Department of Biotechnology, Bannari Amman Institute of Technology, Sathyamangalam, Erode 638 401, Tamil Nadu, India.
Saudi Pharm J. 2012 Jul;20(3):263-71. doi: 10.1016/j.jsps.2011.09.004. Epub 2011 Sep 24.
Chitosan-graft-poly (2-hydroxyethyl methacrylate-co-itaconic acid) has been synthesized for different feed ratios of 2-hydroxyethyl methacrylate and itaconic acid and characterized by FT-IR, thermogravimetry and swelling in simulated biological fluids (SBF) and evaluated as a drug carrier with model drug, tramadol hydrochloride (TRM). Grafting decreased the thermal stability of chitosan. FT-IR spectra of tablet did not reveal any molecular level (i.e. at <10 nm scale) drug-polymer interaction. But differential scanning calorimetric studies indicated a probable drug-polymer interaction at a scale >100 nm level. The observed Korsmeyer-Peppas's power law exponents (0.19-1.21) for the in vitro release profiles of TRM in SBF and other drugs such as 5-fluorouracil (FU), paracetamol (PCM) and vanlafaxine hydrochloride (VNF) with the copolymer carriers revealed an anomalous drug release mechanism. The decreased release rates for the grafted chitosan and the enhanced release rate for the grafts with increasing itaconic acid content in the feed were more likely attributed to the enhanced drug-matrix interaction and polymer-SBF interactions, respectively. The different release profiles of FU, PCM, TRM and VNF with the copolymer matrix are attributed to the different chemical structures of drugs. The above features suggest the graft copolymer's candidature for use as a promising oral drug delivery system.
壳聚糖接枝共聚物（2-羟乙基甲基丙烯酸酯-co-衣康酸）已合成，用于不同的 2-羟乙基甲基丙烯酸酯和衣康酸的进料比，并通过 FT-IR、热重分析和在模拟生物流体（SBF）中的溶胀进行了表征，并作为模型药物曲马多盐酸盐（TRM）的药物载体进行了评估。接枝降低了壳聚糖的热稳定性。片剂的 FT-IR 光谱没有显示任何分子水平（即<10nm 尺度）的药物-聚合物相互作用。但是，差示扫描量热法研究表明，在>100nm 尺度上可能存在药物-聚合物相互作用。在 SBF 和其他药物（如 5-氟尿嘧啶（FU）、对乙酰氨基酚（PCM）和盐酸文拉法辛（VNF））中，观察到的体外释放曲线的 Korsmeyer-Peppas 幂律指数（0.19-1.21）表明药物释放机制异常。接枝壳聚糖的释放速率降低和接枝物中衣康酸含量增加时释放速率提高，可能归因于药物-基质相互作用和聚合物-SBF 相互作用的增强。FU、PCM、TRM 和 VNF 与共聚物基质的不同释放曲线归因于药物的不同化学结构。上述特征表明接枝共聚物有希望作为一种有前途的口服药物递送系统使用。
