Chitosan-based thermosensitive hydrogel as a promising ocular drug delivery system: preparation, characterization, and in vivo evaluation.

Abstract

The purpose of this study was to evaluate the feasibility of in situ thermosensitive hydrogel based on chitosan in combination with disodium α-d-Glucose 1-phosphate (DGP) for ocular drug delivery system. Aqueous solution of chitosan/DGP underwent sol-gel transition as temperature increased which was flowing sol at room temperature and then turned into non-flowing hydrogel at physiological temperature. The properties of gels were characterized regarding gelation time, gelation temperature, and morphology. The sol-to-gel phase transition behaviors were affected by the concentrations of chitosan, DGP and the model drug levocetirizine dihydrochloride (LD). The developed hydrogel presented a characteristic of a rapid release at the initial period followed by a sustained release and remarkably enhanced the cornea penetration of LD. The results of ocular irritation demonstrated the excellent ocular tolerance of the hydrogel. The ocular residence time for the hydrogel was significantly prolonged compared with eye drops. The drug-loaded hydrogel produced more effective anti-allergic conjunctivitis effects compared with LD aqueous solution. These results showed that the chitosan/DGP thermosensitive hydrogel could be used as an ideal ocular drug delivery system in terms of the suitable sol-gel transition temperature, mild pH environment in the hydrogel as well as the organic solvent free.

• Authors: Xingwei Chen, Xinru Li, Yanxia Zhou, Xiaoning Wang, Yanhui Zhang, Yating Fan, Yanqing Huang, Yan Liu
• Journal: Journal of biomaterials applications (J Biomater Appl) Vol. 27 Issue 4 Pg. 391-402 (Nov 2012) ISSN: 1530-8022 [Electronic] England
• PMID: 21750179 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Delayed-Action Preparations
• Glucosephosphates
• Histamine H1 Antagonists, Non-Sedating
• Hydrogel, Polyethylene Glycol Dimethacrylate
• levocetirizine
• Chitosan
• glucose-1-phosphate
• Cetirizine

Topics

• Animals
• Cetirizine (administration & dosage, pharmacokinetics, therapeutic use)
• Chitosan (chemistry)
• Conjunctivitis, Allergic (drug therapy)
• Cornea (drug effects, metabolism)
• Delayed-Action Preparations (chemistry)
• Female
• Glucosephosphates (chemistry)
• Guinea Pigs
• Histamine H1 Antagonists, Non-Sedating (administration & dosage, pharmacokinetics, therapeutic use)
• Hydrogel, Polyethylene Glycol Dimethacrylate (chemistry)
• Male
• Phase Transition
• Rabbits
• Temperature