Novel Bos indicus Fat-Based Nanoparticulate Lipospheres of Miconazole Nitrate as Enhanced Mucoadhesive Therapy for Oral Candidiasis

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, exvivo 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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Materials

The following materials were used in the study: miconazole nitrate USP (Gutic Biosciences Ltd., India), Daktarin® oral gel (Janssen Pharma, Beerse, Belgium), Phospholipon® 90H (P90H) (Phospholipid GmbH, Köln, Germany), Polycarbophil® (BASF, Germany), sorbitol (Gulshan Polyols Limited, India), sorbic acid (Apac Chemicals, USA), polysorbate 80 (Tween® 80) (Merck KGaA, Darmstadt, Germany), sodium sulfide (Krishna Chemicals, India), sodium chloride, potassium chloride, calcium chloride dehydrate, sodium hydroxide (BDH Chemicals Ltd., Pooles, England), methanol, ethanol (Sigma Aldrich, USA), urea BP (Anmol Chemicals, India), sodium dihydrogen phosphate (Shreeji Pharma International, India), Sabouraud dextrose agar (Titan Biotech Ltd., India), chloramphenicol (Sunways, India), glycerol (Wuppertal, Germany), bentonite (Opta Minerals, USA), activated charcoal (Taupo Carbon Producers Ltd., India), hydrochloric acid (GFS Chemicals, Inc., Columbus, OH). Clinical isolates of Candida albicans were obtained from the diagnostic laboratories of a secondary level hospital (Bishop Shanahan Hospital, Nsukka, Nigeria).

Franklin Chimaobi Kenechukwu  , Chisom Flora Kalu  , Mumuni Audu Momoh  , Ikechukwu Anthony Onah  , Anthony Amaechi Attama  , Vincent Chima Okore, Biointerface Research in Applied Chemistry, Volume 13, Issue 1, 2023, 24, https://doi.org/10.33263/BRIAC131.024