Thakkar Hetal, Sharma R K, Mishra A K, Chuttani Krishna, Murthy R S R
New Drug Delivery System Laboratory, Pharmacy Department, Donor's Plaza, Opp. To University main office, M. S. University of Baroda, Fatehgunj, Vadodara-390 002, India.
J Pharm Pharmacol. 2004 Sep;56(9):1091-9. doi: 10.1211/0022357044166.
The use of polymeric carriers in formulations of therapeutic drug delivery systems has gained widespread application, due to their advantage of being biodegradable and biocompatible. In this study, we aimed to prepare celecoxib-loaded chitosan microspheres for intra-articular administration and to compare the retention of the celecoxib solution and chitosan microspheres in the joint cavity. The microspheres were characterized for entrapment efficiency, particle size and surface morphology by scanning electron microscopy. In-vitro drug release studies of microspheres revealed that the microspheres are able to control the release of celecoxib over a period of 96 h. Biodistribution studies of celecoxib and chitosan microspheres were performed by radiolabelling with( 99m)Tc and injecting intraarticularly in rats. The study indicated that following intra-articular administration the distribution of the drug to the organs, like liver and spleen, is very rapid compared with that of the microspheres. Compared with the drug solution, a 10-fold increase in the concentration of the drug in the joint was observed 24 h post intra-articular injection (P < 0.005) when drug was encapsulated in microspheres.
由于具有可生物降解和生物相容性的优点，聚合物载体在治疗性药物递送系统制剂中的应用已得到广泛应用。在本研究中，我们旨在制备用于关节内给药的载塞来昔布壳聚糖微球，并比较塞来昔布溶液和壳聚糖微球在关节腔内的滞留情况。通过扫描电子显微镜对微球的包封率、粒径和表面形态进行了表征。微球的体外药物释放研究表明，微球能够在96小时内控制塞来昔布的释放。通过用（99m）Tc进行放射性标记并在大鼠关节内注射，对塞来昔布和壳聚糖微球进行了生物分布研究。研究表明，关节内给药后，与微球相比，药物向肝脏和脾脏等器官的分布非常迅速。与药物溶液相比，当药物封装在微球中时，关节内注射24小时后关节内药物浓度增加了10倍（P < 0.005）。
