Study of valsartan interaction with micelles as a model system for biomembranes
Abstract
In this study, the interaction of valsartan (VAL), an angiotensin II receptor antagonist, with cationic surfactant cetyltrimethylammonium bromide (CTAB) was investigated. The effect of cationic micelles on spectroscopic and acid-base properties of VAL was carried out using UV spectrophotometry at physiological conditions (pH 7.4). The binding of VAL to CTAB micelles implied a shift in drug acidity constant (pK(a)(water) - pK(a)(micelle) = 1.69) proving the great affinity of VAL dianion for the positively charged CTAB micelle surface. To quantify the degree of VAL/CTAB interaction, two constants were calculated by using mathematical models: micelle/water partition coefficient (K-x) and drug/micelle binding constant (K-b). The decrease of K-x with VAL concentration, obtained by using pseudo-phase model, is consistent with an adsorption-like phenomenon. From the dependence of differential absorbance at lambda = 295 nm on CTAB concentration, by using mathematical model that treats the solu...bilization of VAL dianion as its binding to specific sites in the micelles (Langmuir adsorption isotherm), the binding constant (K-b = (2.50 +/- 10.49) x 10(4) M-1) was obtained. Binding constant VAL/CTAB was also calculated using micellar liquid chromatography (MLC).
Keywords:
valsartan / micelles / CTAB / binding constant / partition coefficientSource:
Colloids and Surfaces B: Biointerfaces, 2008, 65, 1, 80-84Publisher:
- Elsevier Science BV, Amsterdam
Funding / projects:
- Supstance za farmaceutsku upotrebu: modeliranje, sinteza, fizičko-hemijske i biološke osobine, stepen čistoće i ispitivanje doziranih oblika (RS-MESTD-MPN2006-2010-142072)
DOI: 10.1016/j.colsurfb.2008.03.002
ISSN: 0927-7765
PubMed: 18439806
WoS: 000257618200013
Scopus: 2-s2.0-44649165054
Collections
Institution/Community
PharmacyTY - JOUR AU - Čudina, Olivera AU - Brborić, Jasmina AU - Janković, I. AU - Karljiković-Rajić, Katarina AU - Vladimirova, S. PY - 2008 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/1090 AB - In this study, the interaction of valsartan (VAL), an angiotensin II receptor antagonist, with cationic surfactant cetyltrimethylammonium bromide (CTAB) was investigated. The effect of cationic micelles on spectroscopic and acid-base properties of VAL was carried out using UV spectrophotometry at physiological conditions (pH 7.4). The binding of VAL to CTAB micelles implied a shift in drug acidity constant (pK(a)(water) - pK(a)(micelle) = 1.69) proving the great affinity of VAL dianion for the positively charged CTAB micelle surface. To quantify the degree of VAL/CTAB interaction, two constants were calculated by using mathematical models: micelle/water partition coefficient (K-x) and drug/micelle binding constant (K-b). The decrease of K-x with VAL concentration, obtained by using pseudo-phase model, is consistent with an adsorption-like phenomenon. From the dependence of differential absorbance at lambda = 295 nm on CTAB concentration, by using mathematical model that treats the solubilization of VAL dianion as its binding to specific sites in the micelles (Langmuir adsorption isotherm), the binding constant (K-b = (2.50 +/- 10.49) x 10(4) M-1) was obtained. Binding constant VAL/CTAB was also calculated using micellar liquid chromatography (MLC). PB - Elsevier Science BV, Amsterdam T2 - Colloids and Surfaces B: Biointerfaces T1 - Study of valsartan interaction with micelles as a model system for biomembranes VL - 65 IS - 1 SP - 80 EP - 84 DO - 10.1016/j.colsurfb.2008.03.002 ER -
@article{ author = "Čudina, Olivera and Brborić, Jasmina and Janković, I. and Karljiković-Rajić, Katarina and Vladimirova, S.", year = "2008", abstract = "In this study, the interaction of valsartan (VAL), an angiotensin II receptor antagonist, with cationic surfactant cetyltrimethylammonium bromide (CTAB) was investigated. The effect of cationic micelles on spectroscopic and acid-base properties of VAL was carried out using UV spectrophotometry at physiological conditions (pH 7.4). The binding of VAL to CTAB micelles implied a shift in drug acidity constant (pK(a)(water) - pK(a)(micelle) = 1.69) proving the great affinity of VAL dianion for the positively charged CTAB micelle surface. To quantify the degree of VAL/CTAB interaction, two constants were calculated by using mathematical models: micelle/water partition coefficient (K-x) and drug/micelle binding constant (K-b). The decrease of K-x with VAL concentration, obtained by using pseudo-phase model, is consistent with an adsorption-like phenomenon. From the dependence of differential absorbance at lambda = 295 nm on CTAB concentration, by using mathematical model that treats the solubilization of VAL dianion as its binding to specific sites in the micelles (Langmuir adsorption isotherm), the binding constant (K-b = (2.50 +/- 10.49) x 10(4) M-1) was obtained. Binding constant VAL/CTAB was also calculated using micellar liquid chromatography (MLC).", publisher = "Elsevier Science BV, Amsterdam", journal = "Colloids and Surfaces B: Biointerfaces", title = "Study of valsartan interaction with micelles as a model system for biomembranes", volume = "65", number = "1", pages = "80-84", doi = "10.1016/j.colsurfb.2008.03.002" }
Čudina, O., Brborić, J., Janković, I., Karljiković-Rajić, K.,& Vladimirova, S.. (2008). Study of valsartan interaction with micelles as a model system for biomembranes. in Colloids and Surfaces B: Biointerfaces Elsevier Science BV, Amsterdam., 65(1), 80-84. https://doi.org/10.1016/j.colsurfb.2008.03.002
Čudina O, Brborić J, Janković I, Karljiković-Rajić K, Vladimirova S. Study of valsartan interaction with micelles as a model system for biomembranes. in Colloids and Surfaces B: Biointerfaces. 2008;65(1):80-84. doi:10.1016/j.colsurfb.2008.03.002 .
Čudina, Olivera, Brborić, Jasmina, Janković, I., Karljiković-Rajić, Katarina, Vladimirova, S., "Study of valsartan interaction with micelles as a model system for biomembranes" in Colloids and Surfaces B: Biointerfaces, 65, no. 1 (2008):80-84, https://doi.org/10.1016/j.colsurfb.2008.03.002 . .