Host-guest complex of β-cyclodextrin and pluronic F127 with Luteolin: Physicochemical characterization, anti-oxidant activity and molecular modeling studies

被引:34
作者
Alshehri, Sultan [1 ]
Imam, Syed Sarim [1 ]
Altamimi, Mohammad A. [1 ]
Jafar, Mohammed [2 ]
Hassan, Mohd Zaheen [3 ]
Hussain, Afzal [1 ]
Ahad, Abdul [1 ]
Mandi, Wael [1 ]
机构
[1] King Saud Univ, Coll Pharm, Dept Pharmaceut, Riyadh 11451, Saudi Arabia
[2] Imam Abdulrahman Bin Faisal Univ, Coll Clin Pharm, Dept Pharmaceut, Dammam 31441, Saudi Arabia
[3] King Khalid Univ, Coll Pharm, Dept Pharmaceut Chem, Abha, Saudi Arabia
关键词
Luteolin; Inclusion complex; Anti-oxidant; Solubility enhancement; Molecular docking; INCLUSION COMPLEXES; SOLID DISPERSIONS; L-ARGININE; DISSOLUTION; SOLUBILITY; SOLVENTS; DELIVERY; RELEASE;
D O I
10.1016/j.jddst.2019.101356
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The purpose of this investigation was to ameliorate the solubility and dissolution rate of luteolin (LUT) in aqueous phase by LUT: beta-cyclodextrin (beta CD) binary and LUT: beta-cyclodextrin (beta CD) : Pluronic F127 (PLF) ternary complex. Phase solubility study was performed with beta CD as well as with beta CD-PLF to assess the solubilizing efficiency. The solid complexes were prepared by solvent evaporation (SE), and microwave irradiation (MI) techniques. The in-vitro dissolution study was performed for the developed systems. The selected ternary complex was evaluated for solid state characterization, anti-oxidant effect and further molecular docking study was performed to provide structural insights and to identify the favorable role of beta CD in improving the solubility of LUT. The key results of phase solubility studies indicated that 6.23 fold and 10 folds increase in LUT solubility with beta CD and beta CD-PLF respectively in comparison to pure LUT solubility. The formulation TIC-MI showed maximum drug release 97.06 +/- 4.23% followed by TIC-SE (83.679 +/- 3.78%) > BIC-MI (76.35 +/- 3.57%) > BIC-SE (57.39 +/- 2.11%) > TNPM (42.72 +/- 2.45%) > BNPM (26.16 +/- 1.71%). Most importantly IR, NMR study results revealed that there is no interaction was observed between LUT and used excipients. The antioxidant effect of the complex was found higher than that of LUT. The docking results demonstratethat LUT is completely embedded into the beta CD cavity. Therefore, LUT: beta CD: PLF ternary complex prepared by MI method found to be efficient with improved solubility, dissolution and antioxidant effect.
引用
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页数:11
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