期刊
JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION
卷 32, 期 13, 页码 1678-1702出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/09205063.2021.1932359
关键词
Tacrolimus; pluronic F127; chitosan; thermoresponsive in situ gel; ocular drug delivery system
资金
- DST [SR/WOS-A/LS-414-2018]
The thermoresponsive in situ gel system containing pluronic F127 and chitosan was optimized to enhance precorneal retention and sustain drug release, resulting in improved corneal permeation. In vitro studies showed sustained release of tacrolimus and increased corneal permeation with the optimized gel formulation.
To overcome problems associated with topical delivery of tacrolimus (TCS), a thermoresponsive in situ gel system containing pluronic F127 (PL), and chitosan (CS) was developed, to enhance the precorneal retention, and to sustain the release of the drug. The PL-CS in situ gel was optimized using a 2-factor-3-level central composite experimental design by selecting the concentration of PL and CS as independent variables while gelation time, gelation temperature, and spreadability as dependent variables. The optimized formulation was developed using 22.5 g PL and 0.3 g CS, gels at 33.6 degrees C, in 22.93 s, and showed the spreadability of 6.2 cm. In vitro studies conducted for the optimized gel revealed the sustained release of TCS (81.73% in 4 h) and improved corneal permeation (74.13% in 4 h), compared with TCS solution. The mechanism of release of TCS followed the Higuchi model with Fickian diffusion transport. Further, histopathology and HET-CAM studies revealed that the developed gel was non-irritating and safe for ocular administration.
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