SOLIDIFIED REVERSE MICELLAR SOLUTION-BASED MUCOADHESIVE NANO-EMULGEL IMPROVES THE DISSOLUTION OF POORLY SOLUBLE IMIDAZOLE ANTIFUNGAL
FRANKLIN CHIMAOBI KENECHUKWU* , MUMUNI AUDU MOMOH, GOD’SPOWER TOCHUKWU ISAAC, LILIAN CHINONSO NWEKWO, ANTHONY AMAECHI ATTAMA AND EMMANUEL CHINEDU IBEZIM
Delivery and Nanomedicines Research Unit, Department of Pharmaceutics, University of Nigeria, Nsukka 410001, Enugu, Nigeria.
Afr. J Pharm Res Dev; Volume 12(1): 015-025 ; 2020
Surface-modification using solidified reverse micellar solutions (SRMS) is a promising technique for improving the biopharmaceutical properties of active pharmaceutical ingredients. Here, we report on the formulation and characterization of colloidal nano-enabled emulsion impregnated gel delivery system based on SRMS containing mineral fat (beeswax) and surface-modifier [Phospholipon ® 90H (P90H)] (3:7) – phospholipid-modified beeswax-based nano-emulgels – for prolonged duration of action and improved oromucosal bioavailabiliy of miconazole nitrate (MN), a poorly water-soluble imidazole antifungal that is commonly associated with poor aqueous solubility and dissolution, low bioavailability and short half-life in the treatment of oropharyngeal candidiasis. Solid lipid nanoparticles (SLNs) prepared with P90H-modified beeswax-based lipid matrix (SRMS) by high-shear hot homogenization (melt-emulsification) had low polydispersity indices, with average particle size and encapsulation efficiency values in the range of 204.0 ± 2.9 to 263.0 ± 7.1 nm and 36.23 ± 2.01 to 58.87 ± 3.56%, respectively. SRMS-based nano-emulgels developed from the SLNs by dispersion in polycarbophil (a mucoadhesive polymer) were stable and had better prolonged drug release (T12h = 36.25 – 63.67 %) than marketed formulation (Daktarin® oral gel) which showed fast drug release (T6h = 100%) in simulated salivary fluid (pH=6.8). This study has shown that phospholipid-modified beeswax-based lipid nano-emulgels could be employed as better alternative delivery system than Daktarin® oral gel to improve oropharyngeal dissolution and delivery of MN.
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KEYWORDS: Solidified reverse micellar solution (SRMS); Miconazole nitrate (MN); Oropharyngeal drug delivery; Solid lipid nano-dispersions (SLN)-based nano-emulgel; Phospholipon® 90H; Beeswax.