SPONTANEOUS FORMATION OF DRUG-CONTAINING AMPHIPHILIC BETA-CYCLODEXTRIN NANOCAPSULES

A new colloidal carrier system, nanocapsules, using 2,3-diacyl-O-beta- cyclodextrins is described. The nanocapsules were prepared by adding a mixture of an organic solution of 2,3-diacyl-O-beta-cyclodextrins (wi th or without a lipophilic surfactant) and an oily phase to an aqueous solution (with or without a hydrophilic surfactant) whilst stirring. Nanocapsules with a mean size of 200 nm are formed progressively. Dire ct microscopic observation of the particles was carried out using tran smission electron microscopy (TEM) combined with the freeze-fracture m ethod. The influence of different constituents on the preparation proc ess was studied: type of 2,3-diacyl-O-beta-cyclodextrins (beta-CD-C-6, beta-CD-C-12 and beta-CD-C-14), nature of the oily phase (benzyl benz oate, Miglyol 812(R)), and the surfactants used (Pluronic PEF68(R), Sp an 85(R)). An investigation of lipophilic drug encapsulation was also carried out. The results of this study suggest that nanocapsules of 2, 3-diacyl-O-beta-cyclodextrins could be considered as a potential collo idal drug carrier system. Copyright (C) 1996 Elsevier Science B.V.