Effect on in-vitro release of individual and dual contraceptive drug loading from gelatin electrospun fibers

Abstract

The transdermal route of drug administration provides many advantages for delivering a wide variety of drugs or other beneficial agents. The aim of this work was to investigate the suitability of electrospinning process to develop a drug delivery system for two contraceptive drugs levonorgestrel (LNG) and ethinylestradiol (EE). The study describes both individual (LNG-alone and EE-alone) and dual drug (LNG and EE) incorporation in gelatin matrix, their loading properties and their release kinetics for extended time of 7 days in different formulations. Scanning electron microscopy (SEM) reveals decrease in fiber diameter for dual drug incorporated fibers compared to individual drug loaded fibers. XRD and DSC results showed that both the drugs were amorphously distributed in the fibers and there was no effect on the polymer property after drug incorporation. A high encapsulation efficiency (∼90–100%) and drug loading (>90%) were observed for individual as well as dual drug loaded fibers. In in-vitro release studies, the release kinetics was found to be satisfactorily described by zero-order and first –order model for LNG, whereas in EE the release kinetics was found to be suitably fit to Higuchi model. We also observed that release of EE was affected by the drug content, whereas no significant difference was seen on LNG release for individual drug loaded samples. However, LNG release was found to increase in dual drug loaded samples. The in vitro permeability studies showed that both drugs were permeable through membrane filter and zero order sustained drug release was attained with dual drug incorporated gelatin fibers for a period of 7 days. The electrospun fibers were found to be biocompatible with L929 fibroblast cells. Thus, the present study establishes the feasibility of using these fibers for application in transdermal drug delivery system for contraceptive steroids.