Format

Send to

Choose Destination
Int J Pharm. 2014 Nov 20;475(1-2):324-34. doi: 10.1016/j.ijpharm.2014.07.018. Epub 2014 Jul 15.

Water solubilization capacity of pharmaceutical microemulsions based on Peceol®, lecithin and ethanol.

Author information

1
Institut Charles Gerhardt Montpellier, UMR 5253 CNRS-ENSCM-UM2-UM1, Equipe MACS, 8 rue de l'Ecole Normale, 34296 Montpellier, France; Medesis Pharma, Avenue du Golf, L'Orée des Mas, Les Cyprès, 34670 Baillargues, France.
2
Institut de Chimie Séparative de Marcoule, ICSM UMR 5257 (CEA/CNRS/UM2/ENSCM), 30206 Bagnols sur Cèze, France.
3
Institut Charles Gerhardt Montpellier, UMR 5253 CNRS-ENSCM-UM2-UM1, Equipe MACS, 8 rue de l'Ecole Normale, 34296 Montpellier, France.
4
Institut des Biomolécules Max Mousseron, UMR CNRS 5247, Université de Montpellier I, 34060 Montpellier, France.
5
Medesis Pharma, Avenue du Golf, L'Orée des Mas, Les Cyprès, 34670 Baillargues, France.
6
Institut Charles Gerhardt Montpellier, UMR 5253 CNRS-ENSCM-UM2-UM1, Equipe MACS, 8 rue de l'Ecole Normale, 34296 Montpellier, France. Electronic address: philippe.legrand@enscm.fr.

Abstract

Biocompatible microemulsions composed of Peceol(®), lecithin, ethanol and water developed for encapsulation of hydrophilic drugs were investigated. The binary mixture Peceol(®)/ethanol was studied first. It was shown that the addition of ethanol to pure Peceol(®) has a significant fluidifying and disordering effect on the Peceol(®) supramolecular structure with an enhancement in water solubilization. The water solubilization capacity was improved by adding lecithin as a third component. It was then demonstrated that the ethanol/lecithin weight ratio played an important role in determining the optimal composition in term of water solubilization efficiency, a necessary property for a nutraceutical or pharmaceutical application. The optimal ethanol/lecithin weight ratio in the Peceol(®) rich region was found to be 40/60. Combination different techniques such as SAXS, fluorimetry, rheology and conductivity, we analyzed the water uptake within the microemulsion taking into account the partitioning of ethanol between polar and apolar domains. This ethanol distribution quantified along a water dilution line has a major effect on microemulsion properties.

KEYWORDS:

Ethanol partitioning; Microemulsion; Peceol(®); Phase diagram; Water solubilization capacity

PMID:
25034800
DOI:
10.1016/j.ijpharm.2014.07.018
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center