4.4 Article

Effect of different polysorbates on development of self-microemulsifying drug delivery systems using medium chain lipids

Journal

DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
Volume 44, Issue 2, Pages 215-223

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.1080/03639045.2017.1386202

Keywords

Lipid-based drug delivery; polysorbates; Tweens (R); self-microemulsifying drug delivery systems (SMEDDS); phase diagram; monoglyceride; triglyceride; drug dispersion

Funding

  1. ABITEC Corporation, Columbus, OH, USA

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The primary objective of this study was to develop lipid-based self-microemulsifying drug delivery systems (SMEDDS) without using any organic cosolvents that would spontaneously form microemulsions upon dilution with water. Cosolvents were avoided to prevent possible precipitation of drug upon dilution and other stability issues. Different polysorbates, namely, Tween 20, Tween 40, Tween 60, and Tween 80, were used as surfactants, and Captex 355 EP/NF (glycerol tricaprylate/caprate) or its 1: 1 mixture with Capmul MCM NF (glycerol monocaprylocaprate) were used as lipids. Captex 355-Tween-water ternary phase diagrams showed that oil-in-water microemulsions were formed only when the surfactant content was high (80-90%) and the lipid content low (10-20%). Thus, mixtures of Tweens with Captex 355 alone were not suitable to prepare SMEDDS with substantial lipid contents. However, when Captex 355 was replaced with the 1: 1 mixture of Captex 355 and Capmul MCM, clear isotropic microemulsion regions in phase diagrams with sizes in the increasing order of Tween 20

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