PMID: 11934234Apr 6, 2002Paper

A biodegradable injectable implant sustains systemic and ocular delivery of an aldose reductase inhibitor and ameliorates biochemical changes in a galactose-fed rat model for diabetic complications

Pharmaceutical Research
J V AukunuruU B Kompella

Abstract

To fabricate and characterize in vitro and in vivo performance of a sustained release biodegradable implant for N-4-(benzoylaminophenylsulfonyl glycine) (BAPSG), a novel aldose reductase inhibitor. The ability of BAPSG to inhibit aldose reductase activity and glucose-induced vascular endothelial growth factor (VEGF) expression was assessed in a retinal pigment epithelial cell line (ARPE-19). A poly (DL-lactic-co-glycolic acid) implant containing 50% w/w BAPSG was fabricated and characterized for drug loading, in vitro drug release, and the thermal behavior of the drug and the polymer. Implants were injected subcutaneously into a galactose-fed diabetic rat model and cataract scores, plasma and tissue drug levels, galactitol levels in the lens and the retina, glutathione levels in the plasma, lens, cornea and retina and VEGF expression in the retina were determined on or until 18 days. BAPSG inhibited aldose reductase activity and reduced VEGF expression in ARPE-19 cells. Implants (1 x 4 mm), with a loading efficiency of 106 +/- 7% for BAPSG, were fabricated. Upon implant fabrication, while the glass transition temperature of the polymer decreased, the melting point of the drug was not affected. In vivo drug release correlated we...Continue Reading

Citations

Mar 17, 2009·Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics·Surya P AyalasomayajulaUday B Kompella
Mar 15, 2011·Therapeutic Delivery·Uday B KompellaVincent H L Lee
Mar 20, 2012·Expert Opinion on Drug Metabolism & Toxicology·Bruno SarmentoDomingos Ferreira
Mar 9, 2010·Expert Opinion on Drug Delivery·Aniruddha AmriteUday Kompella
Aug 22, 2017·Nanomaterials·Maria Porta-I-BatallaLluis F Marsal
Jul 11, 2003·World Journal of Gastroenterology : WJG·Jun-Fei JinWei Xie
Mar 18, 2004·The Journal of Pharmacy and Pharmacology·Gangadhar SunkaraUday B Kompella
Feb 9, 2010·Annals of Biomedical Engineering·Cheng-Wen Lin, Fan Yuan
May 14, 2016·Expert Opinion on Drug Delivery·Jayabalan NirmalRupesh Agrawal

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