The effect of monosialylganglioside mix modifying the PEGylated liposomal epirubicin on the accelerated blood clearance phenomenon

PEGylated liposomes are potential candidates to improve the pharmacokinetic characteristics of encapsulated drugs, to extend their circulation half-life and facilitate their passive accumulation at tumour sites. However, PEG-modified liposomes can induce accelerated blood clearance (ABC) upon repeat...

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Main Authors: Ting Zhang, Songlei Zhou, Le Kang, Xiang Luo, Yang Liu, Yanzhi Song, Xinrong Liu, Yihui Deng
Format: Article
Language:English
Published: Elsevier 2017-03-01
Series:Asian Journal of Pharmaceutical Sciences
Subjects:
Online Access:http://www.sciencedirect.com/science/article/pii/S1818087616300605
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author Ting Zhang
Songlei Zhou
Le Kang
Xiang Luo
Yang Liu
Yanzhi Song
Xinrong Liu
Yihui Deng
author_facet Ting Zhang
Songlei Zhou
Le Kang
Xiang Luo
Yang Liu
Yanzhi Song
Xinrong Liu
Yihui Deng
author_sort Ting Zhang
collection DOAJ
description PEGylated liposomes are potential candidates to improve the pharmacokinetic characteristics of encapsulated drugs, to extend their circulation half-life and facilitate their passive accumulation at tumour sites. However, PEG-modified liposomes can induce accelerated blood clearance (ABC) upon repeated administration, and the extent of ABC phenomenon on the cytotoxic drugs-containing PEGylated liposomes is related to the dose of the cytotoxic drugs. In this study, EPI served as a model cytotoxic drug, a hydrophilic surfactant molecule, monosialylganglioside (GM1) was chosen and modified on the liposomes together with PEG. It was shown that upon mixed modification, when GM1 contents reached 10% or 15% mol, the ABC phenomenon of the PEGylated liposomal EPI significantly reduced. We also found that GM1 played an important role in abrogating the ABC phenomenon in both the induction phase and the effectuation phase. The results suggested that GM1 incorporation unfortunately did not avoid occurrence of ABC phenomenon completely, but GM1 modification on PEGylated liposomes may provide a significant improvement in clinical practice of PEGylated liposomes. Further study must be necessary.
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spelling doaj.art-3173bb1578fe484e8a5867b69b0ce2632022-12-22T03:36:57ZengElsevierAsian Journal of Pharmaceutical Sciences1818-08762017-03-0112213414210.1016/j.ajps.2016.06.005The effect of monosialylganglioside mix modifying the PEGylated liposomal epirubicin on the accelerated blood clearance phenomenonTing ZhangSonglei ZhouLe KangXiang LuoYang LiuYanzhi SongXinrong LiuYihui DengPEGylated liposomes are potential candidates to improve the pharmacokinetic characteristics of encapsulated drugs, to extend their circulation half-life and facilitate their passive accumulation at tumour sites. However, PEG-modified liposomes can induce accelerated blood clearance (ABC) upon repeated administration, and the extent of ABC phenomenon on the cytotoxic drugs-containing PEGylated liposomes is related to the dose of the cytotoxic drugs. In this study, EPI served as a model cytotoxic drug, a hydrophilic surfactant molecule, monosialylganglioside (GM1) was chosen and modified on the liposomes together with PEG. It was shown that upon mixed modification, when GM1 contents reached 10% or 15% mol, the ABC phenomenon of the PEGylated liposomal EPI significantly reduced. We also found that GM1 played an important role in abrogating the ABC phenomenon in both the induction phase and the effectuation phase. The results suggested that GM1 incorporation unfortunately did not avoid occurrence of ABC phenomenon completely, but GM1 modification on PEGylated liposomes may provide a significant improvement in clinical practice of PEGylated liposomes. Further study must be necessary.http://www.sciencedirect.com/science/article/pii/S1818087616300605PEGylated liposomesEpirubicinMonosialylganglioside (GM1)Mixed modificationAccelerated blood clearance (ABC) phenomenon
spellingShingle Ting Zhang
Songlei Zhou
Le Kang
Xiang Luo
Yang Liu
Yanzhi Song
Xinrong Liu
Yihui Deng
The effect of monosialylganglioside mix modifying the PEGylated liposomal epirubicin on the accelerated blood clearance phenomenon
Asian Journal of Pharmaceutical Sciences
PEGylated liposomes
Epirubicin
Monosialylganglioside (GM1)
Mixed modification
Accelerated blood clearance (ABC) phenomenon
title The effect of monosialylganglioside mix modifying the PEGylated liposomal epirubicin on the accelerated blood clearance phenomenon
title_full The effect of monosialylganglioside mix modifying the PEGylated liposomal epirubicin on the accelerated blood clearance phenomenon
title_fullStr The effect of monosialylganglioside mix modifying the PEGylated liposomal epirubicin on the accelerated blood clearance phenomenon
title_full_unstemmed The effect of monosialylganglioside mix modifying the PEGylated liposomal epirubicin on the accelerated blood clearance phenomenon
title_short The effect of monosialylganglioside mix modifying the PEGylated liposomal epirubicin on the accelerated blood clearance phenomenon
title_sort effect of monosialylganglioside mix modifying the pegylated liposomal epirubicin on the accelerated blood clearance phenomenon
topic PEGylated liposomes
Epirubicin
Monosialylganglioside (GM1)
Mixed modification
Accelerated blood clearance (ABC) phenomenon
url http://www.sciencedirect.com/science/article/pii/S1818087616300605
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