Metal–organic
frameworks (MOFs) have been applied in chemotherapeutic drug loading
for cancer treatment, but challenging for cases with large and malignant
lesions. To overcome these difficulties, combinational therapies of
chemotherapy and photothermal therapy (PTT) with potentially high
selectivity and slight aggressiveness have drawn tremendous attention
to treat various tumors. However, current MOF-based nanohybrids with
photothermal agents involve tedious synthesis processes and heterogeneous
structures. Herein, we employ MIL-53 as a microreactor to grow polypyrrole
(PPy) nanoparticles in situ for the fabrication of PPy@MIL-53 nanocomposites.
Fe3+ in MIL-53, as an intrinsic oxidizing agent, can oxidize
the pyrrole monomer to generate PPy nanoparticles. The prepared PPy@MIL-53
nanocomposites integrate the intrinsic advantages of MOFs with high
drug loading ability and magnetic resonance imaging (MRI) capacity,
and PPy nanoparticles with outstanding PTT ability and excellent biocompatibility.
The versatile PPy@MIL-53 nanocomposites with multiple functions displayed
in vitro and in vivo synergism of photothermal–chemotherapy
for cancer, potentially MRI-guided. The proposed MOF microreactor-based
synthesis strategy shows a promising prospect in the fabrication of
diverse multifunctional nanohybrids for tumor theranostics in vivo.