Design, characterization and pharmaceutical/pharmacological applications of ibuprofen conjugates based on hydroxyethylcellulose

We synthesized polymeric prodrugs in which ibuprofen (IBU) was conjugated in a one-pot preparation to the hydrophilic polysaccharide hydroxyethylcellulose (HEC). The amphiphilic conjugates formed nanoparticles of 450–700 nm diameter at a water/DMSO interface. Synthesized HEC-IBU conjugates showed si...

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Veröffentlicht in:RSC advances 2017, Vol.7 (80), p.50672-50679
Hauptverfasser: Abbas, Khawar, Amin, Muhammad, Hussain, Muhammad Ajaz, Sher, Muhammad, Abbas Bukhari, Syed Nasir, Edgar, Kevin J.
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Sprache:eng
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Zusammenfassung:We synthesized polymeric prodrugs in which ibuprofen (IBU) was conjugated in a one-pot preparation to the hydrophilic polysaccharide hydroxyethylcellulose (HEC). The amphiphilic conjugates formed nanoparticles of 450–700 nm diameter at a water/DMSO interface. Synthesized HEC-IBU conjugates showed significant anti-inflammatory (44–77% inhibition) and immunomodulatory potential in paw-edema and cytokine release assays, respectively. Cell viability studies on L929 cell lines were performed for HEC-IBU prodrugs. Pharmacokinetic studies in rabbit models revealed that IBU from the conjugate reaches a peak plasma concentration ( C max ) of 20 μg mL −1 in 4 h while the plasma half-life was noted to be 5.82 h μg mL −1 .
ISSN:2046-2069
2046-2069
DOI:10.1039/C7RA08502H