Preloading of hydrophobic anti-cancer drug into multifunctional nanocarrier for multi-modal imaging, NIR-responsive drug release and synergistic therapy

• Published in: Small (Weinheim an der Bergstrasse, Germany) Germany), 2016-09, Vol.12 (46), p.6388-6397
• Main Authors: Wang, Hui, Wang, Kui, Tian, Bowei, Revia, Richard, Mu, Qingxin, Jeon, Mike, Chang, Fei-Chien, Zhang, Miqin
• Format: Article
• Language: English
• ISSN: 1613-6810; 1613-6829
• DOI: 10.1002/smll.201602263

Applications of hydrophobic drug-based nanocarriers (NCs) remain largely limited because of their low loading capacity. Here, we report development of a multifunctional hybrid NC made of a magnetic Fe 3 O 4 nanoparticle core and a mesoporous silica shell embedded with fluorescent carbon dots (CDs) and paclitaxel (PTX), and covered by another layer of silica. The NC is prepared via a one-pot process under mild condition. The PTX loading method introduced in this study simplifies drug loading process and demonstrates a high loading capacity as a result of the mesoporous silica dual-shell structure, supramolecular π-stacking between the conjugated rings of PTX molecules and aromatic rings of the CDs in the hybrid NC. The CDs also serve as both confocal and two-photon fluorescence imaging probes, while the Fe 3 O 4 core serves as an MRI contrast agent. Significantly, NC releases PTX in response to NIR irradiation as a result of local heating of the embedded CDs and the heating of CDs also provides an additional therapeutic effect by thermally killing cancer cells in tumor in addition to the chemotherapeutic effect of released PTX. Both in vitro and in vivo results show that NC demonstrates high therapeutic efficacy through a synergistic effect from the combined chemo-photothermal treatments. The manuscript reports a new nanocarrier comprised of a magnetic Fe 3 O 4 core, fluorescent carbon dots, preloaded hydrophobic drug paclitaxel, and mesoporous silica for optical bioimaging, magnetic resonance imaging, and near infrared-responsive drug release. Results demonstrate that the hybrid NCs have high therapeutic efficacy through synergistic effect due to the combined chemo-photothermal treatments.