Assessement of anti-inflammatory properties of microspheres prepared with chitosan and 5-amino salicylic acid over inflamed Caco-2 cells

被引：16

作者：

Aguzzi, C. ^{[1
]}

Ortega, A. ^{[2
]}

Bonferoni, M. C. ^{[3
]}

Sandri, G. ^{[3
]}

Cerezo, P. ^{[1
]}

Salcedo, I. ^{[1
]}

Sanchez, R. ^{[1
]}

Viseras, C. ^{[1
,4
]}

Caramella, C. ^{[3
]}

机构：

[1] Univ Granada, Sch Pharm, Dept Pharm & Pharmaceut Technol, Granada, Spain

[2] Univ Pablo de Olavide, Dept Mol Biol & Biochem Engn, Andalusian Mol Biol & Regenerat Med Ctr CABIMER, Ctr Invest Biomed Red Diabet Enfermedades Metab A, Seville, Spain

[3] Univ Pavia, Sch Pharm, Dept Drug Sci, I-27100 Pavia, Italy

[4] CSIC, Andalusian Inst Earth Sci, Granada, Spain

来源：

CARBOHYDRATE POLYMERS | 2011年 / 85卷 / 03期

关键词：

5-ASA; Chitosan; Cytokines; Inflammation; Drug release; Spray drying; INFLAMMATORY-BOWEL-DISEASE; COLON-SPECIFIC DELIVERY; IN-VITRO EVALUATION; DRUG-DELIVERY; 5-AMINOSALICYLIC ACID; ULCERATIVE-COLITIS; DISSOLUTION PROPERTIES; THERAPY; RELEASE; NANOPARTICLES;

D O I：

10.1016/j.carbpol.2011.03.027

中图分类号：

O69 [应用化学];

学科分类号：

070301 [无机化学];

摘要：

Microspheres based on the interaction between 5-amino salicylic acid (5-ASA) and chitosan were designed as a new colonic delivery system. Microspheres were prepared by a spray drying technique and characterised by physical properties, morphology and drug dissolution characteristics. Effects of the microspheres over inflamed Caco-2 cells were also evaluated, by determining cell viability and expression of mRNA levels of biomarkers involved in the pathogenesis of Inflammatory Bowel Diseases (IBD) (IL-1 beta and IL-8). Results showed that chitosan improved dissolution properties of 5-ASA. The amount of free drug released over 120 min did not exceed 9 mg/cm(2), while microspheres showed a high dissolution rate reaching approximately 50 mg/cm(2) of drug released. Contact of inflamed cells with free 5-ASA reduced mRNA levels of IL-1 beta and IL-8. Microspheres did not show cytotoxic activity and maintained ILs levels observed in non-inflamed cells, mimicking the anti-inflammatory effect of 5-ASA alone. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：638 / 644

页数：7

共 49 条

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Chitosan-silicate biocomposites to be used in modified drug release of 5-aminosalicylic acid (5-ASA) [J].