Biocompatibility and Stability of Polysaccharide Polyelectrolyte Complexes Aimed at Respiratory Delivery

Materials

Susana Rodrigues¹  Lurdes Cardoso¹  Ana M. Rosa da Costa²  Ana Grenha¹ 

[1] CBMR—Centre for Biomedical Research, University of Algarve, Faculty of Sciences and Technology, Campus de Gambelas, Faro 8005-139, Portugal; E-Mails:;CIQA—Algarve Chemistry Research Centre and Department of Chemistry and Pharmacy, Faculty of Sciences and Technology, University of Algarve, Campus de Gambelas, Faro 8005-139, Portugal; E-Mail:

关键词: biocompatibility;    chitosan;    chondroitin sulfate;    nasal delivery;    polyelectrolyte complexes;    polysaccharides;    protein delivery;    pulmonary delivery;   

DOI  :  10.3390/ma8095268

来源: mdpi

【 摘 要 】

Chitosan (CS) and chondroitin sulfate (CHS) are natural polymers with demonstrated applicability in drug delivery, while nanoparticles are one of the most explored carriers for transmucosal delivery of biopharmaceuticals. In this work we have prepared CS/CHS nanoparticles and associated for the first time the therapeutic protein insulin. Fluorescein isothiocyanate bovine serum albumin (FITC-BSA) was also used to enable comparison of behaviors regarding differences in molecular weight (5.7 kDa versus 67 kDa). Nanoparticles of approximately 200 nm and positive zeta potential around +20 mV were obtained. These parameters remained stable for up to 1 month at 4 °C. Proteins were associated with efficiencies of more than 50%. The release of FITC-BSA in PBS pH 7.4 was more sustained (50% in 24 h) than that of insulin (85% in 24 h). The biocompatibility of nanoparticles was tested in Calu-3 and A549 cells by means of three different assays. The metabolic assay MTT, the determination of lactate dehydrogenase release, and the quantification of the inflammatory response generated by cell exposure to nanoparticles have indicated an absence of overt toxicity. Overall, the results suggest good indications on the application of CS/CHS nanoparticles in respiratory transmucosal protein delivery, but the set of assays should be widened to clarify obtained results.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.