Abstract
BackgroundSynergistic therapy of tumor is a promising way in curing cancer and in order to achieve effective tumor therapy with real-time drug release monitoring, dynamic cellular imaging and antitumor activity.ResultsIn this work, a polymeric nanoparticle with Forster resonance energy transfer (FRET) effect and chemo-photodynamic properties was fabricated as the drug vehicle. An amphiphilic polymer of cyclo(RGDfCSH) (cRGD)-poly(ethylene glycol) (PEG)-Poly(l-histidine) (PH)-poly(ε-caprolactone) (PCL)-Protoporphyrin (Por)-acting as both a photosensitizer for photodynamic therapy (PDT) and absorption of acceptor in FRET was synthesized and self-assembled into polymeric nanoparticles with epirubicin (EPI)-acting as an antitumor drug for chemotherapy and fluorescence of donor in FRET. Spherical EPI-loaded nanoparticles with the average size of 150 ± 2.4 nm was procured with negatively charged surface, pH sensitivity and high drug loading content (14.9 ± 1.5%). The cellular uptake of EPI-loaded cRGD-PEG-PH-PCL-Por was monitored in real time by the FRET effect between EPI and cRGD-PEG-PH-PCL-Por. The polymeric nanoparticles combined PDT and chemotherapy showed significant anticancer activity both in vitro (IC50 = 0.47 μg/mL) and better therapeutic efficacy than that of free EPI in vivo.ConclusionsThis work provided a versatile strategy to fabricate nanoassemblies for intracellular tracking of drug release and synergistic chemo-photodynamic therapy.
Highlights
Cancer is currently treated with surgical excision, radiation and chemotherapy, but not yet could cure cancer completely [1,2,3]
The destination of this work was fabricating a polymeric nanoparticle with Forster resonance energy transfer (FRET) effect and synergistic chemophotodynamic therapy for effective antitumor effect and monitoring the antitumor drug delivery of EPI
Scheme 2 The synthesis of amphiphiles of Por-PCL-PH-poly(ethylene glycol) (PEG)-cRGD as drug vehicles and the results showed that only one narrow peak was observed in all the GPC spectra in Fig. 3a with no other un-reacted compound observed in the spectra
Summary
Cancer is currently treated with surgical excision, radiation and chemotherapy, but not yet could cure cancer completely [1,2,3]. Du et al J Nanobiotechnol (2019) 17:113 and especially real-time drug release monitoring in blood circulation and tumor cell for co-delivery. As the weak acidic of lysosomes or endosomes in cytoplasm in tumor cells, the pH sensitivity could contribute triggering the massive release of antitumor drugs [18], which could improve the utilization ratio of antitumor drug and efficacy of chemotherapy. When the pH value is lower than its pKa, PH could be protonized so that it makes the drug carrier release the antitumor drug rapidly after entering tumor cells for effective chemotherapy. Synergistic therapy of tumor is a promising way in curing cancer and in order to achieve effective tumor therapy with real-time drug release monitoring, dynamic cellular imaging and antitumor activity
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