All4Nutra
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.
Read more here
Mady, O. Y., Khaled, S., Hedaya, A. A., Abdine, N., & Haggag, Y. (2025). Formulation and Characterization of Novel Oral pH-Sensitive Electrospun Nanofibers for Boosting Dissolution and Penetration of Model Class IV Drug. Pharmaceutical Development and Technology, 1–19. https://doi.org/10.1080/10837450.2025.2517709
See our next webinar:
Smarter Stabilization for Lipid Nanoparticles: Formulating Biopharmaceuticals with Sucrose
Date: Jun 24, 2025, Time: 4:00 PM (Amsterdam, Berlin)
