期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 486, 期 1-2, 页码 195-206出版社
ELSEVIER
DOI: 10.1016/j.ijpharm.2015.03.050
关键词
Amphiphilic polymers; Insulin; Polymeric micelles; Lyophilization; Stability
资金
- Fundacao para a Ciencia e a Tecnologia, Portugal [SFRH/BD/73062/2010, SFRH/BD/78127/2011]
- European Regional Development Fund (ERDF) through the Programa Operacional Factores de Competitividade - COMPETE
- Portuguese funds through FCT in the framework of the project [PEst-C/SAU/LA0002/2013]
- North Portugal Regional Operational Programme (ON.2 - O Novo Norte) in the framework of project SAESCTN-PIIC&DT, under the National Strategic Reference Framework (NSRF)
- Fundação para a Ciência e a Tecnologia [SFRH/BD/73062/2010, SFRH/BD/78127/2011] Funding Source: FCT
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. (C) 2015 Elsevier B.V. All rights reserved.
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