ajopred.com 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
semanticscholar(2020)
摘要
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 beeswaxbased 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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