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Published on: February 9, 2019
Physiochemical Characterization of Lipidic Nanoformulations Encapsulating the Antifungal Drug Natamycin
Luigi Talarico1,2,3, Ilaria Clemente1,3, Alessandro Gennari1
1Department of Biotechnology Chemistry and Pharmacy, University of Siena, Via Aldo Moro 2, 53100 Siena, Italy.
Abstract:
Natamycin is a tetraene polyene that exploits its antifungal properties by irreversibly binding components of fungal cell walls, blocking the growth of infections. However, topical ocular treatments with natamycin require frequent application due to the low ability of this molecule to permeate the ocular membrane. This limitation has limited the use of natamycin as an antimycotic drug, despite it being one of the most powerful known antimycotic agents. In this work, different lipidic nanoformulations consisting of transethosomes or lipid nanoparticles containing natamycin are proposed as carriers for optical topical administration. Size, stability and zeta potential were characterized via dynamic light scattering, the supramolecular structure was investigated via small- and wide-angle X-ray scattering and 1H-NMR, and the encapsulation efficiencies of the four proposed formulations were determined via HPLC-DAD.
Insights
Natamycin, a potent antifungal, faces delivery challenges in eye infections. New lipid nanoformulations, including transethosomes and lipid nanoparticles, show promise for improved topical ocular delivery of natamycin.
Area of Science:
- Ophthalmology
- Pharmaceutics
- Mycology
Background:
- Natamycin is a powerful tetraene polyene antifungal agent.
- Its efficacy is limited by poor ocular membrane permeability for topical treatments.
- Frequent application is needed, hindering its clinical use despite potent antifungal properties.
Purpose of the Study:
- To develop novel lipid nanoformulations for topical ocular natamycin delivery.
- To overcome the low ocular permeation limitation of natamycin.
- To enhance the delivery of natamycin for treating fungal eye infections.
Main Methods:
- Preparation of lipid nanoparticles and transethosomes encapsulating natamycin.
- Characterization of size, stability, and zeta potential using dynamic light scattering.
- Investigation of supramolecular structure via X-ray scattering and 1H-NMR.
- Determination of encapsulation efficiencies using HPLC-DAD.
Main Results:
- Successfully developed four distinct lipid nanoformulations for natamycin.
- Characterized physical and structural properties of the nanoformulations.
- Quantified encapsulation efficiencies, indicating successful drug loading.
Conclusions:
- Lipid nanoformulations offer a viable strategy for topical ocular delivery of natamycin.
- These formulations have the potential to improve natamycin's therapeutic efficacy.
- Further studies are warranted to evaluate in vivo performance and clinical utility.
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