The effect of chitosan as internal or external coating on the 5-ASA release from calcium alginate microparticles.
The effect of chitosan as internal or external coating on the mesalamine (5-ASA) release from calcium alginate microparticles (CaAl) was studied, and a delayed release of 5-ASA system intended for colonic drug delivery was developed. The external chitosan coating was developed by immersion of wetted CaAl in chitosan solution and the internal coating by mixing 5-ASA with chitosan solution and drying before the preparation of CaAl. Both systems were coated with Acryl-EZE® using combined fluid bed coating and immersion procedure. The results showed that in phosphate medium (pH 7.5), chitosan as 5-ASA coating promotes a quick erosion process accelerating drug release, but chitosan as external coating (CaAlCS) does not increase the T (50) value compared with the microparticles without chitosan (CaAl). Chitosan as internal or external coating was not effective to avoid the quick 5-ASA release in acidic medium (pH 1.2). The presence of β-glucosidase enzymes increases significantly the 5-ASA release for CaAl, while no effect was observed with chitosan as internal or external coating. Fourier transform infrared spectroscopy, thermogravimetric analysis, and X-ray data revealed that 5-ASA did not form a solid solution but was dispersed in the microparticles. The Acryl-EZE® coating of microparticles was effective because all the formulations showed a low release, less than 15%, of 5-ASA in acid medium at pH 1.2. Significant differences in the percentage of 5-ASA released between formulations were observed in phosphate buffer at pH 6.0. In phosphate buffer at pH 7.2, all the formulations released 100% of 5-ASA.
Tapia
Cristián
C
Laboratorio de Operaciones Unitarias, Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, Casilla 233, Santiago 1, Chile. ctapia@uchile.cl
Molina
Sergio
S
Diaz
Alvaro
A
Abugoch
Lilian
L
Diaz-Dosque
Mario
M
Valenzuela
Fernando
F
Yazdani-Pedram
Mehrdad
M
D000464:Alginates / Q000737:chemistry*; D000636:Aminosalicylic Acids / Q000008:administration & dosage / Q000737:chemistry*; D002214:Capsules; D020099:Coated Materials, Biocompatible / Q000737:chemistry*; D003553:Cystine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D003692:Delayed-Action Preparations / Q000737:chemistry*; D004058:Diffusion; D004339:Drug Compounding / Q000379:methods*; D004343:Drug Implants / Q000737:chemistry*; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry
D000464:Alginates; D000636:Aminosalicylic Acids; D002214:Capsules; D020099:Coated Materials, Biocompatible; D003692:Delayed-Action Preparations; D004343:Drug Implants; D006603:Hexuronic Acids; C528877:N,N'-bis(5-aminosalicyl)cystine; D003553:Cystine; D020723:Glucuronic Acid