Paclitaxel prodrug based mixed micelles for tumor-targeted chemotherapy

An effective chemotherapy is usually subject to an insufficient loading of hydrophobic drugs as well as severe side effects. In order to address these dilemmas in one formulation, we herein construct paclitaxel prodrug based mixed micelles (MMs) for tumor-targeted chemotherapy. The paclitaxel prodru...

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Published inRSC advances Vol. 8; no. 1; pp. 38 - 389
Main Authors Tang, Dongyang, Zhao, Xin, Yang, Tie, Wang, Cheng
Format Journal Article
LanguageEnglish
Published Cambridge Royal Society of Chemistry 02.01.2018
Subjects
adverse effects
Anticancer properties
Biocompatibility
Chemotherapy
cytotoxicity
drug therapy
drugs
endocytosis
Fluorescence
Fluoroscopic imaging
hemolysis
hydrophilicity
hydrophobicity
image analysis
Micelles
nanoparticles
neoplasms
paclitaxel
Polyethylene glycol
Side effects
Taxol
Toxicity
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Abstract An effective chemotherapy is usually subject to an insufficient loading of hydrophobic drugs as well as severe side effects. In order to address these dilemmas in one formulation, we herein construct paclitaxel prodrug based mixed micelles (MMs) for tumor-targeted chemotherapy. The paclitaxel prodrug containing a hydrophobic PTX and a hydrophilic PEG chain can self-assemble into uniform MMs with distearoyl phosphoethanolamine-polyethylene glycol-folate (DSPE-PEG-FA). The resultant MMs with preferable stability and hemolysis compatibility could improve the cellular uptake of nanoparticles via FA receptor-mediated endocytosis as compared to the single micelles (SMs). This tumor targetability was also confirmed in vivo by fluorescent imaging. MMs with a stable drug loading as well as tumor targetability displayed elevated in vitro cytotoxicity and in vivo antitumor efficacy compared with Taxol, which could be a potential formulation for cancer therapy. Paclitaxel prodrug based mixed micelles with high drug loading and tumor targeting capacity for elevated chemotherapy.
AbstractList An effective chemotherapy is usually subject to an insufficient loading of hydrophobic drugs as well as severe side effects. In order to address these dilemmas in one formulation, we herein construct paclitaxel prodrug based mixed micelles (MMs) for tumor-targeted chemotherapy. The paclitaxel prodrug containing a hydrophobic PTX and a hydrophilic PEG chain can self-assemble into uniform MMs with distearoyl phosphoethanolamine–polyethylene glycol–folate (DSPE–PEG–FA). The resultant MMs with preferable stability and hemolysis compatibility could improve the cellular uptake of nanoparticles via FA receptor-mediated endocytosis as compared to the single micelles (SMs). This tumor targetability was also confirmed in vivo by fluorescent imaging. MMs with a stable drug loading as well as tumor targetability displayed elevated in vitro cytotoxicity and in vivo antitumor efficacy compared with Taxol, which could be a potential formulation for cancer therapy.
An effective chemotherapy is usually subject to an insufficient loading of hydrophobic drugs as well as severe side effects. In order to address these dilemmas in one formulation, we herein construct paclitaxel prodrug based mixed micelles (MMs) for tumor-targeted chemotherapy. The paclitaxel prodrug containing a hydrophobic PTX and a hydrophilic PEG chain can self-assemble into uniform MMs with distearoyl phosphoethanolamine–polyethylene glycol–folate (DSPE–PEG–FA). The resultant MMs with preferable stability and hemolysis compatibility could improve the cellular uptake of nanoparticles via FA receptor-mediated endocytosis as compared to the single micelles (SMs). This tumor targetability was also confirmed in vivo by fluorescent imaging. MMs with a stable drug loading as well as tumor targetability displayed elevated in vitro cytotoxicity and in vivo antitumor efficacy compared with Taxol, which could be a potential formulation for cancer therapy.
An effective chemotherapy is usually subject to an insufficient loading of hydrophobic drugs as well as severe side effects. In order to address these dilemmas in one formulation, we herein construct paclitaxel prodrug based mixed micelles (MMs) for tumor-targeted chemotherapy. The paclitaxel prodrug containing a hydrophobic PTX and a hydrophilic PEG chain can self-assemble into uniform MMs with distearoyl phosphoethanolamine-polyethylene glycol-folate (DSPE-PEG-FA). The resultant MMs with preferable stability and hemolysis compatibility could improve the cellular uptake of nanoparticles via FA receptor-mediated endocytosis as compared to the single micelles (SMs). This tumor targetability was also confirmed in vivo by fluorescent imaging. MMs with a stable drug loading as well as tumor targetability displayed elevated in vitro cytotoxicity and in vivo antitumor efficacy compared with Taxol, which could be a potential formulation for cancer therapy. Paclitaxel prodrug based mixed micelles with high drug loading and tumor targeting capacity for elevated chemotherapy.
Author Tang, Dongyang
Wang, Cheng
Yang, Tie
Zhao, Xin
AuthorAffiliation Henan Institute of Science and Technology
Department of Experimental Center
Department of Pharmacy
Nanjing Research Center
Jiangsu Chiatai Tianqing Pharmaceutical Co. Ltd
College of Pharmaceutical Sciences
Xinxiang Central Hospital
Zhejiang University
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Snippet An effective chemotherapy is usually subject to an insufficient loading of hydrophobic drugs as well as severe side effects. In order to address these dilemmas...
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SubjectTerms adverse effects
Anticancer properties
Biocompatibility
Chemotherapy
cytotoxicity
drug therapy
drugs
endocytosis
Fluorescence
Fluoroscopic imaging
hemolysis
hydrophilicity
hydrophobicity
image analysis
Micelles
nanoparticles
neoplasms
paclitaxel
Polyethylene glycol
Side effects
Taxol
Toxicity
Title Paclitaxel prodrug based mixed micelles for tumor-targeted chemotherapy
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