absorption of drugs via intestinal lymphatic pathways. In the last two decades, the phenomenal success of SEDDS as a potential tool for oral delivery of drugs has extrapolated their applications to non-oral delivery also. Various innovative approaches and patented techniques have been reported on formulation of diverse oral and non-oral self-emulsifying (SE) systems not only of various synthetic and semisynthetic drugs, but also of several phytopharmaceuticals, nutraceuticals, and biological macromolecules. Of late, an escalating number of reports have been pouring in on special types of SE systems, mostly nanosized, employing functional excipients such as polar lipids, phospholipids, cellulosic polymer, diblock polymers, etc. This review paper provides an updated bird's-eye view account on the publications and patents of such novel SE approaches for use in both oral and non-oral therapeutics. Providing a relatively pithy overview, this paper thus endeavors to act as a repertoire of knowledge and know-how to guide the product development scientist in formulating variegated SE systems.
当今当代药物递送科学面临的最大挑战之一是提高大量胃肠道吸收不良且不稳定的药物的口服生物利用度。自乳化药物递送系统（SEDDS）已被证明是非常有用的技术创新，凭借其微小的液滴尺寸、对疏水性药物更高的增溶趋势、强大的制剂优势以及在工业环境中更容易扩大规模，克服了此类生物利用度问题。此外，这些系统还已知可抑制P-糖蛋白（P-gp）外排、减少肠道细胞色素P-450酶的代谢，并规避肝脏首过效应，通过肠道淋巴途径促进药物吸收。在过去二十年中，SEDDS作为口服给药潜在工具的显著成功也将其应用扩展到了非口服给药。关于各种口服和非口服自乳化（SE）系统的制剂，不仅有各种合成和半合成药物，还有几种植物药、营养保健品和生物大分子，已经报道了各种创新方法和专利技术。最近，越来越多关于特殊类型SE系统的报道不断涌现，这些系统大多是纳米级的，采用了极性脂质、磷脂、纤维素聚合物、二嵌段聚合物等功能性辅料。这篇综述文章提供了关于此类用于口服和非口服治疗的新型SE方法的出版物和专利的最新全景式介绍。因此，本文提供了一个相对简洁的概述，力图成为知识和技术诀窍的宝库，以指导产品开发科学家配制各种SE系统。
