MilliporeSigma
  • Home
  • Search Results
  • Cationic triblock copolymer micelles enhance antioxidant activity, intracellular uptake and cytotoxicity of curcumin.

Cationic triblock copolymer micelles enhance antioxidant activity, intracellular uptake and cytotoxicity of curcumin.

International journal of pharmaceutics (2015-06-01)
Krassimira Yoncheva, Katya Kamenova, Teodora Perperieva, Vera Hadjimitova, Petar Donchev, Kaloyan Kaloyanov, Spiro Konstantinov, Magdalena Kondeva-Burdina, Virginia Tzankova, Petar Petrov
ABSTRACT

The aim of the present study was to develop curcumin loaded cationic polymeric micelles and to evaluate their loading, preservation of curcumin antioxidant activity and intracellular uptake ability. The micelles were prepared from a triblock copolymer consisting of poly(ϵ-caprolactone) and very short poly(2-(dimethylamino) ethyl methacrylate) segments (PDMAEMA9-PCL70-PDMAEMA9). The micelles showed monomodal size distribution, mean diameter of 145 nm, positive charge (+72 mV), critical micellar concentration around 0.05 g/l and encapsulation efficiency of 87%. The ability of the micellar curcumin to scavenge the ABTS radical and hypochlorite ions was higher than that of the free curcumin. Confocal microscopy revealed that the uptake of curcumin by chronic myeloid leukemia derived K-562 cells and human multiple myeloma cells U-266 was more intensive when curcumin was loaded into the micelles. These results correlated with the higher cytotoxicity of the micellar curcumin compared to free curcumin. Intraperitoneal treatment of Wistar rats indicated that PDMAEMA-PCL-PDMAEMA copolymer, comprising very short cationic chains, did not change the levels of malondialdehyde and glutathione in livers indicating an absence of oxidative stress. Thus, PDMAEMA-PCL-PDMAEMA triblock micelles could be considered efficient and safe platform for curcumin delivery.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Triethylamine, ≥99.5%
Sigma-Aldrich
1,4-Dioxane, anhydrous, 99.8%
Sigma-Aldrich
Copper(I) chloride, ≥99.995% trace metals basis
Sigma-Aldrich
Tetrahydrofuran, contains 250 ppm BHT as inhibitor, ACS reagent, ≥99.0%
Sigma-Aldrich
Tetrahydrofuran, anhydrous, contains 250 ppm BHT as inhibitor, ≥99.9%
Sigma-Aldrich
Methanol, anhydrous, 99.8%
Sigma-Aldrich
Tetrahydrofuran, suitable for HPLC, ≥99.9%, inhibitor-free
Sigma-Aldrich
Methanol, suitable for HPLC, gradient grade, 99.93%
Sigma-Aldrich
Tetrahydrofuran, anhydrous, ≥99.9%, inhibitor-free
Sigma-Aldrich
5,5′-Dithiobis(2-nitrobenzoic acid), ReagentPlus®, 99%
Sigma-Aldrich
Triethylamine, for amino acid analysis, ≥99.5% (GC)
Sigma-Aldrich
Triethylamine, BioUltra, ≥99.5% (GC)
Sigma-Aldrich
Triethylamine, for protein sequence analysis, ampule, ≥99.5% (GC)
Sigma-Aldrich
Triethylamine, puriss. p.a., ≥99.5% (GC)
Sigma-Aldrich
Triethylamine, ≥99.5%
Sigma-Aldrich
Triethylamine, ≥99%
Sigma-Aldrich
2-Thiobarbituric acid, ≥98%
Sigma-Aldrich
5,5′-Dithiobis(2-nitrobenzoic acid), ≥98%, BioReagent, suitable for determination of sulfhydryl groups
Sigma-Aldrich
Methanol, NMR reference standard
Sigma-Aldrich
Copper(I) chloride, AnhydroBeads, ≥99.99% trace metals basis
Sigma-Aldrich
Methanol, HPLC Plus, ≥99.9%, poly-coated bottles
Sigma-Aldrich
Calcium hydride, purum p.a., ≥97.0% (gas-volumetric), powder
Sigma-Aldrich
Curcumin, ≥94% (curcuminoid content), ≥80% (Curcumin)
Sigma-Aldrich
Curcumin, from Curcuma longa (Turmeric), powder
Sigma-Aldrich
2,2′-Bipyridyl, ReagentPlus®, ≥99%
Sigma-Aldrich
Dichloromethane, anhydrous, ≥99.8%, contains 40-150 ppm amylene as stabilizer
Sigma-Aldrich
Calcium hydride, powder, 0-2 mm, reagent grade, ≥90% (gas-volumetric)
Sigma-Aldrich
α-Bromoisobutyryl bromide, 98%
Sigma-Aldrich
Dichloromethane, suitable for HPLC, ≥99.9%, contains 40-150 ppm amylene as stabilizer
Supelco
Dichloromethane, ≥99.9%