Skip to Content
Merck
  • Flavonoid-based pH-responsive hydrogels as carrier of unstable drugs in oxidative conditions.

Flavonoid-based pH-responsive hydrogels as carrier of unstable drugs in oxidative conditions.

Pharmaceutical development and technology (2013-12-03)
Umile Gianfranco Spizzirri, Giuseppe Cirillo, Manuela Curcio, Nevio Picci, Francesca Iemma
ABSTRACT

In this study, pH-responsive hydrogels, synthesized by the coupling reaction of polyacrylic acid and catechin, are proposed as carriers of oxidable drugs toward the GI tract. The presence of polyphenolic moieties in the network gives the polymers properties suitable for the release of unstable drugs in oxidative conditions. The characterization of the hydrogels is obtained by means of morphological and physico-chemical analyses, antioxidant assays and evaluation of the swelling behavior in media simulating the gastric (pH 1.0) and the intestinal (pH 7.4) tracts. The hydrogels are tested as pH-responsive carriers in in vitro release studies of folic acid and thiamine, two model drugs easily degraded by oxidative conditions simulated by UV irradiation and t-butyl hydroperoxide treatment, respectively. Results show that catechin-based carriers are able to control the release of drugs at different pH values, giving a remarkable improvement in the stability of the therapeutics.

MATERIALS
Product Number
Brand
Product Description

Supelco
Ethanol, standard for GC
Sigma-Aldrich
Ethanol, tested according to Ph. Eur.
Sigma-Aldrich
Sodium phosphate, 96%
Sigma-Aldrich
Potassium persulfate, 99.99% trace metals basis
Sigma-Aldrich
Sodium carbonate-12C, 99.9 atom % 12C
Supelco
Sodium carbonate concentrate, 0.1 M Na2CO3 in water, eluent concentrate for IC
Sigma-Aldrich
Methanol-12C, 99.95 atom % 12C
Sigma-Aldrich
Ethyl alcohol, Pure, 200 proof, ACS reagent, ≥99.5%
Sigma-Aldrich
Potassium phosphate monobasic, ACS reagent, ≥99.0%
Sigma-Aldrich
Ethanol, BioUltra, for molecular biology, ≥99.8%, (absolute alcohol, without additive, A15 o1)
USP
Methyl alcohol, United States Pharmacopeia (USP) Reference Standard
USP
Monobasic potassium phosphate, United States Pharmacopeia (USP) Reference Standard
Sigma-Aldrich
Ethanol, purum, absolute ethanol, denaturated with 1% cyclohexane, A15 CYCLO1, ≥99.8% (based on denaturant-free substance)
Sigma-Aldrich
Ethyl alcohol, Pure, 200 proof
Sigma-Aldrich
Potassium phosphate monobasic, powder, suitable for cell culture, suitable for insect cell culture, suitable for plant cell culture, ≥99.0%
Sigma-Aldrich
Potassium persulfate, ACS reagent, ≥99.0%
Sigma-Aldrich
Ethyl alcohol, Pure 200 proof, for molecular biology
Supelco
Ethanol standards 10% (v/v), 10 % (v/v) in H2O, analytical standard
Sigma-Aldrich
Ethyl alcohol, Pure, 190 proof, meets USP testing specifications
Sigma-Aldrich
Phosphorus pentoxide, powder, ACS reagent, ≥98.0%
Supelco
Methanol, analytical standard
Supelco
Sodium carbonate, reference material for titrimetry, certified by BAM, >99.5%
Sigma-Aldrich
Methanol, anhydrous, 99.8%
Sigma-Aldrich
Hydrochloric acid, 36.5-38.0%, BioReagent, for molecular biology
Supelco
Methanol, Pharmaceutical Secondary Standard; Certified Reference Material
USP
Dehydrated Alcohol, United States Pharmacopeia (USP) Reference Standard
Sigma-Aldrich
Methanol, Absolute - Acetone free
Sigma-Aldrich
Sodium carbonate, ACS reagent, anhydrous, ≥99.5%, powder or granules
Sigma-Aldrich
Diethyl ether, reagent grade, ≥98%, contains ≤2% ethanol and ≤10ppm BHT as inhibitor
Sigma-Aldrich
Diethyl ether, contains BHT as inhibitor, puriss. p.a., ACS reagent, reag. ISO, reag. Ph. Eur., ≥99.8% (GC)