Predicting the Intestinal Permeability and Oral Absorbable Fraction of Vancomycin-Loaded Eudragit RS-100 Nanoparticles Using Single-Pass Intestinal Perfusion in Rats

Abstract

Background: Particle size strongly affects antibiotic efficacy by influencing drug permeability and tissue penetration. Vancomycin (VCM) hydrochloride, due to its large hydrophilic nature, cannot effectively cross the intestinal barrier and is usually given intravenously. Reducing particle size to nanoparticles is a strategy to improve absorption and transport across biological membranes. Objectives: The present study evaluated the intestinal permeability coefficient and the orally absorbable fraction of VCM nanoparticles in comparison to their conventional form. Methods: The single-pass intestinal perfusion (SPIP) technique was used to evaluate the effective permeability (Peff), fraction absorbed (Fa), and total absorption of VCM in nanoparticle and solution forms at concentrations of 200, 300, and 400 µg/mL, with a flow rate of 0.2 mL/min for 80 minutes. Results: The data revealed that the Peff of VCM in nanoparticle form was 2.16, 1.43, and 2.66 times greater than that of conventional VCM at concentrations of 200, 300, and 400 µg/mL, respectively. Stability testing further showed that VCM nanoparticles remained intact with no signs of degradation after 0, 1, and 2 hours. Conclusions: These results indicate that VCM nanoparticles have the potential to enhance intestinal permeability and may represent a promising approach for oral delivery, pending confirmation in further in vivo and clinical investigations.