Biopharmaceutical Evaluation of Bigels Containing Ciclopirox Olamine
| Date |
|---|
2021-10-22 |
Abstracts. Scientists Section
ISBN 978-9955-15-711-3
Bibliogr.: p. 17
Introduction: When modelling semi-solid dosage forms, it is important to properly select the excipients, their amounts, and the site of incorporation of the active substance, as this affects the release of the drug substance and its penetration into human skin [1,2]. The aim of this study was to determine influence of ratio of hydrogel and oleogel and to released amount of ciclopirox olamine, ex vivo skin penetration. Materials and methods: Poloxamer 408 (25%) and distilled water was used to form hydrogel. Sorbitan monopalmitate (18%) and sunflower oil was used to form oleogel. Bigels were prepared by mixing different amounts of hydrogel and oleogel (from 60:40 to 90:10). Ciclopirox olamine (CPO) was in hydrogel, in oleogel or in both phases. In vitro release test and ex vivo human skin penetration study have been performed. Results: With increasing hydrogel concentration (from 60% to 90%) in the bigel, the release of CPO increased regardless of its presence in a certain phase. It was mostly released (630.7 μg / cm2) by a bigel in which the total amount of CPO was dissolved in the oleogel and the hydrogel concentration was 90%. Ex vivo skin penetration studies revealed that the highest flux of CPO (136.1 μg / cm2) into human skin was from a bigel in which all of this compound was dissolved in oleogel and the hydrogel concentration was 90%. However, there was no statistically significant correlation either between the amount of CPO penetrated into the skin and the concentration of hydrogel in the bigel, nor between the amount of CPO penetrated into the skin and its presence in a certain phase. Assessing the distribution of CPO between epidermis and dermis, the results of flux showed that CPO as a relatively lipophilic substance (logP = 2.22) tends to accumulate in the epidermis. Conclusions: For higher release of CPO from the bigel and penetration into the human skin, the hydrogel should be 90% and the CPO should be incorporated into the oelogel.