Valsartan inclusion by methyl-β-cyclodextrin: Thermodynamics, molecular modelling, Tween 80 effect and evaluation

被引：29

作者：

Chadha, Renu ^{[1
]}

Bala, Madhu ^{[1
]}

Arora, Poonam ^{[1
]}

Jain, D. V. S. ^{[2
]}

Pissurlenkar, Raghuvir R. S. ^{[3
]}

Coutinho, Evans C. ^{[3
]}

机构：

[1] Panjab Univ, Univ Inst Pharmaceut Sci, Chandigarh 160014, India

[2] Panjab Univ, Dept Chem, Chandigarh 160014, India

[3] Bombay Coll Pharm, Dept Pharmaceut Chem, Bombay 400098, Maharashtra, India

来源：

CARBOHYDRATE POLYMERS | 2014年 / 103卷

关键词：

Valsartan; Molecular modelling; NMR; Solubility; Enthalpy; Permeability; WATER-SOLUBLE POLYMERS; PHARMACEUTICAL APPLICATIONS; COMPLEX-FORMATION; SOLUBILITY; VINPOCETINE; IMPROVEMENT; NAPROXEN; VIVO;

D O I：

10.1016/j.carbpol.2013.12.047

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

The rationale of present study is to investigate the effect of Tween 80 on encapsulation ability of valsartan (VAL) by methyl-beta-cyclodextrin (M-beta-CD) and to determine the exact mode of binding. Phase solubility studies indicated 1:1 stoichiometry between VAL and M-beta-CD both in the presence and absence of Tween 80. The NMR and molecular modelling studies indicated the insertion of both aromatic and aliphatic regions of VAL into the M-beta-CD cavity suggesting the coexistence of two 1:1 complexes in equilibrium with each other. The stability constants, K-1 (aromatic) and K-2 (aliphatic), were enhanced in the presence of Tween 80 as evident by higher value of stability constants (K-1 1992.0 M-1, K-2 1864.0 M-1) for ternary system in comparison to binary system (K-1 1741.6 M-1, K-2 1499.2 M-1). Efficacy of ternary complex was established by significant decrease in the systolic blood pressure of deoxycorticosterone acetate (DOCA) induced hypertensive rats. (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：300 / 309

页数：10

共 43 条

[1]

[Anonymous], NIH PUBLICATION

[2]

Araujo M. V. G., 2007, BIOORGAN MED CHEM, V15, P5752

[3] Cationic mixed micelles in the presence of β-cyclodextrin:: A host-guest study [J].

Bakshi, MS .

JOURNAL OF COLLOID AND INTERFACE SCIENCE, 2000, 227 (01) :78-83

[4] The Protein Data Bank [J].

Berman, HM ;

Westbrook, J ;

Feng, Z ;

Gilliland, G ;

Bhat, TN ;

Weissig, H ;

Shindyalov, IN ;

Bourne, PE .

NUCLEIC ACIDS RESEARCH, 2000, 28 (01) :235-242

[5] Solubilization of tropicamide by hydroxypropyl-β-cyclodextrin and water-soluble polymers:: in vitro/in vivo studies [J].

Cappello, B ;

Carmignani, C ;

Iervolino, M ;

La Rotonda, MI ;

Saettone, MF .

INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2001, 213 (1-2) :75-81

[6] Improvement of solubility and stability of valsartan by hydroxypropyl-β-cyclodextrin [J].

Cappello, Brunella ;

Di Maio, Clelia ;

Iervolino, Maria ;

Miro, Agnese .

JOURNAL OF INCLUSION PHENOMENA AND MACROCYCLIC CHEMISTRY, 2006, 54 (3-4) :289-294

[7] Binding constants of inclusion complexes of nitroirnidazoles with β-cyclodextrins in the absence and presence of PVP [J].

Chadha, Renu ;

Jain, D. V. S. ;

Aggarwal, Amit ;

Singh, Surjit ;

Thakur, Deepika .

THERMOCHIMICA ACTA, 2007, 459 (1-2) :111-115

[8]

Chadha Renu, 2011, Results Pharma Sci, V1, P38, DOI 10.1016/j.rinphs.2011.07.002

[9] Complexation of nevirapine with β-cyclodextrins in the presence and absence of Tween 80: characterization, thermodynamic parameters, and permeability flux [J].

Chadha, Renu ;

Arora, Poonam ;

Gupta, Sushma ;

Jain, Dharamvir Singh .

JOURNAL OF THERMAL ANALYSIS AND CALORIMETRY, 2011, 105 (03) :1049-1059

[10] Characterization and in vivo efficacy of inclusion complexes of sulphadoxine with β-cyclodextrin: calorimetric and spectroscopic studies [J].

Chadha, Renu ;

Gupta, Sushma ;

Shukla, Geeta ;

Jain, D. V. S. ;

Singh, Surjit .

JOURNAL OF INCLUSION PHENOMENA AND MACROCYCLIC CHEMISTRY, 2011, 71 (1-2) :149-159

← 1 2 3 4 5 →