Synthesis and in vitro evaluation of a pH-sensitive PLA–PEG–folate based polymeric micelle for controlled delivery of docetaxel

Hami, Zahra; Amini, Mohsen; Ghazi‐Khansari, Mahmoud; Rezayat, Seyed Mehdi; Gilani, Kambiz

doi:10.1016/j.colsurfb.2014.01.015

Cited by 62 publications

(43 citation statements)

References 31 publications

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“…The obvious fluorescence images were found after the cells were incubated with FITC/TS-CS-PEG-FA micelles in 2 h. From Figure 3, the rapid cell internalization ability of TS-CS-EG-FA was clearly visible compared to TS-CS micelles. This result was consistent with previously published reports Hami, 2014). Furthermore to evaluate the cellular uptake of the micelles quantitatively, the fluorescence intensity was measured after the cells were incubated with FITC/ CS-TS and FITC/TS-CS-PEG-FA for different time.…”

Section: In Vitro Cellular Uptake Of Targeted and Non-targeted Micellessupporting

confidence: 80%

In vivopharmacokinetics, biodistribution and anti-tumor effect of paclitaxel-loaded targeted chitosan-based polymeric micelle

Rezazadeh¹,

Emami²,

Hasanzadeh³

et al. 2014

Drug Delivery

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A water-insoluble anti-tumor agent, paclitaxel (PTX) was successfully incorporated into noveltargeted polymeric micelles based on tocopherol succinate-chitosan-polyethylene glycol-folic acid (PTX/TS-CS-PEG-FA). The aim of the present study was to evaluate the pharmacokinetics, tissue distribution and efficacy of PTX/TS-CS-PEG-FA in comparison to Anzatax Õ in tumor bearing mice. The micellar formulation showed higher in vitro cytotoxicity against mice breast cancer cell line, 4T1, due to the folate receptor-mediated endocytosis. The IC 50 value of PTX, a concentration at which 50% cells are killed, was 1.17 and 0.93 mM for Anzatax Õ and PTX/TS-CS-PEG-FA micelles, respectively. The in vivo anti-tumor efficacy of PTX/TS-CS-PEG-FA, as measured by reduction in tumor volume of 4T1 mouse breast cancer injected in Balb/c mice was significantly greater than that of Anzatax Õ . Pharmacokinetic study in tumor bearing mice revealed that the micellar formulation prolonged the systemic circulation time of PTX and the AUC of PTX/TS-CS-PEG-FA was obtained 0.83-fold lower than Anzatax Õ . Compared with Anzatax Õ , the V d , T 1/2ß and MRT of PTX/TS-CS-PEG-FA was increased by 2.76, 2.05 and 1.68-fold, respectively. As demonstrated by tissue distribution, the PTX/TS-CS-PEG-FA micelles increased accumulation of PTX in tumor, therefore, resulted in anti-tumor effects enhancement and drug concentration in the normal tissues reduction. Taken together, our evaluations show that PTX/TS-CS-PEG-FA micelle is a potential drug delivery system of PTX for the effective treatment of the tumor and systematic toxicity reduction, thus, the micellar formulation can provide a useful alternative dosage form for intravenous administration of PTX. KeywordsBiodistribution, in vivo anti-tumor effect, Paclitaxel, pharmacokinetics, targeted polymeric micelle History

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Section: In Vitro Cellular Uptake Of Targeted and Non-targeted Micellessupporting

confidence: 80%

In vivopharmacokinetics, biodistribution and anti-tumor effect of paclitaxel-loaded targeted chitosan-based polymeric micelle

Rezazadeh¹,

Emami²,

Hasanzadeh³

et al. 2014

Drug Delivery

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show abstract

“…Similar phenomenon was observed in the hydrazide-aldehyde crosslinking system in the literature (Oommen et al, 2013). The degradation products of LEV-PEG-LEV are biocompatible PEG and LEV (Hami, Amini, Khansan, Rezayat, & Gilani, 2014). 3.6.…”

Section: Degradation Behaviorsupporting

confidence: 74%

Hyaluronic acid hydrogel scaffolds with a triple degradation behavior for bone tissue engineering

Cui

Qian

Liu

et al. 2015

Carbohydrate Polymers

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“…The self-assembling and targeting behaviors of FA-F87-PLA copolymer in aqueous solutions were examined. To our knowledge, there are only few reports regarding the synthesis of similar block copolymers FA-poly(ethylene oxide)-PLA (FA-PEO-PLA) and no study at all on the synthesis of FA-F87-PLA [20,24,25]. It was reported that poly(ethylene imine)-Pluronic (PEI-Pluronic) block copolymer exhibited higher transfection efficiency toward plasmid DNA than PEI-PEO copolymer due to the amphiphilic property of Pluronic block copolymer [26].…”

Section: Introductionmentioning

confidence: 97%

“…One of the most interesting molecules for targeting polymeric nanoparticle systems to tumor cells is folic acid (FA) because FA has many advantages including non-immunogenicity, small size, low molecular weight and stability. Furthermore, folic acid binds to the folate receptor, which is over-expressed in some cancer cells including ovary, breast, brain and other human tumors and has little expression in normal tissues [20][21][22][23].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, drug release and targeting behaviors of Novel Folated Pluronic F87/poly(lactic acid) block copolymer

Xiong

Qin

et al. 2015

European Polymer Journal

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Synthesis and in vitro evaluation of a pH-sensitive PLA–PEG–folate based polymeric micelle for controlled delivery of docetaxel

Cited by 62 publications

References 31 publications

In vivopharmacokinetics, biodistribution and anti-tumor effect of paclitaxel-loaded targeted chitosan-based polymeric micelle

In vivopharmacokinetics, biodistribution and anti-tumor effect of paclitaxel-loaded targeted chitosan-based polymeric micelle

Hyaluronic acid hydrogel scaffolds with a triple degradation behavior for bone tissue engineering

Synthesis, drug release and targeting behaviors of Novel Folated Pluronic F87/poly(lactic acid) block copolymer

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