Preparation of ginsenoside compound-K mixed micelles with improved retention and antitumor efficacy

Xin Jin, Qing Yang, Ning Cai Department of Hospital Pharmacy, Suqian Branch Jiangsu Province Hospital, Suqian 223800, China Introduction: Ginsenoside compound K (CK) has effects on cell-cycle regulation, tumor growth inhibition, and apoptosis induction. However, it has limited applications in clin...

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Autores principales: Jin X, Yang Q, Cai N
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Publicado: Dove Medical Press 2018
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spelling oai:doaj.org-article:446225aee97f427eb3d414cd6ff78f0d2021-12-02T10:38:05ZPreparation of ginsenoside compound-K mixed micelles with improved retention and antitumor efficacy1178-2013https://doaj.org/article/446225aee97f427eb3d414cd6ff78f0d2018-07-01T00:00:00Zhttps://www.dovepress.com/preparation-of-ginsenoside-compound-k-mixed-micelles-with-improved-ret-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Xin Jin, Qing Yang, Ning Cai Department of Hospital Pharmacy, Suqian Branch Jiangsu Province Hospital, Suqian 223800, China Introduction: Ginsenoside compound K (CK) has effects on cell-cycle regulation, tumor growth inhibition, and apoptosis induction. However, it has limited applications in clinical settings because of its low solubility and poor absorption. Methods: To overcome these limitations, we aimed to develop a mixed micellar system composed of phosphatidylcholine (PC) and 1,2-distearoyl-sn-glycero-3-phosphoethanolamine polyethylene glycol 2000 (DSPE PEG 2000; DP). CK encapsulated in PC/DP mixed micelles had enhanced solubility, permeability, and retention effects. Results: Compared to free CK, the CK PC/DP micellar system exhibited improved anticancer effects in vitro, including cell-cycle arrest, apoptosis, and anti-invasion in human lung carcinoma A549 cells. The significant proapoptotic effect was reflected by increased chromosomal condensation, annexin V/propidium iodide staining, and related protein expression. In vitro cellular uptake and optical mouse imaging in vivo suggested that the improved antitumor effect was caused primarily by enhanced uptake and tumor targeting. Furthermore, an in vivo antitumor efficacy study indicated that the CK mixed micelles significantly inhibited tumor growth, thereby decreasing tumor volume at the end of the experiment as compared with that in the control mice. Histological analysis confirmed the antitumor effect with low toxicity. Conclusion: The PC/DP micellar system was an effective drug delivery system for CK in tumor therapy. Keywords: mixed micellar system, ginsenoside compound-K, targeted effect, antitumor, lung cancerJin XYang QCai NDove Medical Pressarticlemixed micellar systemginsenoside compound-Ktargeted effectantitumorlung cancerMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 13, Pp 3827-3838 (2018)
institution DOAJ
collection DOAJ
language EN
topic mixed micellar system
ginsenoside compound-K
targeted effect
antitumor
lung cancer
Medicine (General)
R5-920
spellingShingle mixed micellar system
ginsenoside compound-K
targeted effect
antitumor
lung cancer
Medicine (General)
R5-920
Jin X
Yang Q
Cai N
Preparation of ginsenoside compound-K mixed micelles with improved retention and antitumor efficacy
description Xin Jin, Qing Yang, Ning Cai Department of Hospital Pharmacy, Suqian Branch Jiangsu Province Hospital, Suqian 223800, China Introduction: Ginsenoside compound K (CK) has effects on cell-cycle regulation, tumor growth inhibition, and apoptosis induction. However, it has limited applications in clinical settings because of its low solubility and poor absorption. Methods: To overcome these limitations, we aimed to develop a mixed micellar system composed of phosphatidylcholine (PC) and 1,2-distearoyl-sn-glycero-3-phosphoethanolamine polyethylene glycol 2000 (DSPE PEG 2000; DP). CK encapsulated in PC/DP mixed micelles had enhanced solubility, permeability, and retention effects. Results: Compared to free CK, the CK PC/DP micellar system exhibited improved anticancer effects in vitro, including cell-cycle arrest, apoptosis, and anti-invasion in human lung carcinoma A549 cells. The significant proapoptotic effect was reflected by increased chromosomal condensation, annexin V/propidium iodide staining, and related protein expression. In vitro cellular uptake and optical mouse imaging in vivo suggested that the improved antitumor effect was caused primarily by enhanced uptake and tumor targeting. Furthermore, an in vivo antitumor efficacy study indicated that the CK mixed micelles significantly inhibited tumor growth, thereby decreasing tumor volume at the end of the experiment as compared with that in the control mice. Histological analysis confirmed the antitumor effect with low toxicity. Conclusion: The PC/DP micellar system was an effective drug delivery system for CK in tumor therapy. Keywords: mixed micellar system, ginsenoside compound-K, targeted effect, antitumor, lung cancer
format article
author Jin X
Yang Q
Cai N
author_facet Jin X
Yang Q
Cai N
author_sort Jin X
title Preparation of ginsenoside compound-K mixed micelles with improved retention and antitumor efficacy
title_short Preparation of ginsenoside compound-K mixed micelles with improved retention and antitumor efficacy
title_full Preparation of ginsenoside compound-K mixed micelles with improved retention and antitumor efficacy
title_fullStr Preparation of ginsenoside compound-K mixed micelles with improved retention and antitumor efficacy
title_full_unstemmed Preparation of ginsenoside compound-K mixed micelles with improved retention and antitumor efficacy
title_sort preparation of ginsenoside compound-k mixed micelles with improved retention and antitumor efficacy
publisher Dove Medical Press
publishDate 2018
url https://doaj.org/article/446225aee97f427eb3d414cd6ff78f0d
work_keys_str_mv AT jinx preparationofginsenosidecompoundkmixedmicelleswithimprovedretentionandantitumorefficacy
AT yangq preparationofginsenosidecompoundkmixedmicelleswithimprovedretentionandantitumorefficacy
AT cain preparationofginsenosidecompoundkmixedmicelleswithimprovedretentionandantitumorefficacy
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