Formulation and Characterization of Novel Oral pH-Sensitive Electrospun Nanofibers for Boosting Dissolution and Penetration of Model Class IV Drug

Abstract

Sulpiride, (a model class IV drug) is a central dopamine antagonist, that is commonly used in the treatment of various psychiatric and gastrointestinal conditions. However, its poor aqueous solubility and low oral bioavailability (20-30%) limit its therapeutic efficacy. Electrospun nanofibers offer a promising method to enhance the oral absorption of poorly water-soluble drugs.

This study, for the first time, aimed to investigate the feasibility of electrospun Eudragit S100-loaded sulpiride nanofibers as an enhanced oral delivery system, compared to drug-loaded solid dispersion. The physicochemical properties of the nanofibers were characterized. The drug’s intestinal permeability was evaluated using an ex vivo non-everted sac technique. Sulpiride-loaded nanofibers exhibited uniform morphology with a very narrow nanosize range of (98.4-123.6 nm) and a high drug-loading efficiency of > 98%. In vitro, dissolution demonstrated a significant enhancement in the sulpiride’s dissolution rates from the nanofiber formulations (> 94% of the drug released within 4 hours) compared to the solid dispersion formulation (˂77% of the drug released).

The nanofiber formulations exhibited a 2-fold increase in the drug’s intestinal permeability and a 4-fold increase in apparent permeability (Papp) compared to the free drug. The improved dissolution and intestinal permeability of sulpiride-loaded nanofibers suggest their potential application for enhancing the oral delivery and therapeutic efficacy of class IV drugs.