Gupta Meher Kanta, Bajpai Jaya, Bajpai Anil Kumar
Bose Memorial Research Laboratory, Department of Chemistry, Govt. Model Science (Autonomous) College, Jabalpur, M.P., 482001, India.
Bose Memorial Research Laboratory, Department of Chemistry, Govt. Model Science (Autonomous) College, Jabalpur, M.P., 482001, India.
Mater Sci Eng C Mater Biol Appl. 2016 Jan 1;58:852-62. doi: 10.1016/j.msec.2015.09.043. Epub 2015 Sep 12.
Drug encapsulated nanocarriers are vehicles to transport the drug molecules and release them at the immediate vicinity of the diseased sites. The aim of this study was to design poly (2-hydroxyethyl methacrylate) nanoparticles (PHEMANPs) as a swelling and diffusion controlled drug release system for achieving sustained release of (cis-dichlorodiamminoplatinum II) CDDP. The study undertakes designing and characterization of nanocarriers, optimization of drug encapsulation, and investigating release dynamics of the CDDP drug. PHEMANPs were prepared by suspension polymerization method followed by post loading of the CDDP onto the nanocarriers. The physicochemical and biopharmaceutical properties were evaluated by FTIR, TEM, FESEM, EDX, DLS, surface charge, water intake studies, in vitro cytotoxicity, protein adsorption and percent haemolysis. Chemical stability of the drug was assessed and in vitro release experiments were performed to optimize formulation by UV spectral analysis. The obtained cumulative release data were fitted to zero, first and Korsmeyer-Peppas kinetic models to gain insights into release kinetics and prevailing drug transport mechanisms. The successful encapsulation of CDDP was achieved in different PHEMANP formulations with maximum drug encapsulation efficiency of approx. 60% and the release kinetics was found to follow the Korsmeyer-Peppas model having non-Fickian mechanism. The results indicated that the CDDP can be formulated with a high payload of PHEMANPs which can serve as promising nanomedicine and help in achieving sustained delivery of drug for targeting tumour.
药物包封纳米载体是用于运输药物分子并在患病部位附近释放它们的载体。本研究的目的是设计聚甲基丙烯酸2-羟乙酯纳米颗粒(PHEMANPs)作为一种溶胀和扩散控制的药物释放系统,以实现顺二氯二氨铂(II)(CDDP)的持续释放。该研究进行了纳米载体的设计与表征、药物包封的优化以及CDDP药物释放动力学的研究。PHEMANPs通过悬浮聚合法制备,随后将CDDP后加载到纳米载体上。通过傅里叶变换红外光谱(FTIR)、透射电子显微镜(TEM)、场发射扫描电子显微镜(FESEM)、能量色散X射线光谱(EDX)、动态光散射(DLS)、表面电荷、水摄取研究、体外细胞毒性、蛋白质吸附和溶血百分比来评估其物理化学和生物药剂学性质。评估了药物的化学稳定性,并通过紫外光谱分析进行体外释放实验以优化制剂。将获得的累积释放数据拟合到零级、一级和Korsmeyer-Peppas动力学模型,以深入了解释放动力学和主要的药物转运机制。在不同的PHEMANP制剂中成功实现了CDDP的包封,最大药物包封效率约为60%,并且发现释放动力学遵循具有非菲克机制的Korsmeyer-Peppas模型。结果表明,CDDP可以与高载药量的PHEMANPs一起配制,这可以作为有前景的纳米药物,并有助于实现药物的持续递送以靶向肿瘤。