Synthesis and characterization of a novel drug-loaded polymer, poly(lactic acid-co-aminomethyl benzimidazole)
Synthesis and characterization of a novel drug-loaded polymer, poly(lactic acid-co-aminomethyl benzimidazole)
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DOI：
10.1080/15685551.2015.1041085
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发表时间：
2015-05
影响因子：
1.6
通讯作者：
Guang-Zhen Mo;Yan-Cheng Wu;Z. Hao;Qiao-Fang Luo;Xinghui Liang;Liangyu Guan;Zhao‐Yang Wang
中科院分区：
文献类型：
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作者：
Guang-Zhen Mo;Yan-Cheng Wu;Z. Hao;Qiao-Fang Luo;Xinghui Liang;Liangyu Guan;Zhao‐Yang Wang
以氨甲基苯并咪唑（AMB）为苯并咪唑类药物的模型化合物，以d，l-乳酸（LA）为原料，通过直接熔融缩聚法合成了一种潜在的生物可降解载药聚合物聚乳酸-氨甲基苯并咪唑共聚物（PLAAMB）。在LA/AMB摩尔比为40/1时，考察了催化剂种类、用量、缩聚温度、共聚时间等合成条件对合成的影响。以0.4wt%的氧化锡（SnO）为催化剂，在140 ° C预聚8h后，于160 ° C熔融共聚合6h，得到最大重均分子量（Mw）为5300Da的共聚物。差示扫描量热法和X射线衍射法。研究了不同投料比对PLAAMB性能的影响，得到了分子量最大为9400 Da的共聚物PLAAMB。在缩合过程中将药物模型AMB作为单体引入到聚乳酸中后，所得PLAAMB的Tg低于均聚物聚（d，l-乳酸）（PDLLA）的Tg。PLAAMB的分子量和结晶度均能满足载药聚合物在药物释放方面的要求。
Using aminomethyl benzimidazole (AMB) as a model of benzimidazole-type drugs, a potential biodegradable drug-loaded polymer poly(lactic acid-co-aminomethyl benzimidazole) (PLAAMB) is synthesized as designed via direct melt polycondensation starting from d,l-lactic acid (LA). When the molar feed ratio LA/AMB is 40/1, the optimal synthetic conditions, including catalyst type and dosage, polycondensation temperature, and copolymerization time are discussed. After the prepolymerization at 140 °C for 8 h, using 0.4 wt% stannous oxide (SnO) as the catalyst, the melt copolymerization at 160 °C for 6 h gives the copolymer with the biggest weight-average molecular weight (Mw) 5300 Da. The structure and properties of the copolymer are systematically characterized with Fourier transform infrared, 1H NMR, gel permeation chromatography, differential scanning calorimetry, and X-ray diffraction. And the investigations on the influences of different molar feed ratios on the properties of PLAAMB show that, the copolymer PLAAMB with the biggest Mw of 9400 Da can be obtained. After the drug model AMB as a monomer is introduced into polylactic acid during the condensation, the Tg of the obtained PLAAMB is lower than the Tg of homopolymer poly(d,l-lactic acid) (PDLLA). The Mw and crystallinity of PLAAMBs can meet the requirement of drug-loaded polymers in the drug delivery.