Chemical Laboratory, Central Leather Research Institute, Council of Scientific and Industrial Research, Adyar, Chennai 600020, India.
Mater Sci Eng C Mater Biol Appl. 2013 Dec 1;33(8):4651-9. doi: 10.1016/j.msec.2013.07.020. Epub 2013 Jul 24.
Formulation of biodegradable collagen-poly-ε-caprolactone (PCL) based biomaterials for the sustained release of insulin is the main objective of the present work. PCL has been employed to modulate the physico-chemical behavior of collagen to control the drug release. Designed formulations were employed to statistically optimize insulin release parameter profile at different collagen to PCL molar ratios. Circular dichroism, thermoporometry, FTIR, impedance and scanning electron microscopy techniques have been employed to investigate the effect of PCL on hydration dynamics of the collagen molecule, which in turn changes the dissolution parameters of the drug from the systems. Drug entrapment efficiency has been found to be maximum for collagen to PCL molar ratio of 1:2 (>90%). In vitro dissolution test reveals that 99% of the drug was released from composite at collagen to PCL molar ratio of 1:3 and 1:4 within 2h, which indicates that hydrophobicity of the matrix results in weak interaction between lipophilic drug and carrier materials. The least burst release was observed for collagen to PCL molar ratio at 1:2 as synergistic interactions between collagen and PCL was maximum at that particular polymer-polymer ratios. The drug release data indicates super case-II transport of drug (n>1.0).
本工作的主要目标是制备可生物降解的胶原蛋白-聚己内酯（PCL）基生物材料，以实现胰岛素的持续释放。PCL 已被用于调节胶原蛋白的物理化学行为，以控制药物释放。设计的配方被用于在不同胶原蛋白与 PCL 摩尔比下统计优化胰岛素释放参数曲线。圆二色性、热膨胀法、傅里叶变换红外光谱、阻抗和扫描电子显微镜技术已被用于研究 PCL 对胶原蛋白分子水合动力学的影响，这反过来又改变了系统中药物的溶解参数。对于胶原蛋白与 PCL 的摩尔比为 1:2（>90%），药物包封效率最高。体外溶解试验表明，在胶原蛋白与 PCL 的摩尔比为 1:3 和 1:4 时，99%的药物在 2 小时内从复合材料中释放出来，这表明基质的疏水性导致亲脂性药物与载体材料之间的相互作用较弱。对于胶原蛋白与 PCL 的摩尔比为 1:2，观察到最小的突释释放，因为在该特定的聚合物-聚合物比下，胶原蛋白和 PCL 之间的协同相互作用最大。药物释放数据表明药物的超 II 型（n>1.0）传递。
