Accueil > Publications > Recherche par années > Années 2010 > 2017

Goncalves, C., Gomez, J.-P., Même, W., Rasolonjatovo, B., Gosset, D., Nedellec, S., Hulin, P., Huin, C., Le Gall, T., Montier, T., Lehn, P., Pichon, C., Guegan, P., Cheradame, H. and Midoux, P.

Curcumin/poly(2-methyl-2-oxazoline-b-tetrahydrofuran-b-2-methyl-2-oxazoline) formulation : An improved penetration and biological effect of curcumin in F508del-CFTR cell lines

European journal of pharmaceutics and biopharmaceutics (2017) 117, 168-181

par Frapart - publié le

Abstract :

Neutral amphiphilic triblock ABA copolymers are of great interest to solubilize hydrophobic drugs. We reported that a triblock ABA copolymer consisting of methyl-2-oxazoline (MeOx) and tetrahydrofuran (THF) (MeOx6-THF19-MeOx6) (TBCP2) can solubilize curcumin (Cur) a very hydrophobic molecule exhibiting multiple therapeutic effects but whose insolubility and low stability in water is a major drawback for clinical applications. Here, we provide evidences by flow cytometry and confocal microscopy that Cur penetration in normal and DeltaF508-CFTR human airway epithelial cell lines is facilitated by TBCP2. When used on DeltaF508-CFTR cell lines, the Cur/TBCP2 formulation promotes the restoration of the expression of the CFTR protein in the plasma membrane. Furthermore, patch-clamp and MQAE fluorescence experiments show that this effect is associated with a correction of a Cl- selective current at the membrane surface of F508del-CFTR cells. The results show the great potential of the neutral amphiphilic triblock copolymer MeOx6-THF19-MeOx6 as carrier for curcumin in a Cystic Fibrosis context. We anticipate that other MeOxn-THFm-MeOxn copolymers could have similar behaviours for other highly insoluble therapeutic drugs or cosmetic active ingredients.

Voir en ligne : 10.1016/j.ejpb.2017.04.015