Abstract

Density, viscosity and surface tension of Kolliphor® ELP, the nonionic surfactant aqueous solutions were measured at temperature T = 293–318 K and at 5K interval. Steady-state fluorescence measurements have been also made using pyrene as a probe. On the basis of the obtained results, a number of thermodynamic, thermo-acoustic and anharmonic parameters of the studied surfactant have been evaluated and interpreted in terms of structural effects and solute–solvent interactions. The results suggest that the molecules of studied surfactant at concentrations higher than the critical micelle concentration act as structure makers of the water structure.

Highlights

  • Considering the landscape of current drug development, it can be stated, that40% of NCE are characterized by poor water solubility [1]

  • These parameters include: CMC, surfactant efficiency for water surface tension reduction, which means the concentration of the surfactant for 20 mN/m reduction of the surface tension (C20 ), preference of the surfactant for adsorption in relation to the micelle formation with the pointer indicating possible reduction of water surface tension due to the surfactant presence (CMC/C20 ), the surface pressure at the CMC (ΠCMC ), the surface excess concentration at the surface saturation (Γm ), the minimum surface area per molecule (Am ), as well as the standard free enthalpy (∆G0mic and ∆G0ad ), 0 and ∆H0 ) and entropy (∆S0 and ∆S0 ) of micellization and adsorption [11,12,13]

  • Its aqueous solutions were obtained at the concentrations 10−6 to 10−2 M applying the doubly distilled and deionized water provided by a Destamat Bi18E distiller

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Summary

Introduction

Considering the landscape of current drug development, it can be stated, that40% of NCE (new chemical entities) are characterized by poor water solubility [1]. There is a need for excipients to solubilize such candidates in both the early preclinical and clinical evaluation, as well as for the development of the marketed drug dosage forms. Solubilization is the process of drug uptake through complex formation into, e.g., oligomers of dextrose and fatty acids, through the cosolvent systems (such as ethanol, polyethyleneglycol and glycerol), or through the surfactant systems [2]. Nonionic Kolliphors which were known earlier as Cremophors, find application in pharmaceutical formulations as the forms of solid dosage and delivery systems based on lipids aimed at improvement of poorly water-soluble drugs bioavailability [2,6]. Kolliphor® EL (EL), being the most often used Kolliphor, was applied as a vehicle in the case of solubilization of some hydrophobic drugs, including cyclosporin

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