Preparation, Characterization, and in vivo Evaluation of NK4-Conjugated Hydroxycamptothecin-Loaded Liposomes
Ting Zhou,1,* Wei Zhang,1,* Dongliang Cheng,1 Xin Tang,2 Jianfang Feng,3 Wei Wu1 1School of Pharmacy, Guilin Medical University, Guilin 541004, People’s Republic of China; 2School of Public Health, Guilin Medical University, Guilin 541004, People’s Republic of China; 3School of P...
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2020
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oai:doaj.org-article:05200d844a36465fac563a01f93168722021-12-02T08:48:08ZPreparation, Characterization, and in vivo Evaluation of NK4-Conjugated Hydroxycamptothecin-Loaded Liposomes1178-2013https://doaj.org/article/05200d844a36465fac563a01f93168722020-03-01T00:00:00Zhttps://www.dovepress.com/preparation-characterization-and-in-vivo-evaluation-of-nk4-conjugated--peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Ting Zhou,1,* Wei Zhang,1,* Dongliang Cheng,1 Xin Tang,2 Jianfang Feng,3 Wei Wu1 1School of Pharmacy, Guilin Medical University, Guilin 541004, People’s Republic of China; 2School of Public Health, Guilin Medical University, Guilin 541004, People’s Republic of China; 3School of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530200, People’s Republic of China*These authors contributed equally to this workCorrespondence: Wei WuSchool of Pharmacy, Guilin Medical University, 109 North 2nd Huancheng Road, Guilin 541004, People’s Republic of ChinaEmail wuwei@glmc.edu.cnJianfang FengSchool of Pharmacy, Guangxi University of Chinese Medicine, 13 Wuhe Avenue, Nanning 530200, People’s Republic of ChinaEmail fengjianfang@vip.163.comPurpose: In this study, NK4-conjugated hydroxycamptothecin liposomes (NK4-HCPT-Lips) were prepared with the aim of improving drug targeting to the liver.Methods: NK4-HCPT-Lips were prepared using the thin-film dispersion method. In vitro antitumor activities were evaluated by MTT assay. HCPT levels in plasma and tissues were determined via high-performance liquid chromatography (HPLC) with camptothecin as the internal standard, and the characteristics, pharmacokinetics, and bio-distribution of NK4-HCPT-Lips were evaluated.Results: The liposomes showed a regular spherical-shaped morphology, and the entrapment efficiency and drug loading capacity reached 82.5 ± 2.4% and 3.01 ± 0.23%, respectively, with a particle size of 155.6 ± 2.6 nm and a zeta potential of − 24.8 ± 3.3 mV. Inhibition effect experiments found that NK4-HCPT-Lips had a good inhibition on the HepG2 cells. Pharmacokinetic studies revealed an increase in the area under the curve and mean residence time as well as a decrease in plasma clearance (p < 0.05) of the NK4-HCPT-Lips compared to those of HCPT liposomes and a commercial HCPT injection. Tissue distribution studies showed that NK4-HCPT-Lips were present at high levels in the liver but were cleared from the kidneys.Conclusion: These results demonstrate that NK4-HCPT-Lips possess excellent liver-targeting attributes, which could enhance the therapeutic effects of drug treatments for hepatic diseases.Keywords: hydroxycamptothecin, NK4, liposomes, pharmacokinetics, bio-distributionZhou TZhang WCheng DTang XFeng JWu WDove Medical Pressarticlehydroxycamptothecinnk4liposomespharmacokineticsbio-distributionMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 15, Pp 2277-2286 (2020) |
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hydroxycamptothecin nk4 liposomes pharmacokinetics bio-distribution Medicine (General) R5-920 |
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hydroxycamptothecin nk4 liposomes pharmacokinetics bio-distribution Medicine (General) R5-920 Zhou T Zhang W Cheng D Tang X Feng J Wu W Preparation, Characterization, and in vivo Evaluation of NK4-Conjugated Hydroxycamptothecin-Loaded Liposomes |
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Ting Zhou,1,* Wei Zhang,1,* Dongliang Cheng,1 Xin Tang,2 Jianfang Feng,3 Wei Wu1 1School of Pharmacy, Guilin Medical University, Guilin 541004, People’s Republic of China; 2School of Public Health, Guilin Medical University, Guilin 541004, People’s Republic of China; 3School of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530200, People’s Republic of China*These authors contributed equally to this workCorrespondence: Wei WuSchool of Pharmacy, Guilin Medical University, 109 North 2nd Huancheng Road, Guilin 541004, People’s Republic of ChinaEmail wuwei@glmc.edu.cnJianfang FengSchool of Pharmacy, Guangxi University of Chinese Medicine, 13 Wuhe Avenue, Nanning 530200, People’s Republic of ChinaEmail fengjianfang@vip.163.comPurpose: In this study, NK4-conjugated hydroxycamptothecin liposomes (NK4-HCPT-Lips) were prepared with the aim of improving drug targeting to the liver.Methods: NK4-HCPT-Lips were prepared using the thin-film dispersion method. In vitro antitumor activities were evaluated by MTT assay. HCPT levels in plasma and tissues were determined via high-performance liquid chromatography (HPLC) with camptothecin as the internal standard, and the characteristics, pharmacokinetics, and bio-distribution of NK4-HCPT-Lips were evaluated.Results: The liposomes showed a regular spherical-shaped morphology, and the entrapment efficiency and drug loading capacity reached 82.5 ± 2.4% and 3.01 ± 0.23%, respectively, with a particle size of 155.6 ± 2.6 nm and a zeta potential of − 24.8 ± 3.3 mV. Inhibition effect experiments found that NK4-HCPT-Lips had a good inhibition on the HepG2 cells. Pharmacokinetic studies revealed an increase in the area under the curve and mean residence time as well as a decrease in plasma clearance (p < 0.05) of the NK4-HCPT-Lips compared to those of HCPT liposomes and a commercial HCPT injection. Tissue distribution studies showed that NK4-HCPT-Lips were present at high levels in the liver but were cleared from the kidneys.Conclusion: These results demonstrate that NK4-HCPT-Lips possess excellent liver-targeting attributes, which could enhance the therapeutic effects of drug treatments for hepatic diseases.Keywords: hydroxycamptothecin, NK4, liposomes, pharmacokinetics, bio-distribution |
format |
article |
author |
Zhou T Zhang W Cheng D Tang X Feng J Wu W |
author_facet |
Zhou T Zhang W Cheng D Tang X Feng J Wu W |
author_sort |
Zhou T |
title |
Preparation, Characterization, and in vivo Evaluation of NK4-Conjugated Hydroxycamptothecin-Loaded Liposomes |
title_short |
Preparation, Characterization, and in vivo Evaluation of NK4-Conjugated Hydroxycamptothecin-Loaded Liposomes |
title_full |
Preparation, Characterization, and in vivo Evaluation of NK4-Conjugated Hydroxycamptothecin-Loaded Liposomes |
title_fullStr |
Preparation, Characterization, and in vivo Evaluation of NK4-Conjugated Hydroxycamptothecin-Loaded Liposomes |
title_full_unstemmed |
Preparation, Characterization, and in vivo Evaluation of NK4-Conjugated Hydroxycamptothecin-Loaded Liposomes |
title_sort |
preparation, characterization, and in vivo evaluation of nk4-conjugated hydroxycamptothecin-loaded liposomes |
publisher |
Dove Medical Press |
publishDate |
2020 |
url |
https://doaj.org/article/05200d844a36465fac563a01f9316872 |
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