Particle size tailoring of ursolic acid nanosuspensions for improved anticancer activity by controlled antisolvent precipitation
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AbstractThe present study was aimed at tailoring the particle size of ursolic acid (UA) nanosuspension for improved anticancer activity. UA nanosuspensions were prepared by antisolvent precipitation using a four-stream multi-inlet vortex mixer (MIVM) under defined conditions of varying solvent composition, drug feeding concentration or stream flow rate. The resulting products were characterized for particle size and polydispersity. Two of the UA nanosuspensions with mean particle sizes of 100 and 300 nm were further assessed for their in-vitro activity against MCF-7 breast cancer cells using fluorescence microscopy with 4′,6-diamidino-2-phenylindole (DAPI) staining, as well as flow cytometry with propidium (PI) staining and with double staining by fluorescein isothiocyanate. It was revealed that the solvent composition, drug feeding concentration and stream flow rate were critical parameters for particle size control of the UA nanosuspensions generated with the MIVM. Specifically, decreasing the UA feeding concentration or increasing the stream flow rate or ethanol content resulted in a reduction of particle size. Excellent reproducibility for nanosuspension production was demonstrated for the 100 and 300 nm UA preparations with a deviation of not more than 5% in particle size from the mean value of three independent batches. Fluorescence microscopy and flow cytometry revealed that these two different sized UA nanosuspensions, particularly the 300 nm sample, exhibited a higher anti-proliferation activity against the MCF-7 cells and afforded a larger population of these cells in both early and late apoptotic phases. In conclusion, MIVM is a robust and pragmatic tool for tailoring the particle size of the UA nanosuspension. Particle size appears to be a critical determinant of the anticancer activity of the UA nanoparticles.
All Author(s) ListWang Y., Song J., Chow S.F., Chow A.H.L., Zheng Y.
Journal nameInternational Journal of Pharmaceutics
Year2015
Month10
Day15
Volume Number494
Issue Number1
PublisherElsevier BV
Place of PublicationNetherlands
Pages479 - 489
ISSN0378-5173
eISSN1873-3476
LanguagesEnglish-United Kingdom
KeywordsAntisolvent nanoprecipitation, Breast cancer, In-vitro anticancer activity, Multi-inlet vortex mixer (MIVM), Nanoparticles, Ursolic acid

Last updated on 2020-17-10 at 02:38