Instituto de Desarrollo Tecnológico para la Industria Química, Universidad Nacional del Litoral - Consejo Nacional de Investigaciones Científicas y Técnicas, Colectora Ruta Nac 168, Paraje El Pozo, Santa Fe CP 3000, Argentina.
Polymer Chemistry and Biomaterials Research Group, Ghent University, Krijgslaan 281, Building S4, Ghent 9000, Belgium.
J Pharm Sci. 2017 Aug;106(8):2106-2114. doi: 10.1016/j.xphs.2017.05.012. Epub 2017 May 20.
Paclitaxel (PTX) incorporation in poly(lactic-co-glycolic acid) (PLGA) matrices produce films with high tensile rigidity and slow release that fail to deliver the required release rate for most biomedical applications such as in drug eluting stents and cancer treatments. To modify and improve this behavior, a set of poly(diol sebacate)s were synthesized and fully characterized as possible additives. The tensile properties of PLGA blends were evaluated as these materials could be used as coatings in drug eluting stent applications. A significant improvement in mechanical flexibility was observed with 20% additive content, as it reduced the Young's modulus value and increased the maximum deformation at break. PTX release was studied and correlated with the release of additive from PLGA films. An increase in the initial burst release phase was observed on all blends when compared to the control films of PLGA. Modulation of PTX release was achieved by altering the hydrophilicity degree of the additive or its percentage content on the blend. This supports the possibility that PTX was partitioned into the additive phase. Cytotoxicity analyses of novel additives were performed on mouse embryonic fibroblasts NIH/3T3.
紫杉醇(PTX)掺入聚(乳酸-共-乙醇酸)(PLGA)基质中会产生具有高拉伸刚性和缓慢释放的薄膜,但无法为大多数生物医学应用(如药物洗脱支架和癌症治疗)提供所需的释放速率。为了改善这种行为,合成了一系列聚(二醇癸二酸酯)并对其进行了全面表征,作为可能的添加剂。研究了 PLGA 共混物的拉伸性能,因为这些材料可用作药物洗脱支架应用中的涂层。添加 20%的添加剂可显著提高机械柔韧性,因为它降低了杨氏模量值并增加了断裂时的最大变形。研究了 PTX 的释放情况,并与 PLGA 薄膜中添加剂的释放进行了相关性研究。与 PLGA 对照薄膜相比,所有共混物的初始突释阶段的释放均增加。通过改变添加剂的亲水性程度或其在共混物中的含量百分比,可以调节 PTX 的释放。这支持了 PTX 被分配到添加剂相的可能性。对新型添加剂进行了小鼠胚胎成纤维细胞 NIH/3T3 的细胞毒性分析。