Flurbiprofen conjugates based on hydroxyethylcellulose: Synthesis, characterization, pharmaceutical and pharmacological applications
| Autor: | Khawar Abbas, Sheshanath V. Bhosale, Syed Nasir Abbas Bukhari, Muhammad Ajaz Hussain, Muhammad Nawaz Tahir, Muhammad Amin |
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| Jazyk: | angličtina |
| Rok vydání: | 2020 |
| Předmět: |
Chromatography
Macromolecular prodrugs Chemistry General Chemical Engineering Flurbiprofen 02 engineering and technology General Chemistry Prodrug 010402 general chemistry 021001 nanoscience & nanotechnology 01 natural sciences 0104 chemical sciences lcsh:Chemistry Pharmacokinetics lcsh:QD1-999 Rabbit model medicine Viability assay 0210 nano-technology Conjugate Paw edema medicine.drug |
| Zdroj: | Arabian Journal of Chemistry, Vol 13, Iss 1, Pp 2101-2109 (2020) |
| ISSN: | 1878-5352 |
| Popis: | 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. Keywords: Hydroxyethylcellulose, Flurbiprofen, Prodrug, Immunomodulatory assay, Anti-inflammatory activity |
| Databáze: | OpenAIRE |
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