Synthesis and characterization of novel dextran-conjugated macromolecules of aceclofenac

Authors

  • A Rasheed Department of Pharmaceutical Chemistry, Sree Vidyanikethan College of Pharmacy, Sree Sainath Nagar, Tirupati-517102, Andhra Pradesh, India
  • U Krishna Department of Pharmaceutical Chemistry, Sree Vidyanikethan College of Pharmacy, Sree Sainath Nagar, Tirupati-517102, Andhra Pradesh, India
  • P Sivakrishna Reddy Department of Pharmaceutical Chemistry, Sree Vidyanikethan College of Pharmacy, Sree Sainath Nagar, Tirupati-517102, Andhra Pradesh, India
  • A Mishra Acharya Narendradev College of Pharmacy, Babhnan, Gonda, Uttar Pradesh, India

Keywords:

Aceclofenac, polymeric prodrug, dextran, ulcer index, histopathology

Abstract

The study involves the condensation of acylimidazole derivatives of acaclofenac (AC) with dextran 10,000 and 20,000 to obtain aceclofenac-dextran prodrugs AC10 and AC20 respectively with an aim to improve aqueous solubility, increase therapeutic efficiency and reduce the gastrointestinal side effects. The structure of synthesized prodrugs was confirmed by IR and NMR spectroscopy. The molecular weight was determined by Mark-Howink Sakurada equation and the degree of substitution was obtained as 13.3 and 16 % for the prodrugs. In vitro hydrolysis carried out in simulated gastric fluid (SGF), simulated intestinal fluid (SIF) and simulated colonic fluid (SCF) showed faster hydrolysis in SIF and SCF. The percentage anti-inflammatory activity of AC was found as 49.56 whereas an improved value of 56.44 and 61.82 % were obtained for AC10 and AC20 respectively. The prodrugs showed improved analgesia and reduced ulcerogenicity than aceclofenac, thereby proving to be better in action than the parent drug.

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Published

2011-03-20

How to Cite

1.
Rasheed A, Krishna U, Sivakrishna Reddy P, Mishra A. Synthesis and characterization of novel dextran-conjugated macromolecules of aceclofenac. Ars Pharm [Internet]. 2011 Mar. 20 [cited 2024 Jul. 22];52(1):5-11. Available from: https://revistaseug.ugr.es/index.php/ars/article/view/4696

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