A Dual-Function Gastroretentive System: Enhancing Ofloxacin Bioavailability via Floating-Bioadhesive Pellets Based on...

This study aimed to design and characterize a novel dual-function floating-bioadhesive drug delivery system based on a hollow structure to extend gastroretentive time and enhance the bioavailability of ofloxacin.

Hollow spherical shells were fabricated via fluidized-bed coating using a blended polymer film composed of (SuE (Surelease^® E-7-19040) and EuN (Eudragit^® NE 30D)). The system integrated a hollow spherical shell, a waterproof layer, a drug layer, a release-retarding ethylcellulose (EC) film, and an outer bioadhesive layer. The mechanical properties, in vitro floating and bioadhesive behavior, drug release profile, and in vivo pharmacokinetics were comprehensively evaluated.

The blended film at a SuE/EuN ratio of 4:4 exhibited optimal mechanical rigidity and strength for the hollow shell. Analysis of the release profile showed a zero-order release for the first 4 h, which was in accordance with the predicted value. The optimized formulation demonstrated excellent buoyancy with a floating rate of 96.3±0.5% and 100% bioadhesion on gastric mucosa. In vivo pharmacokinetic studies in New Zealand rabbits revealed that the test formulation had a prolonged elimination half-life (6.65±0.94 h) and a relative bioavailability of 112.2±14.9% compared to the reference tablet.

The developed floating-bioadhesive system successfully combined hollow-structure buoyancy with mucoadhesion to achieve prolonged gastric retention and sustained drug release, offering a feasible approach for gastroretentive drug delivery systems.