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首页> 外文期刊>International Journal of Pharmaceutics >PLGA-PEG microspheres of teverelix: influence of polymer type on microsphere characteristics and on teverelix in vitro release.
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PLGA-PEG microspheres of teverelix: influence of polymer type on microsphere characteristics and on teverelix in vitro release.

机译：teverelix的PLGA-PEG微球：聚合物类型对微球特性和teverelix体外释放的影响。

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Teverelix microspheres were produced by coacervation using a new type of poly(ester-carbonates) made of block copolymers of poly(lactic-glycolic acid) (PLGA) and poly(ethylene glycol) (PEG). Five different PLGA-PEG copolymers and one PLGA were used. The 'stability window' has been determined for all polymers. It varied depending on the molecular weight and the weight percentage of PEG. With increasing core loading (from 9.4 to 34.2%), the microparticle size increased from 10-50 to 5-1000 micrometer. The core loading did not have any influence on encapsulation yield, which remained above 80%. The influence of polymer type on microsphere characteristics was studied at two different core loadings: 9.4 and 28%. At a low core loading, the nature of the polymer had no influence on microsphere characteristics whereas at 28%, only PLGA-PEG copolymers gave acceptable microparticles in term of particle size. At 28%, the glass transition temperature (T(g)) of loaded particles was 1-8 degrees C higher than the T(g) of the corresponding polymer. Increasing the core loading increased teverelix release whereas polymer degradation was decreased. All microparticles made of PLGA-PEG copolymers showed a faster release of teverelix than PLGA-based microspheres, whatever the core loading. One PLGA-PEG was selected on the basis of in vitro release rate for further in vivo investigations.
机译：通过使用由聚乳酸-乙醇酸（PLGA）和聚乙二醇（PEG）的嵌段共聚物制成的新型聚（酯-碳酸酯）凝聚来生产Teverelix微球。使用了五种不同的PLGA-PEG共聚物和一种PLGA。已为所有聚合物确定了“稳定性窗口”。它根据PEG的分子量和重量百分比而变化。随着核心负载的增加（从9.4％增至34.2％），微粒尺寸从10-50微米增加到5-1000微米。芯负载对包封率没有任何影响，包封率保持在80％以上。研究了聚合物类型对微球特性的影响，这是在两种不同的核心载荷下进行的：9.4％和28％。在低芯负荷下，聚合物的性质对微球特性没有影响，而在28％的情况下，只有PLGA-PEG共聚物在粒径方面提供可接受的微粒。负载颗粒的玻璃化转变温度（T（g））为28％，比相应聚合物的T（g）高1-8摄氏度。增加核心负载增加了teverelix的释放，而降低了聚合物的降解。无论核心负载如何，所有由PLGA-PEG共聚物制成的微粒都比基于PLGA的微球显示出更快的teverelix释放。基于体外释放速率选择一种PLGA-PEG用于进一步的体内研究。

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