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Enhancement of dissolution rate and bioavailability of aceclofenac: A chitosan-based solvent change approach

Mutalik, Srinivas and Parambil, Anju and Krishnan, Manoj and Nayak, Usha Achutha (2008) Enhancement of dissolution rate and bioavailability of aceclofenac: A chitosan-based solvent change approach. International Journal of Pharmaceutics, 350 (1-2). pp. 279-290. ISSN 0378-5173/$

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Abstract

In this study the significant effect of chitosan on improving the dissolution rate and bioavailability of aceclofenac has been demonstrated by simple solvent change method. Chitosan was precipitated on aceclofenac crystals using sodium citrate as the salting out agent. The pure drug and the prepared co-crystals with different concentrations of chitosan (0.05–0.6%) were characterized in terms of solubility, drug content, particle size, thermal behaviour (differential scanning calorimetry, DSC), X-ray diffraction (XRD), morphology (scanning electron microscopy, SEM), in vitro drug release and stability studies. The in vivo performance was assessed by preclinical pharmacodynamic (analgesic and anti-inflammatory activity) and pharmacokinetic studies. The particle size of the prepared co-crystals was drastically reduced during the formulation process. The DSC showed a decrease in the melting enthalpy indicating disorder in the crystalline content. The XRD also revealed a characteristic decrease in crystallinity. The dissolution studies demonstrated a marked increase in the dissolution rate in comparison with pure drug. The considerable improvement in the dissolution rate of aceclofenac from optimized crystal formulation was attributed to the wetting effect of chitosan, decreased drug crystallinity, altered surface morphology and micronization. The optimized co-crystals exhibited excellent stability on storage at accelerated conditions. The in vivo studies revealed that the optimized crystal formulation provided a rapid pharmacological response in mice and rats besides exhibiting improved pharmacokinetic parameters in rats.

Item Type: Article
Uncontrolled Keywords: Aceclofenac; Chitosan; Crystals; Sodium citrate; Dissolution; Pharmacokinetics; Pharmacodynamics Aceclofenac; Chitosan; Crystals; Sodium citrate; Dissolution; Pharmacokinetics; Pharmacodynamics Aceclofenac; Chitosan; Crystals; Sodium citrate; Dissolution; Pharmacokinetics; Pharmacodynamics Aceclofenac; Chitosan; Crystals; Sodium citrate; Dissolution; Pharmacokinetics; Pharmacodynamics
Subjects: Pharmacy > MCOPS Manipal > Pharmaceutics
Depositing User: KMC Manipal
Date Deposited: 28 Apr 2012 04:12
Last Modified: 28 Apr 2012 04:12
URI: http://eprints.manipal.edu/id/eprint/76347

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