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Biodegradation of in situ-forming gel of poly(DLLA-co-CL) in vivo

机译:聚(DLLA-co-CL)原位形成凝胶在体内的生物降解

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Poly(dl-lactide-co-caprolactone) was dissolved in N-methyl-2-pyrolidone (NMP) for preparing blank group formulation, and drug group was prepared by dissolving testosterone undecanoate (TU) as model drug in blank group. These formulations rapidly gelled by solvent diffusion effect after subcutaneous injection. The in vivo degradation of copolymer gel in rabbits was investigated after injection. The GPC and ~1H NMR results showed that no matter the gel contained drug or not, it had no effect on degradation rate for the P(DLLA-co-CL) carrier. Degradation products of copolymer were absorbed or excreted based on metabolism. Copolymer molar composition changed slightly in 3 months. The structures and characteristic of copolymers were characterized via DSC, TGA, and SEM, respectively. Experimental results showed that the copolymer had excellent heat resistance. Crystallinity increased gradually during degradation process. A dense cross-sectional structure formed after 90 days. In addition, it can be obviously found that the degradation process of the copolymer proceeded in two steps. Mechanism of copolymer biodegradation in vivo was bulk degradation. The gel could well administrate the release of TU in a sustained way without significant burst features.
机译:将聚(dl-丙交酯-己内酯)溶解在N-甲基-2-吡咯烷酮(NMP)中以制备空白组制剂,并通过将十一烷酸睾丸激素(TU)溶解为空白组来制备药物组。这些制剂在皮下注射后通过溶剂扩散作用迅速胶凝。注射后研究了共聚物凝胶在兔体内的降解。 GPC和〜1H NMR结果表明,无论凝胶中是否含有药物,它都对P(DLLA-co-CL)载体的降解速率没有影响。共聚物的降解产物根据新陈代谢被吸收或排出。共聚物的摩尔组成在3个月内略有变化。分别通过DSC,TGA和SEM表征了共聚物的结构和特性。实验结果表明该共聚物具有优异的耐热性。在降解过程中,结晶度逐渐增加。 90天后形成致密的横截面结构。另外,显然可以发现共聚物的降解过程分两个步骤进行。共聚物在体内的生物降解机理是本体降解。该凝胶可以很好地持续释放TU,而没有明显的破裂特征。

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