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Investigating the role of cholesterol in the formation of non-ionic surfactant based bilayer vesicles: thermal analysis and molecular dynamics.

Abstract：

:The aim of this research was to investigate the molecular interactions occurring in the formulation of non-ionic surfactant based vesicles composed monopalmitoyl glycerol (MPG), cholesterol (Chol) and dicetyl phosphate (DCP). In the formulation of these vesicles, the thermodynamic attributes and surfactant interactions based on molecular dynamics, Langmuir monolayer studies, differential scanning calorimetry (DSC), hot stage microscopy and thermogravimetric analysis (TGA) were investigated. Initially the melting points of the components individually, and combined at a 5:4:1 MPG:Chol:DCP weight ratio, were investigated; the results show that lower (90 °C) than previously reported (120-140 °C) temperatures could be adopted to produce molten surfactants for the production of niosomes. This was advantageous for surfactant stability; whilst TGA studies show that the individual components were stable to above 200 °C, the 5:4:1 MPG:Chol:DCP mixture show ∼2% surfactant degradation at 140 °C, compared to 0.01% was measured at 90 °C. Niosomes formed at this lower temperature offered comparable characteristics to vesicles prepared using higher temperatures commonly reported in literature. In the formation of niosome vesicles, cholesterol also played a key role. Langmuir monolayer studies demonstrated that intercalation of cholesterol in the monolayer did not occur in the MPG:Chol:DCP (5:4:1 weight ratio) mixture. This suggests cholesterol may support bilayer assembly, with molecular simulation studies also demonstrating that vesicles cannot be built without the addition of cholesterol, with higher concentrations of cholesterol (5:4:1 vs 5:2:1, MPG:Chol:DCP) decreasing the time required for niosome assembly.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Wilkhu JS,Ouyang D,Kirchmeier MJ,Anderson DE,Perrie Y

doi

10.1016/j.ijpharm.2013.11.063

subject

Has Abstract

pub_date

2014-01-30 00:00:00

pages

331-41

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(13)01068-5

journal_volume

461

pub_type

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Investigating the role of cholesterol in the formation of non-ionic surfactant based bilayer vesicles: thermal analysis and molecular dynamics.