pH-sensitive drug-delivery Systems for Tumor Targeting

He, Xi; Li, Jianfeng; An, Sai; Jiang, Chen

doi:10.4155/tde.13.120

Cited by 127 publications

(91 citation statements)

References 96 publications

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“…Therefore, pH-sensitive CPPs provide a strategy to overcome the non-specific shortcoming caused by traditional CPPs. The widely used pH-sensitive CPPs include GALA (a peptide composed of repeating sequences of Glu-Ala-Leu-Ala), histidine-containing peptides, pH low insertion peptide (pHLIP) and other pH-sensitive peptides (He et al, 2013).…”

Section: Introductionmentioning

confidence: 99%

A smart tumor targeting peptide–drug conjugate, pHLIP-SS-DOX: synthesis and cellular uptake on MCF-7 and MCF-7/Adr cells

et al. 2015

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Doxorubicin (DOX) is a potent anticancer drug for the treatment of tumors, but the poor specificity and multi-drug resistance (MDR) on tumor cells have restricted its application. Here, a pH and reduction-responsive peptide-drug conjugate (PDC), pHLIP-SS-DOX, was synthesized to overcome these drawbacks. pH low insertion peptide (pHLIP) is a cell penetrating peptide (CPP) with pH-dependent transmembrane ability. And because of the unique cell membrane insertion pattern, it might reverse the MDR. The cellular uptake study showed that on both drug-sensitive MCF-7 and drug-resistant MCF-7/Adr cells, pHLIP-SS-DOX obviously facilitated the uptake of DOX at pH 6.0 and the uptake level on MCF-7/Adr cells was similar with that on MCF-7 cells, indicating that pHLIP-SS-DOX had the ability to target acidic tumor cells and reverse MDR. In vitro cytotoxicity study mediated by GSH-OEt demonstrated that the cytotoxic effect of pHLIP-SS-DOX was reduction responsive, with obvious cytotoxicity at pH 6.0; while it had poor cytotoxicity at pH 7.4, no matter with or without GSH-OEt pretreatment. This illustrated that pHLIP could deliver DOX into tumor cells with acidic microenvironment specifically and could not deliver drugs into normal cells with neutral microenvironment. In summary, pHLIP-SS-DOX is a promising strategy to target drugs to tumors and provides a possibility to overcome MDR.

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Section: Introductionmentioning

confidence: 99%

A smart tumor targeting peptide–drug conjugate, pHLIP-SS-DOX: synthesis and cellular uptake on MCF-7 and MCF-7/Adr cells

et al. 2015

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“…Then, NPs broke down through degradation activated by secreted lysosomal proteinases and drugs escaped from lysosomes and were transferred into the cytoplasm ( Figure 1). [34][35][36][37] 5-fluorouracil (5-Fu) as a model drug was encapsulated into mAb GRP78-NPs for the drug loading and in vitro release studies. Furthermore, the cell uptake, in vitro cytotoxicity, and cellular apoptosis were investigated to prove the mAb GRP78-mediated tumor targeting ability of mAb GRP78-NPs.…”

mentioning

confidence: 99%

Nanoparticles inhibit cancer cell invasion and enhance antitumor efficiency by targeted drug delivery via cell surface-related GRP78

Zhao¹,

Li²,

Shi³

et al. 2014

IJN

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Nanoparticles (NPs) which target specific agents could effectively recognize the target cells and increase the stability of chemical agents by encapsulation. As such, NPs have been widely used in cancer treatment research. Recently, over 90% of treatment failure cases in patients with metastatic cancer were attributed to resistance to chemotherapy. Surface-exposed glucose-regulated protein of 78 kDa (GRP78) is expressed highly on many tumor cell surfaces in many human cancers and is related to the regulation of invasion and metastasis. Herein, we report that NPs conjugated with antibody against GRP78 (mAb GRP78-NPs) inhibit the adhesion, invasion, and metastasis of hepatocellular carcinoma (HCC) and promote drug delivery of 5-fluorouracil into GRP78 high-expressed human hepatocellular carcinoma cells. Our new findings suggest that mAb GRP78-NPs could enhance drug accumulation by effectively transporting NPs into cell surface GRP78-overexpressed human hepatocellular carcinoma cells and then inhibit cell proliferation and viability and induce cell apoptosis by regulating caspase-3. In brief, mAb GRP78-NPs effectively inhibit cancer cell invasion and enhance antitumor efficiency by targeted drug delivery.

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“…Although various drug-polymer conjugates involving pH-sensitive linkages have generally been used to release a drug in intracellular endosomes [13,14], the drug release kinetics from these hydrolysable delivery systems is difficult to adjust, with the system being either too liable or overly stable due to the small pH difference between normal tissues and pathological sites [15,16]. In contrast, a titratable polymer containing polycarboxylate or poly-L-histidine is preferable due to its pH-tuning and prompt response that can be produced by controlling the length of the titratable segment [16].…”

Section: Introductionmentioning

confidence: 99%

Dual-responsive mPEG-PLGA-PGlu hybrid-core nanoparticles with a high drug loading to reverse the multidrug resistance of breast cancer: An in vitro and in vivo evaluation

Yang

Cai

et al. 2015

Acta Biomaterialia

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pH-sensitive drug-delivery Systems for Tumor Targeting

Cited by 127 publications

References 96 publications

A smart tumor targeting peptide–drug conjugate, pHLIP-SS-DOX: synthesis and cellular uptake on MCF-7 and MCF-7/Adr cells

A smart tumor targeting peptide–drug conjugate, pHLIP-SS-DOX: synthesis and cellular uptake on MCF-7 and MCF-7/Adr cells

Nanoparticles inhibit cancer cell invasion and enhance antitumor efficiency by targeted drug delivery via cell surface-related GRP78

Dual-responsive mPEG-PLGA-PGlu hybrid-core nanoparticles with a high drug loading to reverse the multidrug resistance of breast cancer: An in vitro and in vivo evaluation

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