Synthesis of liver-targeting dual-ligand modified GCGA/5-FU nanoparticles and their characteristics in vitro and in vivo

Cheng, Mingrong; Gao, Xiaoyan; Wang, Yong; Chen, Houxiang; He, Bing; Li, Yingchun; Han, Jing; Zhang, Zhiping

doi:10.2147/ijn.s52877

Cited by 9 publications

(2 citation statements)

References 25 publications

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“…Amphiphilic macromolecular materials such as hydrophobically modified polysaccharide polymers can be self-assembled into nano-sized particles. The size of the NP plays an important role in its functions of targeting and drug release control [ 21 ]. The hydrophobic group in the polymer is a driving force for the formation of the nuclear structure of the NP.…”

Section: Introductionmentioning

confidence: 99%

Pullulan-Based Nanoparticle-HSA Complex Formation and Drug Release Influenced by Surface Charge

et al. 2018

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The nanomaterial composition of nanoparticles and their protein adsorption in the blood is of great significance in the design of drug-loaded nanoparticles. To explore the interaction between the different surface components of nanoparticles (NPs) and protein, we synthesized three kinds of pullulan NP polymers: cholesteric hydrophobically (CH) modified pullulan (CHP), CH-modified animated pullulan (CHAP), and CH-modified carboxylated pullulan (CHSP). Pullulan NPs were prepared by the dialysis method. Dynamic light scattering was used to determine the charge and size of the three NPs. The size of NPs was altered by the number of charge groups when polymers contain the same degree of cholesterol substitution. The zeta potentials were + 12.9, − 15.4, and − 0.698 mV for CHAP, CHSP, and CHP, respectively, and the dimensions were 116.9, 156.9, and 73.1 nm, respectively. Isothermal titration calorimetry was used to determine the thermodynamic changes of NPs with different surface charge, and the effect of human serum albumin (HSA) on the titration was investigated. The changes of enthalpy and entropy demonstrated an interaction between NPs and HSA; the binding constant (Kb) for CHSP, CHP, and CHAP was 1.41, 27.7, and 412 × 104 M−1, respectively, with the positive charge for CHAP–HSA, uncharged for CHP–HSA, and negative charge for CHSP–HSA complex. Fluorescence and circular dichroism spectroscopy were used to determine the protein structure change after the complexation between NPs and HSA. The NP and HSA complexation is a complicated process composed of protein α-helical content reduction and the peptide chain extension; CHP NPs had the largest reduction in HSA α-helical content. The drug release rates of all compounds of NP and HSA were significantly lower than those of free drug and drug-loaded NPs after 48 h. The highest and lowest rates were observed in CHSP–HSA and CHP–HSA, respectively. The drug release was significantly influenced by the adsorption of HSA on NPs, and the size and surface charge of NPs played an important role in this process.

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Section: Introductionmentioning

confidence: 99%

Pullulan-Based Nanoparticle-HSA Complex Formation and Drug Release Influenced by Surface Charge

et al. 2018

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“…The tumor targeting ligands play a crucial role in the development of tumor contrast agents and targeted anticancer drugs. [3-10]…”

Section: Introductionmentioning

confidence: 99%

The targeting mechanism of DHA ligand and its conjugate with Gemcitabine for the enhanced tumor therapy

Qin

Tian

et al. 2014

Oncotarget

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Docosahexaenoic acid (DHA), an omega-3 C22 natural fatty acid serving as a precursor for metabolic and biochemical pathways, was reported as a targeting ligand of anticancer drugs. However, its tumor targeting ability and mechanism has not been claimed. Here we hypothesized that the uptake of DHA by tumor cells is related to the phosphatidylethanolamine (PE) contents in cell membranes. Thus, in this manuscript, the tumor-targeting ability of DHA was initially demonstrated in vitro and in vivo on different tumor cell lines by labeling DHA with fluorescence dyes. Subsequently, the tumor targeting ability was then correlated with the contents of PE in cell membranes to study the uptake mechanism. Further, DHA was conjugated with anticancer drug gemcitabine (DHA-GEM) for targeted tumor therapy. Our results demonstrated that DHA exhibited high tumor targeting ability and PE is the main mediator, which confirmed our hypothesis. The DHA-GEM displayed enhanced therapeutic efficacy than that of GEM itself, indicating that DHA is a promising ligand for tumor targeted therapy.

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Targeting of somatostatin receptors expressed in blood cells using quantum dots coated with vapreotide

Abdellatif

Abou-Taleb

Ghany

et al. 2018

Saudi Pharmaceutical Journal

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Cancer may be difficult to target, however, if cancer targeted this provides the chance for a better and more effective treatment. Quantum dots (Qdots) coated vapreotide (VAP) as a somatostatin receptors (SSTRs) agonist can be efficient targeting issue since may reduce side effects and increase drug delivery to the target tissue. This study highlights the active targeting of cancer cells by cells imaging with improving the therapeutic outcomes. VAP was conjugated to Qdots using amine-to-sulfhydryl crosslinker. The synthesized Qdots-VAP was characterized by determination of size, measuring the zeta-potential and UV fluorometer. The cellular uptake was studied using different cell lines. Finally, the Qdots-VAP was injected into a rat model. The results showed a size of 479.8 ± 15 and 604.88 ± 17 nm for unmodified Qdots and Qdots-VAP respectively, while the zeta potential of particles went from negative to positive charge which proved the conjugation of VAP to Qdots. The fluorometer recorded a redshift for Qdots-VAP compared with unmodified Qdots. Moreover, cellular uptake exhibited high specific binding with cells which express SSTRs using confocal microscopy and flow cytometry (17.3 MFU comparing to 3.1 MFU of control, P < 0.001). Finally, an in vivo study showed a strong accumulation of Qdots-VAP in the blood cells (70%). In conclusion, Qdots-VAP can play a crucial role in cancer diagnosis and treatment of blood cells diseases when conjugated with VAP as SSTRs agonist.

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Synthesis of liver-targeting dual-ligand modified GCGA/5-FU nanoparticles and their characteristics in vitro and in vivo

Cited by 9 publications

References 25 publications

Pullulan-Based Nanoparticle-HSA Complex Formation and Drug Release Influenced by Surface Charge

Pullulan-Based Nanoparticle-HSA Complex Formation and Drug Release Influenced by Surface Charge

The targeting mechanism of DHA ligand and its conjugate with Gemcitabine for the enhanced tumor therapy

Targeting of somatostatin receptors expressed in blood cells using quantum dots coated with vapreotide

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