Design of functionalized folic acid–chitosan nanoparticles for delivery of tetracycline, doxorubicin, and tamoxifen

Design of functionalized folic acid–chitosan nanoparticles for delivery of tetracycline, doxorubicin, and tamoxife

Biomolecular study and conjugation of two paraaminobenzoic acid derivatives with serum proteins: drug binding efficacy and protein structural analysis.

Two aminobenzoic acid derivatives DAB-0 and DAB-1 showed distinct biological properties on murine bladder cancer (BCa) cell line MB49-I. In contrast to DAB-1, DAB-0 does not possess any anti-inflammatory activity and is less toxic. Furthermore, DAB-0 does not interfere with INFc-induced STAT1 activation and TNFa-induced IjB phosphorylation, while DAB-1 does. In order to rationalize these results, the binding efficacy of DAB-0 and DAB-1 with serum proteins such a human serum albumin (HSA), bovine serum albumin (BSA) and beta-lactoglobulin (b-LG) was investigated in aqueous solution at physiological pH. Multiple spectroscopic methods and thermodynamic analysis were used to determine the binding efficacy of DAB-0 and DAB-1 with serum proteins. Drug-protein conjugation was observed via through ionic contacts. DAB-1 forms stronger adducts than DAB-0, while b-LG shows more affinity with the order of stability b-LG>BSA>HSA. The stronger complexation of DAB-1 with serum proteins might account for its biological potential and transport in the blood. The binding efficacy ranged from 40 to 60%. Major alterations of protein secondary structures were detected upon drug complexation. Serum proteins are capable of delivering DAB-1 in vitro.Abbreviations: BSA: bovine serum albumin; DAB-0: N0-[4-(2,5-dioxo-pyrrolidin-1-yl)-benzoyl]-hydrazine carboxylic acid tert-butyl ester; DAB-1: N0-[4-(2,5-dioxo-2,5-dihydro-pyrrol-1-yl)-benzoyl]-hydrazine carboxylic acid tert-butyl est; FTIR: Fourier transform infrared; b-LG, beta-lactoglobulin; HAS: human serum albuminFil: Chanphai, P.. Université du Québec a Montreal; CanadáFil: Cloutier, F.. Université du Québec a Montreal; CanadáFil: Oufqir, Y.. Université du Québec a Montreal; CanadáFil: Leclerc, M.F.. Université du Québec a Montreal; CanadáFil: Eijan, Ana Maria. Universidad de Buenos Aires. Facultad de Medicina. Instituto de Oncología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Reyes Moreno, C.. Université du Québec a Montreal; CanadáFil: Bérubé, G.. Université du Québec a Montreal; CanadáFil: Tajmir Riahi, H.A.. Université du Québec a Montreal; Canad