Solid state formulations composed by amphiphilic polymers for delivery of proteins: characterization and stability

• Type: Article in International Scientific Journal
• Date: 2015

Authors

Fernanda Andrade (Author) Other; Pedro Fonte (Author) Other; Mireia Oliva (Author) Other; Mafalda Videira (Author) Other; Domingos Ferreira (Author) FFUP; Bruno Sarmento (Author) Other

Journal

Title: International Journal of Pharmaceutics

Vol. 486

Pages: 195-206

ISSN: 0378-5173

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 11 Citations

Scopus - 19 Citations

Scientific classification

FOS: Medical and Health sciences > Basic medicine

Other information

Authenticus ID: P-00A-BSS

DOI: 10.1016/j.ijpharm.2015.03.050

Abstract (EN): Nanocomposite powders composed by polymeric micelles as vehicles for delivery proteins were developed in this work, using insulin as model protein. Results showed that size and polydispersity of micelles were dependent on the amphiphilic polymer used, being all lower than 300 nm, while all the formulations displayed spherical shape and surface charge close to neutrality. Percentages of association efficiency and loading capacity up to 94.15 +/- 3.92 and 8.56 +/- 0.36, respectively, were obtained. X-ray photoelectron spectroscopy (XPS) measurements confirmed that insulin was partially present at the hydrophilic shell of the micelles. Lyophilization did not significantly change the physical characteristics of micelles, further providing easily dispersion when in contact to aqueous medium. The native-like conformation of insulin was maintained at high percentages (around 80%) after lyophilization as indicated by Fourier transform infrared spectroscopy (FTIR) and far-UV circular dichroism (CD). Moreover, Raman spectroscopy did not evidenced significant interactions among the formulation components. The formulations shown to be physically stable upon storage up to 6 months both at roomtemperature (20 degrees C) and fridge (4 degrees C), with only a slight loss (maximum of 15%) of the secondary structure of the protein. Among the polymers tested, Pluronic (R) F127 produced the carrier formulations more promising for delivery of proteins.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 12