Abstract

Nanoparticulate lipospheres of miconazole nitrate were formulated and incorporated into mucoadhesive gels for enhanced treatment of oral candidiasis. Extracted cow fat and Phospholipon® 90H (7:3) were used to prepare a lipid matrix by fusion. Nanoparticulate lipospheres with drug concentrations (0, 0.125, 0.25, 0.5 % w/w) were prepared using the lipid matrix (5.0 % w/w), polysorbate 80 (2.0 % w/w), sorbitol (4.0 % w/w) and distilled water by melt homogenization. The lipospheres characterized encapsulation efficiency (EE), drug loading capacity (DL), particle size, polydispersity index, morphology, and compatibility. Lipid-based gels were prepared using Polycarbophil® (1.0 % w/w), the nanoparticles and other excipients, by dispersion, then characterized regarding drug content, compatibility, rheology, ex-vivo mucoadhesive, in-vitro drug release, and anti-candidal activity. The EE, DL, and mucoadhesive strengths of the formulated gels were influenced by drug loads. The particles were smooth, nanometric, and spherical, with polydispersity indices in the range of 0.247 ‒ 0.293. The gels were pseudoplastic. The gels ' extensive drug release profiles and anti-candidal activity were significantly superior to commercial Daktarin®. FT-IR confirmed the compatibility of the drug with excipients used in the formulations. The prospects of this study necessitate further optimization.

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