Effect of akyl-γ-cyclodextrins on the stability of retinol |
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Authors: | S Sapino M E Carlotti R Cavalli M Trotta F Trotta D Vione |
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Institution: | (1) Dip. di Scienza e Tecnologia del Farmaco-Università degli Studi di Torino, via P. Giuria 9, 10125 Turin, Italy;(2) Dip. di Chimica IFM-Università degli Studi di Torino, via P. Giuria 7, 10125 Turin, Italy;(3) Dip. di Chimica Analitica- Università degli Studi di Torino, via P. Giuria 5, 10125 Turin, Italy |
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Abstract: | Inclusion complexation between retinol (RET) and two synthetic alkyl carbonates of γ-cyclodextrin (alkyl-γ-CD) derivatives, ethyl-γ-cyclodextrin (E-CD) and octyl-γ-cyclodextrin (O-CD), was investigated by means of different techniques. The complexes were characterized by differential
scanning calorimetry (DSC). Phase solubility studies, according to the method of Higuchi and Connors 1] were used to evaluate the complexation in aqueous solution at room temperature. In the present study inclusion complexes
of retinol with E-CD and with O-CD were prepared to prevent its rapid degradation. In order to investigate the behavior of
retinol under UV light, test of irradiation was performed separately on samples prepared dispersing retinol (0.1% w/w) or
an equivalent amount of retinol/alkyl-γ-CD respectively in hydroxyethylcellulose (HEC) gel and in an O/W emulsion. The stability over time of retinol was also investigated
storing the samples at 40 °C. Moreover retinol permeation through porcine skin has been evaluated employing Franz cells 2]. Retinol solubility was increased in presence of cyclodextrins while DSC analysis suggest that this inclusion agents are
able to interact with retinol. Data for skin accumulation in porcine ear skin showed that alkyl-CDs increase of approximatively
1,5-fold retinol skin accumulation. Studies on the stability showed that both the inclusion complexes considered are able
to increase retinol stability to light exposure and also to heat. |
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Keywords: | Retinol Ethylcarbonate of γ -cyclodextrin Octylcarbonate of γ -cyclodextrin Phase-solubility diagrams DSC thermograms Skin permeation |
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