Gupta Swati, Agarwal Abhinav, Gupta Nishant Kumar, Saraogi Gauravkant, Agrawal Himanshu, Agrawal G P
Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, Dr. H. S. Gour University , Sagar,Madhya Pradesh , India.
Drug Dev Ind Pharm. 2013 Dec;39(12):1866-73. doi: 10.3109/03639045.2012.662510. Epub 2012 Mar 8.
The present study explores prospective of surface tailored nanoparticles for targeted delivery of acyclovir along with the interception of minimal side effects. Acyclovir loaded plain and galactosylated poly lectic co glycolic acid (PLGA) nanoparticles were efficiently prepared and characterized by Fourier transform infrared spectroscopy, scanning electron microscopy (SEM), size, polydispersity index, zeta potential, and entrapment efficiency. The formulations were evaluated for in vitro drug release and hemolysis. Further, biodistribution study and fluorescent microscopic studies were carried out to determine the targeting potential of formulations. SEM revealed smooth morphology and spherical shape of the nanoparticles. In vitro, the galactosylated nanoparticles were found to be least hemolytic and exhibited a sustained release pattern. In vivo studies exhibited an augmented bioavailability, increased residence time and enhanced delivery of acyclovir to the liver upon galactosylation. It may therefore be concluded that galactose conjugated PLGA nanoparticles can be used suitably as vehicles for delivery of bioactives specifically to the hepatic tissues and may be thus exploited in the effective management of various liver disorders.
本研究探索了表面修饰纳米颗粒用于阿昔洛韦靶向递送并减少副作用的前景。高效制备了负载阿昔洛韦的普通和半乳糖基化聚乳酸-乙醇酸共聚物（PLGA）纳米颗粒，并通过傅里叶变换红外光谱、扫描电子显微镜（SEM）、粒径、多分散指数、zeta电位和包封率进行了表征。对制剂进行了体外药物释放和溶血评估。此外，进行了生物分布研究和荧光显微镜研究以确定制剂的靶向潜力。SEM显示纳米颗粒形态光滑且呈球形。在体外，发现半乳糖基化纳米颗粒溶血最少且呈现持续释放模式。体内研究表明，半乳糖基化后阿昔洛韦的生物利用度提高、停留时间延长且向肝脏的递送增强。因此可以得出结论，半乳糖共轭PLGA纳米颗粒可作为生物活性物质向肝组织特异性递送的合适载体，从而可用于各种肝脏疾病的有效治疗。
