Chitosan-alginate microparticles as a protein carrier

被引:107
作者
Coppi, G [1 ]
Iannuccelli, V [1 ]
Leo, E [1 ]
Bernabei, MT [1 ]
Cameroni, R [1 ]
机构
[1] Univ Modena & Reggio Emilia, Dept Pharmaceut Sci, I-41100 Modena, Italy
关键词
alginate; chitosan; microparticles; protein complexation; spray-drying;
D O I
10.1081/DDC-100104314
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The oral administration of peptidic drugs requires their protection from degradation in the gastric environment and the improvement of their absorption in the intestinal tract. For these requirements, a microsystem based on cross-lined alginate as the carrier of bovine serum albumin (BSA), used as a model protein, was proposed. A spray-drying technique was applied to BSA/sodium alginate solutions to obtain spherical particles having a mean diameter less than 10 mum. the microparticles were hardened using first a solution of calcium chloride and then a solution of chitosan (CS) to obtain stable microsystems. The cross-linking process was carried out at different CS concentrations and pH values of the cross-linking medium. The CS concentration affected the BSA loading in the micro particles prepared at a pH value less than the protein isoelectric point (pI). Moreover, the BSA loading at a pH value less than the pI was higher than that at a pH similar to the pI regardless of the CS concentration. This finding could be attributable to the formation of a BSA/alginate complex. The evaluation of the interaction between BSA and alginate at different pH values by means rheological measurements confirmed this hypothesis. This approach may represent a promising way to devise a microcarrier system with appropriate size for targeting the Peyer's patches, with appropriate immobilization capacity, and suitable for the oral administration of peptidic drugs.
引用
收藏
页码:393 / 400
页数:8
相关论文
共 31 条
[2]   KINETICS AND MECHANISM OF DRUG-RELEASE FROM CALCIUM ALGINATE MEMBRANE COATED TABLETS [J].
BHAGAT, HR ;
MENDES, RW ;
MATHIOWITZ, E ;
BHARGAVA, HN .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 1994, 20 (03) :387-394
[3]   SPHERICAL AGGLOMERATES OF WATER-INSOLUBLE DRUGS [J].
BODMEIER, R ;
PAERATAKUL, O .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1989, 78 (11) :964-967
[4]   THE INFLUENCE OF PEPTIDE STRUCTURE ON TRANSPORT ACROSS CACO-2 CELLS .2. PEPTIDE-BOND MODIFICATION WHICH RESULTS IN IMPROVED PERMEABILITY [J].
CONRADI, RA ;
HILGERS, AR ;
HO, NFH ;
BURTON, PS .
PHARMACEUTICAL RESEARCH, 1992, 9 (03) :435-439
[5]  
DESAY PB, 1984, MICROENCAPSULATION R, P181
[6]   Inclusion and release of proteins from polysaccharide-based polyion complexes [J].
Dumitriu, S ;
Chornet, E .
ADVANCED DRUG DELIVERY REVIEWS, 1998, 31 (03) :223-246
[7]   Microparticle targeting to M cells [J].
Ermak, TH ;
Giannasca, PJ .
ADVANCED DRUG DELIVERY REVIEWS, 1998, 34 (2-3) :261-283
[8]   Production of BCG alginate-PLL microcapsules by emulsification internal gelation [J].
Esquisabel, A ;
Hernandez, RM ;
Igartua, M ;
Gascon, AR ;
Calvo, B ;
Pedraz, JL .
JOURNAL OF MICROENCAPSULATION, 1997, 14 (05) :627-638
[9]  
Florence AT, 1993, PHARM PARTICULATE CA, P65
[10]   Protein release from alginate matrices [J].
Gombotz, WR ;
Wee, SF .
ADVANCED DRUG DELIVERY REVIEWS, 1998, 31 (03) :267-285