Preparation and in vitro/in vivo evaluations of novel ocular micelle formulations of hesperetin with glycyrrhizin as a nanocarrier.

Abstract

The purpose of this study was to explore the potential of formulating hesperetin into an ophthalmic solution with dipotassium glycyrrhizinate (DG) as a micelle nanocarrier. A DG-based micelle ophthalmic solution encapsulating hesperetin (DG-Hes) was developed and its in vitro/in vivo characterizations were evaluated. The optimal formulation featured a DG/hesperetin (Hes) weight ratio of 12:1 and an encapsulation efficiency of 90.4 ± 1.7%; The optimized DG-Hes was characterized as small uniform spheres with an average micelle size of 70.93 ± 3.41 nm, a polydispersity index of 0.11 ± 0.02, and an electrically negative surface (-36.12 ± 2.79 mV). The DG-Hes ophthalmic solution had good tolerance in rabbit eyes. DG-Hes significantly improved the in vitro passive permeation, ex vivo corneal permeation, and in vivo ocular bioavailability of Hes. DG-Hes showed markedly increases in in vitro antioxidant activity. In vitro antibacterial activity tests revealed a lower minimum inhibitory concentration and lower minimum bactericidal concentration for DG-Hes ophthalmic solution were lower than for free Hes. DG-Hes ophthalmic solution also significantly reduced symptoms of eye infection in the rabbit bacterial keratitis model when compared to a Hes suspension. These results suggest that DG-Hes eye drops may be useful as a new ophthalmic preparation for the treatment of ocular diseases, especially bacterial ophthalmopathy.

• Authors: Fan Zhang, Huabo Chen, Jie Lan, Kaichao Song, Xianggen Wu
• Journal: Experimental eye research (Exp Eye Res) Vol. 202 Pg. 108313 (01 2021) ISSN: 1096-0007 [Electronic] England
• PMID: 33080302 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2020 Elsevier Ltd. All rights reserved.

Chemical References

• Drug Carriers
• Micelles
• Ophthalmic Solutions
• Pharmaceutical Preparations
• Glycyrrhizic Acid
• Hesperidin
• hesperetin

Topics

• Administration, Ophthalmic
• Animals
• Biological Availability
• Cornea (metabolism)
• Corneal Ulcer (drug therapy, microbiology, pathology)
• Drug Carriers (chemistry)
• Drug Delivery Systems
• Eye Infections, Bacterial (drug therapy, microbiology, pathology)
• Glycyrrhizic Acid (chemistry)
• Hesperidin (chemistry, pharmacokinetics, pharmacology)
• Micelles
• Microscopy, Electron, Transmission
• Nanoparticles
• Ophthalmic Solutions
• Particle Size
• Pharmaceutical Preparations (chemistry)
• Rabbits
• Staphylococcal Infections (drug therapy, microbiology, pathology)
• Surface Properties