Abstract
Objective: The principal objective of this research work was to formulate tioconazole into mucoadhesive microspheres which were inserted into the vagina for sustaining the anti-fungal activity and protecting the liver and the kidney from the harmful drug side effects.Methods: Microspheres were prepared by the emulsion solvent evaporation method, using different ratios of the drug with either ethyl cellulose N14 or hydroxypropylmethylcellulose K100M (HPMC K100M) as mucoadhesive polymers. The formulated microspheres were evaluated for the particle size, entrapment efficiency, yield percentage, mucoadhesion strength, swelling percentage, pH, in vitro release of the drug and finally in vitro antifungal activity.Results: The optimized formulae were F3 and F6, which showed drug entrapment of 88.4±2.5 % and 97.8±1.6 %, yield percentage of 85.0±2.3% and 95.2±1.2%, mucoadhesion strength of 31.5±1.6 and 38.1±1.6 *103 dyne/cm2, swelling percentages of 143.1±1.3 and 154.2±0.8, pH of 4.7±0.1 and 4.6±0.5, and particle size of 400±3.5 µm and435±7. 8 µm respectively. F3 and F6 released about 72.8%±3.2 and 58.4%±2.7 of the drug after 8 h respectively. F3 and F6 showed a significant anti-fungal activity.Conclusion: Ethyl cellulose and hydroxyl propyl methylcellulose mucoadhesive microspheres are considered a good way to increase the duration of the anti-fungal activity of tioconazole with minimum side effects.
Highlights
MethodsMicrospheres were prepared by the emulsion solvent evaporation method, using different ratios of the drug with either ethyl cellulose N14 or hydroxypropylmethylcellulose K100M (HPMC K100M) as mucoadhesive polymers
Vaginal cavity is an important and alternative area for the drugs that suffer from either first pass metabolism or extensive destruction in the stomach
Ethyl cellulose N14, carbopol 940 (Cbp 940) and HPMC K100 M were kindly supplied by EIPICO Company, Egypt
Summary
Microspheres were prepared by the emulsion solvent evaporation method. The drug and the polymer were accurately weighed by electron digital balance (Metter-Toledo, Ag, CH 8606, Greifense, Switzerland), and were dissolved into 20 ml methylene chloride at ambient room temperature. A significant reduction in the yield percentage with the increase of either stirring rate [18] or surfactant concentration [20] was observed (tables 4 and 5) This could be ascribed to the formation of smaller particles which were lost during the filtration and the collection of the microspheres. The increase of the drug to polymer ratio from 1:1 to 1:5, resulted in a significant decrease in the percentage of tioconazole which released after 8 h from 74.1±0.6 (F4) to 58.4±0.3 (F6), and from 88.2±0.5 (F1) to 72.8±0.3 (F3). It can be concluded that both ethyl cellulose and HPMC loaded tioconazole mucoadhesion microspheres produced a significant antifungal activity against Candida Albicans. Formula Tioconazole solution Tioconazole free ethyl cellulose microspheres, control Tioconazole free HPMC microspheres, control F3 F6
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