TY  - JOUR
T1  - Cationic Leciplex Nanocarriers for Oral Delivery of Vancomycin Hydrochloride: Design Optimization and Pharmacokinetic Evaluation
A1  - Jinwoo Park
A1  - Minji Kim
A1  - Seung Lee
JF  - Pharmaceutical Sciences and Drug Design
JO  - Pharm Sci Drug Des
SN  - 3062-4428
Y1  - 2026
VL  - 6
IS  - 1
DO  - 10.51847/p78COfv6m5
SP  - 230
EP  - 248
N2  - The aim was to examine how the cationic nanocarrier leciplex (LPX) could boost the oral bioavailability of vancomycin hydrochloride (VAN) through enhancement of its permeation across the intestinal wall. A D-optimal design was employed to evaluate the impact of several variables—namely, lipid molar ratio, cationic surfactant molar ratio, cationic surfactant type, and lipid type—on the attributes of LPX, such as entrapment efficiency (EE%), particle size (P.S.), polydispersity index (P.I.), zeta potential (Z.P.), and steady-state flux (Jss). The optimal formulation underwent additional characterization of morphological features, ex vivo permeation, storage stability, cytotoxicity, and in vivo pharmacokinetics. The optimal LPX displayed a spherical configuration, registering an E.E. of 85.2 ± 0.95%, a P.S. of 52.74 ± 0.91 nm, a P.I. of 0.21 ± 0.02, a Z.P. of + 60.8 ± 1.75 mV, and a Jss of 175.03 ± 1.68 µg/cm²/h. Compared with the plain drug solution, the formulation increased VAN’s intestinal permeation by 2.3-fold. The system also proved to be stable, exhibited strong mucoadhesive behavior, and was well accepted via the oral route. The in vivo pharmacokinetic assessment revealed that, compared with the drug solution, VAN’s Cmax increased 2.99-fold and its AUC0-12 increased 3.41-fold. Collectively, these results underscore the capability of LPX to elevate the oral bioavailability of drugs with inherently poor absorption.
UR  - https://galaxypub.co/article/cationic-leciplex-nanocarriers-for-oral-delivery-of-vancomycin-hydrochloride-design-optimization-an-f2gmt9xhoxoqxzk
ER  -