Formulation of Bicelles Based on Lecithin-Nonionic Surfactant Mixtures

基于卵磷脂-非离子表面活性剂混合物的双层脂质体配方

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Abstract

Bicelles have been intensively studied for use as drug delivery carriers and in biological studies, but their preparation with low-cost materials and via a simple process would allow their use for other purposes as well. Herein, bicelles were prepared through a semi-spontaneous method using a mixture of hydrogenated soybean lecithin (SL) and a nonionic surfactant, polyoxyethylene cholesteryl ether (ChEO(10)), and then we investigated the effect of composition and temperature on the structure of bicelles, which is important to design tailored systems. As the fraction of ChEO(10) (X(C)) was increased, a bimodal particle size distribution with a small particle size of several tens of nanometers and a large particle size of several hundred nanometers was obtained, and only small particles were observed when X(C) ≥ 0.6, suggesting the formation of significant structure transition (liposomes to bicelles). The small-angle neutron scattering (SANS) spectrum for these particles fitted a core-shell bicelle model, providing further evidence of bicelle formation. A transition from a monomodal to a bimodal size distribution occurred as the temperature was increased, with this transition taking place at lower temperatures when higher SL-ChEO(10) concentrations were used. SANS showed that this temperature-dependent size change was reversible, suggesting the SL-ChEO(10) bicelles were stable against temperature, hence making them suitable for several applications.

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