PURPOSE: In order to improve formulation of targeting chemotherapy, cisplatin-loaded magnetic solid lipid nanoparticles (MSLNs) were prepared. In present study, the deliberate loading of Fe3O4 magnetic nanoparticles (MNs) into cisplatin SLNs was developed. METHODS: SLNs were produced by film scattering ultrasonic technique. The effects of two different loading procedures of MNs on the microstructure and physicochemical properties of MSLNs were investigated by transmission electron microscopy (TEM), zetasizer, infrared spectroscopy (IR), and fluorescence spectroscopy. In vitro drug release and cytotoxicity against human cervical carcinoma SiHa cells, in vivo tumor cell uptake and target tissue distribution of MSLNs under external magnetic field were investigated. RESULTS: The encapsulation efficiency of cisplatin and the content of MNs in procedure I SLNs were 69.20 ± 4.5% and 2.16 ± 0.53 mg/mL, respectively, which were higher than those of procedure II MSLNs. In procedure I, the MNs, which were combined with lipids during film formation, distributed in the middle of the lipid layer in SLNs. Differently, in procedure II, the MNs and cisplatin were contained in an interior compartment in SLNs, resulting from mixing with drugs during hydration of lipid film. The procedure I MSLNs had higher cytotoxicity than procedure II MSLNs or free cisplatin. With in vivo intratumoral administration, cisplatin concentration in the tumor tissue was maintained at higher level for MSLNs than that for free cisplatin, especially under external magnetic field. CONCLUSIONS: Procedure I, the developed deliberate MNs loading method, was superior over procedure II in cisplatin encapsulation efficiency, MNs content and cell cytotoxicity.
PURPOSE: In order to improve formulation of targeting chemotherapy, cisplatin-loaded magnetic solid lipid nanoparticles (MSLNs) were prepared. In present study, the deliberate loading of Fe3O4 magnetic nanoparticles (MNs) into cisplatin SLNs was developed. METHODS: SLNs were produced by film scattering ultrasonic technique. The effects of two different loading procedures of MNs on the microstructure and physicochemical properties of MSLNs were investigated by transmission electron microscopy (TEM), zetasizer, infrared spectroscopy (IR), and fluorescence spectroscopy. In vitro drug release and cytotoxicity against human cervical carcinoma SiHa cells, in vivo tumor cell uptake and target tissue distribution of MSLNs under external magnetic field were investigated. RESULTS: The encapsulation efficiency of cisplatin and the content of MNs in procedure I SLNs were 69.20 ± 4.5% and 2.16 ± 0.53 mg/mL, respectively, which were higher than those of procedure II MSLNs. In procedure I, the MNs, which were combined with lipids during film formation, distributed in the middle of the lipid layer in SLNs. Differently, in procedure II, the MNs and cisplatin were contained in an interior compartment in SLNs, resulting from mixing with drugs during hydration of lipid film. The procedure I MSLNs had higher cytotoxicity than procedure II MSLNs or free cisplatin. With in vivo intratumoral administration, cisplatin concentration in the tumor tissue was maintained at higher level for MSLNs than that for free cisplatin, especially under external magnetic field. CONCLUSIONS: Procedure I, the developed deliberate MNs loading method, was superior over procedure II in cisplatin encapsulation efficiency, MNs content and cell cytotoxicity.
Authors: Alfonso Toro-Cordova; Mario Flores-Cruz; Jaime Santoyo-Salazar; Ernesto Carrillo-Nava; Rafael Jurado; Pavel A Figueroa-Rodriguez; Pedro Lopez-Sanchez; Luis A Medina; Patricia Garcia-Lopez Journal: Molecules Date: 2018-09-06 Impact factor: 4.411