2014
DOI: 10.1371/journal.pone.0097358
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Cellular Uptake and Antitumor Activity of DOX-hyd-PEG-FA Nanoparticles

Abstract: A PEG-based, folate mediated, active tumor targeting drug delivery system using DOX-hyd-PEG-FA nanoparticles (NPs) were prepared. DOX-hyd-PEG-FA NPs showed a significantly faster DOX release in pH 5.0 medium than in pH 7.4 medium. Compared with DOX-hyd-PEG NPs, DOX-hyd-PEG-FA NPs increased the intracellular accumulation of DOX and showed a DOX translocation from lysosomes to nucleus. The cytotoxicity of DOX-hyd-PEG-FA NPs on KB cells was much higher than that of free DOX, DOX-ami-PEG-FA NPs and DOX-hyd-PEG NPs… Show more

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Cited by 36 publications
(31 citation statements)
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“…Consistently, several drugs have conducted toward tumor tissues through various FA-conjugated NPs (Fig. 2) [8]. In here, we summarize the recent advances regarding the use of folateconjugated NPs in cancer therapy.…”
Section: Introductionmentioning
confidence: 65%
See 1 more Smart Citation
“…Consistently, several drugs have conducted toward tumor tissues through various FA-conjugated NPs (Fig. 2) [8]. In here, we summarize the recent advances regarding the use of folateconjugated NPs in cancer therapy.…”
Section: Introductionmentioning
confidence: 65%
“…As chitosan is soluble in acid condition, it can be applied for drug delivery in an acidic environment [141,8]. In addition to pH, degree of deacetylation, molecular weight, and ionic strength of the solution can potently affect the chitosan solubility [142].…”
Section: Chitosan Nanoparticlesmentioning
confidence: 99%
“…[36,65,66] For instance, Dox has been coupled to poly(ethylene glycol) (PEG)-folic acid conjugates to generate hydrophobically modified PEG derivatives that self-assembled into nanoparticles, which showed an enhanced Dox release at pH 5 as compared to pH 7.4. [10] Instead of using the hydrazone bond to couple the drug to a polymer carrier, this pH sensitive motif can also be used to connect the hydrophobic and hydrophilic segments of amphiphiles that are designed to self-assemble into poly mer micelles or nanoparticles. Cleaving the hydrazone bond in the endolysosomal compartments leads to dissociation of these nanoparticles and concomitant release of the entrapped drug.…”
Section: Functionality Examplesmentioning
confidence: 99%
“…[9] The decoration of nanoparticles, micelles, and linear polymers with folic acid (FA) has been shown to result in enhanced intracellular accumulation in folate positive cell lines as compared to the receptornegative cells. [9][10][11] The α v β 3 integrin is another receptor that is frequently targeted and exploited to enhance cellular internalization by decorating delivery systems with the arginine-glycine-aspartic acid tripeptide ligand. [12][13][14] A third example of a receptor that is exploited for tumor targeting is the epidermal growth factor receptor (EGFR), which is generally overexpressed and therefore used in the treatment of neck cancer, glioblastoma, and lung adenocarcinoma.…”
Section: Introductionmentioning
confidence: 99%
“…These properties have made FA one of the most popular ligands for targeted drug delivery. Actually, the unique properties of FA enable it to be near ideal vector for targeted liposomes, nanoparticles, quantum dots (Syu et al 2012;Ye et al 2014;Parveen and Sahoo 2010;Suriamoorthy et al 2010;Chattopadhyay et al 2013). This approach offers an opportunity to significantly enhance the efficacy of anticancer drugs.…”
Section: Introductionmentioning
confidence: 99%