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
Dehydrated Alcohol, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
Hydrogen chloride solution, 3 M in cyclopentyl methyl ether (CPME)
Supelco
Ethanol solution, certified reference material, 2000 μg/mL in methanol
Sigma-Aldrich
Diethyl ether, contains 1 ppm BHT as inhibitor, anhydrous, ≥99.7%
Sigma-Aldrich
N,N-Dimethylformamide, anhydrous, 99.8%
Sigma-Aldrich
Sodium carbonate, anhydrous, powder, 99.999% trace metals basis
Sigma-Aldrich
Diethyl ether
Sigma-Aldrich
Ethanol Fixative 80% v/v, suitable for fixing solution (blood films)
Supelco
Phosphorus pentoxide, ≥99.99% trace metals basis
Sigma-Aldrich
N,N-Dimethylformamide, ACS reagent, ≥99.8%
Sigma-Aldrich
Potassium peroxodisulfate, puriss. p.a., ACS reagent, ≥99.0% (RT)
Sigma-Aldrich
Sodium carbonate, BioUltra, anhydrous, ≥99.5% (calc. on dry substance, T)
Supelco
Methanol, analytical standard
Sigma-Aldrich
Phosphorus pentoxide, puriss. p.a., ACS reagent, ≥98.0% (T)
Supelco
Sodium carbonate, reference material for titrimetry, certified by BAM, >99.5%
Sigma-Aldrich
Methanol, anhydrous, 99.8%
Sigma-Aldrich
Diethyl ether, puriss., dried over molecular sieve (H2O ≤0.005%), ≥99.8% (GC)
Sigma-Aldrich
N,N-Dimethylformamide, suitable for HPLC, ≥99.9%
Sigma-Aldrich
Methanol, HPLC Plus, ≥99.9%, poly-coated bottles
Supelco
N,N-Dimethylformamide, analytical standard
Supelco
Diethyl ether, analytical standard
USP
Dehydrated Alcohol, United States Pharmacopeia (USP) Reference Standard
Sigma-Aldrich
Hydrochloric acid solution, 32 wt. % in H2O, FCC
Sigma-Aldrich
Hydrochloric acid, puriss., 24.5-26.0%
Sigma-Aldrich
Sodium carbonate, anhydrous, free-flowing, Redi-Dri, ReagentPlus®, ≥99.5%
Sigma-Aldrich
Sodium carbonate, anhydrous, powder or granules, free-flowing, Redi-Dri, ACS reagent, ≥99.5%
Sigma-Aldrich
Diethyl ether, ACS reagent, ≥98.0%, contains ≤2% ethanol and ≤10ppm BHT as inhibitor
Sigma-Aldrich
Sodium carbonate, anhydrous, free-flowing, Redi-Dri, ACS reagent (primary standard), 99.95-100.05% dry basis
Sigma-Aldrich
Hydrochloric acid, ACS reagent, 37%
Sigma-Aldrich
Diethyl ether, reagent grade, ≥98%, contains ≤2% ethanol and ≤10ppm BHT as inhibitor