Characterization of a dextran–coated layered double hydroxide acetylsalicylic acid delivery system and its pharmacokinetics in rabbit

The aim of this study was to prepare a dextran–coated layered double hydroxide acetylsalicylic acid (DEX–LDH–ASA) delivery system by co-precipitation of LDH–ASA and its in-situ compositing with DEX. The structure of the system was investigated using X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR) and thermogravimetry (TG). Its in vitro drug release properties and in vivo pharmacokinetics in rabbit were also determined. The results show that the DEX–LDH–ASA system retained the crystal structure of LDH–ASA and gave a marked improvement in its dispersion. It also prolonged the release of ASA and shifted the release pattern from first-order to zero-order kinetics. The pharmacokinetics of ASA administered in the DEX–LDH–ASA system to rabbits produced two absorption peaks with a Cmax of 14.8±1.7 mg/L at 2.11±0.69 h and an elimination half-life of 2.25±0.84 h for the first peak. The fact that delivery of ASA in the DEX–LDH–ASA system was sustained with improved bioavailability indicates the potential of the system as a controlled release formulation with application to other drugs.

A three-level supramolecular drug delivery system has been produced by coating a layered double hydroxide-acetylsalicylic acid complex with dextran. The composite showed improved dispersion of ASA-loaded particles and both the in vitro and in vivo controlled release performance. The system should be useful for development of controlled release formulations of other drugs to reduce their adverse effects and increase their therapeutic efficacy.Figure optionsDownload as PowerPoint slide