Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, Haryana, India.
Recent Adv Drug Deliv Formul. 2022;16(1):16-44. doi: 10.2174/2667387815666211207112803.
The oral route is a highly recommended route for the delivery of a drug. But most lipophilic drugs are difficult to deliver via this route due to their low aqueous solubility. Selfemulsifying drug delivery systems (SEDDS) have emerged as a potential approach of increasing dissolution of a hydrophobic drug due to spontaneous dispersion in micron or nano sized globules in the GI tract under mild agitation.
The main motive of this review article is to describe the mechanisms, advantages, disadvantages, factors affecting, effects of excipients, possible mechanisms of enhancing bioavailability, and evaluation of self-emulsifying drug delivery systems.
Self emulsifying systems incorporate the hydrophobic drug inside the oil globules, and a monolayer is formed by surfactants to provide the low interfacial tension, which leads to improvement in the dissolution rate of hydrophobic drugs. The globule size of self-emulsifying systems depends upon the type and ratio of excipients in which they are used. The ternary phase diagram is constructed to find out the range of concentration of excipients used. This review article also presents recent and updated patents on self-emulsifying drug delivery systems. Self-emulsifying systems have the ability to enhance the oral bioavailability and solubility of lipophilic drugs.
This technique offers further advantages such as bypassing the first pass metabolism via absorption of drugs through the lymphatic system, easy manufacturing, reducing enzymatic hydrolysis, inter and intra subject variability, and food effects.
口服是药物给药的首选途径。但由于大多数亲脂性药物的水溶性低,因此很难通过该途径给药。自乳化药物传递系统 (SEDDS) 作为一种增加疏水性药物溶解的潜在方法,由于在胃肠道中温和搅拌下自发分散成微米或纳米大小的球体而出现。
本文主要介绍自乳化药物传递系统的机制、优点、缺点、影响因素、辅料的影响、提高生物利用度的可能机制和评价。
自乳化系统将疏水性药物包裹在油球内,表面活性剂形成单分子层以提供低界面张力,从而提高疏水性药物的溶解速率。自乳化系统的液滴大小取决于所用辅料的类型和比例。通过构建三元相图来确定所用辅料的浓度范围。本文还介绍了自乳化药物传递系统的最新专利。自乳化系统能够提高亲脂性药物的口服生物利用度和溶解度。
该技术具有进一步的优势,例如通过吸收药物通过淋巴系统绕过首过代谢、易于制造、减少酶水解、个体间和个体内变异性以及食物效应。