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脂质纳米乳剂的给药和靶向传递 - 综述。

Drug delivery and drug targeting with parenteral lipid nanoemulsions - A review.

机构信息

Fresenius Kabi Austria GmbH, Hafnerstraße 36, A-8055 Graz, Austria.

Karl-Franzens-University of Graz, Institute of Pharmaceutical Sciences, Department of Pharmaceutical Technology, Member of BioTechMed Graz, Universitätsplatz 1, A-8010 Graz, Austria.

出版信息

J Control Release. 2016 Feb 10;223:85-98. doi: 10.1016/j.jconrel.2015.12.016. Epub 2015 Dec 14.

DOI:10.1016/j.jconrel.2015.12.016
PMID:26699427
Abstract

Lipid nanosized emulsions or nanoemulsions (NE) are oil in water dispersions with an oil droplet size of about 200nm. This size of oil droplets dispersed in a continuous water phase is a prerequisite for the parenteral, namely intravenous administration. Many parenteral nutrition and drug emulsions on the market confirm the safe use of NE over years. Parenteral emulsions loaded with APIs (active pharmaceutical ingredients) are considered as drug delivery systems (DDS). DDS focuses on the regulation of the in vivo dynamics, such as absorption, distribution, metabolism, and extended bioavailability, thereby improving the effectiveness and the safety of the drugs. Using an emulsion as a DDS, or through the use of surface diversification of the dispersed oil droplets of emulsions, a targeted increase of the API concentration in some parts of the human body can be achieved. This review focuses on NE similar to the marketed once with no or only low amount of additional surfactants beside the emulsifier from a manufacturing point of view (technique, used raw materials).

摘要

脂质纳米乳液或纳米乳(NE)是一种油包水型分散体系,其油滴粒径约为 200nm。这种大小的油滴分散在连续的水相中是进行肠外给药(即静脉给药)的前提。多年来,市场上许多肠外营养和药物乳剂证实了 NE 的安全使用。载有 API(活性药物成分)的肠外乳剂被认为是药物传递系统(DDS)。DDS 侧重于调节体内动力学,如吸收、分布、代谢和延长生物利用度,从而提高药物的有效性和安全性。将乳剂用作 DDS,或者通过使用乳化剂对乳液的分散油滴进行表面多样化,可以实现人体某些部位 API 浓度的靶向增加。本综述从制造角度(技术、使用的原材料)关注类似于市售产品的 NE,除了乳化剂外,几乎没有或只有少量额外的表面活性剂。

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