Abstract
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. Keywords: Nanospheres, desolvation and cross-linking method, ethyl cellulose, betamethazone, in-vitro diffusion studies.> Tropical Journal of Pharmaceutical Research Vol. 4 (2) 2005: pp. 495-500
Highlights
In recent years, there has been a considerable interest in the development of novel drug delivery systems in order to modify and control pharmacokinetic behavior of the drugs
Many of the conventional vehicles such as creams, ointments requires high concentration of active ingredients for effective therapy due to their low efficiency as delivery systems[5]. Particulate carriers such as liposomes and microspheres have been investigated for the delivery of drugs to specific skin compartments in order to control drug input, release, retention and action in/into the skin and to reduce systemic absorption and adverse reactions
In vitro and in vivo experiments proved particulate carriers to be worthwhile for increasing cutaneous bioavailability and decreasing systemic absorption of many drugs[6]
Summary
There has been a considerable interest in the development of novel drug delivery systems in order to modify and control pharmacokinetic behavior of the drugs. Nanoparticles are colloidal drug delivery systems that offer site-specific as well as controlled drug delivery[2,3,4]. Particulate carriers such as liposomes and microspheres have been investigated for the delivery of drugs to specific skin compartments in order to control drug input, release, retention and action in/into the skin and to reduce systemic absorption and adverse reactions. Incorporation of corticosteroids in liposomes provided a higher concentration and efficient delivery of corticosteroids.[8,9] in the present study, an attempt has been made to formulate ethyl cellulose nanospheres containing betamethazone, which may provide prolonged drug delivery in the treatment of inflammation and minimize side effects such as pruritis, hypertrichosis and erythema. Dialysis membrane (Sigma Chemicals), sodium hydroxide (LR grade), linseed oil (commercial grade), Tween 80 (LR grade, SD Fine Chemicals), toluene and potassium dihydrogen phosphate (LR grade, S.D Fine Chemicals) and ethanol (AR grade) were used
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