Self-assembly supramolecular drug delivery system for combination of photodynamic therapy and chemotherapy.

AIMS

To construct a self-assembly supramolecular drug delivery system (DDS) to co-deliver chlorin e6 (Ce6) and tripeptide tyroseroleutide (YSL) and evaluate the anti-tumour effects.

METHODS

A supramolecular DDS was constructed via self-assembly of Ce6 and YSL based on π-π stacking and hydrogen-bond interaction. The size, morphology, stability, drug release, cellular uptake, cytotoxicity, pharmacokinetics analysis and pharmacodynamics analysis were respectively studied.

RESULTS

Ce6-YSL nanoparticles with a uniform size of 75 ± 3.5 nm (PDI = 0.128) and monodispersed spherical morphology were constructed. The nanoparticles exhibited good stability with zeta potential -21.2 ± 1.73 mV. Under the weak acidic conditions, the accumulative drug release was 82.8% (w/w) (pH = 6.0) and 91.5% (w/w) (pH = 5.0), respectively, indicating that nanoparticles performed smart responsive properties and achieved controlled release characteristics in acidic tumour microenvironment. In addition, nanoparticles could easily enter the tumour cells and induce ROS production and inhibit cell proliferation in SMMCC-7721 cells with IC value 3.4 ± 0.023 μg/mL under laser irradiation. Furthermore, the nanoparticles could retain a much higher blood concentration and displayed excellent antitumor effect in tumour-bearing mice, showing no influence on body weight.

CONCLUSIONS

This self-assembly supramolecular DDS can be used for combination of photodynamic therapy and chemotherapy in future research.