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

The Poly (ethylene glycol) methyl ether-block-poly (lactide-co-glycolide) (mPEG-PLGA) 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 en...

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Main Authors: Wang, Qi, Wei, Na, Liu, Xiaofeng, Luo, Kathy Qian
Other Authors: School of Chemical and Biomedical Engineering
Format: Article
Language:English
Published: 2018
Online Access:https://hdl.handle.net/10356/88491
http://hdl.handle.net/10220/44625
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Institution: Nanyang Technological University
Language: English
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spelling sg-ntu-dr.10356-884912023-12-29T06:51:57Z 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 Wang, Qi Wei, Na Liu, Xiaofeng Luo, Kathy Qian School of Chemical and Biomedical Engineering The Poly (ethylene glycol) methyl ether-block-poly (lactide-co-glycolide) (mPEG-PLGA) 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. Published version 2018-03-27T08:00:49Z 2019-12-06T17:04:26Z 2018-03-27T08:00:49Z 2019-12-06T17:04:26Z 2017 Journal Article Wang, Q., Wei, N., Liu, X., & Luo, K. Q. (2017). 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. Oncotarget, 8(7), 12013-12030. https://hdl.handle.net/10356/88491 http://hdl.handle.net/10220/44625 10.18632/oncotarget.14481 en Oncotarget © 2017 The Author(s) (published by Impact Journals). This paper is licensed under a Creative Commons Attribution 3.0 License. This paper was published in Oncotarget and is made available as an electronic reprint (preprint) with permission of The Author(s) (published by Impact Journals). The published version is available at: [http://dx.doi.org/10.18632/oncotarget.14481]. One print or electronic copy may be made for personal use only. Systematic or multiple reproduction, distribution to multiple locations via electronic or other means, duplication of any material in this paper for a fee or for commercial purposes, or modification of the content of the paper is prohibited and is subject to penalties under law. 18 p. application/pdf
institution Nanyang Technological University
building NTU Library
continent Asia
country Singapore
Singapore
content_provider NTU Library
collection DR-NTU
language English
description The Poly (ethylene glycol) methyl ether-block-poly (lactide-co-glycolide) (mPEG-PLGA) 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.
author2 School of Chemical and Biomedical Engineering
author_facet School of Chemical and Biomedical Engineering
Wang, Qi
Wei, Na
Liu, Xiaofeng
Luo, Kathy Qian
format Article
author Wang, Qi
Wei, Na
Liu, Xiaofeng
Luo, Kathy Qian
spellingShingle Wang, Qi
Wei, Na
Liu, Xiaofeng
Luo, Kathy Qian
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
author_sort Wang, Qi
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
title_short 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
title_full 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
title_fullStr 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
title_full_unstemmed 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
title_sort 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
publishDate 2018
url https://hdl.handle.net/10356/88491
http://hdl.handle.net/10220/44625
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