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NaCl-triggered self-assembly of hydrophilic poloxamine block copolymers

Year: 2015

Journal: INTERNATIONAL JOURNAL OF PHARMACEUTICS, Vol. 494, p 453-462, 20170208

Authors: Bahadur, Anita; Cabana-Montenegro, Sonia; Aswal, Vinod Kumar; Lage, Emilio V.; Sandez-Macho, Isabel; Concheiro, Angel; Alvarez-Lorenzo, Carmen; Bahadur, Pratap

Organizations: PT Sarvajanik Coll Sci, Dept Zool, Surat 395001, India; Univ Santiago de Compostela, Fac Farm, Dept Farm & Tecnol Farmaceut, Santiago De Compostela 15782, Spain; Bhabha Atom Res Ctr, Div Solid State Phys, Bombay 400085, Maharashtra, India; Univ Santiago de Compostela, Fac Farm, Dept Quim Fis, Santiago De Compostela 15782, Spain; Veer Narmad South Gujarat Univ, Dept Chem, Surat 395001, India

Tetronic 1307 (T1307) is a hydrophilic poloxamine (HLB > 24) with a high molecular mass owing to its long PEO and PPO blocks. In spite of good biocompatibility, its use as a component of drug delivery systems is limited by its high critical micelle concentration (CMC) and temperature (CMT). The aim of this work was to elucidate whether the addition of NaCl or the combination of salts and temperature may bring T1307 micellization and gelling features into more practically useful values. Increasing NaCl concentration in the 0.154 M (isotonic) to 2 M (hypertonic) range made the copolymer more hydrophobic and more prone to self-assemble into unimodal micelles, as observed by means of pi-A isotherms, H-1 NMR, dynamic light scattering (DLS), small-angle neutron scattering (SANS), and pyrene fluorescence. The decrease in CMC and CMT observed for T1307 in 0.5 M NaCl medium (tolerable hypertonic solution), compared to water, notably favored the solubility of hydrophobic drugs such as curcumin and quercetin. Moreover, phase diagram, intrinsic viscosity and sol-to-gel transition were markedly affected by NaCl concentration. Overall, the strong dependence of T1307 self-assembly features on NaCl opens interesting possibilities for tuning the performance of T1307 as a component of nanocarriers and in situ gelling systems. (C) 2015 Elsevier B. V. All rights reserved.