Shen Yan, Ling Xiang, Jiang Weiwei, Du Shuang, Lu Yang, Tu Jiasheng
a Department of Pharmaceutics , China Pharmaceutical University , Nanjing , China .
b Patent Examination Cooperation Center of SIPO , Jiangsu , Suzhou , China , and.
Drug Deliv. 2015;22(7):911-7. doi: 10.3109/10717544.2013.861883. Epub 2014 Jan 8.
Emulgels have been extensively covered as a promising drug delivery system for the administration of lipophilic drugs. This work was conducted to develop an emulgel formulation for Cyclosporin A (CsA) employing polycarbophil as the gelling agent for ocular delivery. The prepared emulgels were evaluated for their physical appearance, rheological behavior, drug release, stability, precorneal clearance and irritation. Results showed that CsA emulgel formulations prepared with polycarbophil exhibited acceptable physical properties and drug release, which remained consistent after storage for 3 months. A prolonged retention time was also observed on the ocular surface with improved ocular bioavailability and no irritation. Therefore, the polycarbophil-based emulgel could be exploited as a potential hydrophobic drug carrier for topical ocular drug delivery.
乳凝胶作为一种用于亲脂性药物给药的有前景的药物递送系统已被广泛报道。本研究旨在开发一种以聚卡波非为凝胶剂的环孢素A（CsA）乳凝胶制剂用于眼部给药。对制备的乳凝胶进行了外观、流变学行为、药物释放、稳定性、角膜前清除率和刺激性评估。结果表明，用聚卡波非制备的CsA乳凝胶制剂具有可接受的物理性质和药物释放特性，在储存3个月后仍保持一致。在眼表面还观察到延长的滞留时间，提高了眼部生物利用度且无刺激性。因此，基于聚卡波非的乳凝胶可作为局部眼部药物递送的潜在疏水性药物载体加以利用。
