Miconazole Prepared by Dana Abdallah Alomoush Supervised by Dr. Samer Al-Adwan
Miconazole Miconazole is an antifungal prescription medicine high in ergosterol content and different in composition from mammalian cells membranes. Approved by the U.S. Food and Drug Administration (FDA) for the treatment of mucocutaneous candidiasis, including: Oropharyngeal candidiasis, a fungal infection of the part of the throat at the back of the mouth Vulvovaginal candidiasis, a fungal infection of the vulva and vagina in females
PHYSICO-CHEMICAL PROPERTIES Origin of the substance : Miconazole is a synthetic antifungal agent belonging to the imidazole group. Chemical structure Structural formula Molecular formula Miconazole C18H14Cl4N20 Molecular weight Miconazole 416.12
PHYSICO-CHEMICAL PROPERTIES Properties of the substance Color White to pale cream State/Form Crystalline or microcrystalline powder Description Odorless or almost odorless Melting point 170.5 °C
PHYSICO-CHEMICAL PROPERTIES Practically insoluble in water; freely soluble in acetone Solubilities are as follows: 1 in 9.5 of alcohol, 1 in 2 of chloroform, 1 in 15 of ether, 1 in 4 of isopropyl alcohol, 1 in 5.3 of methyl alcohol, and 1 in 9 of propylene glycol. pKa (Strongest Basic) Value 6.77 logP Value 5.96
1 Athlete's foot (tinea pedis) 3 Ringworm infections (tinea corporis) 2 Jock itch (tinea cruris) Miconazole is available as both a suppository and cream for the treatment of vaginal yeast infections and the relief of associated vulvar itching and irritation. miconazole cream is effective in treating: Miconazole
Mechanism of action The primary mechanism of action is through inhibition of the CYP450 14α-lanosterol demethylase enzyme, which results in altered ergosterol production and impaired cell membrane composition and permeability, which in turn leads to cation, phosphate, and low molecular weight protein leakage.
Dosage 3 4 1 2 3 4 1 2 Use and dose must be determined by your doctor Teenagers and children younger than 16 years of age: One tablet placed on the upper gum once a day for 14 days Adults and teenagers 16 years of age and older: Vaginal: 5 to 10 g of a 2% cream once daily for 7 to 14 days or tampons containing 100 mg twice a day for 5 days. Oral:
Miconazole-loaded solid lipid nanoparticles: formulation and evaluation of a novel formula with high bioavailability and antifungal activity
The Aim Of The Article 25 % Miconazole is a broad-spectrum antifungal drug that has poor aqueous solubility (<1 µg/mL); as a result, a reduction in its therapeutic efficacy has been reported. The aim of this study was to formulate and evaluate miconazole-loaded solid lipid nanoparticles (MN-SLNs) for oral administration to find an innovative way to alleviate the disadvantages associated with commercially available capsules.
MN-SLNs were prepared by hot homogenization/ultrasonication. The solubility of miconazole in different solid lipids was measured. The effect of process variables, such as surfactant types, homogenization and ultrasonication times, and the charge-inducing agent on the particle size, zeta potential, and encapsulation efficiency were determined. Furthermore, in vitro drug release, antifungal activity against Candida albicans, and in vivo pharmacokinetics were studied in rabbits. Methods
The formulation of miconazole in oral SLNs, which is a novel drug delivery system, enhanced the bioavailability by >2.5-fold compared with the marketed capsules and was more efficient in the treatment of candidiasis. The usage of this formulation could eliminate the major drawbacks of conventionally used capsules. MN-SLNs could be a promising carrier for the oral delivery of miconazole. The optimum MN-SLN formula was composed of 1.5% miconazole, 2% Precirol ATO5, 0.5% Lecithin, 2.5% Cremophor RH40, 0.5% Lecinol, and 0.1% Dicetylphosphate. Results and Conclusion