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Issue 14, 2016
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Anticancer drug delivery systems based on specific interactions between albumin and polyglycerol

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Abstract

Here, we report for the first time a facile method for the preparation of novel drug delivery systems based on supramolecular interactions between β-cyclodextrin-polyglycerol conjugates (β-CD-g-PG) and human serum albumin (HSA). The results obtained by combined experimental/modeling studies showed that the main drivers to the formation of HSA/β-CD-g-PG supramolecular entities are host–guest interactions between β-CD-g-PG and the aromatic side-chains of HSA residues. Due to these interactions, HSA undergoes a confined yet fundamental conformational transition, leading to greater exposure of the hydrophobic protein domains available to hydrophobic drug binding. Next, the binding affinity and loading capacity of the HSA/β-CD-g-PG supramolecular nanovector for doxorubicin (DOX) and paclitaxel (PTX) were investigated. Both drug/HSA binding constants (Kb,HSA/DOX = 3.24 × 103 M−1 and Kb,HSA/PTX = 5.65 × 101 M−1) sensibly increased in the presence of β-CD-g-PG (Kb,HSA/β-CD-g-PG/DOX = 2.78 × 104 M−1 and Kb,HSA/β-CD-g-PG/PTX = 2.82 × 102 M−1). In line, both protein drug loadings increased by about 20% upon HSA/β-CD-g-PG interaction (80% and 71% for DOX and PTX, respectively) with respect to the loading capacity of the bare HSA (60% and 50%). Due to the improved loading capacity with minimal changes in the structure of HSA, this system is a promising vector for future cancer therapy.

Graphical abstract: Anticancer drug delivery systems based on specific interactions between albumin and polyglycerol

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Supplementary files

Article information


Submitted
30 Nov 2015
Accepted
08 Jan 2016
First published
13 Jan 2016

RSC Adv., 2016,6, 11266-11277
Article type
Paper

Anticancer drug delivery systems based on specific interactions between albumin and polyglycerol

Z. Beiranvand, F. Bani, A. Kakanejadifard, E. Laurini, M. Fermeglia, S. Pricl and M. Adeli, RSC Adv., 2016, 6, 11266
DOI: 10.1039/C5RA25463A

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