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Published on: February 14, 2018
Promising Antifungal Potential of Engineered Non-ionic Surfactant-Based Vesicles: In Vitro and In Vivo Studies
Amit Verma1, Ankit Jain1,2, Ankita Tiwari1
1Pharmaceutics Research Projects Laboratory, Department of Pharmaceutical Sciences, Dr. Hari Singh Gour Central University, Sagar, Madhya Pradesh, 470003, India.
Abstract:
Fungal keratitis (FK) is a corneal infection caused by different fungal species. It is treated by the topical application of natamycin (NAT). Nevertheless, this approach faces many limitations like toxic effects, frequent dosing, resistance, and patient discomfort. The present research reports the development of trimethyl chitosan (TMC) coated mucoadhesive cationic niosomes by a modified thin-film hydration method. TMC was synthesized using a one-step carbodiimide method and characterized by 1H-NMR and degree of quaternization (53.74 ± 1.06%). NAT, cholesterol (CHOL), span 60 (Sp60), and dicetyl phosphate (DCP) were used to prepare niosomes which were incubated with TMC to obtain mucoadhesive cationic NAT loaded niosomes (MCNNs). MCNNs showed a spherical shape with 1031.12 ± 14.18 nm size (PDI below 0.3) and 80.23 ± 5.28% entrapment efficiency. In vitro drug release studies showed gradual drug release from TMC coated niosomes as compared to the uncoated niosomes. MIC assay and disk diffusion assay revealed promising in vitro antifungal potential of MCNNs similar to the marketed formulation. For investigating in vivo performance, ocular retention and pharmacokinetics, ocular irritation, and ulcer healing studies were performed using the rabbit model. Mucoadhesive property and prolonged local drug release improved the safety and efficacy of NAT, suggesting that the developed niosomes could be an emerging system for effective treatment of fungal keratitis.
Insights
New trimethyl chitosan coated niosomes offer improved delivery of natamycin for fungal keratitis treatment. These mucoadhesive cationic niosomes enhance ocular drug retention and efficacy, reducing toxicity and dosing frequency.
Area of Science:
- Ophthalmology
- Mycology
- Nanotechnology
- Pharmaceutics
Background:
- Fungal keratitis (FK) is a serious corneal infection.
- Current topical natamycin (NAT) treatment for FK has limitations including toxicity, frequent dosing, and poor patient compliance.
- Novel drug delivery systems are needed to improve FK treatment efficacy and safety.
Purpose of the Study:
- To develop and characterize trimethyl chitosan (TMC) coated mucoadhesive cationic niosomes loaded with natamycin (NAT) for enhanced fungal keratitis treatment.
- To evaluate the in vitro and in vivo performance of these novel niosomes.
Main Methods:
- Mucoadhesive cationic niosomes (MCNNs) were prepared using a modified thin-film hydration method with NAT, cholesterol, span 60, and dicetyl phosphate, followed by coating with synthesized TMC.
- Characterization included size, polydispersity index (PDI), entrapment efficiency, in vitro drug release, MIC assay, and disk diffusion assay.
- In vivo studies in rabbits assessed ocular retention, pharmacokinetics, ocular irritation, and ulcer healing.
Main Results:
- TMC-coated niosomes (MCNNs) exhibited a spherical shape, optimal size (1031.12 nm), and high entrapment efficiency (80.23%).
- MCNNs demonstrated sustained in vitro drug release and potent in vitro antifungal activity comparable to marketed formulations.
- In vivo studies showed improved ocular retention, prolonged drug release, enhanced safety, and accelerated ulcer healing in rabbits.
Conclusions:
- TMC-coated mucoadhesive cationic niosomes represent a promising advanced drug delivery system for topical natamycin in fungal keratitis.
- This formulation improves the safety and efficacy of natamycin by enhancing ocular retention and prolonging local drug release.
- The developed niosomes offer a potential strategy for more effective and patient-friendly treatment of fungal keratitis.
