RCPIPER, Shirpur, Maharashtra, India.
Pharm Dev Technol. 2013 Jul-Aug;18(4):950-6. doi: 10.3109/10837450.2011.644297. Epub 2011 Dec 27.
In the present study, novel environmentally responsive ophthalmic drug delivery system composed of two gelling polymers with different phase transition mechanisms was developed in order to obtain sustained drug release in ocular cavity. Combination of polyacrylic acid (carbopol 934P) and xanthan gum was investigated as ophthalmic vehicle and assessed for its in vitro and in vivo performance. Different ratios of these polymers were used to prepare environmentally responsive ophthalmic drug delivery system by simple mixing procedure. Developed formulation was assessed for physical tests such as appearance/clarity, pH, gelation; and performance characteristics such as drug content, rheological measurement, in vitro release, antimicrobial efficiency, in vivo studies for eye irritation, residence time estimation. Prepared formulation showed agreeable appearance/clarity, acceptable pH and good gelation property. In vitro and in vivo studies demonstrated adequate drug content, desired rheological behavior and reasonable in vitro and in vivo drug release property. In conclusion, the optimum concentration of polymers results in increased residence time and sustained drug release. On the basis of these findings, environmentally responsive system based on combination of carbopol and xanthan gum may be considered as a promising tool for ophthalmic delivery.
在本研究中，开发了一种新型的具有不同相转变机制的两亲性聚合物组成的环境响应性眼科药物传递系统，以在眼腔中获得持续的药物释放。研究了聚丙烯酸（carbopol 934P）和黄原胶的组合作为眼科载体，并评估了其体外和体内性能。通过简单的混合程序，使用这些聚合物的不同比例来制备环境响应性眼科药物传递系统。对开发的制剂进行了物理测试，如外观/透明度、pH 值、胶凝性；以及性能特性，如药物含量、流变学测量、体外释放、抗菌效率、眼部刺激性的体内研究、驻留时间估计。所制备的制剂具有良好的外观/透明度、可接受的 pH 值和良好的胶凝性能。体外和体内研究表明，药物含量适宜，流变学行为理想，体外和体内药物释放性能合理。总之，聚合物的最佳浓度导致滞留时间延长和药物持续释放。基于这些发现，基于 carbopol 和 xanthan 胶的组合的环境响应系统可以被认为是眼科给药的有前途的工具。
