Miconazole nanosuspensions: Influence of formulation variables on particle size reduction and physical stability

Cerdeira, Ana M.; Mazzotti, Marco; Gander, Bruno

doi:10.1016/j.ijpharm.2010.06.020

Cited by 140 publications

(75 citation statements)

References 19 publications

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“…4d). The solubility of miconazole in water is approximately 3 μg mL −1 (29), which is the lowest among the APIs used in this study (the solubility of phenytoin, bezafibrate, and flurbiprofen in water are approximately 32 μg mL −1 (30), 38 μg mL −1 (31), and 32 μg mL −1 (32), respectively). Therefore, a 60-min dissolution test time was insufficient for 100% release of miconazole.…”

Section: Discussionmentioning

confidence: 86%

In Vitro and In Vivo Characterization of Drug Nanoparticles Prepared Using PureNano™ Continuous Crystallizer to Improve the Bioavailability of Poorly Water Soluble Drugs

Tahara

Nishikawa

Matsui³

et al. 2016

Pharm Res

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Section: Discussionmentioning

confidence: 86%

In Vitro and In Vivo Characterization of Drug Nanoparticles Prepared Using PureNano™ Continuous Crystallizer to Improve the Bioavailability of Poorly Water Soluble Drugs

Tahara

Nishikawa

Matsui³

et al. 2016

Pharm Res

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“…A previously optimized formulation [14] containing 20 wt-% miconazole, 5 wt-% HPC, and 0.025 wt-% SDS was selected to evaluate the effect of the milling parameters on miconazole particle size reduction. The results reveal that miconazole particle size reduction depended primarily on the specific energy input, a value that was measured by the energy consumption during the grinding process (Figs.…”

Section: Effect Of Milling Parameters On Miconazole Particle Size Redmentioning

confidence: 99%

“…S EI , which is proportional to NS EB , can be measured by the power consumption over time [12]. The present work focuses on the importance of process parameters of wet-nanogrinding for the particle size reduction of the poorly water-soluble antifungal compounds miconazole and itraconazole, and the antiviral compound etravirine, all having similar mechanical properties in terms of elastic and plastic deformation and formulated according to a previously optimized composition for miconazole [14].…”

Section: Introductionmentioning

confidence: 99%

Role of Milling Parameters and Particle Stabilization on Nanogrinding of Drug Substances of Similar Mechanical Properties

Cerdeira¹,

Gander²,

Mazzotti³

2011

Chem. Eng. Technol.

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The feasibility and efficiency of wet-nanogrinding of three drug substances (miconazole, itraconazole, etravirine) with similar elastic and plastic properties proved to depend primarily on the adequate electrostatic and steric stabilization of the nanoparticles and the specific energy input. Particle stabilization was provided by sodium dodecyl sulfate (SDS) and hydroxypropylcellulose. The specific energy input was defined by the grinding time, grinding bead size, and stirrer tip speed. Miconazole and itraconazole exhibited similar milling behavior, whereas etravirine nanosuspensions revealed agglomerates and increasing viscosity with increasing specific energy input. Agglomeration and viscosity increase were successfully counteracted by increasing the SDS concentration in the nanosuspension from 0 to 0.125 %. Under the provision of proper particle stabilization, the three drug substances could be nanosized to a mean size of ∼ 130 nm, with 90 % of all particles being smaller than ∼ 250 nm.

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“…[7][8][9] Miconazole has been extensively used for the treatment of dermatophytosis, cutaneous mycosis, pityriasis, fungal vaginitis, and oropharyngeal candidiasis. [10][11][12][13] Various approaches have been used to overcome its limitation of poor water solubility, such as the addition of surfactants, co-precipitation techniques, or by incorporating miconazole into colloidal carrier systems, including lipid nanoparticles. [14][15][16] These systems have been shown to enhance the antifungal activity of miconazole.…”

Section: Introductionmentioning

confidence: 99%

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

Aljaeid¹,

Hosny²

2016

IJN

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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.

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Miconazole nanosuspensions: Influence of formulation variables on particle size reduction and physical stability

Cited by 140 publications

References 19 publications

In Vitro and In Vivo Characterization of Drug Nanoparticles Prepared Using PureNano™ Continuous Crystallizer to Improve the Bioavailability of Poorly Water Soluble Drugs

In Vitro and In Vivo Characterization of Drug Nanoparticles Prepared Using PureNano™ Continuous Crystallizer to Improve the Bioavailability of Poorly Water Soluble Drugs

Role of Milling Parameters and Particle Stabilization on Nanogrinding of Drug Substances of Similar Mechanical Properties

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

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