The possible involvement of the primary amino group of doxorubicin (DXR) in the cross-linking process of gelatin nanoparticles stabilized by glutaraldehyde was investigated. Nanoparticles were characterized with regard to particle size, drug content, enzymatic degradation and cross-linking degree. The size of nanoparticles was around 100-200 nm and DXR was loaded with an entrapment efficiency of 42%. Upon the study of crosslinking rate, DXR-loaded nanoparticles showed a greater number of free amino groups than the unloaded ones. This should be due to a competition between the amino group of DXR and the amino groups of the gelatin chains during the cross-linking process. Hence, a binding of a drug fraction to the protein matrix via glutaraldehyde was hypothesized and confirmed by the results of a thin-layer chromatography (TLC) analysis. According to the in vitro study only a little fraction of DXR was released as free drug (8%) when the nanoparticles were put in saline solution. The addition of proteolytic enzymes disrupts the matrix structure producing the release of a further 10-15% of the drug loading which was entrapped in the nanoparticle matrix. The remaining part of the drug corresponds to DXR covalently linked to peptide residues produced by nanoparticle digestion.

Doxorubicin-loaded gelatin nanoparticles stabilized by glutaraldehyde: Involvement of the drug in the cross-linking process / Leo, Eliana Grazia; Vandelli, Maria Angela; Cameroni, Riccardo; Forni, Flavio. - In: INTERNATIONAL JOURNAL OF PHARMACEUTICS. - ISSN 0378-5173. - STAMPA. - 155(1997), pp. 75-82.

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