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

• Main Authors: Li-e Dong, Guojing Gou, Lin Jiao
• Format: Article
• Language: English
• Published: Elsevier 2013-12-01
• Series: Acta Pharmaceutica Sinica B
• Subjects: Controlled release; Acetylsalicylic acid; Dextran; Layered double hydroxide; Pharmacokinetics; Rabbit
• Online Access: http://www.sciencedirect.com/science/article/pii/S2211383513000890

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.