scholarly journals Sorafenib-Loaded Long-Circulating Nanoliposomes for Liver Cancer Therapy

2020 ◽  
Vol 2020 ◽  
pp. 1-12
Author(s):  
Haiwei Ye ◽  
Liping Zhou ◽  
Haili Jin ◽  
Yunhua Chen ◽  
Die Cheng ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Liver Cancer ◽  
Tumor Targeting ◽  
Entrapment Efficiency ◽  
Antitumor Effects ◽  
Therapeutic Efficiency ◽  
Loading Efficiency ◽  
Tumor Region

A type of sorafenib- (SOR-) loaded long-circulating nanoliposome was constructed, and the targeting performance and antitumor effects of the prepared liposome were evaluated in the present study. Polyethylene glycol- (PEG-) modified long-circulating nanoliposomes (LC-NPs) were designed and prepared using reverse evaporation, and the LC-NPs were used for delivering sorafenib (LC-PEG-SOR-NPs). Then, the anti-VEGFR antibody as a targeting moiety was chemically coupled with LC-PEG-SOR-NPs to form liver cancer-targeted nanoliposomes (anti-VEGFR-LC-PEG-SOR-NPs). The drug entrapment and loading efficiency were measured. And the cancer-targeting performance and therapeutic efficiency were evaluated both in vitro and in vivo. The anti-VEGFR-LC-PEG-SOR-NPs with an average of 119.8±4.2 nm showed a uniform spherical structure. The drug entrapment and loading efficiency were 92.5% and 18.5%, respectively. The killing efficiency of anti-VEGFR-LC-PEG-SOR-NPs was up to 18% after incubating with liver cancer cells for 72 h. Furthermore, the anti-VEGFR-LC-PEG-SOR-NPs could actively target at the tumor region and could efficiently inhibit tumor growth with negligible side effects. This newly designed nanoliposomes had desirable dispersibility, high drug entrapment efficiency, tumor targeting and therapeutic efficiency, and good safety. As a biocompatible nanocomposite, it was promising to become a novel and useful tumor-targeting nanodrug for liver cancer therapy.

Mannose Conjugated Starch Nanoparticles for Preferential Targeting of Liver Cancer

2020 ◽  
Vol 17 ◽  
Author(s):  
Akhlesh Kumar Jain ◽  
Hitesh Sahu ◽  
Keerti Mishra ◽  
Suresh Thareja
Keyword(s):  
Side Effects ◽  
Liver Cancer ◽  
Entrapment Efficiency ◽  
Xrd Analysis ◽  
In Vitro Cytotoxicity ◽  
Physical Interaction ◽  
Scanning Calorimetry ◽  
Starch Nanoparticles

Aim: To design D-Mannose conjugated 5-Fluorouracil (5-FU) loaded Jackfruit seed starch nanoparticles (JFSSNPs) for site specific delivery. Background: Liver cancer is the third leading cause of death in world and fifth most often diagnosed cancer is the major global threat to public health. Treatment of liver cancer with conventional method bears several side effects, thus to undertake these side effects as a formulation challenge, it is necessary to develop novel target specific drug delivery system for the effective and better localization of drug into the proximity of target with restricting the movement of drug in normal tissues. Objective: To optimize and characterize the developed D-Mannose conjugated 5-Fluorouracil (5-FU) loaded Jackfruit seed starch nanoparticles (JFSSNPs) for effective treatment of liver cancer. Materials and methods: 5-FU loaded JFSSNPs were prepared and optimized formulation had higher encapsulation efficiency were conjugated with D-Mannose. These formulations were characterized for size, morphology, zeta potential, X-Ray Diffraction, and Differential Scanning Calorimetry. Potential of NPs were studied using in vitro cytotoxicity assay, in vivo kinetic studies and bio-distribution studies. Result and discussion: 5-Fluorouracil loaded NPs had particle size between 336 to 802nm with drug entrapment efficiency was between 64.2 to 82.3%. In XRD analysis, 5-FU peak was diminished in the diffractogram, which could be attributed to the successful incorporation of drug in amorphous form. DSC study suggests there was no physical interaction between 5- FU and Polymer. NPs showed sustained in vitro 5-FU release up to 2 hours. In vivo, mannose conjugated NPs prolonged the plasma level of 5-FU and assist selective accumulation of 5-FU in the liver (vs other organs spleen, kidney, lungs and heart) compared to unconjugated one and plain drug. Conclusion: In vivo, bio-distribution and plasma profile studies resulted in significantly higher concentration of 5- Fluorouracil liver suggesting that these carriers are efficient, viable, and targeted carrier of 5-FU treatment of liver cancer.

scholarly journals Folate-Functionalized Mesoporous Hollow SnO2 Nanofibers as a Targeting Drug Carrier to Improve the Antitumor Effect of Paclitaxel for Liver Cancer Therapy

2018 ◽  
Vol 2018 ◽  
pp. 1-11
Author(s):  
Huiling Lv ◽  
Chao Wu ◽  
Xuan Liu ◽  
Andi Bai ◽  
Yue Cao ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Liver Cancer ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Hollow Structure ◽  
Amorphous State ◽  
Outer Diameter ◽  
Drug Delivery Carrier

In this study, we prepared PTX-loaded mesoporous hollow SnO2 nanofibers conjugated with folic acid (SFNFP) for liver cancer therapy. According to SEM and TEM characterization, SFNF showed a mesoporous hollow structure. The average outer diameter was 200 nm, and the wall thickness was 50 nm. The DSC and XRD study showed that PTX in the channels of nanofibers was present in an amorphous state. The in vitro release experiments demonstrated that SFNF could efficiently improve the dissolution rate of PTX. Both in vitro cell experiments and in vivo antitumor experiments showed that SFNFP could efficiently inhibit the growth of liver cancer cells. Therefore, SFNF is a promising targeting antitumor drug delivery carrier.

Uniform hollow mesoporous silica nanocages for drug delivery in vitro and in vivo for liver cancer therapy

2011 ◽  
Vol 21 (14) ◽  
pp. 5299 ◽  
Author(s):  
Tingting Wang ◽  
Fang Chai ◽  
Qin Fu ◽  
Lingyu Zhang ◽  
Haiyan Liu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Cancer Therapy ◽  
Liver Cancer ◽  
Mesoporous Silica ◽  
Hollow Mesoporous Silica

scholarly journals The Good, the Bad, the Question–H19 in Hepatocellular Carcinoma

Cancers ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 1261 ◽  
Author(s):  
Lysann Tietze ◽  
Sonja M. Kessler
Keyword(s):  
Hepatocellular Carcinoma ◽  
Cancer Therapy ◽  
Liver Cancer ◽  
Primary Liver Cancer ◽  
Human Patient ◽  
In Vivo Models ◽  
Study Results ◽  
Novel Target

Hepatocellular carcinoma (HCC), the most common primary liver cancer, is challenging to treat due to its typical late diagnosis, mostly at an advanced stage. Therefore, there is a particular need for research in diagnostic and prognostic biomarkers and therapeutic targets for HCC. The use of long noncoding (lnc) RNAs can widen the list of novel molecular targets improving cancer therapy. In hepatocarcinogenesis, the role of the lncRNA H19, which has been known for more than 30 years now, is still controversially discussed. H19 was described to work either as a tumor suppressor in vitro and in vivo, or to have oncogenic features. This review attempts to survey the conflicting study results and tries to elucidate the potential reasons for the contrary findings, i.e., different methods, models, or readout parameters. This review encompasses in vitro and in vivo models as well as studies on human patient samples. Although the function of H19 in HCC remains elusive, a short outlook summarizes some ideas of using the H19 locus as a novel target for liver cancer therapy.

scholarly journals Antitumor effects of Tv1 venom peptide in liver cancer

2019 ◽  
Author(s):  
Prachi Anand ◽  
Petr Filipenko ◽  
Jeannette Huaman ◽  
Michael Lyudmer ◽  
Marouf Hossain ◽  
...  
Keyword(s):  
Liver Cancer ◽  
Transient Receptor Potential ◽  
Receptor Potential ◽  
Cancer Therapies ◽  
Antitumor Effects ◽  
Venom Peptides ◽  
Calcium Dependent ◽  
Venom Peptide

AbstractA strategy for treating the most common type of liver cancer, hepatocellular carcinoma (HCC) applies a targeted therapy using venom peptides that are selective for ion channels and transporters overexpressed in tumor cells. Here, we report selective anti-HCC properties of Tv1, a venom peptide from the predatory marine terebrid snail, Terebra variegata. Tv1 was applied in vitro to liver cancer cells and administered in vivo to allograft tumor mouse models. Tv1 inhibited the proliferation of murine HCC cells via calcium dependent apoptosis resulting from down-regulation of the cyclooxygenase-2 (COX-2) pathway. Additionally, tumor sizes were significantly reduced in Tv1-treated syngeneic tumor-bearing mice. Tv1’s mechanism of action involves binding to specific transient receptor potential (TRP) cation channels that are overexpressed in HCC cell models. Our findings demonstrate the unique potential of venom peptides to function as tumor specific ligands in the quest for targeted cancer therapies.

scholarly journals Transferrin-Conjugated Erianin-Loaded Liposomes Suppress the Growth of Liver Cancer by Modulating Oxidative Stress

2021 ◽  
Vol 11 ◽  
Author(s):  
Anhui Yang ◽  
Zhen Sun ◽  
Rui Liu ◽  
Xin Liu ◽  
Yue Zhang ◽  
...  
Keyword(s):  
Liver Cancer ◽  
Tumor Targeting ◽  
Tumor Model ◽  
Aqueous Solubility ◽  
Ethanol Injection ◽  
Expression Levels ◽  
Tumor Tissues ◽  
Induced Apoptosis

BackgroundLiver cancer is one of the most malignant human cancers, with few treatments and a poor prognosis. Erianin (ERN) is a natural compound with multiple pharmacological activities that has been reported to have numerous excellent effects against liver cancer in experimental systems. However, its application in vivo has been limited due to its poor aqueous solubility and numerous off-target effects. This study aimed to improve the therapeutic efficacy of ERN by developing novel ERN-loaded tumor-targeting nanoparticles.ResultsIn this study, ERN was loaded into liposomes by ethanol injection (LP-ERN), and the resulting LP-ERN nanoparticles were treated with transferrin to form Tf-LP-ERN to improve the solubility and enhance the tumor-targeting of ERN. LP-ERN and Tf-LP-ERN nanoparticles had smooth surfaces and a uniform particle size, with particle diameters of 62.60 nm and 88.63 nm, respectively. In HepG2 and SMMC-7721 cells, Tf-LP-ERN induced apoptosis, decreased mitochondrial membrane potentials and increased ERN uptake more effectively than free ERN and LP-ERN. In xenotransplanted mice, Tf-LP-ERN inhibited tumor growth, but had a minimal effect on body weight and organ morphology. In addition, Tf-LP-ERN nanoparticles targeted tumors more effectively than free ERN and LP-ERN nanoparticles, and in tumor tissues Tf-LP-ERN nanoparticles promoted the cleavage PARP-1, caspase-3 and caspase-9, increased the expression levels of Bax, Bad, PUMA, and reduced the expression level of Bcl-2. Moreover, in the spleen of heterotopic tumor model BALB/c mice, ERN, LP-ERN and Tf-LP-ERN nanoparticles increased the expression levels of Nrf2, HO-1, SOD-1 and SOD-2, but reduced the expression levels of P-IKKα+β and P-NF-κB, with Tf-LP-ERN nanoparticles being most effective in this regard. Tf-LP-ERN nanoparticles also regulated the expression levels of TNF-α, IL-10 and CCL11 in serum.ConclusionTf-LP-ERN nanoparticles exhibited excellent anti-liver cancer activity in vivo and in vitro by inducing cellular apoptosis, exhibiting immunoregulatory actions, and targeting tumor tissues, and did so more effectively than free ERN and LP-ERN nanoparticles. These results suggest that the clinical utility of a Tf-conjugated LP ERN-delivery system for the treatment of liver cancer warrants exploration.

Cytotoxic Stilbenes and Derivatives as Promising Antimitotic Leads for Cancer Therapy

2019 ◽  
Vol 24 (36) ◽  
pp. 4270-4311 ◽  
Author(s):  
Célia Faustino ◽  
Ana P. Francisco ◽  
Vera M. S. Isca ◽  
Noélia Duarte
Keyword(s):  
Cancer Therapy ◽  
Targeted Delivery ◽  
Biological Evaluation ◽  
Chemotherapeutic Agents ◽  
Cytotoxic Agents ◽  
Stable Configuration ◽  
Antiangiogenic Agents ◽  
Antitumor Effects

The growing incidence of cancer, the toxic side-effects associated with conventional chemotherapeutic agents and the development of multidrug resistance (MDR) drive the search for novel and more effective drugs with multi-target activity and selectivity towards cancer cells. Stilbenes are a group of naturally occurring phenolic compounds of plant origin derived from the phenylpropanoid pathway that may exist as cis- or trans-isomers. Although the trans-isomer is the more common and stable configuration, resveratrol being a representative compound, cis-stilbenes are potent cytotoxic agents that bind to and inhibit tubulin polymerization, destabilizing microtubules. This review summarizes the chemistry and biological evaluation of cytotoxic stilbenes and their synthetic derivatives as promising antimitotic leads for cancer therapy, focusing on the most potent compounds, the combretastatins. Combretastatins isolated from the South African bushwillow Combretum caffrum are among the most potent antimitotic and vascular disrupting agents (VDAs) of natural origin. Preclinical studies have demonstrated their potent antitumor effects in a wide variety of tumors, both in vitro and in vivo, being currently under evaluation in phase 2 and phase 3 clinical trials for several types of solid tumors. Topics covered herein include synthetic medicinal chemistry, modes of action, structure-activity relationships (SAR), preclinical and clinical studies as VDAs in cancer therapy, either as single agents or in combination with cytotoxic anticancer drugs, antiangiogenic agents, or radiation therapy, and development of appropriate formulations based on nanocarriers (e.g., liposomes, nanoemulsions, polymeric, lipid and ceramic nanoparticles, carbon nanotubes) for improved bioavailability and targeted delivery of combretastatins to the tumor vasculature.

Hydrophobized SN38 to redox-hypersensitive nanorods for cancer therapy

2019 ◽  
Vol 7 (2) ◽  
pp. 265-276 ◽  
Author(s):  
Yaxin Zheng ◽  
Xueling Yan ◽  
Yalun Wang ◽  
Xing Duan ◽  
Xinming Wang ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Antitumor Effects ◽  
Self Assembled

Redox-hypersensitive hydrophobized SN38 self-assembled into rod-shaped nanoaggregates with uncompromised in vitro cytotoxicity and potent in vivo antitumor effects.

Doxorubicin nanomedicine based on ginsenoside Rg1 with alleviated cardiotoxicity and enhanced antitumor activity

Nanomedicine ◽  
2021 ◽  
Vol 16 (29) ◽  
pp. 2587-2604
Author(s):  
Chaoqi Li ◽  
Xiangbo Gou ◽  
Hui Gao
Keyword(s):  
Antitumor Activity ◽  
Protective Effect ◽  
Tumor Targeting ◽  
Antitumor Effect ◽  
Ginsenoside Rg1 ◽  
Antitumor Effects ◽  
Tumor Bearing ◽  
Targeting Ability

Aim: The authors aimed to develop Dox@Rg1 nanoparticles with decreased cardiotoxicity to expand their application in cancer. Materials & methods: Dox@Rg1 nanoparticles were developed by encapsulating doxorubicin (Dox) in a self-assembled Rg1. The antitumor effect of the nanoparticles was estimated using 4T1 tumor-bearing mice and the protective effect on the heart was investigated in vitro and in vivo. Results: Different from Dox, the Dox@Rg1 nanoparticles induced increased cytotoxicity to tumor cells, which was decreased in cardiomyocytes by the inhibition of apoptosis. The study in vivo revealed that the Dox@Rg1 nanoparticles presented a perfect tumor-targeting ability and improved antitumor effects. Conclusion: Dox@Rg1 nanoparticles could enhance the antitumor effects and decrease the cardiotoxicity of Dox.

Preparation of paclitaxel-folic acid functionalized gelatin grafted mesoporous hollow carbon nanospheres for enhancing antitumor effects toward liver cancer (SMMC-7721) cell lines

2019 ◽  
Vol 34 (8) ◽  
pp. 1071-1080 ◽  
Author(s):  
Yu Gao ◽  
Tao Liu ◽  
Xuan Liu ◽  
Chao Wu
Keyword(s):  
Folic Acid ◽  
Liver Cancer ◽  
Cell Lines ◽  
Carbon Nanospheres ◽  
Adsorption Method ◽  
Antitumor Effects ◽  
Human Liver Cancer ◽  
Hollow Carbon

Folic acid functionalized gelatin-coated mesoporous hollow carbon nanospheres (FGMCN) were synthesized and applied to enhance the antitumor curative effect of paclitaxel (PTX) for human liver cancer cell lines (SMMC-7721). PTX was loaded in FGMCN by the adsorption method and the PTX-loaded samples (PTX-FGMCN) had a drug content of 29.8 ± 1.06%. The PTX-FGMCN with a sustained release effect was characterized by X-ray diffraction and differential scanning calorimeter in order to analyze the PTX state in FGMCN. In vitro cell experiments showed that FMHSN improves the uptake of PTX and promotes apoptosis due to the nano-targeting effect of FMHSN. An in vivo tumor bearing experiment in mice indicated that the PTX-FGMCN significantly inhibited the growth of tumors. All of these results suggested that the PTX-FGMCN may be an effective anti-hepatoma drug in the future.

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