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

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) (MeOx$_6$-THF$_{19}$-MeOx$_6$) (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 MeOx$_6$-THF$_{19}$-MeOx$_6$ as carrier for curcumin in a Cystic Fibrosis context. We anticipate that other MeOx$_n$-THF$_m$-MeOx$_n$ copolymers could have similar behaviours for other highly insoluble therapeutic drugs or cosmetic active ingredients.
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Cristine Gonçalves, Pierre Gomez, William Même, Bazoly Rasolonjatovo, David Gosset, et al.. 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, Elsevier, 2017, 117, pp.168-181. ⟨10.1016/j.ejpb.2017.04.015⟩. ⟨hal-01618274⟩

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