Degradation behaviour of microspheres prepared by spray-drying poly(D,L-lactide) and poly(D,L-lactide-co-glycolide) polymers

被引:58
作者
Blanco, M. Dolores [1 ]
Sastre, Roberto L. [1 ]
Teijon, Cesar [1 ]
Olmo, Rosa [1 ]
Teijon, Jose M. [1 ]
机构
[1] Univ Complutense Madrid, Fac Med, Dept Bioquim & Biol Mol, E-28040 Madrid, Spain
关键词
poly(D; L-lactide); poly(lactide-co-glycolide); spray-dryer; microspheres; degradation;
D O I
10.1016/j.ijpharm.2006.07.030
中图分类号
R9 [药学];
学科分类号
1007 [药学];
摘要
Polymeric microsphere degradation must be taken into account in the design of drug delivery systems to be injected in in vivo systems, thus a prior analysis of in vitro degradation behaviour of microspheres appears to be necessary. In this study degradation characteristics of poly(lactide-co-glycolide) (PLGA) and Poly(D,L-lactide) (PLA) microspheres prepared by the spray-drying technique have been examined. It was found that a slow decrease in molecular weight took place during the first stage of degradation, and the value of the rate constant decreased with the increase of the percentage of lactic acid of the polymer in a linear way. Thus, the period of time of this first stage decreased with the increase of content of glycolidyl units of the polymer, and it was the unique stage observed in PLA microspheres after 5 months of study. During this period of time, significant mass loss was not observed in the microspheres. The second stage of degradation of PLGA microspheres showed a larger rate constant, whose value increased with the content of glycolidyl units of the polymer. Mass loss was observed from number-average molecular weight about 6000. A sharp decrease of glass transition temperature (T-g) was observed coinciding with the start of mass loss. This fact was accompanied by a physical change of the samples, fusion of microspheres to form large particles, which also fusion to form a unique mass of polymer; moment from that the degradation process was quicker. (c) 2006 Published by Elsevier B.V.
引用
收藏
页码:139 / 147
页数:9
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