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Merck

Optimization, characterization and evaluation of chitosan-tailored cubic nanoparticles of clotrimazole.

International journal of biological macromolecules (2014-12-03)
Purnima Verma, Munish Ahuja
RESUMO

The present study deals with improvement of the mucoadhesive properties of monoolein based cubic nanoparticles by incorporating chitosan. Chitosan-tailored cubic nanoparticles were prepared by thin film hydration followed by ultrasonication employing clotrimazole as model drug. The effect of Pluronic F127 fraction and concentration of chitosan on particle size and % mucin binding of the formulations was studied using 2-factor, 3-level, central composite experimental design. The concentration of chitosan was found to influence particle size and % mucin binding of cubic nanoparticles while Pluronic F127 fraction influenced only the % mucin binding. Studies indicated 8.33(%w/w) fraction of Pluronic F127 and 0.17 (%w/v) concentration of chitosan as optimum concentration. Finally, the optimized batch was characterized by polarized light microscopy, small-angle X-ray scattering (SAXS) and transmission electron microscopy. The results unveiled incorporation of chitosan did not disrupt the inner cubic structure of nanoparticles. Peak indexing of SAXS data revealed the coexistence of P-type and D-type cubic phases in nanoparticles. Further, comparative evaluation studies showed significantly higher anti-fungal activity of clotrimazole-loaded chitosan-tailored cubic nanoparticles than conventional suspension of clotrimazole against Candida albicans.

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Sigma-Aldrich
Metronidazole, BioXtra
Sigma-Aldrich
Clotrimazole
Supelco
Metronidazole, analytical standard
Supelco
Metronidazole, Pharmaceutical Secondary Standard; Certified Reference Material
Supelco
Clotrimazole, Pharmaceutical Secondary Standard; Certified Reference Material
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Metronidazole, VETRANAL®, analytical standard
Clotrimazole, European Pharmacopoeia (EP) Reference Standard
Metronidazole, European Pharmacopoeia (EP) Reference Standard
Clotrimazole for peak identification, European Pharmacopoeia (EP) Reference Standard