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自乳化口服脂质药物递送系统:进展与挑战。

Self-Emulsifying Oral Lipid Drug Delivery Systems: Advances and Challenges.

机构信息

Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandarsindri, Ajmer, Rajasthan, 305817, India.

School of Pharmacy and Technology Management, NMIMS, Mukesh Patel Technology Park, Babulde, Near Bank of Tapi River, Mumbai Agra Highway, Shirpur, Maharashtra, 425405, India.

出版信息

AAPS PharmSciTech. 2019 Feb 27;20(3):129. doi: 10.1208/s12249-019-1335-x.

DOI:10.1208/s12249-019-1335-x
PMID:30815765
Abstract

The attempts to oral delivery of lipids can be challenging. Self-emulsifying drug delivery system (SEDDS) plays a vital role to tackle this problem. SEDDS is composed of an oil phase, surfactants, co-surfactants, emulsifying agents, and co-solvents. SEDDS can be categorized into self-nano-emulsifying agents (SNEDDS) and self-micro-emulsifying agents (SMEDDS). The characterization of SEDDS includes size, zeta potential analysis, and surface morphology via electron microscopy and phase separation methods. SEDDS can be well characterized through different techniques for size and morphology. Supersaturation is the phenomenon applied in case of SEDDS, in which polymers and copolymers are used for SEDDS preparation. A supersaturated SEDDS formulation kinetically and thermodynamically inhibits the precipitation of drug molecules by retarding nucleation and crystal growth in the aqueous medium. Self-emulsification approach has been successful in the delivery of anti-cancer agents, anti-viral drugs, anti-bacterial, immunosuppressant, and natural products such as antioxidants as well as alkaloids. At present, more than four SEDDS drug products are available in the market. SEDDS have tremendous capabilities which are yet to be explored which would be beneficial in oral lipid delivery.

摘要

经口递药存在挑战。自乳化药物传递系统(SEDDS)在解决这个问题方面发挥着至关重要的作用。SEDDS 由油相、表面活性剂、助表面活性剂、乳化剂和共溶剂组成。SEDDS 可分为自微乳给药系统(SMEDDS)和自纳米乳给药系统(SNEDDS)。SEDDS 的特性包括粒径、Zeta 电位分析以及通过电子显微镜和相分离方法观察到的表面形态。SEDDS 可以通过不同的技术进行很好的表征,包括粒径和形态。在 SEDDS 中应用的超饱和现象中,聚合物和共聚物被用于 SEDDS 的制备。超饱和 SEDDS 制剂通过延缓水相中药物分子的成核和晶体生长来抑制药物分子的沉淀,从而在动力学和热力学上抑制药物分子的沉淀。自乳化方法已成功应用于抗癌药物、抗病毒药物、抗菌药物、免疫抑制剂以及抗氧化剂和生物碱等天然产物的传递。目前,市场上有超过四种 SEDDS 药物产品。SEDDS 具有巨大的潜力有待探索,这将有益于口服脂质传递。

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