# Enhancement of oral bioavailability of risedronate through xyloglucan rafts

## TL;DR

This study improves the absorption of a drug called risedronate by creating a protective raft in the stomach, reducing irritation and increasing effectiveness.

## Contribution

A novel raft-forming formulation enhances risedronate bioavailability and reduces gastrointestinal irritation.

## Key findings

- The XR5 formulation showed 99.97% risedronate release in simulated gastric fluid within 20 minutes.
- XR5 demonstrated better pharmacokinetic performance compared to the Actonel® tablet.
- The raft formulation improved risedronate bioavailability and chemical stability.

## Abstract

Bisphosphonates irritate the stomach and oesophagus and have a very limited absorption. The purpose of this study was to increase risedronate (RDN) oral bioavailability by causing a raft to form in the stomach. The creation of a raft prevents the irritation of the stomach and oesophagus caused by bisphosphonates. FTIR, TGA, and DSC were used to characterise the RDN, XLG, and the created formulation. In addition to a cell viability analysis utilising Caco-2 cells, the release of RDN was investigated in 0.1 N HCl, 0.5 N HCl, 1 N HCl, and simulated gastric fluid (SGF). For the pharmacokinetic investigation, the XR5 formulation and the Actonel® tablet were chosen as the test and reference formulations, respectively. Using a parallel design, twelve healthy albino rats were split into two groups, and blood samples were gathered for a whole day. RDN was distributed uniformly throughout the raft and demonstrated chemical stability by the FTIR. The formulation’s thermal stability was demonstrated by the TGA and DSC. At 20 min, the SGF showed a 99.97% RDN release. When compared to the RDN suspension, the pharmacokinetics revealed better RDN values from the XLG raft. The RDN from the recently developed XR5 has a better bioavailability than the Actonel® tablet.