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Ocular amphotericin B delivery by chitosan-modified nanostructured lipid carriers for fungal keratitis-targeted
Tian Fu1,2, Jinglin Yi3, Songyi Lv4
1a Department of Ophthalmology , Medical college of Nanchang University , Nanchang , Jiangxi , China.
Context:
Fungal keratitis, a corneal fungal infection of the eye caused mainly by Candida species, has become the leading cause of blindness resulting from corneal disease in China. Present limitations in the management of ophthalmic fungal infections include the inability to provide long-term extraocular drug delivery without compromising intraocular structures and/or systemic drug exposure.
Objective:
The aim of this study was to construct amphotericin B (AmB) loaded, chitosan-modified, nanostructured lipid carriers (AmB-CH-NLC) for prolonged ocular application and for the improvement of the targeted delivery of AmB to the ocular mucosa.
Materials And Methods:
The AmB-CH-NLC was produced by the method of emulsion evaporation-solidification at low temperature. The particle size, zeta potential, and encapsulation efficiency, drug-release behavior, and corneal penetration ability were performed in vitro and in vivo.
Results And Discussion:
The prepared AmB-CH-NLC nanoparticles exhibited a measured size of 185.4 nm, a zeta potential of 27.1 mV, and an entrapment efficiency of 90.9%. Sustained drug release behavior was observed in vitro. The in vivo ocular pharmacokinetic study indicated improved bioavailability of AmB-CH-NLC. The corneal penetration study showed that the AmB-CH-NLC could successfully penetrate into the cornea with no obvious irritation to the rabbits' eyes.
Conclusion:
The results support that this novel nanomedicine could be a promising system for effective ocular delivery of amphotericin B for fungal keratitis-targeted therapy.
Insights
This study developed novel nanocarriers for amphotericin B (AmB) to treat fungal keratitis. The AmB-loaded nanostructured lipid carriers show promise for improved ocular drug delivery and reduced side effects.
Area of Science:
- Ophthalmology
- Nanomedicine
- Pharmacology
Background:
- Fungal keratitis, primarily caused by Candida species, is a leading cause of blindness in China.
- Current treatments for ophthalmic fungal infections face limitations in sustained ocular drug delivery and avoiding systemic exposure.
Purpose of the Study:
- To develop amphotericin B (AmB) loaded, chitosan-modified, nanostructured lipid carriers (AmB-CH-NLC) for prolonged ocular application.
- To enhance targeted delivery of AmB to ocular mucosa for improved fungal keratitis treatment.
Main Methods:
- AmB-CH-NLC were synthesized using emulsion evaporation-solidification at low temperature.
- Characterization included particle size, zeta potential, encapsulation efficiency, drug release kinetics, and corneal penetration studies (in vitro and in vivo).
Main Results:
- The nanoparticles measured 185.4 nm with a zeta potential of 27.1 mV and 90.9% entrapment efficiency.
- Sustained in vitro drug release and improved in vivo ocular bioavailability were observed.
- Successful corneal penetration with no significant ocular irritation in rabbit models was demonstrated.
Conclusions:
- The developed AmB-CH-NLC system demonstrates effective ocular delivery of amphotericin B.
- This nanomedicine holds potential as a promising therapeutic strategy for targeted fungal keratitis treatment.
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