SOLUBILITY INCREASE OF BETA-LAPACHONE USING POLOXAMINES AND LAPONITE RD® FOR ANTICANCER THERAPY.
Micelles; Nanotechnology; β-lapachone; Laponite; Tetronic,
thermosponsive
Tetronics® are copolymers that form micelles and have the ability to reversibly
transition between the sol-gel phases according to their concentration, pH and
temperature, and can be used in controlled release systems for low aqueous soluble
drugs. Tetronics® T904, T90R4 and T1304 were tested for incorporation of β-
lapachone (BLPC) which was chosen because of its very low aqueous solubility (0.038
mg.ml-1), which limits its bioavailability and systemic administration, and several
characterized biological activities, especially anticancer and anti-inflammatory. To help
in the physical-chemical stability of the micelles, as a rheological modifier was added
synthetic hectorite Laponite RD® (LAP), which forms hydrogels. The samples were
prepared by simple magnetic stirring of their components with varying concentrations.
The parameters analyzed were: increased BLPC solubility, rheological behavior of the
systems, particle size by dynamic light scattering, characterization by
thermogravimetry and Infrared Spectrometry. Hybrid systems have increased the
solubility of BLPC by more than 50 times, showed a viscosity increase and sol-gel
transition with the temperature rise, increased viscosity with addition of BLPC, formed
stable compounds, and BLPC shows encapsulation signals in the micelles created.