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  • Preparation and properties of a pH sensitive carrier based on three kinds of polymer blend to control the release of 5-amino salicylic acid.

Preparation and properties of a pH sensitive carrier based on three kinds of polymer blend to control the release of 5-amino salicylic acid.

Pharmaceutical development and technology (2013-12-11)
Yuming Dong, Zhengjie Zhou, Hongyan Ding, Shujiang Zhang
ABSTRACT

High concentration of 5-amino salicylic acid (5-ASA) in the distal ileum and colon is necessary for the treatment of inflammatory bowel disease (IBD). The control of small molecules, drugs, released from a polymeric matrix remains a great challenge. To study the preparation and properties of a pH-sensitive carrier for targeting delivery of 5-ASA. The carrier was prepared by ternary blends method based on polyvinyl alcohol (PVA), sodium alginate (SA) and polylactic acid. It was characterized by infrared spectrometry and scanning electronic microscopy. The adsorption and release of 5-ASA in different pH media were investigated. We found out the best ratio of the materials for synthetic carrier. The vector exhibited good performance by the controlled release of the target drug experiment. The adsorption capacity of the carrier for 5-ASA was 70.34% in phosphate buffer saline at pH 1.00, and the release rate was 100.49% in phosphate buffer solution at pH 6.80. PVA is vector backbone of the carrier, and SA plays key role in its pH performance. It is a promising material to effectively deliver 5-ASA to the specific sites of IBD.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Lactic acid, meets USP testing specifications
Sigma-Aldrich
Lactic acid, natural, ≥85%
Sigma-Aldrich
Alginic acid sodium salt, powder
Sigma-Aldrich
Poly(vinyl alcohol), Mw 13,000-23,000, 87-89% hydrolyzed
Sigma-Aldrich
Poly(vinyl alcohol), 87-90% hydrolyzed, average mol wt 30,000-70,000
Sigma-Aldrich
Alginic acid sodium salt from brown algae, BioReagent, suitable for plant cell culture, low viscosity, powder
Sigma-Aldrich
Poly(vinyl alcohol), Fully hydrolyzed
Sigma-Aldrich
Lactic acid, 85%, FCC
Sigma-Aldrich
Poly(vinyl alcohol), Mw 89,000-98,000, 99+% hydrolyzed
Mesalazine for system suitability, European Pharmacopoeia (EP) Reference Standard
Supelco
Lactic acid, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
Sodium alginate
Sigma-Aldrich
Lactic acid solution, ACS reagent, ≥85%
Sigma-Aldrich
Polylactic acid, Mw ~60,000