RESUMO
This paper focused on formulating high-performance curcumin spray-dried powders for inhalation (curcumin-DPIs) to achieve a high lung concentration. Curcumin-DPIs were produced using wet milling combined with the spray drying method. The effects of different milling times on particle size and aerodynamic performance were investigated. The curcumin-DPIs were characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR), and in vitro dissolution. Furthermore, the in vivo pharmacokinetic behavior and tissue distribution after pulmonary administration were also evaluated. Results showed that the drug dissolution was significantly enhanced by processing into curcumin-DPIs. The aerodynamic results indicated that the DPIs displayed a good aerosol performance. The plasma curcumin concentration was obviously enhanced by inhalation, and most of the curcumin-DPIs were deposited in the lung. This study demonstrated that inhalation was an effective way to carry drug to the lung, and curcumin-DPIs were hopeful for lung cancer treatment in the future.
RESUMO
BACKGROUND: The current study aimed to investigate whether the novel folate (FT) modified nanoparticles (NPs) co-loaded with docetaxel (DT) and curcumin (CU) (named as FT-NPs) could enhance the delivery efficiency to tumor compared with the NPs without FT (non-targeted NPs). METHODS: FT-NPs were successfully formulated in this article. In vitro cytotoxic activity against A549 cells and in vivo antitumor activity of FT-NPs in S180 cell bearing mice were conducted. Cellular uptake test was used to evaluate uptake efficiency of FT-NPs. Histological observation was used to determine the lung security. Besides, the physical chemical properties such as stability, particle size, zeta potential, drug encapsulation efficiency, transmission electron microscopy (TEM) were also conducted. RESULTS: FT-NPs exhibited stronger growth inhibition effects on A549 cells compared with non-targeted NPs, moreover, the novel FT-NPs indicated more effective antitumor efficacy in inhibiting tumor growth. Confocal laser scanning microscopy indicated that the uptake of FT-NPs was facilitated and effective. Histological observation meant that FT-NPs were biocompatible and appropriate for pulmonary administration. CONCLUSION: These results confirmed that FT-NPs with relatively high drug loading capacity could effectively inhibit tumor growth and reduce toxicity. The novel FT-NPs could produce as an outstanding nanocarrier for the targeted treatment of cancers.