School of Pharmacy, Shenyang Medical College, Shenyang, China.
School of Pharmacy, Shenyang Medical College, Shenyang, China.
J Pharm Sci. 2020 May;109(5):1703-1713. doi: 10.1016/j.xphs.2020.01.021. Epub 2020 Feb 1.
The herein work elucidated colloid performances of thermosensitive in situ-forming ophthalmic gel established by poloxamer 407 (F127), mainly including facile and simple methods (load-bearing method, tilting plate method, and eye simulation method) to analyze and evaluate F127 gel and intensively addressed capacity of F127 gel for loading drugs. The results demonstrated that the poorly water-soluble berberine hydrochloride improved entangled intensity of F127 and therefore reduced the sol dynamic rate, which contributed to lower gelation temperature and enhancement of cornea adhesion, further lowering the rate of gel corrosion together with drug release. Importantly, the addition of hydroxy propyl methyl cellulose (HPMC) K15M contributed to stronger gel strength because strong interaction forces were formed between HPMC K15M and F127 when the molecular chain segments of HPMC K15M interspersed among F127 network. All the aforementioned results provide valuable instruction for designing and evaluating thermosensitive in situ-forming ophthalmic gel.
本文阐述了由泊洛沙姆 407（F127）构建的温敏型原位形成眼科凝胶的胶体性能，主要包括分析和评估 F127 凝胶的简便方法（承载法、倾斜板法和眼模拟法），并深入研究了 F127 凝胶载药的能力。结果表明，疏水性较差的盐酸小檗碱提高了 F127 的缠结强度，从而降低了溶液的动态速率，有助于降低凝胶的成胶温度和增强角膜黏附性，进一步降低了凝胶的腐蚀速度和药物释放速度。重要的是，羟丙基甲基纤维素（HPMC）K15M 的加入增强了凝胶的强度，因为 HPMC K15M 的分子链段穿插在 F127 网络中时，HPMC K15M 与 F127 之间形成了较强的相互作用力。所有这些结果为设计和评估温敏型原位形成的眼科凝胶提供了有价值的指导。
