<i>In vitro</i> and <i>in vivo</i> evaluation of macromolecular prodrug GC-FUA based nanoparticle for hepatocellular carcinoma chemotherapy

Huang, Can; Li, Na-Mei; Gao, Pei; Yang, Sa; Ning, Qian; Huang, Wen; Li, Zhiping; Ye, Peng-Ju; Li, Xiang; He, Dongxiu; Tan, Xiang-Wen; Yu, Cui‐Yun

doi:10.1080/10717544.2016.1264499

Cited by 26 publications

(17 citation statements)

References 31 publications

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“…5-FU induces apoptosis in cancer cells 62 – 64 , and 5-FA is believed to kill tumor cells with a similar mechanism as 5-FU 65 . Therefore, to confirm the apoptotic activity induced by various 5-FA formulations, FITC Annexin V/PI (propidium iodide) flow cytometry assay was performed on A431 cells to identify externalization of phosphotidylserine (PS), a prevalent sign of apoptosis.…”

Section: Discussionmentioning

confidence: 99%

Targeted delivery of 5-fluorouracil-1-acetic acid (5-FA) to cancer cells overexpressing epithelial growth factor receptor (EGFR) using virus-like nanoparticles

Gan

Rullah

Yong

et al. 2020

Sci Rep

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Chemotherapy is widely used in cancer treatments. However, non-specific distribution of chemotherapeutic agents to healthy tissues and normal cells in the human body always leads to adverse side effects and disappointing therapeutic outcomes. Therefore, the main aim of this study was to develop a targeted drug delivery system based on the hepatitis B virus-like nanoparticle (VLNP) for specific delivery of 5-fluorouracil-1-acetic acid (5-FA) to cancer cells expressing epithelial growth factor receptor (EGFR). 5-FA was synthesized from 5-fluorouracil (5-FU), and it was found to be less toxic than the latter in cancer cells expressing different levels of EGFR. The cytotoxicity of 5-FA increased significantly after being conjugated on the VLNP. A cell penetrating peptide (CPP) of EGFR was displayed on the VLNP via the nanoglue concept, for targeted delivery of 5-FA to A431, HT29 and HeLa cells. The results showed that the VLNP displaying the CPP and harboring 5-FA internalized the cancer cells and killed them in an EGFR-dependent manner. This study demonstrated that the VLNP can be used to deliver chemically modified 5-FU derivatives to cancer cells overexpressing EGFR, expanding the applications of the VLNP in targeted delivery of chemotherapeutic agents to cancer cells overexpressing this transmembrane receptor.

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Section: Discussionmentioning

confidence: 99%

Targeted delivery of 5-fluorouracil-1-acetic acid (5-FA) to cancer cells overexpressing epithelial growth factor receptor (EGFR) using virus-like nanoparticles

Gan

Rullah

Yong

et al. 2020

Sci Rep

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“…In Huang's work, the N -galactosylated-chitosan-5-FU (GC-FU) acetic acid conjugate was evaluated by different experiments with HepG2 and A549 cells in vitro and in vivo 116. The half-life of GC-FU-NPs (i.v. )…”

Section: Chemotherapy and Molecular Targeted Therapy Of Hepatoma Withmentioning

confidence: 99%

Evaluation of Polymer Nanoformulations in Hepatoma Therapy by Established Rodent Models

Wang

Zhang

et al. 2019

Theranostics

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Hepatoma is one of the most severe malignancies usually with poor prognosis, and many patients are insensitive to the existing therapeutic agents, including the drugs for chemotherapy and molecular targeted therapy. Currently, researchers are committed to developing the advanced formulations with controlled drug delivery to improve the efficacy of hepatoma therapy. Numerous inoculated, induced, and genetically engineered hepatoma rodent models are now available for formulation screening. However, animal models of hepatoma cannot accurately represent human hepatoma in terms of histological characteristics, metastatic pathways, and post-treatment responses. Therefore, advanced animal hepatoma models with comparable pathogenesis and pathological features are in urgent need in the further studies. Moreover, the development of nanomedicines has renewed hope for chemotherapy and molecular targeted therapy of advanced hepatoma. As one kind of advanced formulations, the polymer-based nanoformulated drugs have many advantages over the traditional ones, such as improved tumor selectivity and treatment efficacy, and reduced systemic side effects. In this article, the construction of rodent hepatoma model and much information about the current development of polymer nanomedicines were reviewed in order to provide a basis for the development of advanced formulations with clinical therapeutic potential for hepatoma.

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“…HCC incidence continues to increase with approximately 700,000 cases per year worldwide. The issue of greatest concern is the poor survival rate [3,4]. HCC is usually diagnosed in the advanced stages when prognosis for the disease recovery is meager, and survival is one to two months [5,6].…”

Section: Introductionmentioning

confidence: 99%

“…Furthermore, if receptor-mediated endocytosis follows receptor binding, this entry method could be used to direct drug-containing nanovehicles to any type of target cell [8]. The asialoglycoprotein receptor (ASGPR) is abundantly expressed on hepatocyte membranes (500,000 ASGPR/hepatocyte) and minimally expressed in extrahepatic tissues [4,6]. In vivo , the ASGPR recognizes and captures proteins and peptides that carry exposed galactose residues [4] and the receptor cargo enters the cell via receptor-mediated endocytosis.…”

Section: Introductionmentioning

confidence: 99%

Lactosylated Albumin Nanoparticles: Potential Drug Nanovehicles with Selective Targeting Toward an In Vitro Model of Hepatocellular Carcinoma

et al. 2019

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Hepatocellular carcinoma (HCC) ranks fifth in occurrence and second in mortality of all cancers. The development of effective therapies for HCC is urgently needed. Anticancer drugs targeted to the liver-specific asialoglycoprotein receptors (ASGPRs) are viewed as a promising potential treatment for HCC. ASGPRs facilitate the recognition and endocytosis of molecules, and possibly vehicles with galactose end groups, by the liver. In this study, bovine serum albumin (BSA) was conjugated with lactose using a thermal treatment. The formation of lactosylated BSA (BSA-Lac) was confirmed by a change of the chemical structure, increased molecular mass, and Ricinus communis lectin recognition. Subsequently, the low-crosslinking BSA-Lac nanoparticles (LC BSA-Lac NPs) and high-crosslinking BSA-Lac nanoparticles (HC BSA-Lac NPs) were synthesized. These nanoparticles presented spherical shapes with a size distribution of 560 ± 18.0 nm and 539 ± 9.0 nm, as well as an estimated surface charge of −26 ± 0.15 mV and −24 ± 0.45 mV, respectively. Both BSA-Lac NPs were selectively recognized by ASGPRs as shown by biorecognition, competition, and inhibition assays using an in vitro model of HCC. This justifies pursuing the strategy of using BSA-Lac NPs as potential drug nanovehicles with selective direction toward hepatocellular carcinoma.

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In vitro and in vivo evaluation of macromolecular prodrug GC-FUA based nanoparticle for hepatocellular carcinoma chemotherapy

Cited by 26 publications

References 31 publications

Targeted delivery of 5-fluorouracil-1-acetic acid (5-FA) to cancer cells overexpressing epithelial growth factor receptor (EGFR) using virus-like nanoparticles

Targeted delivery of 5-fluorouracil-1-acetic acid (5-FA) to cancer cells overexpressing epithelial growth factor receptor (EGFR) using virus-like nanoparticles

Evaluation of Polymer Nanoformulations in Hepatoma Therapy by Established Rodent Models

Lactosylated Albumin Nanoparticles: Potential Drug Nanovehicles with Selective Targeting Toward an In Vitro Model of Hepatocellular Carcinoma

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