| خلاصه مقاله | Solubility measurement and modeling data of some poorly water soluble drugs in deep eutectic solvent systems
Samira Zad Ali Asghara, Ali Shayanfarb, Abolghasem Jouybanc
a. Student Research Committee, Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran
b. Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, Iran
c.Pharmaceutical Analysis Research Center, Tabriz University of Medical Sciences, Tabriz, Iran
Introduction:
Nowadays a new generation of solvents named deep eutectic solvent systems (DESs) has received great attention at various fields such as drug delivery because of their unique properties. These solvents are prepared by mixing a hydrogen bond acceptor (e.g. choline chloride) and a hydrogen bond donor (e.g. urea, glycerol) with various molar ratio. The melting point of the mixture is decreased because the formation of hydrogen bond between DES components reduces the lattice energy of component of the eutectic systems. As compared to the ionic liquids, DESs derived from choline chloride possess good advantages such as low price, easy to prepare, biodegradable, biocompatible, non-toxic and chemical inertness with water. In this study, solubilities of Glibenclamide, Tadalafi, Piroxicam, Lamotrigine, Benzoic acid, Salicylic acid, Ibuprofen, Ketoconazole, Phenothiazine, Carbamazepine, Carvedilol, Phenytoin, Atenolo as very poor soluble drugs have been investigated in two DES systems (choline chloride + urea/ glycerol).
Methods:
DES systems were prepared by mixing 1:2 molar ratio of choline chloride: urea/glycerol, respectively. Then, the 10% and 50% mass fraction of DES were made and excess amount of poorly soluble drugs were added into glassy vials and aqueous solution were shaken in an incubator for a period of 48h at 310 K until the equilibrium was obtained. Finally, the absorption of diluted samples was read by UV spectrophotometer and the concentrations of samples were calculated based on calibration curves
Results:
The solubility of some poorly water soluble drugs significantly increased with the addition of DES to the aqueous solutions. Quantitative structure property relationship (QSPR) models based on solubilization ratio and structural parameters with an acceptable statistical parameters were obtained
Conclusion:
The obtained experimental data show the possibility of applying DES as a medium for solubility enhancement of poorly water soluble drugs and encourage to investigate solubility in other DES + water systems. QSPR models indicated that various parameters can effect on solubillization of solute in DES + water mixtures
References:
E.L. Smith, A.P. Abbott, K.S. Ryder, Deep eutectic solvents (DESs) and their applications, Chem. Rev., 21 (2014) 11060-11082.
Q. Zhang, K.D.O. Vigier, S. Royer, F. Jerome, Deep eutectic solvents: syntheses, properties and applications, Chem. Soc. Rev.21(2012)7108-7146.
D. Sikarra, V. Shukla, A.A. Kharia, D. Chatterjee, Techniques for solubility enhancement of poorly soluble drugs: an overview, J. Med. Pharm. Allied Sci. 1 (2012) 1-22 |