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Interaction of retinol with dipalmitoylphosphatidylcholine and their formation of small dispersed particles.
Authors:Y Asai  S Watanabe
Institution:Formulation Research Laboratory, Kawashima, Eisai Co., Ltd., Japan.
Abstract:Stable aqueous dispersions of all-trans-retinol (vitamin A, VA) were obtained by sonication with dipalmitoylphos-phatidylcholine (DPPC) in the VA mole fraction range 0.1-0.7. In order to clarify the dispersal mechanism, the dispersed particles were characterized and the interaction between VA and DPPC was investigated using several physicochemical techniques. Dynamic light scattering measurements showed that the diameter of the dispersed particles was 50-70 nm. A limited amount of VA was incorporated into DPPC bilayer membranes (approximately 5 mol%). The trapped aqueous volume inside the particles was determined fluorometrically using the aqueous space marker calcein and the volume in the VA/DPPC particles was decreased markedly with the addition of VA into small unilamellar vesicles of DPPC. The decline in the fraction of vesicular particles was also confirmed by fluorescence quenching of N-dansylhexadecylamine in the DPPC membrane by the addition of the quencher CuSO4. These results indicate that the excess VA separated from the DPPC bilayers is stabilized as emulsion particles by the DPPC surface monolayer.
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