Miconazole Nitrate-loaded Microparticles For Buccal Use: Immediate Drug Release and Antifungal Effect

Miconazole Nitrate-loaded Microparticles For Buccal Use: Immediate Drug Release and Antifungal Effect

Miconazole nitrate has been widely employed in treatment of oral mycoses, however your immediate bio-availability and location in the affected area is critical. The aim of this study was to prepare and evaluate Eudragit® L100 and Gantrez MS-955 microparticles containing miconazole nitrate for oral d...

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Bibliographic Details
Published in:Current drug delivery Vol. 14; no. 8; p. 1144
Main Authors: Cartagena, Andres Felipe, Lyra, Amanda Martinez, Kapuchczinski, Aline Cristina, Urban, Amanda Migliorini, Esmerino, Luis Antonio, Klein, Traudi, Nadal, Jessica Mendes, Farago, Paulo Vitor, Campanha, Nara Hellen
Format: Journal Article
Language:English
Published: United Arab Emirates 01-12-2017
Subjects:
Administration, Oral
Antifungal Agents - administration & dosage
Antifungal Agents - pharmacokinetics
Antifungal Agents - pharmacology
Candida albicans - drug effects
Candida albicans - growth & development
Drug Delivery Systems
Humans
Maleates - administration & dosage
Maleates - chemistry
Miconazole - administration & dosage
Miconazole - pharmacokinetics
Miconazole - pharmacology
Microbial Sensitivity Tests
Particle Size
Polymethacrylic Acids - administration & dosage
Polymethacrylic Acids - chemistry
Polyvinyls - administration & dosage
Polyvinyls - chemistry
Surface Properties
Temperature
Antifungal activity
polymeric microparticles
drug delivery
relative solubility
candidiasis
miconazole nitrate
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Summary:Miconazole nitrate has been widely employed in treatment of oral mycoses, however your immediate bio-availability and location in the affected area is critical. The aim of this study was to prepare and evaluate Eudragit® L100 and Gantrez MS-955 microparticles containing miconazole nitrate for oral delivery. Microparticles were prepared by spray-drying method to achieve high encapsulation efficiency and increase the drug solubility. The microparticles were formed containing 10% and 20% of drug on polymer Eudragit® L100 (E10 and E20), Gantrez MS-955 (G10 and G20) or their combination (EG10 and EG20). The influence of formulation factors (polymer:drug ratio, type of polymer) on yield percent, encapsulation efficiency, particle size, Fourier-transformed infrared spectroscopy (FTIR), X-ray diffraction, differential scanning calorimetry, in vitro drug release and antifungal activity were investigated. Acceptable yield, micrometer-sized and drug-loading efficiencies higher than 89% were obtained. No change in FTIR assignments was recorded after the microencapsulation procedure. X-ray and differential scanning calorimetry studies revealed amorphous/non-crystalline formulations. Miconazole nitrate-microparticles provided a remarkable increase of dissolution rate of the drug. Miconazole nitrate and G10, G20 and EG20 microparticles fitted to biexponential kinetic model, and E10, E20 and EG10 microparticles, monoexponential kinetic model. The antifungal activity test demonstrated that miconazole nitrate-microparticles possessed the same anti-Candida albicans activity as the pure drug. These results indicate that miconazole nitrate-microparticles are feasible carriers for increased release of miconazole at oral environment.
ISSN:1875-5704
DOI:10.2174/1567201813666161006115041