Department of Pharmaceutics, P.E. Society's Modern College of Pharmacy, Nigdi, Pune-411044, Maharashtra State, India.
Saudi Pharm J. 2013 Oct;21(4):327-35. doi: 10.1016/j.jsps.2012.10.003.
Drug release from various polymers is generally governed by the type of polymer/s incorporated in the formulation and mechanism of drug release from polymer/s. A single polymer may show one or more mechanisms of drug release out of which one mechanism is majorly followed for drug release. Some of the common mechanisms of drug release from polymers were, diffusion, swelling, matrix release, leaching of drug, etc. Mechanism or rate of drug release from a polymer or a combination of polymers can be predicted by using different computational methods or models. These models were capable of predicting drug release from its dosage form in advance without actual formulation and testing of drug release from dosage form. Quantitative structure-property relationship (QSPR) is an important tool used in the prediction of various physicochemical properties of actives as well as inactives. Since last several decades QSPR has been applied in new drug development for reducing the total number of drugs to be synthesized, as it involves a selection of the most desirable compound of interest. This technique was also applied in predicting in vivo performance of drug/s for various parameters. QSPR serves as a predictive tool to correlate structural descriptors of molecules with biological as well as physicochemical properties. Several researchers have contributed at different extents in this area to modify various properties of pharmaceuticals. The present review is focused on a study of different polymers that influence the transportability profiles of drugs along with the application of QSPR either to study different properties of polymers that regulate drug release or in predicting drug transportability from different polymer systems used in formulations.
各种聚合物的药物释放通常受配方中聚合物类型和药物从聚合物中释放的机制控制。单一聚合物可能表现出一种或多种药物释放机制,其中一种机制主要用于药物释放。聚合物中药物释放的一些常见机制包括扩散、溶胀、基质释放、药物浸出等。可以使用不同的计算方法或模型来预测聚合物或聚合物组合中药物的释放机制或释放速率。这些模型能够在不进行实际制剂和药物释放测试的情况下,提前预测药物从制剂中的释放情况。定量构效关系(QSPR)是一种用于预测活性和非活性物质各种物理化学性质的重要工具。几十年来,QSPR 已应用于新药开发,以减少需要合成的药物总数,因为它涉及到选择最理想的感兴趣化合物。该技术还应用于预测药物的体内性能的各种参数。QSPR 是一种预测工具,用于将分子的结构描述符与生物和物理化学性质相关联。许多研究人员在这一领域做出了不同程度的贡献,以改变药物的各种性质。本综述重点研究了不同聚合物对药物输送特性的影响,以及 QSPR 的应用,无论是研究调节药物释放的聚合物的不同性质,还是预测不同聚合物系统中药物的输送能力。