Abstract
Modifying the surface properties of nanoparticles is crucial for enhancing the oral absorption of encapsulated drugs. Although both mucoadhesion and mucus permeability are essential properties for improving oral absorption, their opposing characteristics render their combination in a single formulation challenging. The present study aimed to integrate both strategies and design a novel oral formulation by creating nanofibers from a mucoadhesive polymer solution containing approximately 100 nm PEGylated liposomes. First, we evaluated the physicochemical properties of PEGylated liposomes released from nanofibers made of sodium carboxymethylcellulose (CMC-Na) and polyvinyl alcohol (PVA), as well as from PVA alone nanofibers. Liposomes released from CMC-Na/PVA nanofibers had a particle size of 533.9 ± 85.0 nm, showing aggregation, while those from PVA nanofibers maintained a particle size without aggregation (142.8 ± 7.31 nm). To increase the liposome content in PVA nanofibers, we used hydroxypropyl-β-cyclodextrin (HPβCD) as a cryoprotectant, converting the suspension to powder and increasing liposome content by approximately 30-fold. PVA nanofibers increasing liposome content had a fiber diameter of 355.5 ± 77.1 nm, and liposomes released from nanofibers retained their morphology. We then used the flow-through method to evaluate the formulation's adhesive properties, and our findings confirmed its better mucosal adhesion and reduced excretion by mucus clearance (about 1/10) compared to a liposome suspension. Subsequent application to rat intestinal tissue showed that the mucus partially dissolved the nanofibers, allowing PEGylated liposomes to penetrate the mucus layer. Oral administration to rats showed improved gastrointestinal retention, thereby confirming that this novel oral formulation may improve drug oral absorption.
Published Version
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