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Macromolecular prodrugs (MPDs) of aspirin and salicylic acid were synthesized by covalent attachment to hydroxypropylcellulose (HPC) using p-toluenesulfonyl chloride in N,N-dimethylacetamide. The present synthesis strategy resulted in organo-soluble MPDs with 78–86 % yield and degree of drug substitution 0.53–1.96 and 0.68–2.10 for aspirin and salicylic acid, respectively. The size exclusion chromatography...
Novel macromolecular prodrugs of the second-generation fluoroquinolone antibiotic ofloxacin were fabricated based on the hydrophilic biopolymers hydroxypropylcellulose (HPC) and hydroxyethylcellulose (HEC). HPC- and HEC-ofloxacin conjugates were synthesized by activation of ofloxacin with p-toluenesulfonyl chloride under homogeneous reaction conditions at 70 °C in a one-pot synthesis. Structures of...
This article presents synthesis of novel macromolecular prodrugs of aceclofenac (an anti-inflammatory drug) onto hydroxypropylcellulose (HPC). The HPC-aceclofenac conjugates were prepared using an acylating agent 1,1′-carbonyldiimidazole (CDI) under homogenous reaction conditions. Aceclofenac was first activated by using CDI to form its N-acylimidazole. The N-acylimidazole of aceclofenac was then...
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