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Reduced administration frequency for the treatment of fungal keratitis: a sustained natamycin release from a micellar
Yiyuan Guo1,2, Fatemeh Karimi2,3, Qiang Fu2,4
1Department of Ophthalmology, The First Affiliated Hospital of Harbin Medical University, Harbin, Peoples Republic of China.
Abstract:
Background: Natamycin is the only topical ophthalmic antifungal drug approved by the Food and Drug Administration (FDA) of the United States, but has unsatisfactory factors such as high dosing frequency.Methods: We report the synthesis and preparation of self-assembled poly(ethylene glycol)-block-poly(glycidyl methacrylate) (PEG-b-PGMA) micelles. These nanoparticles exhibit sustained delivery of a hydrophobic natamycin by topical administration on eye due to the hydrolysable properties of PGMA segments of micelle. Hydrolysis of glycidyl groups within a physiologically relevant environment provides an additional driving force for drug release by generation of hydrophilic hydroxyl groups to 'push' the encapsulated hydrophobic drug away from the resultant hydrophilic domains and into surrounding environment.Results: In vitro and in vivo results revealed that the self-assembled micelles and the encapsulated natamycin were not cytotoxic and the released drug have strong antifungal ability to Candida albicans. Importantly, sustained natamycin release from micelles leads to the reduced administration frequency of natamycin from 8 times per day to 3 times per day in rabbits suffering from fungal keratitis (FK).Conclusion: This study demonstrates a facile method that can greatly reduce dosing frequency of natamycin administration and thus improve long-term patient compliance.
Insights
New micelles improve ophthalmic antifungal drug delivery. This study developed self-assembled nanoparticles for sustained release of natamycin, reducing dosing frequency for fungal keratitis treatment and enhancing patient compliance.
Area of Science:
- Ophthalmic pharmacology
- Nanotechnology in drug delivery
- Polymer science
Background:
- Natamycin is the sole FDA-approved topical ophthalmic antifungal.
- Current natamycin formulations require frequent administration, impacting patient compliance.
- There is a need for improved drug delivery systems for ophthalmic antifungals.
Purpose of the Study:
- To synthesize and characterize self-assembled poly(ethylene glycol)-block-poly(glycidyl methacrylate) (PEG-b-PGMA) micelles for sustained natamycin delivery.
- To evaluate the efficacy and safety of these micelles in treating fungal keratitis.
- To reduce the dosing frequency of topical ophthalmic natamycin.
Main Methods:
- Synthesis of PEG-b-PGMA micelles encapsulating hydrophobic natamycin.
- Evaluation of micelle-induced sustained drug release via hydrolysis of PGMA segments.
- In vitro and in vivo assessment of cytotoxicity and antifungal activity against Candida albicans.
- In vivo study in rabbits with fungal keratitis to determine dosing frequency reduction.
Main Results:
- The synthesized micelles demonstrated sustained release of natamycin.
- Both micelles and released natamycin showed no cytotoxicity.
- The released natamycin exhibited potent antifungal activity against Candida albicans.
- In rabbits, micelle-based natamycin reduced administration frequency from 8 to 3 times daily for fungal keratitis.
Conclusions:
- Self-assembled PEG-b-PGMA micelles offer a promising approach for sustained ophthalmic drug delivery.
- This formulation significantly reduces the dosing frequency of natamycin.
- The improved delivery system has the potential to enhance patient compliance in treating fungal keratitis.
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