Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Innsbruck, Austria.
Department of Industrial Pharmacy, Faculty of Pharmacy, University of Medicine and Pharmacy at Ho Chi Minh city, Ho Chi Minh city, Vietnam.
Drug Dev Ind Pharm. 2021 Jan;47(1):22-35. doi: 10.1080/03639045.2020.1851241. Epub 2020 Dec 6.
The aim of this study was the evaluation of the influence of bile salts and fatty acids, important components of intestinal fluids, on physical characteristics of self-emulsifying drug delivery systems (SEDDS) such as size, polydispersity (PDI), zeta potential (Zp), turbidity (T%), cloud point temperature (CPT) and drug release. At this purpose, nonionic (ni-SEDDS) and cationic (c-SEDDS) were emulsified in aqueous media containing increasing concentrations of bile salts (BS) and decanoate (Dec). Zp of ni-SEDDS and c-SEDDS became highly negative at 15 mM BS and Dec. Size of ni-SEDDS decreased of 112 nm and of 76 nm at 15 mM BS and Dec, respectively. Size of c-SEDDS decreased of 53 nm at 15 mM BS, but it was not affected by 15 mM Dec. PDI and T% of ni- and c-SEDDS were lowered as well. CPT of ni-SEDDS increased from 70 °C to 97 °C and 84 °C at 15 mM BS and Dec. CPT of c-SEDDS decreased from above 100 °C to 80 °C and to 85 °C at 1.5 mM BS and at 5 mM Dec, respectively. Generally, BS had a more pronounced effect on SEDDS Zp, size, PDI, T %, and CPT than Dec. The release of the model drug quinine was accelerated by BS and Dec. As BS and fatty acids affect the physical characteristics and drug release behavior of SEDDS, their impact should be addressed during the development process.
本研究旨在评估胆汁盐和脂肪酸（肠液的重要组成部分）对自乳化药物传递系统（SEDDS）物理特性的影响，如粒径、多分散性（PDI）、Zeta 电位（Zp）、浊度（T%）、相转变温度（CPT）和药物释放。为此，非离子型（ni-SEDDS）和阳离子型（c-SEDDS）在含有不同浓度胆汁盐（BS）和癸酸（Dec）的水介质中乳化。ni-SEDDS 和 c-SEDDS 的 Zp 在 15mMBS 和 Dec 时变为高度负电性。ni-SEDDS 的粒径分别降低了 112nm 和 76nm，c-SEDDS 的粒径降低了 53nm。ni-和 c-SEDDS 的 PDI 和 T%也降低了。ni-SEDDS 的 CPT 从 70°C 增加到 97°C 和 84°C，BS 和 Dec 浓度分别为 15mM。c-SEDDS 的 CPT 从高于 100°C 降低到 80°C 和 85°C，BS 和 Dec 浓度分别为 1.5mM 和 5mM。一般来说，BS 对 SEDDS 的 Zp、粒径、PDI、T%和 CPT 的影响大于 Dec。BS 和 Dec 加速了模型药物奎宁的释放。由于 BS 和脂肪酸会影响 SEDDS 的物理特性和药物释放行为，因此在开发过程中应考虑其影响。
