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Preparation and Characterization of Nanoliposomes for the Entrapment of Bioactive Hydrophilic Globular Proteins
Published on: August 31, 2019
Development and characterization of the voriconazole loaded lipid-based nanoparticles
Petra Füredi1, Zsófia Edit Pápay1, Kristóf Kovács1
1Semmelweis University, Department of Pharmaceutics, H-1092 Budapest Hőgyes Endre St 7., Hungary.
Abstract:
The number of topical fungal infections is growing, mostly owing to immunosuppressive therapy. Several topical fungal infections, such as eye mycoses, can be treated by local administration of antimycotic drugs. One major group of the antifungal agents is triazole, such as voriconazole (VCZ), which is used as the first line treatment of aspergillosis. A disadvantage of VCZ is its low water solubility making the drug difficult to administer in a liquid preparation. The lipid-based nanoparticles (LNP) have attracted increasing attention due to their advantageous properties. Contrarily to the conventional carrier systems, LNP can improve the poor solubility of topically used drugs, such as VCZ. Therefore, LNP represents promising alternatives to traditional carrier systems. The aim of the study was to formulate VCZ loaded lipid-based nanoparticles (VCZ-LNP) by high pressure homogenization (HPH). The developed LNPs were characterized by particle size analysis, IR spectroscopy, differential scanning calorimetry, dialysis test and antifungal efficacy studies. The particle size of the optimized nanoparticles from the selected lipid base, Witepsol® W35, was 182±4.1nm after five cycles of homogenization at 600bar. The antifungal study confirmed that the optimized VCZ-LNP inhibited the fungus reproduction.
Insights
This study developed voriconazole-loaded lipid-based nanoparticles (VCZ-LNP) to address the poor water solubility of voriconazole (VCZ). The optimized VCZ-LNP formulation demonstrated effective inhibition of fungal growth, offering a promising alternative for topical antifungal treatments.
Area of Science:
- Pharmaceutical Nanotechnology
- Mycology
- Drug Delivery Systems
Background:
- Topical fungal infections are increasing, necessitating improved drug delivery methods.
- Voriconazole (VCZ), a key triazole antifungal, suffers from poor water solubility, limiting its topical application.
- Lipid-based nanoparticles (LNP) offer enhanced solubility and improved drug delivery for poorly soluble compounds.
Purpose of the Study:
- To formulate voriconazole-loaded lipid-based nanoparticles (VCZ-LNP) using high-pressure homogenization (HPH).
- To characterize the physicochemical properties and antifungal efficacy of the developed VCZ-LNP.
Main Methods:
- Formulation of VCZ-LNP using high-pressure homogenization (HPH) with Witepsol® W35.
- Characterization techniques included particle size analysis, IR spectroscopy, differential scanning calorimetry, and dialysis testing.
- Antifungal efficacy studies were conducted to evaluate the inhibitory effect against fungal reproduction.
Main Results:
- Optimized VCZ-LNP achieved a particle size of 182±4.1nm after five homogenization cycles at 600bar.
- Physicochemical characterization confirmed the successful encapsulation of VCZ within the lipid nanoparticles.
- Antifungal efficacy studies demonstrated that the optimized VCZ-LNP effectively inhibited fungal reproduction.
Conclusions:
- Lipid-based nanoparticles are a promising system for improving the topical delivery of poorly soluble drugs like voriconazole.
- The developed VCZ-LNP formulation shows potential for effective treatment of topical fungal infections.
- High-pressure homogenization is a viable method for producing effective VCZ-LNP.
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