Miconazole-loaded solid lipid nanoparticles: formulation and evaluation of a novel formula with high bioavailability and antifungal activity

Abstract

Background and objective 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. Methods 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. Results The MN-SLN, consisting of 1.5% miconazole, 2% Precirol ATO5, 2.5% Cremophor RH40, 0.5% Lecinol, and 0.1% Dicetylphosphate, had an average diameter of 23 nm with a 90.2% entrapment efficiency. Furthermore, the formulation of MN-SLNs enhanced the antifungal activity compared with miconazole capsules. An in vivo pharmacokinetic study revealed that the bioavailability was enhanced by >2.5-fold. Conclusion MN-SLN was more efficient in the treatment of candidiasis with enhanced oral bioavailability and could be a promising carrier for the oral delivery of miconazole.

Design, Optimization and Characterization of a Transfersomal Gel Using Miconazole Nitrate for the Treatment of Candida Skin Infections

“…Conventional formulations are given in higher doses to overcome this issue and compensate for low permeability. In recent years, the use of lipid vesicles as carriers for topical drugs has attracted great attention due to their ability to overcome the barrier properties of the skin [ 5 ].…”

Preparation and Characterization of Itraconazole- or Miconazole-Loaded PLGA Microspheres

“…Several studies have reported amorphization of ITCZ in various polymers, such as cellulose acetate phthalate, polyvinyl acetate phthalate, hydroxypropylmethylcellulose, hydroxypropylmethylcellulose acetate succinate and polyvinylpyrrolidone. [5][6][7] However, to our knowledge, no articles have yet been published on amorphization of ITCZ or MCZ in PLGA. Therefore, the existence of amorphized drug in ITCZ-and MCZ-PLGA MS was examined using DSC.…”

“…1,2) A number of strategies have been tried for enhancing the release rates and bioavailabilities of oral dosage forms of these antifungal drugs. [3][4][5][6][7] In injectable formulations, the use of cosolvents, such as ethanol, macrogol and propylene glycol, or surfactants, has been shown to successfully enhance the solubilization of the drugs. 8) Recently, in order to achieve sustained-release delivery, an approach using biodegradable microspheres (MS) containing antimicrobial agents or other types of drug has been tried.…”

Intranasal administration of brain-targeted HP-β-CD/chitosan nanoparticles for delivery of scutellarin, a compound with protective effect in cerebral ischaemia

“…The entrapment efficiency was determined by centrifugation method as reported previously . One millilitre of CD/CS‐SCU‐NPs was centrifuged at 15 000 rpm 24 400 g for 15 min (4°C), and the clear supernatant solutions were obtained.…”

“…The entrapment efficiency was determined by centrifugation method as reported previously. [23,24] One millilitre of CD/CS-SCU-NPs was centrifuged at 15 000 rpm 24 400g for 15 min (4°C), and the clear supernatant solutions were obtained. After dilution by 10-fold methanol, concentrations of SCU in the supernatant (free drug) were determined by HPLC consisting of a pump (Model LC-20A; Shimadzu, Kyoto, Japan), a reversed-phase C 18 column (150 9 4.5 mm, 3 lm) maintained at room temperature, a variable wavelength UV detector (Model SPD-20A; Shimadzu, Kyoto, Japan) at 335 nm.…”