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A Spray-Drying Method for Mass Production of Liposomes.

1991; Pharmaceutical Society of Japan; Volume: 39; Issue: 6 Linguagem: Inglês

10.1248/cpb.39.1522

1347-5223

Hiroshi KUKUCHI, Hitoshi Yamauchi, Sadao Hirota,

Analytical Chemistry and Chromatography

A spray-drying method for the mass production of liposomes was developed : lipids were dissolved in a volatile organic solvent such as chloroform in which, in some cases, a core material such as mannitol was additionally suspended, and the organic solution or suspension was then spray-dried. Addition of core material particles or the use of hydrogenated lecithins increased the recovery of the lipid mixture prepared by spray-drying. Since the obtained spray-dried product was very amorphous, it could be easily hydrated with an aqueous solution, and lipid vesicles (lisopomes) were spontaneously formed by agitating. These spray-dried (SD) liposomes were characterized in comparison with the traditional liposomes known as Bangham's liposomes.Incorporation of cholesterol into the SD-liposomal membrane was confirmed by differential scanning calorimetry and gel filtraiton chromatography. Incorporation of charged lipids was confirmed by the zeta potential of liposomes.The size distribution of the unextruded SD-liposomes was similar to that of Bangham's liposomes, and a more homogeneous size distribution could be obtained by the extrusion technique. When glucose and dextran were used as water-soluble model drugs, the encapsulation efficiency was 15-65% depending on the total lipid concentration. Increasing the practical surface area of the lipid mixture using a core material was considered to cause a noticeably high encapsulation efficiency of dextran into the SD-liosomes.This spray-drying method was found to be useful and valuable for the mass production of liposomes.