Abstract
Guest-host complex formation of three drug derivatives of anthranilic acid, mefenamic acid, niflumic acid, and flufenamic acid with 2-hydroxypropyl-β-cyclodextrin (2HP-β-CD) in aqueous solutions was investigated using “Phase solubility study” with UV-vis spectrophotometry. Solubility of sparingly soluble drugs has been improved by addition of 2HP-β-CD at two temperatures 298.15 K and 310.15 K and two pH values 2 and 7. The influence of different 2HP-β-CD concentration on solubility of drugs at different pH and temperatures has been investigated. The 2HP-β-CD-drug complex stability constants (Ks), and dissociations constants (Kd), as well as the thermodynamic parameters of reaction, i.e., the free energy change (ΔG), the enthalpy change (ΔH) and the entropy change (ΔS), were determined. The experimental data indicated formation of 1:1 inclusion complexes, which were found effective binders increasing the solubility of drugs.
Highlights
Cyclodextrins (CDs), the natural oligosaccharides possessing a hydrophilic exterior and hydrophobic cavity, are well-known safe encapsulating materials [1,2,3]
Different CDs including β-CD were used to complex formation with candesartan cilexetil showing the highest constant of complex formation for β-CD with large enthalpy effect [8]
The phase solubility diagram of the drugs in buffer aqueous solutions showed that the solubility of drugs increased linearly as a function of 2HP-β-CD concentration
Summary
Cyclodextrins (CDs), the natural oligosaccharides possessing a hydrophilic exterior and hydrophobic cavity, are well-known safe encapsulating materials [1,2,3]. CDs are continually being examined for their ability to improve complexity in order to obtain both higher solubility of drugs, and stabilizing or solubilizing agents [4,5,6]. The mechanism for this solubilization is rooted in the ability of CDs to form non-covalent dynamic inclusion complexes in solution. MEF is an anthranilic and indole acetic-type acid It is a poorly soluble pharmaceutical, 0.17 × 10−4 mmol·. To understand the character and properties of the association, we investigated the effect of 2HP-β-CD on aqueous solubility and we evaluated the stoichiometry and stability of the complexes
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