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Preparation and characterization of bear bile-loaded pH sensitive in-situ gel eye drops for ocular drug delivery.
- Source :
-
Iranian journal of basic medical sciences [Iran J Basic Med Sci] 2020 Jul; Vol. 23 (7), pp. 922-929. - Publication Year :
- 2020
-
Abstract
- Objectives: In this study, a stable bear bile-loaded pH sensitive in-situ eye drop gel was prepared for sustain delivery and enhanced therapeutic application.<br />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 <superscript>°</superscript> 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 <superscript>°</superscript> . 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&E staining of eye-ball tissues, respectively.<br />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.<br />Conclusion: pH sensitive in-situ ocular gel provides new research opportunities to efficiently treat eye diseases.
Details
- Language :
- English
- ISSN :
- 2008-3866
- Volume :
- 23
- Issue :
- 7
- Database :
- MEDLINE
- Journal :
- Iranian journal of basic medical sciences
- Publication Type :
- Academic Journal
- Accession number :
- 32774815
- Full Text :
- https://doi.org/10.22038/IJBMS.2020.45386.10562