Chemo-photothermal therapy with the combination of chemotherapy and photothermal therapy has emerged as a promising anticancer treatment for its synergistic effects. In this work, the functionalized mesoporous carbon nanoparticles (FA/PEI/O-MCN) were constructed by modifying the mesoporous carbon nanoparticles (MCN) with polyethylenimine (PEI) and folic acid (FA) for the targeted chemo-photothermal therapy. The FA/PEI/O-MCN exhibited strong light absorption and high photothermal conversion efficiency in the near-infrared (NIR) region due to the graphitic structure of MCN. Meanwhile, FA/PEI/O-MCN displayed high drug loading capacity using doxorubicin hydrochloride (DOX) as a model drug. Flow cytometry analysis and competitive binding experiments verified that the FA modification could significantly enhance the uptake of FA/PEI/O-MCN by HeLa cells with folate receptors (FR) over-expressing. Comparing with chemotherapy or photothermal therapy alone, the DOX-loaded FA/PEI/O-MCN demonstrated the synergistic effects and resulted in the higher therapeutic efficacy. We believe that the FA/PEI/O-MCN could be applied as an efficient chemo-photothermal platform to realize the targeted synergistic therapy.
Hongyan Lu,Guangzhao Yang,Fu Ran,Tianbin Gao,Changshan Sun,Qinfu Zhao,Siling Wang
Oral administration of nanoparticles is extremely limited due to the two processes of mucus permeation and epithelial absorption, which requires completely opposite surface properties of the nanocarriers. To tackle the contradiction, we developed a rational strategy to modify the surface of mesoporous carbon nanoparticles with chitosan concealed by a hydrophilic N-(2-hydroxypropyl) methacrylamide copolymer (pHPMA) layer. Probucol (PB) with the low poor permeability and solubility was loaded in optimal nanocarriers to realize the high loading efficacy and controlled release. The pHPMA polymer is a hydrophilic “mucus-inert” material, which could be dissociable from the surface of nanoparticles in the mucus, thus promoting their mucus permeation and causing exposure of chitosan in transepithelial transport. The swelling effect of chitosan under acidic conditions allowed regulation of PB release behavior. In conclusion, the mucus-permeable nanocarrier could effectively overcome multiple gastrointestinal absorption barriers and the oral bioavailability of PB-loaded HCMCN was 2.76-fold that of commercial preparation.