Thursday, April 12, 2012

Comparision of Solutol HS15 and Cremophor EL

Solutol HS 15 is a non-ionic detergent obtained by reacting 15 moles of ethylene oxide with 1 mole of 12-hydroxy stearic acid. It is also known as Polyethylene glycol stearate 15, polyethylene glycol -12 - hydroxy stearic acid.Solutol HS 15 is mainly used as a non-ionic solubilizer,it is used in injection, emulsions, liposomes and other formulations. It merits consideration as a potential therapeutic agent because of its effectiveness for reversing multidrug resistance in vitro and its low toxicity in vivo.
From ncbi.nlm.nih.gov;
Solutol HS15Cremophor EL and Solutol HS 15are modulators of multidrug resistance in vitro and in vivo. Because they are polydisperse, and their active component(s) have not been identified, the therapeutic potential of such surfactants is unclear. To better define the active components of Solutol HS 15 and to make more potent surfactant multidrug resistance modulators, highly purified C-18 fatty acids were esterified with ethylene oxide at 5-200 molar ratios. Unexpectedly, ethylene oxide esters of pure 12-hydroxy stearic acid, the major components of Solutol HS 15, displayed negligible resistance modification activity compared with Solutol HS 15 itself or to stearic and oleic acid esters synthesized under identical conditions. Since oleic acid esters appeared to have good activity, a series of these compounds was prepared to determine the optimal ethylene oxide/fatty acid ratio. The optimal ratio was found to be 20 mole ethylene oxide: I mole fatty acid, with a steep decline in activity for products made with ratios above and below the optimum. The most active oleic acid ester, designated CRL 1337, was 8.4-fold as potent as Solutol HS 15 and over 19-fold as potent as Cremophor EL in promoting rhodamine 123 accumulation in multidrug-resistant KB 8-5-11 cells in vitro. Our results show that the structure of the hydrophobic domain (fatty acid) of surfactants as well as its hydrophile-lipophile balance are critical in determining the potency of surfactants as reversing agents.
Read More:  Solutol HS15 price

No comments:

Post a Comment