A simple method to improve the stability of docetaxel micelles

Self-assembled polymeric micelles have been widely applied in drug delivery systems. In this study, we found that pH value of micellar system solution was the decisive factor of physical stability. Furthermore, the weak basic solution could maintain the solution clarification for a relative long tim...

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Veröffentlicht in:Scientific reports 2016-11, Vol.6 (1), p.36957, Article 36957
Hauptverfasser: Zhang, Lan, Tan, LiWei, Chen, LiJuan, Chen, XiaoXin, Long, ChaoFeng, Peng, JinRong, Qian, ZhiYong
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container_start_page 36957
container_title Scientific reports
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creator Zhang, Lan
Tan, LiWei
Chen, LiJuan
Chen, XiaoXin
Long, ChaoFeng
Peng, JinRong
Qian, ZhiYong
description Self-assembled polymeric micelles have been widely applied in drug delivery systems. In this study, we found that pH value of micellar system solution was the decisive factor of physical stability. Furthermore, the weak basic solution could maintain the solution clarification for a relative long time. To investigate the stability of polymeric micelles in different pH solutions, the micellar particle size and the docetaxel content remaining in solution were detected at predetermined time points. The crystallographic assay of freeze-drying powder was characterized by an X-ray diffractometer. In vitro release results indicated that the PBS had little influence on the sustained-release effect of docetaxel-loaded polymeric micelles (DPM). Besides, the safety of micellar formulation was determined by an MTT assay on HEK293 cells, and the anti-tumor activity was tested on MCF-7 cells. The results demonstrated that DPM adjusted with PBS (DPM (PBS)) was of low toxicity and maintained the effectiveness of docetaxel. In vivo antitumor results indicated that DPM (PBS) had better antitumor efficacy than common docetaxel injection (DTX). Thus it was concluded that regulation of micellar solution PH by PBS is a safe and effective method to improve the physical stability of DPM. It might promote the application of micellar formulation in clinical applications.
doi_str_mv 10.1038/srep36957
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In vivo antitumor results indicated that DPM (PBS) had better antitumor efficacy than common docetaxel injection (DTX). Thus it was concluded that regulation of micellar solution PH by PBS is a safe and effective method to improve the physical stability of DPM. 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subjects 140/131
631/154/152
692/308/153
Antitumor activity
Antitumor agents
Breast cancer
Clinical trials
Controlled release
Drug delivery
Drug delivery systems
Drugs
Freeze drying
Humanities and Social Sciences
Lung cancer
Micelles
multidisciplinary
Particle size
pH effects
Polymers
Powder
Science
Therapeutic applications
Toxicity
title A simple method to improve the stability of docetaxel micelles
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