@misc{yang_preparation_and_2013, author={Yang, X., Zhao, L., Almasy, L., Haramus, V.M., Zou, A., Willumeit, R., Fan, S.}, title={Preparation and characterization of 4-dedimethylamino sancycline (CMT-3) loaded nanostructured lipid carrier (CMT-3/NLC) formulations}, year={2013}, howpublished = {journal article}, doi = {https://doi.org/10.1016/j.ijpharm.2013.04.021}, abstract = {Chemically modified tetracyclines (CMTs) have been reported to strongly inhibit proliferation and metastasis of various cancers, but their efficacy is restricted by poor water solubility. In the present study, a hydrophilic 4-dedimethylamino sancycline (CMT-3) loaded nanostructured lipid carrier (CMT-3/NLC) was produced by high pressure homogenization (HPH). The physical properties of CMT-3/NLC formulations were characterized by dynamic light scattering (DLS), high efficiency liquid chromatography (HPLC), atomic force microscopy (AFM), scanning electron microscopy (SEM), small-angle neutron scattering (SANS), small-angle X-ray scattering (SAXS) and wide-angle X-ray powder diffraction (XRD). The lipid and surfactant ingredients, as well as drug/lipid concentrations (m/m) were optimized to produce stable and sustained NLC formulations. In vitro cytotoxicity of CMT-3/NLC against HeLa cells was evaluated by MTT assay. The diameter of CMT-3/NLC was found to increase from 153.1 ± 3.0 nm to a maximum of 168.5 ± 2.0 nm after 30 days of storage, while the entrapment efficiency remained constant at >90%. CMT-3/NLC demonstrated a burst-sustained release profile in release media with different pH, a property attributed to the 3-dimensional structure of CMT-3/NLC. Cell uptake and localization studies indicated that NLC reached the cytoplasm and could thereby facilitate CMT-3 entry into HeLa cells.}, note = {Online available at: \url{https://doi.org/10.1016/j.ijpharm.2013.04.021} (DOI). Yang, X.; Zhao, L.; Almasy, L.; Haramus, V.; Zou, A.; Willumeit, R.; Fan, S.: Preparation and characterization of 4-dedimethylamino sancycline (CMT-3) loaded nanostructured lipid carrier (CMT-3/NLC) formulations. International Journal of Pharmaceutics. 2013. vol. 450, no. 1-2, 225-234. DOI: 10.1016/j.ijpharm.2013.04.021}}