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Polyester-based microparticles of different hydrophobicity: the patterns of lipophilic drug entrapment and release

机译:疏水性不同的聚酯基微粒:亲脂性药物的截留和释放方式

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The paper is devoted to the investigation of the effect of polyester hydrophobicity and ability for crystallisation on lipophilic drug loading and release from microparticles fabricated on the base of these polymers. Poly(l-lactic acid), poly(d, l-lactic acid) and poly (lactic acid-co-glycolic acid) were synthesised by ring-opening polymerisation using stannous octoate as catalyst, while poly(caprolactone) (PCL) and poly(-pentadecalactone) (PPDL) formation was catalysed by lipase. The particles were formed via single emulsion evaporation/diffusion method. The particles obtained were studied using SEM, XRD and DSC methods. The degradation of particles based on different polyesters, entrapment and release of a model hydrophobic drug (risperidone (R)) were thoroughly studied. The effect of particles hydrophobicity and crystallinity on these parameters was of most interest. The drug entrapment is greater for the hydrophobic polymers. Drug release was more rapid from crystalline particles (PLLA, PCL, PPDL), than from amorphous PDLLA and PLGA ones.
机译:该论文致力于研究聚酯疏水性和结晶能力对亲脂性药物负载和从基于这些聚合物制造的微粒中释放的影响。以辛酸亚锡为催化剂,通过开环聚合反应合成了聚(l-乳酸),聚(d,l-乳酸)和聚(乳酸-乙醇酸共聚物),而聚(己内酯)(PCL)和脂肪酶催化聚(十五碳内酯)(PPDL)的形成。通过单乳液蒸发/扩散方法形成颗粒。使用SEM,XRD和DSC方法研究获得的颗粒。彻底研究了基于不同聚酯的颗粒的降解,典型疏水性药物(利培酮(R))的截留和释放。颗粒疏水性和结晶度对这些参数的影响是最令人感兴趣的。对于疏水性聚合物,药物截留更大。结晶颗粒(PLLA,PCL,PPDL)的药物释放比无定形PDLLA和PLGA的药物释放更快。

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