Mandal T K, Lopez-Anaya A, Onyebueke E, Shekleton M
College of Pharmacy, Xavier University of Louisiana, New Orleans 70125, USA.
J Microencapsul. 1996 May-Jun;13(3):257-67. doi: 10.3109/02652049609026014.
Sustained release biodegradable microcapsules of AZT were prepared using different concentrations of copolymer of poly(lactic/glycolic) acid (PLGA 50:50 and PLGA 90:10). Solid microcapsules were collected following the complete evaporation of the solvent. The yield of microcapsules was increased two fold with a two-fold increase of the polymer concentration. The efficiency of encapsulation of AZT was also increased with the increase of the polymer concentration. These microcapsules were characterized using scanning electron microscopy. The dissolution of AZT from the microcapsules of PLGA (50: 50) was higher than the microcapsules of PLGA (90:10); the PLGA (50:50) microcapsules containing 1:10 drug/polymer ratio showed higher dissolution than the microcapsules containing 1:20 drug/polymer ratio. The PLGA (90:10) microcapsules containing 1:6 drug/polymer ratio showed higher dissolution than the microcapsules containing 1:10 drug/polymer ratio. In conclusion, the dissolution of AZT was dependent on the type of the copolymer used and the relative concentrations of the drug and the copolymer.
使用不同浓度的聚乳酸/乙醇酸共聚物(PLGA 50:50和PLGA 90:10)制备了齐多夫定的缓释可生物降解微胶囊。在溶剂完全蒸发后收集固体微胶囊。微胶囊的产率随着聚合物浓度的两倍增加而增加了两倍。齐多夫定的包封效率也随着聚合物浓度的增加而提高。使用扫描电子显微镜对这些微胶囊进行了表征。PLGA(50:50)微胶囊中齐多夫定的溶出度高于PLGA(90:10)微胶囊;药物/聚合物比例为1:10的PLGA(50:50)微胶囊的溶出度高于药物/聚合物比例为1:20的微胶囊。药物/聚合物比例为1:6的PLGA(90:10)微胶囊的溶出度高于药物/聚合物比例为1:10的微胶囊。总之,齐多夫定的溶出度取决于所用共聚物的类型以及药物和共聚物的相对浓度。