Enhancement of the bioavailability of a novel anticancer compound (acetyltanshinone IIA) by encapsulation within mPEG-PLGA nanoparticles: A study of formulation optimization, toxicity, and pharmacokinetics

Qi Wang; Na Wei; Xiaofeng Liu; Alex Chang; Kathy Qian Luo

doi:10.18632/oncotarget.14481

Enhancement of the bioavailability of a novel anticancer compound (acetyltanshinone IIA) by encapsulation within mPEG-PLGA nanoparticles: A study of formulation optimization, toxicity, and pharmacokinetics

Qi Wang, Na Wei, Xiaofeng Liu, Alex Chang, Kathy Qian Luo

School of Medicine

Research output: Contribution to journal › Article › peer-review

9 Scopus citations

Abstract

The Poly (ethylene glycol) methyl ether-block-poly (lactide-co-glycolide) (mPEGPLGA) nanoparticles carrying acetyltanshinone IIA (ATA), a novel anti-breast cancer agent, were prepared by ultrasonic emulsion method to enhance the bioavailability and reduce the toxicity. Systematic optimization of encapsulation process was achieved using an orthogonal design. Drug efficacy analysis showed that ATA nanoparticles were as effective as free ATA against estrogen receptor positive breast cancer cells, but much less toxic towards human endothelial cells. Furthermore, in zebrafish, ATA nanoparticles displayed much lower toxicity than free ATA. More importantly, the blood concentration of ATA nanoparticles indicated by 24 hour-area under the curve (AUC_0-24h) was 10 times higher than free ATA. These results indicated the potential of ATA-loaded mPEG-PLGA nanoparticles for the delivery of ATA in a clinical formulation, and their potential for use in tumor therapy in the future.

Original language	English (US)
Pages (from-to)	12013-12030
Number of pages	18
Journal	Oncotarget
Volume	8
Issue number	7
DOIs	https://doi.org/10.18632/oncotarget.14481
State	Published - 2017

Keywords

Acetyltanshinone IIA
Anticancer drugs
Bioavailability
MPEG-PLGA
Pharmacokinetics
Toxicity

ASJC Scopus subject areas

Oncology

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title = "Enhancement of the bioavailability of a novel anticancer compound (acetyltanshinone IIA) by encapsulation within mPEG-PLGA nanoparticles: A study of formulation optimization, toxicity, and pharmacokinetics",

abstract = "The Poly (ethylene glycol) methyl ether-block-poly (lactide-co-glycolide) (mPEGPLGA) nanoparticles carrying acetyltanshinone IIA (ATA), a novel anti-breast cancer agent, were prepared by ultrasonic emulsion method to enhance the bioavailability and reduce the toxicity. Systematic optimization of encapsulation process was achieved using an orthogonal design. Drug efficacy analysis showed that ATA nanoparticles were as effective as free ATA against estrogen receptor positive breast cancer cells, but much less toxic towards human endothelial cells. Furthermore, in zebrafish, ATA nanoparticles displayed much lower toxicity than free ATA. More importantly, the blood concentration of ATA nanoparticles indicated by 24 hour-area under the curve (AUC0-24h) was 10 times higher than free ATA. These results indicated the potential of ATA-loaded mPEG-PLGA nanoparticles for the delivery of ATA in a clinical formulation, and their potential for use in tumor therapy in the future.",

keywords = "Acetyltanshinone IIA, Anticancer drugs, Bioavailability, MPEG-PLGA, Pharmacokinetics, Toxicity",

author = "Qi Wang and Na Wei and Xiaofeng Liu and Alex Chang and Luo, {Kathy Qian}",

note = "Funding Information: We would like to thank To Sing Fung for his careful editing and proofreading of the manuscript. This study was supported by the grant from Johns Hopkins Singapore Research Fund awarded to Kathy Qian Luo, the Start-Up Fund from the Faculty of Health Sciences, and the Start-Up Research Grant (SRG2016-00068-FHS) from the University of Macau.",

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AU - Liu, Xiaofeng

AU - Chang, Alex

AU - Luo, Kathy Qian

N1 - Funding Information: We would like to thank To Sing Fung for his careful editing and proofreading of the manuscript. This study was supported by the grant from Johns Hopkins Singapore Research Fund awarded to Kathy Qian Luo, the Start-Up Fund from the Faculty of Health Sciences, and the Start-Up Research Grant (SRG2016-00068-FHS) from the University of Macau.

PY - 2017

Y1 - 2017

N2 - The Poly (ethylene glycol) methyl ether-block-poly (lactide-co-glycolide) (mPEGPLGA) nanoparticles carrying acetyltanshinone IIA (ATA), a novel anti-breast cancer agent, were prepared by ultrasonic emulsion method to enhance the bioavailability and reduce the toxicity. Systematic optimization of encapsulation process was achieved using an orthogonal design. Drug efficacy analysis showed that ATA nanoparticles were as effective as free ATA against estrogen receptor positive breast cancer cells, but much less toxic towards human endothelial cells. Furthermore, in zebrafish, ATA nanoparticles displayed much lower toxicity than free ATA. More importantly, the blood concentration of ATA nanoparticles indicated by 24 hour-area under the curve (AUC0-24h) was 10 times higher than free ATA. These results indicated the potential of ATA-loaded mPEG-PLGA nanoparticles for the delivery of ATA in a clinical formulation, and their potential for use in tumor therapy in the future.

AB - The Poly (ethylene glycol) methyl ether-block-poly (lactide-co-glycolide) (mPEGPLGA) nanoparticles carrying acetyltanshinone IIA (ATA), a novel anti-breast cancer agent, were prepared by ultrasonic emulsion method to enhance the bioavailability and reduce the toxicity. Systematic optimization of encapsulation process was achieved using an orthogonal design. Drug efficacy analysis showed that ATA nanoparticles were as effective as free ATA against estrogen receptor positive breast cancer cells, but much less toxic towards human endothelial cells. Furthermore, in zebrafish, ATA nanoparticles displayed much lower toxicity than free ATA. More importantly, the blood concentration of ATA nanoparticles indicated by 24 hour-area under the curve (AUC0-24h) was 10 times higher than free ATA. These results indicated the potential of ATA-loaded mPEG-PLGA nanoparticles for the delivery of ATA in a clinical formulation, and their potential for use in tumor therapy in the future.

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Enhancement of the bioavailability of a novel anticancer compound (acetyltanshinone IIA) by encapsulation within mPEG-PLGA nanoparticles: A study of formulation optimization, toxicity, and pharmacokinetics

Abstract

Keywords

ASJC Scopus subject areas

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