Design of cellulose ether-based macromolecular prodrugs of ciprofloxacin for extended release and enhanced bioavailability

International Journal of Biological Macromolecules
Muhammad AminKevin J Edgar

Abstract

The present study reveals the syntheses of hydroxypropylcellulose‑(HPC) and hydroxyethylcellulose‑(HEC) based macromolecular prodrugs (MPDs) of ciprofloxacin (CIP) using homogeneous reaction methodology. Covalently loaded drug content (DC) of each prodrug was quantified using UV-Vis spectrophotometry to determine degree of substitution (DS). HPC-ciprofloxacin (HPC-CIP) conjugates showed DS of CIP in the range 0.87-1.15 whereas HEC-ciprofloxacin (HEC-CIP) conjugates showed DS range 0.51-0.75. Transmission electron microscopy revealed that HPC-CIP conjugate 2 and HEC-CIP conjugate 6 self-assembled into nanoparticles of 150-300 and 180-250nm, respectively. Size exclusion chromatography revealed HPC-CIP conjugate 2 and HEC-CIP conjugate 6 as monodisperse systems. In vitro drug release studies indicated 15 and 43% CIP release from HPC-CIP conjugate 2 after 6h in simulated gastric and simulated intestinal fluids (SGF and SIF), respectively. HEC-CIP conjugate 6 showed 16% and 46% release after 6h in SGF and SIF, respectively. HPC-CIP conjugate 2 and HEC-CIP conjugate 6 exhibited half-lives of 10.87 and 11.71h, respectively with area under the curve values of 164 and 175hμgmL-1, respectively, indicating enhanced bioavailability and imp...Continue Reading

References

Apr 1, 1991·European Journal of Clinical Microbiology & Infectious Diseases : Official Publication of the European Society of Clinical Microbiology·V T Andriole
Jan 1, 1986·Antimicrobial Agents and Chemotherapy·T A TartaglioneT M Kerkering
Mar 1, 1985·Antimicrobial Agents and Chemotherapy·G HöffkenP Koeppe
Jun 1, 1987·Antimicrobial Agents and Chemotherapy·K I PlaisanceH C Standiford
Apr 5, 2002·American Journal of Ophthalmology·Rookaya MatherRegis P Kowalski
Apr 19, 2003·The Journal of Antimicrobial Chemotherapy·Monique I Andersson, Alasdair P MacGowan
May 29, 2009·Current Opinion in Chemical Biology·Bernard Testa
Nov 17, 2009·Journal of Medicinal Chemistry·Faustine DubarChristophe Biot
Aug 27, 2010·FEMS Microbiology Reviews·Stephan HeebMiguel Cámara
Sep 8, 2010·Journal of Pharmaceutical Sciences·Valentino J Stella
Jun 16, 2011·Current Topics in Medicinal Chemistry·Suneela S Dhaneshwar, Gaurav Vadnerkar
Jul 9, 2011·Pharmacological Reviews·Kristiina M HuttunenJarkko Rautio
Nov 15, 2011·Current Pharmaceutical Design·Man Chin ChungJean Leandro dos Santos
Apr 13, 2013·Biomacromolecules·Xueyan ZhengKevin J Edgar
Aug 21, 2013·Biomacromolecules·Roselin Rosario-MeléndezKathryn E Uhrich
Apr 22, 2014·International Journal of Pharmaceutics·Catarina FlorindoIsabel M Marrucho
Oct 27, 2016·Infectious Disorders Drug Targets·Prabodh Chander SharmaRakesh Pahwa
Aug 14, 2016·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Di LiXuesi Chen

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