The eye irritation test and pharmacokinetic study of tacrolimus-loaded cationic nanoemulsion-based in-situ gel in rabbits
10.12206/j.issn.2097-2024.202104055
- VernacularTitle:他克莫司阳离子微乳凝胶的兔眼刺激性研究及房水药动学研究
- Author:
Xin LIN
1
;
Jialiang ZHANG
1
;
Xin ZHOU
1
;
Hongtao SONG
1
Author Information
1. Department of Pharmacy, No. 900 Hospital of Joint Logistic Support Force of the PLA, Fuzhou 350025, China.
- Keywords:
tacrolimus;
cationic nanoemulsion-based in-situ gel;
eye irritation;
pharmacokinetics
- From:
Journal of Pharmaceutical Practice
2023;41(3):177-181
- CountryChina
- Language:Chinese
-
Abstract:
Objective To study the eye irritation and the pharmacokinetics of tacrolimus-loaded cationic nanoemulsion-based in-situ gel in rabbits. Methods The eye irritation of tacrolimus-loaded cationic nanoemulsion-based in-situ gel in rabbits was observed by histological cross-sections of external ocular tissues stained with HE. The aqueous humor of rabbit eyes was extracted by corneal puncture and analyzed by HPLC-MS for pharmacokinetic study. Results Tacrolimus-loaded cationic nanoemulsion-based in-situ gel had no significant irritation on rabbit eyes. The pharmacokinetic parameter showed that the AUC of tacrolimus-loaded cationic nanoemulsion-based in-situ gel was (128.34±13.09) ng·h/ml, which was 1.13 times of tacrolimus-loaded cationic nanoemulsion (113.61±12.36) ng·h/ml and 1.88 times of Talymus® (68.25±10.82) ng·h /ml. Conclusion Tacrolimus-loaded cationic nanoemulsion-based in-situ gel had the advantages of low irritation, long retention time and high bioavailability in rabbit eyes. It has a good potential for clinical application.
