Conjugation of Naproxen to Polyethylene Glycol (PEG) and to Evaluate Drug Release Study

Author(s): S. Sourin and DG. Debaprotim

Abstract: The field of polymer therapeutics has evolved over the past decade and has resulted in the development of polymer-drug conjugates with a wide variety of architectures and chemical properties. Aim: Conjugation of naproxen to Poly Ethylene Glycol and to evaluate drug release study. Method: Poly (ethylene glycol) 4000(PEG) was obtained from M/s. Merck. Mumbai. Thionyl chloride, and glycine were obtained from M/s. SD Fine Chemicals and used as such. Glycine and leucine was being obtained from M/s. Loba Chemicals, Mumbai, and used as such. Glycine-leucine, leucine-glycine, were obtained from M/s. Sigma-Aldrich Germany. Dicyclohexyl carbidomide (DCC) and 4-dimethyl amino pyridine (DMAP) were obtained from M/s. Merck, Germany. Triethylamine, Dimethylformamide (DMF) were obtained from M/s. Ranbaxy fine Chemicals. Naproxen was obtained from M/s. Matrix Laboratories Limited, Secunderabad as gift sample, and was used after confirming its purity by its melting point and IR spectrum. All other solvents used were purified by standard techniques. Result: The conjugation of Naproxen to PEG was performed and evaluated for drug release study along with the characterization and the values obtained is discussed and explained below. Conclusion: The use of simple synthetic procedures and the quite general applicability of the drug anchoring strategy render the entire approach suitable for the synthesis of similar conjugates, varying the structure of the NSAID and the polymer length. It is noticeable that, in all cases, the drug-polymer conjugates were obtained with a high degree of purity, avoiding expensive and time consuming purification procedures.

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