Flurbiprofen conjugates based on hydroxyethylcellulose: Synthesis, characterization, pharmaceutical and pharmacological applications

Khawar Abbas, Muhammad Ajaz Hussain, Bukhari Syed Nasir Abbas, Muhammad Amin, Muhammad Nawaz Tahir, Sheshanath V. Bhosale

Research output: Contribution to journalArticle

1 Citation (Scopus)

Abstract

Present study deals with fabrication of macromolecular prodrugs (MPDs) of flurbiprofen (FLB) with hydroxyethylcellulose (HEC). FLB was activated using p-toluenesulfonyl chloride and reacted with pre-dissolved HEC to yield HEC-FLB conjugates 1–3. Resultant prodrugs showed moderate to high degree of substitution (DS: 0.40–1.74) and assembled into nanoparticles of 220–550 nm at water/DMSO interface. Pharmacokinetic studies of HEC-FLB conjugate revealed a tmax of 4.0 h indicating delayed release of FLB while t1/2 of 10.63 h indicated sustained release characteristics of the conjugate in rabbit model. Pharmacological studies revealed that HEC-FLB conjugates had immunomodulatory potential as results showed 34 and 36% inhibition of Interleukin-6 and tumor necrosis factor-α, respectively. A 79% inhibition of paw edema indicated anti-inflammatory properties of the conjugates. Cell viability studies indicated safety of the conjugates to L929 cell lines up to 24 h in the range of 2–10 mM. Moreover, thermal analysis indicated greater stability of MPDs than FLB.

Original languageEnglish
JournalArabian Journal of Chemistry
DOIs
Publication statusAccepted/In press - 1 Jan 2018
Externally publishedYes

Fingerprint

Flurbiprofen
Drug products
Cells
Pharmacokinetics
Pharmaceutical Preparations
Prodrugs
Thermoanalysis
Substitution reactions
Nanoparticles
Fabrication
Water
Dimethyl Sulfoxide
hydroxyethylcellulose
Interleukin-6
Anti-Inflammatory Agents
Tumor Necrosis Factor-alpha

Keywords

  • Anti-inflammatory activity
  • Flurbiprofen
  • Hydroxyethylcellulose
  • Immunomodulatory assay
  • Prodrug

ASJC Scopus subject areas

  • Chemistry(all)
  • Chemical Engineering(all)

Cite this

Flurbiprofen conjugates based on hydroxyethylcellulose : Synthesis, characterization, pharmaceutical and pharmacological applications. / Abbas, Khawar; Hussain, Muhammad Ajaz; Syed Nasir Abbas, Bukhari; Amin, Muhammad; Tahir, Muhammad Nawaz; Bhosale, Sheshanath V.

In: Arabian Journal of Chemistry, 01.01.2018.

Research output: Contribution to journalArticle

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AU - Bhosale, Sheshanath V.

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