Design,characterization and enhanced bioavailability of hydroxypropylcellulose-naproxen conjugates |
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Affiliation: | 1. Department of Chemistry, University of Sargodha, Sargodha 40100, Pakistan;2. Chemistry Department, King Fahd University of Petroleum and Minerals, Dhahran 31261, Saudi Arabia |
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Abstract: | Polysaccharides are beneficially used as drug carriers via prodrug formation and offer a mechanism for better effectiveness and delivery of the drug. The unique geometry of hydroxypropylcellulose (HPC), a polysaccharide, allows the attachment of drug molecules with a higher degree of substitution because the hydroxyls groups are projected outside the HPC chains. Therefore HPC-Naproxen conjugates, i.e., macromolecular prodrugs, were synthesized using a powerful acylation reagent carbonyldiimadazole (CDI) in N,N' dimethylacetamide (DMAc) solvent. The reactions were carried out at 80 °C under stirring for 24 h and inert environment. This reaction strategy appeared efficient to obtain a high degree of drug substitution (DS = 0.88–1.40) on the polymer parent chain as calculated by UV–visible spectrophotometry after hydrolysis of the samples. The method provides high efficacy as product yields were high (77–81%). Macromolecular prodrugs (MPDs) with different DS of naproxen designed were found soluble in organic solvents. |
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Keywords: | Esterification Hydroxypropylcellulose Naproxen Pharmacokinetics Prodrug |
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