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Vol. 8, Issue 7 (2019)

Synthesis, enzymatic stability and oral bioavailability of poly (Ethylene glycol) acyclovir prodrug

M Kumar, S Alexandar, MV Kumudhavalli and BS Venkateshwaralu
Acyclovir a drug for the treatment of vericella-zoster infections (Shingles) orally in immune competent patients, intravenous in immune compromised patients and coupled to PEG through succinic anhydride spacer. The average molecular weight used for PEG1500 through. The procedure of chemical modification for PEG was conducted by two steps protocol (I) preparation of PEG1500 diacid (II) preparation PEG1500 Acyclovir. The in vitro drug release studies were performed in buffer solution with PH values equal to 1.2, 5.5, 6.8 and 7.4. Enzymatic stability of synthesis polymeric-prodrug was assessed in both pepsin and α-chymotrypsin. It was found that prodrug was fairly stable in stimulated gastric juice (in the presence of pepsin), whereas it is susceptible to hydrolytic action of α- chymotrypsin releasing free acyclovir. It was found that drug release from the prodrug was nearly sustained over a period of 12 hrs and bioavailability was increased. After plasma hydrolysis studies were carried out 91% of acyclovir was released from polymeric backbone. The synthesized polymeric prodrug had capacity to prolong the release of free and active drug acyclovir also retained active drug in blood system for a longer time, improved pharmacokinetics of acyclovir, short half life, solubility and oral bioavailability.
Pages: 74-79  |  1007 Views  224 Downloads

The Pharma Innovation Journal
How to cite this article:
M Kumar, S Alexandar, MV Kumudhavalli, BS Venkateshwaralu. Synthesis, enzymatic stability and oral bioavailability of poly (Ethylene glycol) acyclovir prodrug. Pharma Innovation 2019;8(7):74-79.

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