Coadsorption of the sodium salts of two steroid molecules at a silica/interface as induced by the adsorption of a cationic surfactant

Citation
I. Cherkaoui et al., Coadsorption of the sodium salts of two steroid molecules at a silica/interface as induced by the adsorption of a cationic surfactant, INT J PHARM, 201(1), 2000, pp. 71-77
Citations number
20
Categorie Soggetti
Pharmacology & Toxicology
Journal title
INTERNATIONAL JOURNAL OF PHARMACEUTICS
ISSN journal
03785173 → ACNP
Volume
201
Issue
1
Year of publication
2000
Pages
71 - 77
Database
ISI
SICI code
0378-5173(20000515)201:1<71:COTSSO>2.0.ZU;2-O
Abstract
The incorporation of two ionic steroids, namely the sodium salts of hydroco rtisone 21-hernisuccinate (HNa) and prednisolone 21-succinate (PNa), at a s ilica/water interface in the presence of adsorbed cetyltrimethylammonium br omide has been investigated first at a constant pH value. It is shown that this coadsorption effect is qualitatively similar to the adsolubilization e ffect which is described for neutral molecules. The adsorption of the catio nic surfactant induces the coadsorption of the anionic drug molecules altho ugh the silica surface is negatively charged. At surfactant equilibrium con centration above the critical micelle concentration the drug molecules are distributed between the adsorbed aggregates and the free micelles. At large r surfactant concentration, the drugs may be completely depleted from the s ilica/water interface. Based upon Langmuir-type isotherms, the equilibrium constants of the drug molecules with the adsorbed aggregates and the free m icelles are calculated. The constants are about three times larger for the former than for the latter aggregates, The signification of such results is discussed. The coadsorption of HNa at low surfactant surface coverage was also investigated in the pH interval between 3 and 9. HNa is strongly coads orbed at lower pH onto the silica surface. The coadsorption goes through a maximum at a pH value which may be considered as equal to the apparent pK o f the drug and decreases to zero at higher pH values. A pK value equal to 4 .2 is proposed for HNa. This behaviour is interpreted as the result of the interplay of the drug dissociation and that of the surface silanol groups u pon the change of pH. (C) 2000 Elsevier Science B.V. All rights reserved.