TOPICAL LIPOSOMAL LOCAL-ANESTHETICS - DESIGN, OPTIMIZATION AND EVALUATION OF FORMULATIONS

被引：28

作者：

FOLDVARI, M ^{[1
]}

GESZTES, A ^{[1
]}

MEZEI, M ^{[1
]}

CARDINAL, L ^{[1
]}

KOWALCZYK, I ^{[1
]}

BEHL, M ^{[1
]}

机构：

[1] DALHOUSIE UNIV,HALIFAX B3H 3J5,NS,CANADA

来源：

DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY | 1993年 / 19卷 / 19期

关键词：

D O I：

10.3109/03639049309047198

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

To improve the rate of penetration into the skin, and to develop an effective topical anesthetic product, selected local anesthetic agents, benzocaine, lidocaine, dibucaine, etidocaine and tetracaine were encapsulated into liposomes using the solvent evaporation method. After the pilot experiments, tetracaine was selected for further development. Encapsulation efficiency was determined by centrifugation of liposomes and spectrophotometric analysis of liposome pellets and supernatants. Physical stability and organoleptic properties of the various liposomal tetracaine formulas were monitored visually and by microscopy for 1 year. Tetracaine was found to be suitable for the development of a liposomal drug delivery system with high encapsulation efficiency (60-90%) and physical stability. The results showed that encapsulation efficiency of tetracaine into liposomes can be increased by increasing drug concentration and pH, and including negatively charged stearic acid or unsaturated lipids in the formula. Stability of tetracaine increased with higher encapsulation efficiency, however the shelf life of the product was still short (2 months). In-process and finished product quality control parameters are suggested to facilitate the topical liposomal product development in general.

引用

页码：2499 / 2517

页数：19

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