The aim of this work was to formulate sodium alginate nanospheres of amphotericin B by controlled gellification method and to evaluate the role of the nanospheres as a "passive carrier" in targeted antifungal therapy. Methods: Sodium alginate nanospheres of amphotericin B were prepared by controlled gellification method, and the particle size analysis was carried out by scanning electron microscopy. The carrier capacity of sodium alginate was evaluated in terms of drug to polymer ratio. In vitro release study was carried out on all drug loaded nanospheres by the dialysis method. Release kinetics of drug from different drug loaded nanospheres was also determined. The in vivo antifungal efficacy of nanospheres bound drug vis-à-vis the free drug was evaluated in candidiasis-induced mice models. Results: Preparation of nanospheres through controlled gellification method yielded particles with a size range of 419.6 ± 0.28 nm. Studies on drug to polymer ratio showed a linear relationship between concentration of drug and drug loading capacity. In vitro release kinetic study revealed that the release of drug from the nanospheres followed Fickian diffusion. In vivo studies showed that the nanospherebound drug produced a higher antifungal efficacy than the free drug. Conclusion: The formulated sodium alginate nanospheres containing amphotericin B was found to have better antifungal activity when compared to the free drug and also yielded sustained in vitro release.
Purpose: Lipid nanospheres are used for the passive targeting of cosmetic agents to skin, thereby achieving major benefits such as reduction of total dose and avoidance of systemic absorption. The present study was carried out to exploit the feasibility of using polymeric nanospheres as an alternative and cheaper carrier for targeting corticosteroids to the skin. Methods: Nanospheres were prepared from ethyl cellulose by a modified method of desolvation and cross linking. The drug betamethazone was incorporated into nanospheres and the drug: polymer ratio was evaluated to determine the carrier capacity of the polymer. In vitro release studies of drug-loaded nanospheres were carried out by the centrifugal ultrafiltration method. The kinetics of release was determined and fitted to an empirical equation. The release of drug from drug-loaded nanospheres dispersing in a conventional cream was evaluated. A comparative in vitro diffusion study was carried out between a commercial brand of cream and the cream incorporating nanospheres. Results: Formulation of nanospheres of betamethazone by a modified method produced discrete particles. Studies on drug:polymer ratio showed a linear relationship between drug concentration and percentage of loading. The in vitro release of drug-loaded nanospheres was found to be first order. The comparative in vitro diffusion study between the commercial cream and the formulated cream showed a marked reduction in release rate from nanospheres-bound cream. Conclusion: Formulated topical cream containing nanospheres of betamethazone was found to be a potential dermal delivery system for sustaining the release of the drug.
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