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乳化剂浓度、组成和添加顺序对角鲨烯-磷脂酰胆碱油包水乳状液的影响。

Effects of emulsifier concentration, composition, and order of addition in squalene-phosphatidylcholine oil-in-water emulsions.

机构信息

Infectious Disease Research Institute, Seattle, Washington 98104, USA.

出版信息

Pharm Dev Technol. 2011 Oct;16(5):511-9. doi: 10.3109/10837450.2010.495397. Epub 2010 Jun 16.

Abstract

Development and characterization of stable and biocompatible oil-in-water emulsions is important for improved drug and vaccine delivery. In this work, two-component emulsions consisting of squalene and phosphatidylcholine have been developed. The reproducibility of the manufacturing process is established and production efficiency is improved by altering the order of component addition. The effects of emulsifier concentration and composition on emulsion stability and biocompatibility are assessed through dynamic light scattering, zeta potential measurement, viscosity, and hemolytic activity. High concentrations of egg phosphatidylcholine emulsifier decreased initial particle size and increased initial size polydispersity. However, high emulsifier concentrations also appeared to decrease long-term emulsion stability as well as absolute zeta potential values. Substitution of naturally derived egg phosphatidylcholine with synthetic 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC) produced an emulsion with similar physicochemical properties and stability.

摘要

开发和表征稳定且具有生物相容性的油包水乳剂对于改善药物和疫苗的传递至关重要。在这项工作中,开发了由角鲨烯和磷脂酰胆碱组成的两亲性乳剂。通过改变成分添加顺序,建立了制造过程的重现性并提高了生产效率。通过动态光散射、zeta 电位测量、粘度和溶血活性评估乳化剂浓度和组成对乳液稳定性和生物相容性的影响。高浓度的蛋黄磷脂酰胆碱乳化剂降低了初始粒径并增加了初始粒径多分散性。然而,高浓度的乳化剂似乎也降低了长期乳液稳定性和绝对 zeta 电位值。用合成的 1-棕榈酰基-2-油酰基-sn-甘油-3-磷酸胆碱(POPC)代替天然来源的蛋黄磷脂酰胆碱,产生了具有相似理化性质和稳定性的乳液。

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