Oral Conversion of Injectable Therapeutics using Nanoparticle Platforms: A Proof-of-Concept Study

Abstract

The delivery of therapeutic agents via oral administration remains a cornerstone of patient-centric medicine; however, numerous biologics and vaccines are restricted to injectable formats due to poor oral bioavailability and degradation in the gastrointestinal tract. Nanoparticle-based platforms offer a transformative approach for converting injectable therapeutics into orally administrable formulations, providing enhanced stability, targeted delivery, and controlled release. This study presents a proof-of-concept for the oral conversion of select injectable therapeutics, including protein-based drugs and vaccines, using biodegradable lipid and polymeric nanoparticles. Formulations were characterized for particle size, surface charge, encapsulation efficiency, and in vitro release kinetics under simulated gastrointestinal conditions. Pharmacokinetic and bioavailability assessments were conducted in a rodent model to compare oral nanoparticle formulations against standard injectable counterparts. Statistical analyses demonstrated that nanoparticle-mediated oral delivery significantly improved systemic absorption without compromising therapeutic efficacy. Immunogenicity assays confirmed that oral nanoparticle vaccines elicited robust humoral and cellular immune responses comparable to injectable administration. The findings underscore the potential of nanoparticle platforms to expand the therapeutic landscape, reducing patient dependency on injections and enhancing compliance, particularly in populations with needle aversion. This proof-of-concept establishes a foundation for further preclinical development, optimization of formulation parameters, and eventual translation into clinical applications. The study highlights the critical role of nanotechnology in overcoming gastrointestinal barriers and paves the way for a new generation of orally deliverable biologics.