Novel dual VES phospholipid self-assembled liposomes with an extremely high drug loading efficiency

Colloids and Surfaces. B, Biointerfaces
Yongpeng HouXinsong Li

Abstract

Vitamin E succinate (VES), a unique selective anti-cancer drug, has attracted much attention for its ability to induce apoptosis in various cancer cells. Importantly, it has been reported that VES is largely non-toxic to normal cells. However, poor aqueous solubility and bioavailability extensively restricted its clinical utility. In this report, dual VES phospholipid conjugate (di-VES-GPC) prodrug based liposomes were prepared in order to develop an efficient delivery system for VES. Di-VES-GPC was first synthesized by conjugating VES with l-α-glycerophosphorylcholine (GPC) using N,N'-dicyclohexylcarbodiimide (DCC) as a coupling agent. The di-VES-GPC prodrug was able to self-assemble into liposomes by reverse-phase evaporation method. The structure of the liposomes was characterized by dynamic light scattering (DLS), transmission electron microscopy (TEM) and cryo-TEM. The results showed that di-VES-GPC assembled liposomes were spherical with an average diameter approximately 183nm. Cryo-TEM data confirmed the formation of multilamellar liposomes with the bilayer thickness about 5nm by the assembly of the conjugate without any excipient. The VES drug loading highly reaches up to 82.8wt% in the liposomes after a simple calculat...Continue Reading

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