College of Pharmacy, Department of Pharmaceutical Technology, Freie Universität Berlin, Berlin, Germany.
Pharm Dev Technol. 2021 Mar;26(3):262-268. doi: 10.1080/10837450.2020.1863427. Epub 2020 Dec 26.
Self-emulsifying lipids (SEL) were used as a stabilizer for the preparation of dexamethasone lipid nanoparticles by membrane emulsification employing Shirasu porous glass. The effect of process and formulation parameters on the size and polydispersity and dexamethasone solubility in lipids and its release from lipid nanoparticles were investigated. Lipid phase pressure (40-80 kPa), membrane pore-size (0.1 - 0.4 µm) and agitation speed (300 - 900 rpm) did not affect the size and polydispersity of SEL. However, the size was increased with increasing lipid content and fatty acid chain of the lipid. Sizes of < 250 nm were achieved from TEGO care:Gelucire blend and it increased to 487 nm by adding 20% w/w of hard fat. The highest solubility of dexamethasone was found in TEGO care 450 (29 mg/g). Release from the lipid nano-dispersions was extended with no burst effect and the absolute release was increased with increasing lipid content.
自乳化脂质 (SEL) 被用作通过 Shirasu 多孔玻璃的膜乳化制备地塞米松脂质纳米粒的稳定剂。考察了工艺和配方参数对 SEL 的大小、多分散性以及地塞米松在脂质中的溶解度和从脂质纳米粒中释放的影响。脂质相压力（40-80 kPa）、膜孔大小（0.1-0.4 µm）和搅拌速度（300-900 rpm）对地塞米松脂质纳米粒的大小和多分散性没有影响。然而，随着脂质含量和脂质脂肪酸链的增加，尺寸会增大。TEGO care：Gelucire 混合物的粒径小于 250nm，而添加 20%w/w 的硬脂酸后粒径增加到 487nm。TEGO care 450 的地塞米松溶解度最高（29mg/g）。从脂质纳米分散体中的释放没有突释效应，并且随着脂质含量的增加，绝对释放量增加。
