LIPOSOMES AS A CARRIER FOR ORAL-ADMINISTRATION OF INSULIN - EFFECT OF FORMULATION FACTORS

被引:55
作者
CHOUDHARI, KB
LABHASETWAR, V
DORLE, AK
机构
[1] Department of Pharmaceutical Sciences, Nagpur University Campus, Nagpur
关键词
Efficiency; -; Evaporation; Liposomes; Solvents;
D O I
10.3109/02652049409040461
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
The present work was undertaken to study the effect of liposome formulation factors on its efficiency as a carrier for oral administration of insulin. The insulin-liposomes were prepared by two methods: solvent evaporation hydration and solvent spherule evaporation, with various variables such as concentration of insulin (1), lecithin (L), cholesterol (C), and Tween-80 (T). It was found that the insulin-liposomes when administered orally could produce hypoglycaemia. Variation in liposome composition was found to affect the efficiency of liposome as a carrier for oral administration of insulin. A liposome system containing L, 100 mg; C, 20 mg; 1, 150 units; T, 1 per cent v/v, and prepared by the solvent spherule evaporation method was found to be most effective. The effect of insulin-liposome had prolonged action in diabetes-induced rabbits compared with that in normal rabbits. The results of the insulin-liposome system were comparable with the action of 1 unit of insulin/kg administered subcutaneously.
引用
收藏
页码:319 / 325
页数:7
相关论文
共 11 条
[1]  
Deamer D.W., Uster P.S., Liposome preparation: methods and mechanisms. Liposomes, pp. 27-51, (1982)
[2]  
Kakyshkina M.L., Urazmanov R.I., Effect of cholesterol containing liposomes on amphotecilin B activity in perfused rat liver cells. Liposomy zkh vzaimodeisatvie kletkami tkanyami mater vses simp, 1980, pp. 152-158, (1981)
[3]  
Patel H.M., Rayman B.E., Orally administered liposomally entrapped insulin, Biochemistry Society Transactions, 5, pp. 1739-1741, (1977)
[4]  
Sato Y., Kiwada H., Kato Y., Effect of dose and vesicle size on the pharmacokinetics of liposomes, Chemical and Pharmaceutical Bulletin, 34, pp. 4244-4252, (1986)
[5]  
Scheen A.J., Paquot N., Lefebvre P.J., Perspectives on typical routes of insulin administration
[6]  
oral, rectal, and nasal routes, Annates ĎEndocrinologie, 49, pp. 386-390, (1988)
[7]  
Stefanov A.V., Kononenko I.N., Lishko V.K., Shevchnko A.V., Effect of liposomally entrapped insulin administered per os on the blood glucose level in normal and diabetic rats, Ukrainskii Biokhimicheskii Zhurnal, 52, pp. 497-500, (1980)
[8]  
Stefanov A.V., Lishko V.K., Shevchnko A.V., Efimov A.S., Khovaka V.V., Hypoglycemic effect of insulin incorporated into liposomes after oral administration to animals with different types of experimental diabetes, Ukrainskii Biokhimicheskii Zhurnal, 58, pp. 58-64, (1986)
[9]  
Szoka F., Papahadjopoulos D., Comparative properties and methods of preparation of lipid vesicles, Annual Review of Biophysics and Bioengineering, 9, pp. 467-508, (1980)
[10]  
Weissner J.H., Mar H., Baskin D.G., Hwang K.J., Peptide-carrier interaction: induction of liposome fusion and aggregation by insulin, Journal of Pharmaceutical Sciences, 75, pp. 259-263, (1986)