Folate-conjugated polymer micelles for active targeting to cancer cells: preparation,<i>in vitro</i>evaluation of targeting ability and cytotoxicity

You, J. Q.; Li, Xin; Cui, Fu De; Du, Yong; Yuan, Hong; Hu, Fu Qiang

doi:10.1088/0957-4484/19/04/045102

Cited by 89 publications

(62 citation statements)

References 29 publications

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“…Polymer vehicles for doxorubicin may have the form of liposomes (Niu et al, 2010;Pakunlu et al, 2006;Rifkin et al, 2006) and polymeric micelles (Cuong et al, 2011;Gao et al, 2005;Kim et al, 2008;You et al, 2008). Nowadays there has been an enormous amount of research on the doxorubicin union with nanoparticulate carriers (Nawara et al, 2012;Du et al, 2011;Nowicka et al, 2009).…”

Section: Capacity For Antitumor Drug Vehiculization and Tumor Cell Elmentioning

confidence: 99%

“…7.10), cuya excelente utilidad terapéutica en muy diversos tumores está bien demostrada (Minotti et al, 2004). Debe mencionarse sin embargo que, como ocurre con otras antriciclinas, su uso presenta toxicidad cardíaca crónica, acumulativa y dependiente de la dosis, por lo que se han diseñado diversos tipos de métodos para su transporte y liberación, particularmente liposomas (Niu et al, 2010;Pakunlu et al, 2006;Rifkin et al, 2006), micelas poliméricas (Cuong et al, 2011;Gao et al, 2005;Kim et al, 2008;You et al, 2008) y nanopartículas portadoras (Nawara et al, 2012;Du et al, 2011;Nowicka et al, 2009). …”

Section: Aspectos Generalesunclassified

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Maghemite Functionalization for Antitumor Drug Vehiculization

2012

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In this paper we describe the preparation and characterization of magnetic nanocomposites designed for applications in targeted drug delivery. Combining superparamagnetic behavior with proper surface functionalization in a single entity makes it possible to have altogether controlled location and drug loading, and release capabilities. The colloidal vehicles consist of maghemite (γ-Fe2O3) cores surrounded by a gold shell through an intermediate silica coating. The external Au layer confers the particles a high degree of biocompatibility and reactive sites for the transported drug binding. In addition, it permits to take advantage of the strong optical resonance, making it easy to visualize the particles or even control their payload release through temperature changes. The results of the analysis of relaxivity demonstrate that these nanostructures can be used as T 2 contrast agents in magnetic resonance imaging (MRI), but the magnetic cores will be mainly useful in manipulating the particles using external magnetic fields. We describe how optical absorbance and electrokinetic data provide a followup of the progress of the nanostructure formation. Additionally, these techniques, together with confocal microscopy, are employed to demonstrate that the component nanoparticles are capable of loading significant amounts of the antitumor drug doxorubicin, very efficient in the chemotherapy of a wide range of tumors. Colon adenocarcinoma cells were used to test the in vitro release capabilities of the drug-loaded nanocomposites.

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Section: Capacity For Antitumor Drug Vehiculization and Tumor Cell Elmentioning

confidence: 99%

Section: Aspectos Generalesunclassified

Maghemite Functionalization for Antitumor Drug Vehiculization

2012

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“…We used three methods [25][26][27] to prepare HM-loaded micelles when the amount was fixed to 10 mg Lac-TPCS and 1 mg HM.…”

Section: Screening Of Different Methodsmentioning

confidence: 99%

Application of the central composite design to optimize the preparation of novel micelles of harmine

Bei¹,

Zhou²,

You³

et al. 2013

IJN

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Lactose-palmitoyl-trimethyl-chitosan (Lac-TPCS), a novel amphipathic self-assembled polymer, was synthesized for administration of insoluble drugs to reduce their adverse effects. The central composite design was used to study the preparation technique of harmine (HM)-loaded self-assembled micelles based on Lac-TPCS (Lac-TPCS/HM). Three preparation methods and single factors were screened, including solvent type, HM amount, hydration volume, and temperature. The optimal preparation technique was identified after investigating the influence of two independent factors, namely, HM amount and hydration volume, on four indexes, ie, encapsulation efficiency (EE), drug-loading amount (LD), particle size, and polydispersity index (PDI). Analysis of variance showed a high coefficient of determination of 0.916 to 0.994, thus ensuring a satisfactory adjustment of the predicted prescription. The maximum predicted values of the optimal prescription were 91.62%, 14.20%, 183.3 nm, and 0.214 for EE, LD, size, and PDI, respectively, when HM amount was 1.8 mg and hydration volume was 9.6 mL. HM-loaded micelles were successfully characterized by Fourier-transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction, and a fluorescencequenching experiment. Sustained release of Lac-TPCS/HM reached 65.3% in 72 hours at pH 7.4, while free HM released about 99.7% under the same conditions.

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“…ligand exchange reaction. Bio conjugation of CA/BMPA coated SPION with folic acid was done using the same procedures as You et al 29 Prussian blue staining To demonstrate Fe in the target cells (MCF-7, HepG2, A549), 5 × 10 4 cells were seeded on coverslips in twelve well culture plates and grown for 24 hours. Then the cells were incubated with FA-SPION and non-conjugated SPIONs with different concentrations of SPION (25-200 µg/mL).…”

Section: Synthesis Of Spionsmentioning

confidence: 99%

Cellular interaction of folic acid conjugated superparamagnetic iron oxide nanoparticles and its use as contrast agent for targeted magnetic imaging of tumor cells

Kumar¹,

Singh²,

Arora³

et al. 2012

IJN

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Abstract:The purpose of the study was to develop tumor specific, water dispersible superparamagnetic iron oxide nanoparticles (SPIONs) and evaluate their efficacy as a contrast agent in magnetic resonance imaging (MRI). We have developed SPIONs capped with citric acid/2-bromo-2-methylpropionic acid which are compact, water dispersible, biocompatible having narrow range of size dispersity (8-10 nm), and relatively high T 2 relaxivity). The targeting efficacy of unconjugated and folic acid-conjugated SPIONs (FA-SPIONS) was evaluated in a folic acid receptor overexpressing and negative tumor cell lines. Folic acid receptor-positive cells incubated with FA-SPIONs showed much higher intracellular iron content without any cytotoxicity. Ultrastructurally, SPIONs were seen as clustered inside the various stages of endocytic pathways without damaging cellular organelles and possible mechanism for their entry is via receptor mediated endocytosis. In vitro MRI studies on tumor cells showed better T 2 -weighted images in FA-SPIONs. These findings indicate that FA-SPIONs possess high colloidal stability with excellent sensitivity of imaging and can be a useful MRI contrast agent for the detection of cancer.

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Folate-conjugated polymer micelles for active targeting to cancer cells: preparation,in vitroevaluation of targeting ability and cytotoxicity

Cited by 89 publications

References 29 publications

Maghemite Functionalization for Antitumor Drug Vehiculization

Maghemite Functionalization for Antitumor Drug Vehiculization

Application of the central composite design to optimize the preparation of novel micelles of harmine

Cellular interaction of folic acid conjugated superparamagnetic iron oxide nanoparticles and its use as contrast agent for targeted magnetic imaging of tumor cells

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