An evaluation of a fluorometric method for determining binding parameters of drug-carrier complexes using mathematical models based on total drug concentration.
A fluorescence method for determining the mode of binding and estimating binding parameters in a model drug-carrier complex was developed using the lipopeptide antibiotic daptomycin and polyamidoamine (PAMAM) dendrimer. Mathematical simulations of model equations describing fluorescence changes induced by antibiotic-carrier binding in terms of total drug concentration were used to evaluate the sensitivity of parameter variation on binding isotherms for both one- and two-site binding models. Nonlinear regression analysis was used to estimate binding parameters and to identify pH-dependent binding models.
Faculty of Pharmaceutical Science, Chulalongkorn University, Bangkok, Thailand.
Boontarika
B
Chanvorachote
Ubonthip
U
Nimmannit
Walaisiri
W
Muangsiri
Lee
L
Kirsch
D000900:Anti-Bacterial Agents / Q000737:chemistry; D001665:Binding Sites; D003198:Computer Simulation; D017576:Daptomycin / Q000737:chemistry*; D050091:Dendrimers; D004337:Drug Carriers / Q000737:chemistry*; D005453:Fluorescence; D005470:Fluorometry / Q000379:methods*; D006863:Hydrogen-Ion Concentration; D008956:Models, Chemical; D011073:Polyamines / Q000737:chemistry*
D000900:Anti-Bacterial Agents; D050091:Dendrimers; D004337:Drug Carriers; C104700:PAMAM Starburst; D011073:Polyamines; D017576:Daptomycin