Preparation and characterization of bear bile-loaded pH sensitive <i>in-situ</i> gel eye drops for ocular drug delivery

Ni, Xiaomin and Guo, Qin and Zou, Yiqing and Xuan, Yang and Mohammad, Imran Shair and Ding, Qing and Hu, Haiyan (2020) Preparation and characterization of bear bile-loaded pH sensitive <i>in-situ</i> gel eye drops for ocular drug delivery. Iranian Journal of Basic Medical Sciences, 23 (7). pp. 922-929.

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Abstract

Objective(s): In this study, a stable bear bile-loaded pH sensitive in-situ eye drop gel was prepared for sustain delivery and enhanced therapeutic application. Materials and Methods: Bear bile-loaded in-situ ocular gels with different Carbopol/Hydroxypropyl methylcellulose (HPMC) ratios were prepared and their stability was tested in PBS at a series of pH at 40 °C. The morphology was observed by SEM examination and rheology was observed by Rheometer equipped with a 60-mm cone-plate at apex angle of 1°. Gel erosion and release kinetics of Tauroursodeoxycholic acid (TUDCA) was determined by HPLC. While, the in vivo dwelling time was obtained after administering the fluorescent-loaded gel in ocular disease-free New Zealand rabbits. Finally, biocompatibility and toxicity was observed by irritation test and H&amp;E staining of eye-ball tissues, respectively. Results: The bear bile-loaded in-situ ocular gel showed excellent stability at different pH (pH 5.0, 5.5, 6.0, 6.5, 7.0 and 8.0) up to 5 days, and bear bile extract significantly attenuated the gelling ability of the in-situ gel. The viscosity of in-situ gels formulation was decreased with increase in shear rate (0.01 to 100 s-1), and morphological examination of freeze-dried preparation showed three-dimensional reticular structure at physiological pH. The in-situ ocular gel exhibited promising sustained drug release up to 160 min in vitro, and showed prolonged retention time up to 3-folds in vivo. Finally, the biocompability data confirmed that the formulation did not induce any toxic effects and was completely compatible with eye tissues.Conclusion: pH sensitive in-situ ocular gel provides new research opportunities to efficiently treat eye diseases.

Item Type: Article
Uncontrolled Keywords: Bear bile,In-situ ocular gel,pH sensitive,Rheology,Sustain-releas
Subjects: QV pharmacology
Divisions: Journals > Iranian J Basic Medical Sciences
Depositing User: ijbms ijbms
Date Deposited: 16 Jun 2020 07:06
Last Modified: 16 Jun 2020 07:06
URI: http://eprints.mums.ac.ir/id/eprint/19308

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