Invitro efficacy of core shell microparticle to circumvent efflux transporter

摘要

Although particulate delivery systems are more effective in target delivery of drugs than conventional dosage forms, the drugs are still susceptible to the efflux systems in the cell membrane [1]. To overcome the efflux barrier yet retain the advantages of particulate delivery, core shell microparticles (CSM) were developed. Phenethyl Isothiocyanate (PEITC), a potent therapeutic agent, and efflux transporter inhibitors - verapamil HCl, nifedipine or tamoxifen, were encapsulated in the core shell type drug delivery system. The cytotoxicity of CSMs was assessed in Calu3 cell line and used as an index for assessment of inhibitor-induced enhancement of drug transport. This study confirmed the in vitro efficacy of core shell drug delivery system in circumventing efflux transporters.