Ligand based dendritic systems for tumor targeting

Agarwal, Abhinav; Saraf, Surbhi; Asthana, Abhay; Gupta, Umesh; Gajbhiye, Virendra; Jain, Narendra Kumar

doi:10.1016/j.ijpharm.2007.09.024

Cited by 97 publications

(58 citation statements)

References 48 publications

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“…15 Because folate receptors are overexpressed in tumor cells, folate is frequently conjugated with polymeric micelles for targeted drug delivery to improve the drug efficacy and safety of antitumor drugs. 16,17 It is very important to be able to observe drug absorption, and magnetic resonance imaging (MRI) contrast agents, in particular, superparamagnetic iron oxide nanoparticles (SPIONs), which can be readily detected by optical microscopy or electron microscopy, are often selected as a tracer.…”

Section: Introductionmentioning

confidence: 99%

Targeted therapy for human hepatic carcinoma cells using folate-functionalized polymeric micelles loaded with superparamagnetic iron oxide and sorafenib in vitro

Zhang¹,

Gong²,

Zhang³

et al. 2013

IJN

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Background:The purpose of this study was to evaluate the inhibitory effect of targeted folatefunctionalized micelles containing superparamagnetic iron oxide nanoparticles (SPIONs) and sorafenib on human hepatic carcinoma (HepG2) cells in vitro, and to observe the feasibility of surveillance of this targeting therapeutic effect by magnetic resonance imaging. Methods: Sorafenib and SPIONs were loaded into polymeric micelles. The targeted nanocarrier was synthesized by functionalizing the micelles with folate. Folate-free micelles loaded with sorafenib and SPIONs were used as control (nontargeted) micelles. Uptake of the nanocarrier by cells was assessed using Prussian blue staining after 1 hour of incubation with the polymeric micelles. The inhibitory effect of the targeted micelles on HepG2 cell proliferation at various concentrations of sorafenib was assessed in vitro using the methyl thiazolyl tetrazolium (MTT) assay and apoptotic analysis using flow cytometry. Magnetic resonance imaging using a clinical 1.5 T scanner was performed to detect changes in the signal intensity of cells after incubation with the targeted micelles. Results: Prussian blue staining showed significantly more intracellular SPIONs in cells incubated with the targeted micelles than those incubated with nontargeted micelles. The MTT assay showed that the average inhibitory ratio in the targeted group was significantly higher than that in the nontargeted group (38.13% versus 22.54%, P = 0.028). The mean apoptotic rate in the targeted cells, nontargeted cells, and untreated cells was 17.01%, 11.04%, and 7.89%, respectively. The apoptotic rate in the targeted cells was significantly higher than that in the nontargeted cells (P = 0.043). The T2 signal intensity on magnetic resonance imaging of cells treated with the targeted micelles decreased significantly with increasing concentrations of sorafenib in the cell culture medium, but there was no obvious decrease in signal intensity in cells treated with the nontargeted micelles. Conclusion: Folate-functionalized polymeric micelles loaded with SPIONs and sorafenib inhibited proliferation and induced apoptosis of HepG2 cells in vitro. The inhibitory events caused by targeted micelles can be monitored using clinical magnetic resonance.

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Section: Introductionmentioning

confidence: 99%

Targeted therapy for human hepatic carcinoma cells using folate-functionalized polymeric micelles loaded with superparamagnetic iron oxide and sorafenib in vitro

Zhang¹,

Gong²,

Zhang³

et al. 2013

IJN

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“…Tumor is a heterogenic, mutagenic architectural unit, a pathological state with properties which are still incompletely comprehended (Agarwal et al, 2008a;b). Targeting of anti-cancer bioactives at the tumor cells is desirable for two reasons: first, to maximize cytotoxic effect throughout the tumor growth phase during which the majority of the cells remains sensitive to pharmacotherapy and, secondly, to protect the surrounding healthy cells from exposure to the cytotoxic agents.…”

Section: Introductionmentioning

confidence: 99%

“…They offer suitability for industrial manufacture, and can be loaded with small molecules, proteins, or plasmid DNA with different specific methods (Peracchia et al, 1997;Zambaux et al, 2001;Panyam & Labhasetwar, 2003;Swayam & Labhasetwar, 2004). Nanoparticles also prolong drug release (Perez et al, 2001) and present the opportunity for multiple ligand coupling (Mohanraj & Chen, 2006;Agarwal et al, 2008a). These multiple ligand coupled polymeric nanoparticles can be exploited to accomplish both controlled drug release and tumor targeting .…”

Section: Introductionmentioning

confidence: 99%

Development and characterization of hyaluronic acid decorated PLGA nanoparticles for delivery of 5-fluorouracil

et al. 2010

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“…Using any of these ligands as targeting moieties offers a method for targeting the EGFR; especially TGF-and EGF as are the most commonly detected in humans. Ligand binding to EGFR results in activation of intracellular signaling cascades in cancer cell proliferation, apoptosis, migration, sensitivity to chemoradiation therapy, and tumor angiogenesis, and the complex is internalized for destruction and recycling [12,[62][63]. Over one-third of all solid tumors have been shown to express EGFR, and in many of these tumors, EGFR expression characterizes a more advanced disease stage [60].…”

Section: Human Epidermal Receptormentioning

confidence: 99%