Abstract

It is known that cationic surfactants have an antimicrobial effect and act as enhancers. This paper studies three cationic surfactants from the group of alkyldimethylbenzylammonium chlorides (dodecyl-, tetradecyl-, and hexadecyl). Interest is focused on the association of the surfactants with respect to temperature, partition balances and their influence on drug release, rheological properties, and the pH of hydrogels. The critical micelle concentrations (CMC) of the surfactants were estimated from dependencies of conductivity, density, spectrofluorimetry, and UV–VIS spectrophotometry on molarity in the temperature range of 25–50 °C. It was found that the temperature dependence of a CMC is U-shaped, with its minimum at 30 °C, and the CMC value decreases as the length of the chain increases. The pseudo-phase separation model was used for the calculation of various thermodynamic parameters, such as the Gibbs free energies (spontaneous process), enthalpies (exothermic process), and entropies of the micelles’ formation, CMCs, and the degree of counterion binding. All thermodynamic parameters, as functions of the temperature, were estimated. It was found that partition coefficients increase as the length of the alkyl chain and the pH = (5.0–7.0) increase. The influences of surfactants, below and above the CMC, on drug (chlorhexidine dihydrochloride) release from hydrogels, rheological properties, and pH at 30 °C were studied. Also, the amounts of the released drug increase as the alkyl chains of the surfactants prolongate. The amounts of the released drug with the surfactant below the CMC are greater than that above the CMC. All hydrogels (regardless of the length of the alkyl chain) exhibit a non-Newtonian pseudo-plastic flow. The results obtained will be used in the formulation of the drug and surfactants into dosage forms.

Highlights

  • The optimization of drugs to reach their maximum therapeutic effect is a primordial problem of pharmaceutical technology, and it requires deep knowledge about the influences of auxiliary substances

  • Appropriate choices of auxiliary substances determine the first process of LADME, namely

  • The concentration of a surfactant at which micelles appear is known as the critical micelle concentration (CMC)

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Summary

Introduction

The optimization of drugs to reach their maximum therapeutic effect is a primordial problem of pharmaceutical technology, and it requires deep knowledge about the influences of auxiliary substances. Appropriate choices of auxiliary substances determine the first process of LADME, namely. The LADME process should be modelled and analyzed as a whole, which has been a long-lasting research subject of the authors [1,2]. In those studies, various roles of surfactants have been studied, which are known to play a vital role in the process of LADME, and in many processes of interest in both the fundamental and applied sciences [3]. Its value depends on numerous factors, such as temperature, length of alkyl chain, and influence of counter ions [5]

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