Authors: Maculotti, Katia¹; Tira, Enrica²; Sonaggere, Miriam²; Perugini, Paola¹; Conti, Bice¹; Modena, Tiziana¹; Pavanetto, Franca¹

Source: Journal of Microencapsulation, Volume 26, Number 6, September 2009 , pp. 535-543(9)

Publisher: Informa Healthcare

Abstract:

A novel formulation based on chondroitin sulphate/chitosan microspheres (CS/CH) has been investigated for oral delivery of macromolecules using ovalbumin as the model protein (OVA). The microspheres were prepared by a new emulsion-complex coacervation method. Physico-chemical properties of the polymers constituting microparticulate matrix were investigated by IR, DSC, TGA and X-ray diffraction analyses. In vitro tests were performed to evaluate the drug delivery system degradation and the protein release under conditions simulating the intestinal fluids. The ability of colonic enzymes to degrade the microparticulate systems was simulated employing the chondroitinase ABC enzyme. Results showed that the different CS/CH compositions influenced both microparticles stability and the protein release rate. Only the microspheres composed by 1:1 chondroitin sulphate-chitosan ratio achieved an OVA release profile suitable to a possible colon targeting. These microspheres released ∼30% of ovalbumin encapsulated in 24 h in the different aqueous media tested, while they released 100% of protein in the presence of chondroitinase. The preliminary results demonstrated that chondroitin sulphate-chitosan microspheres can be a suitable delivery system for protein drug envisaged to oral administration.

Keywords: Chondroitin-chitosan microspheres; emulsion-complex coacervation method; colon drug delivery; proteins

Document Type: Research article

DOI: http://dx.doi.org/10.1080/02652040802485725

Affiliations: 1: Department of Pharmaceutical Chemistry, University of Pavia, Pavia, Italy 2: Department of Biochemistry 'A. Castellani', University of Pavia, Pavia, Italy

Publication date: 2009-09-01

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