Fabrication, characterization, appraisal of bioavailability and immunomodulatory potential of aceclofenac prodrugs based on hydroxyethylcellulose

Khawar Abbas, Muhammad Ajaz Hussain, Bukhari Syed Nasir Abbas, Muhammad Amin, Muhammad Zaman

Research output: Contribution to journalArticle

Abstract

Present study deals with the synthesis of macromolecular prodrugs of aceclofenac (ACL) on to hydrophilic polysaccharide hydroxyethylcellulose (HEC). ACL prodrugs synthesized were thoroughly characterized by spectroscopic techniques and found organo-soluble. The esterified prodrugs showed self-assembly behaviour at solvent interface of DMSO/water and appeared as nanoparticles of 200–550 nm diameter. The HEC-ACL conjugates showed significant inhibition (43%) in the levels of interleukin 6 (IL-6) which indicated its immunomodulatory potential. The conjugates showed 81% inhibition in edema created after carrageenan injection. HEC-aceclofenac conjugates appeared biocompatible in cell viability studies. Bioavailability studies revealed that ACL from the conjugate shows plasma half-life of 7.90 h which is significantly higher than unmodified ACL (3.93 h). Moreover, tmax of 4.0 h with peak plasma concentration (Cmax) of 8.27 μg mL−1 for ACL from conjugate indicated its enhanced bioavailability.

Original languageEnglish
Pages (from-to)856-862
Number of pages7
JournalJournal of Drug Delivery Science and Technology
Volume52
DOIs
Publication statusPublished - 1 Aug 2019
Externally publishedYes

Fingerprint

Prodrugs
Biological Availability
Carrageenan
Dimethyl Sulfoxide
aceclofenac
hydroxyethylcellulose
Nanoparticles
Polysaccharides
Half-Life
Interleukin-6
Edema
Cell Survival
Injections
Water

Keywords

  • Aceclofenac
  • Bioavailability
  • Hydroxyethylcellulose
  • Immunomodulatory potential
  • Prodrug

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

Fabrication, characterization, appraisal of bioavailability and immunomodulatory potential of aceclofenac prodrugs based on hydroxyethylcellulose. / Abbas, Khawar; Hussain, Muhammad Ajaz; Syed Nasir Abbas, Bukhari; Amin, Muhammad; Zaman, Muhammad.

In: Journal of Drug Delivery Science and Technology, Vol. 52, 01.08.2019, p. 856-862.

Research output: Contribution to journalArticle

Abbas, Khawar ; Hussain, Muhammad Ajaz ; Syed Nasir Abbas, Bukhari ; Amin, Muhammad ; Zaman, Muhammad. / Fabrication, characterization, appraisal of bioavailability and immunomodulatory potential of aceclofenac prodrugs based on hydroxyethylcellulose. In: Journal of Drug Delivery Science and Technology. 2019 ; Vol. 52. pp. 856-862.
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