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

PMID26198460

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

I8280

Sigma-Aldrich

Indomethacin, meets USP testing specifications

I7378

Sigma-Aldrich

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

296082

Sigma-Aldrich

Diethyl ether, contains 1 ppm BHT as inhibitor, anhydrous, ≥99.7%

225789

Sigma-Aldrich

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

494275

Sigma-Aldrich

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

523771

Sigma-Aldrich

Tetramethylsilane, electronic grade, ≥99.99% trace metals basis

E14403

Sigma-Aldrich

Ethyl α-bromoisobutyrate, 98%

431915

Sigma-Aldrich

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

416754

Sigma-Aldrich

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

530735

Sigma-Aldrich

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

151858

Sigma-Aldrich

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

151831

Sigma-Aldrich

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

M55909

Sigma-Aldrich

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

151823

Sigma-Aldrich

Chloroform-d, 99.8 atom % D

87921

Sigma-Aldrich

Tetramethylsilane, ≥99.0% (GC)

570699

Sigma-Aldrich

Chloroform-d, ≥99.8 atom % D, anhydrous

612200

Sigma-Aldrich

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

434876

Sigma-Aldrich

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

676845

Sigma-Aldrich

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

673811

Sigma-Aldrich

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

T24007

Sigma-Aldrich

Tetramethylsilane, ACS reagent, NMR grade, ≥99.9%

32203

Sigma-Aldrich

Diethyl ether, contains BHT as inhibitor, puriss. p.a., ACS reagent, reag. ISO, reag. Ph. Eur., ≥99.8% (GC)

346144

Sigma-Aldrich

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

24004

Sigma-Aldrich

Diethyl ether, puriss., contains ~5 mg/L 2,6-di-tert.-butyl-4-methylphenol as stabilizer, meets analytical specification of Ph. Eur., BP, ≥99.5% (GC)

W400201

Sigma-Aldrich

Methyl methacrylate, 99%, stabilized

09-1830

Sigma-Aldrich

Diethyl ether, JIS 300, ≥99.5%, for residue analysis