Karthikeyan K, Vijayalakshmi Ezhilarasan, Korrapati Purna Sai
Biomaterials Division, CSIR - Central Leather Research Institute, Adyar, Chennai, 600020, India.
AAPS PharmSciTech. 2014 Oct;15(5):1172-80. doi: 10.1208/s12249-014-0151-6. Epub 2014 May 30.
In this study, we have evaluated the interactions of zein microspheres with different class of drugs (hydrophobic, hydrophilic, and amphiphilic) using in vitro and in silico analysis. Zein microspheres loaded with aceclofenac, metformin, and promethazine has been developed by solvent evaporation technique and analyzed for its compatibility. The physical characterization depicted the proper encapsulation of hydrophobic drug in the microspheres. The in vitro release study revealed the sustaining ability of the microspheres in the following order: hydrophobic > hydrophilic > amphiphilic. In silico analysis also confirmed the better binding affinity and greater interactions of hydrophobic drug with zein. The above results revealed that zein is more suitable for hydrophobic drugs in the development of sustained drug delivery systems using solvent evaporation technique. The study therefore envisages a scope for identifying the most suitable polymer for a sustained drug delivery system in accordance with the nature of the drug.
在本研究中，我们使用体外和计算机模拟分析评估了玉米醇溶蛋白微球与不同种类药物（疏水性、亲水性和两亲性）之间的相互作用。通过溶剂蒸发技术制备了负载醋氯芬酸、二甲双胍和异丙嗪的玉米醇溶蛋白微球，并对其相容性进行了分析。物理表征表明疏水性药物在微球中得到了适当的包封。体外释放研究显示微球的缓释能力顺序为：疏水性＞亲水性＞两亲性。计算机模拟分析也证实了疏水性药物与玉米醇溶蛋白具有更好的结合亲和力和更强的相互作用。上述结果表明，在使用溶剂蒸发技术开发缓释药物递送系统时，玉米醇溶蛋白更适合疏水性药物。因此，该研究设想了根据药物性质确定最适合用于缓释药物递送系统的聚合物的可能性。
