Fabrication of pH-responsive PLGA(UCNPs/DOX) nanocapsules with upconversion luminescence for drug delivery

The integration of anticancer drugs and inorganic nanocrystals in polymer nanocapsules is a widely used strategy to improve their functionality, stability and sustained release. However, the complexity in the preparation of functional nanocapsules and their reproducibility still challenge these promising drug carriers in clinical application. Here we introduce a simple one-step self-assembly strategy to prepare multifunctional nanocapsules based on simultaneous poly (DL-lactic-co-glycolic acid) (PLGA) encapsulation of antitumor drug doxorubicin hydrochloride (DOX) and NaYF₄:Yb,Er@NaGdF₄ upconversion nanoparticles (UCNPs) for cancer cell imaging and drug delivery. The obtained PLGA(UCNPs/DOX) nanocapsules with a small size of ≈150 nm possessed bright upconversion fluorescence and could act as T _1- weighted contrast agents for magnetic resonance imaging (MRI). Moreover, the PLGA(UCNPs/DOX) nanocapsules exhibited pH-responsive drug releasing behavior, causing the loaded DOX easily releasing at cancer cells, and an obvious cytotoxicity via MTT assay. The endocytosis process of PLGA (UCNPs/DOX) nanocapsules is evaluated using optical microscopy and upconversion fluorescence microscopy. These results demonstrated that the developed PLGA nanocapsules could serve as multifunctional drug delivery systems for cancer imaging and therapy.