PurposeZinc phthalocyanine (ZnPc) has been applied widely in photodynamic therapy (PDT) with high ROS-production capacity and intense absorption in the near-infrared region. However, weak tumor targeting and the aggregation tendency of ZnPc seriously affect the therapeutic effect of PDT. Therefore, overcoming the aggregation of ZnPc and enhancing its antitumor effect were the purpose of this study.MethodsIn this study, we first found that the aggregation behaviors of the photosensitizer ZnPc(TAP)4, ZnPc substituted by tertiary amine groups, were regulated finely by pH and that ZnPc(TAP)4 could be disaggregated gradually as the pH descended. ZnPc(TAP)4 and human serum albumin (HSA) molecules were assembled into nanoparticles (NPs) for tumor targeting. Meanwhile, the chemotherapy drug paclitaxel (Ptx) was loaded into HSA NPs together with ZnPc(TAP)4 for dual antitumor effects. HSA NPs loading both ZnPc(TAP)4 and Ptx (NP–ZnPc[TAP]4–Ptx) were characterized by particle size and in vitro release. Cytotoxicity, subcellular localization, tumor targeting, and anticancer effect in vivo were investigated respectively.ResultsWe found that NP–ZnPc(TAP)4–Ptx had good stability with qualifying particle size. Interestingly, ZnPc(TAP)4 was released from the NPs and the photodynamic activity enhanced in the acidic environment of tumor. In addition, NP–ZnPc(TAP)4–Ptx had prominent cytotoxicity and time-dependent subcellular localization characteristics. Through a three-dimensional animal imaging system, NP–ZnPc(TAP)4–Ptx showed much-enhanced tumor targeting in tumor-bearing mice. Above all, NP–ZnPc(TAP)4–Ptx was demonstrated to have the synergistic anticancer effect of PDT and chemotherapy.ConclusionNP–ZnPc(TAP)4–Ptx had enhanced tumor targeting for the pH-sensitive property of ZnPc(TAP)4 and the transport function of HSA. NP–ZnPc(TAP)4–Ptx possessed a double-anticancer effect through the combination of ZnPc(TAP)4 and Ptx. This drug-delivery system may also be used to carry chemotherapy drugs other than Ptx for improving antitumor effects.
Rhamnella gilgitica Mansf. et Melch, which belongs to the rhamnus family (Rhamnaceae), is traditionally used to treat rheumatism, swelling and pain in China. However, little is known about the pharmacological activities of this plant. The anti-inflammatory activities of the 70% ethanol extract of R. gilgitica (RG) in RAW264.7 macrophages and complete Freund's adjuvant (CFA)-induced arthritic rats are investigated in this study for the first time. The effects of RG on cell viability were determined by a MTT assay, and the effects of RG on pro-inflammatory mediators were analyzed by ELISA and Western blot. The effects of RG on paw thickness, thymus and spleen index were also examined in CFA-induced arthritic rats. RG suppressed the induction of proinflammatory mediators, including iNOS (inducible nitric oxide synthase), NO (nitric oxide), COX-2 (cyclooxygenase-2) and PG (prostaglandin) E2 in LPS stimulated RAW264.7 macrophages. RG also inhibited the phosphorylation and degradation of I[Formula: see text]B-[Formula: see text], as well as the nuclear translocation of nuclear factor kappa B (NF-[Formula: see text]B) p65. In addition, RG treatment significantly reduced the paw thickness in CFA-induced arthritic rats. Oral administration of RG led to a significant decrease of both the thymus and spleen index at a concentration of 100[Formula: see text]mg/mL. Taken together, these findings suggest that RG might be an agent for further development in the treatment of a variety of inflammatory diseases.
Nicosulfuron (NSF) is a water-insoluble and unstable sulfonylurea herbicide, which is mainly used in the treatment of stems and leaves after the corn seedling stage. Nanosponges (NS) have more interaction sites and higher drug encapsulation capabilities. In this paper, three kinds of β-cyclodextrin nanosponges (CDNS) were prepared by crosslinking β-cyclodextrin with diphenyl carbonate (DPC), pyromellitic dianhydride (PMDA) and epichlorohydrin (EP), respectively. The NSF-loaded CDNS were characterized by TEM, FTIR, DSC, TGA and XRD. The solubility, stability and biological activity of NSF were studied. The results showed NSFEP-CDNS could significantly enhance the solubility of NSF. In vitro release test, the cumulative release of NSF-EP-CDNS was 90.11%. Compared with pure NSF and NSF oil suspension, NSF-EP-CDNS had the strongest inhibitory effect on acetolactate synthase (ALS). In conclusion, CDNS have beneficial effects on the solubility, stability and biological activity of NSF.
A drug co-delivery system composed of selenium nanoparticles (SeNPs) has attracted increasing interest due to its ability to increase the anticancer efficacy against multidrug-resistant cancer cells. In this study, a cancer-targeted drug co-delivery system combining fluorescein-loaded liposomes and SeNPs was designed and evaluated. The system was developed by coating SeNPs and fluorescein-loaded liposomes with folic acid-chitosan conjugates (FA-CS-SeNPs-Lips). Folic acid-chitosan conjugates (FA-CS) were synthesized by coupling folic acid (FA) with chitosan (CS), and the structure was confirmed by performing Fourier transform spectroscopy (FT-IR) and nuclear magnetic resonance (1H-NMR) spectroscopy. Dynamic light scattering (DLS) measurements and transmission electron microscopy (TEM) were used to evaluate the particle size, Zeta potential, and morphology. The cytotoxicity of SeNPs coated with FA-CS conjugates (FA-CS-SeNPs) toward A549 cells and HeLa cells was examined using the MTT assay. The cancer-targeting ability and drug release behaviors were evaluated in vitro by measuring the cellular uptake of fluorescein and dialysis, respectively. The FA-CS-SeNPs were uniform, spherical particles with a ~50 nm diameter and high positive Zeta potential (+57.7 mV). Based on the results of the MTT assay, FA-CS-SeNPs displayed a more significant increase in the anticancer efficacy in HeLa cells than CS-SeNPs. FA-CS-SeNPs-Lips not only slowly released fluorescein but also specifically targeted HeLa cells through selective binding between folate and folate receptors to increase the cellular uptake of fluorescein.
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