Low potential ocular irritation of arginine-based gemini surfactants and their mixtures with nonionic and zwitterionic surfactants.
OBJECTIVE
The aim of this study was to find new biocompatible surfactants and mixtures with low ocular irritant action for application in pharmaceutical formulations and to establish a relationship between their structure and their potential ocular irritant activity.


METHODS
An alternative method to the Draize in vivo test, based on the adverse effects of surfactants on the cytoplasmic membrane of red blood cell, was used to evaluate the potential ocular irritation of the surfactants.


RESULTS
It was found that the hemolytic activity of arginine-based gemini surfactants increased with the aliphatic alkyl chain lengths of the hydrophobic tail. The addition of the surfactant with an alkyl chain length of 10 carbon atoms to cocoamidopropilbetaina (TB), decylglucoside (APG), and Nalpha-lauroyl-arginine ethyl ester (LAE) increases the hemolytic activity moderately for the mixtures with TB and LAE (1.1- and 1.5-fold, respectively) and strongly for APG (five-fold).


CONCLUSIONS
The new arginine-based gemini surfactants constitute a suitable alternative to commercial surfactants because of their natural origins, which make them biocompatible and renewable products. Based on their hemolytic activity as an alternative to the Draize test, these new arginine-based gemini surfactants and their mixtures can be classified as mild irritants. This fact constitutes an advantage, especially for pharmaceutical and cosmetic applications.
Mitjans
Montserrat
M
Dept. Fisiologia-Divisió IV, Facultat de Farmacia (UB), Av Joan XXIII, s/n, 08028, Barcelona, Spain.
Martínez
Verónica
V
Clapés
Pere
P
Pérez
Lourdes
L
Infante
M Rosa
MR
Vinardell
M Pilar
MP
D000818:Animals; D001120:Arginine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000633:toxicity*; D002412:Cations; D004347:Drug Interactions; D005123:Eye / Q000187:drug effects*; D006461:Hemolysis; D006801:Humans; D066298:In Vitro Techniques; D007509:Irritants / Q000737:chemistry / Q000633:toxicity*; D008823:Micelles; D011817:Rabbits; D013329:Structure-Activity Relationship; D013499:Surface Properties; D013501:Surface-Active Agents / Q000737:chemistry / Q000633:toxicity*
D002412:Cations; D007509:Irritants; D008823:Micelles; D013501:Surface-Active Agents; D001120:Arginine