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Study on Self-Assembled Well-Defined PEG Graft Copolymers as Efficient Drug-Loaded Nanoparticles for Anti-Inflammatory Therapy.

Study on Self-Assembled Well-Defined PEG Graft Copolymers as Efficient Drug-Loaded Nanoparticles for Anti-Inflammatory Therapy.

Macromolecular bioscience (2015-07-23)

Paulina Maksym-Bębenek, Dorota Neugebauer

ABSTRACT

The core-shell micelles in aqueous solutions were prepared at low CAC values (<0.1 mg · mL(-1) ) from amphiphilic graft copolymers consisting of poly(methyl methacrylate) backbone (120-165 units) with loosely grafted (17-40%) hydroxyl-capped PEG (9 vs 6 units in side chain) for drug loading. Hydrophobic indomethacin (IMC) was loaded into the micelles with content of 22-88%. Hydrodynamic diameters of particles were ranged in 110-200 nm. In vitro release experiments at various pH indicated faster releasing of IMC at pH 7.4 than that at pH 5.0. The studies on micellization, drug loading and release profiles verified the cumulative influence of hydrophilic/hydrophobic balance, degree of grafting, length of PEG side chains giving advantages in macromolecular design of nanocarriers in drug delivery.

MATERIALS

Product Number

Brand

Product Description

Sigma-Aldrich

Anisole, ReagentPlus^®, 99%

Sigma-Aldrich

Anisole, ≥99%, FCC, FG

Sigma-Aldrich

Anisole, anhydrous, 99.7%

Sigma-Aldrich

Chloroform-d, ≥99.8 atom % D, contains 0.5 wt. % silver foil as stabilizer, 0.03 % (v/v) TMS

Sigma-Aldrich

Chloroform-d, ≥99.8 atom % D, contains 0.5 wt. % silver foil as stabilizer

Sigma-Aldrich

Chloroform-d, "100%", 99.96 atom % D, contains 0.5 wt. % silver wire as stabilizer

Sigma-Aldrich

Diethyl ether

Sigma-Aldrich

Indomethacin, meets USP testing specifications

Sigma-Aldrich

Indomethacin, 98.5-100.5% (in accordance with EP)

Sigma-Aldrich

Chloroform-d, 99.8 atom % D, contains 0.03 % (v/v) TMS

Sigma-Aldrich

Chloroform-d, "100%", 99.96 atom % D

Sigma-Aldrich

Chloroform-d, 99.8 atom % D

Sigma-Aldrich

Chloroform-d, ≥99.8 atom % D, anhydrous

Sigma-Aldrich

Chloroform-d, 99.8 atom % D, contains 0.1 % (v/v) TMS

Sigma-Aldrich

Methyl methacrylate, contains ≤30 ppm MEHQ as inhibitor, 99%

Sigma-Aldrich

Chloroform-d, "100%", 99.96 atom % D, contains 0.03 % (v/v) TMS

Sigma-Aldrich

Ethyl α-bromoisobutyrate, 98%

Sigma-Aldrich

Tetramethylsilane, electronic grade, ≥99.99% trace metals basis

Sigma-Aldrich

Chloroform-d, 99.8 atom % D, contains 0.05 % (v/v) TMS

Sigma-Aldrich

Chloroform-d, 99.8 atom % D, contains 1 % (v/v) TMS

Sigma-Aldrich

Methyl methacrylate, 99%, stabilized

Sigma-Aldrich

Tetramethylsilane, ≥99.0% (GC)

Sigma-Aldrich

Diethyl ether, ACS reagent, ≥98.0%, contains ≤2% ethanol and ≤10ppm BHT as inhibitor

Sigma-Aldrich

Tetramethylsilane, ACS reagent, NMR grade, ≥99.9%

Sigma-Aldrich

Diethyl ether, reagent grade, ≥98%, contains ≤2% ethanol and ≤10ppm BHT as inhibitor

Sigma-Aldrich

Diethyl ether, anhydrous, ACS reagent, ≥99.0%, contains BHT as inhibitor