Cyclic RGD-conjugated Pluronic® blending system for active, targeted drug delivery
Chaemin Lim,1,* Junseong Moon,1,* Taehoon Sim,1 Ngoc Ha Hoang,1 Woong Roeck Won,1 Eun Seong Lee,2 Yu Seok Youn,3 Han-Gon Choi,4 Kyungsoo Oh,1 Kyung Taek Oh1 1College of Pharmacy, Chung-Ang University, Seoul, Republic of Korea; 2Division of Biotechnology, The Catholic University of Korea, Bucheon, R...
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Dove Medical Press
2018
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oai:doaj.org-article:b891443d671f4964aa6224e2dedcb6172021-12-02T00:40:30ZCyclic RGD-conjugated Pluronic® blending system for active, targeted drug delivery1178-2013https://doaj.org/article/b891443d671f4964aa6224e2dedcb6172018-08-01T00:00:00Zhttps://www.dovepress.com/cyclic-rgd-conjugated-pluronicreg-blending-system-for-active-targeted--peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Chaemin Lim,1,* Junseong Moon,1,* Taehoon Sim,1 Ngoc Ha Hoang,1 Woong Roeck Won,1 Eun Seong Lee,2 Yu Seok Youn,3 Han-Gon Choi,4 Kyungsoo Oh,1 Kyung Taek Oh1 1College of Pharmacy, Chung-Ang University, Seoul, Republic of Korea; 2Division of Biotechnology, The Catholic University of Korea, Bucheon, Republic of Korea; 3School of Pharmacy, SungKyunKwan University, Suwon, Republic of Korea; 4College of Pharmacy, Institute of Pharmaceutical Science and Technology, Hanyang University, Ansan, Republic of Korea *These authors contributed equally to this work Background: Blending micellar systems of different types of polymers has been proposed as an efficient approach for tailor-made drug formulations. The lamellar structure of hydrophobic polymers may provide a high drug loading capacity, and hydrophilic polymers may provide good colloidal stability. Methods: In this study, the anticancer model drug docetaxel was loaded onto a nanosized blending micellar system with two pluronics (L121/F127). To achieve increased antitumor activity, the cyclic arginine-glycine-aspartic acid tripeptide (cRGD) as an active tumor targeting ligand was conjugated to the blending system.Results: The docetaxel-loaded Pluronic blending system exhibited a higher drug loading capacity than that of F127 and showed high colloidal stability with a spherical structure. cRGD conjugates demonstrated enhanced drug cellular uptake and anticancer activity against αvβ3 integrin-overexpressing U87MG cancer cells. In vivo animal imaging also revealed that the prepared cRGD-conjugated nanoparticles effectively accumulated at the targeted tumor site through an active and passive targeting strategy. Conclusion: Accordingly, the prepared nanosized system shows potential as a tailor-made, active targeting, nanomedicinal platform for anticancer therapy. We believe that this novel nanoplatform will provide insights for advancement of tumor therapy. Keywords: blending micellar system, docetaxel, cyclic RGD, Pluronic L121/F127, active targeting, nanomedicineLim CMoon JSim THoang NHWon WRLee ESYoun YSChoi HGOh KOh KTDove Medical PressarticleBlending micellar systemDocetaxelCyclic RGDPluronic L121/F127Active targetingNanomedicineMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 13, Pp 4627-4639 (2018) |
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Blending micellar system Docetaxel Cyclic RGD Pluronic L121/F127 Active targeting Nanomedicine Medicine (General) R5-920 |
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Blending micellar system Docetaxel Cyclic RGD Pluronic L121/F127 Active targeting Nanomedicine Medicine (General) R5-920 Lim C Moon J Sim T Hoang NH Won WR Lee ES Youn YS Choi HG Oh K Oh KT Cyclic RGD-conjugated Pluronic® blending system for active, targeted drug delivery |
| description |
Chaemin Lim,1,* Junseong Moon,1,* Taehoon Sim,1 Ngoc Ha Hoang,1 Woong Roeck Won,1 Eun Seong Lee,2 Yu Seok Youn,3 Han-Gon Choi,4 Kyungsoo Oh,1 Kyung Taek Oh1 1College of Pharmacy, Chung-Ang University, Seoul, Republic of Korea; 2Division of Biotechnology, The Catholic University of Korea, Bucheon, Republic of Korea; 3School of Pharmacy, SungKyunKwan University, Suwon, Republic of Korea; 4College of Pharmacy, Institute of Pharmaceutical Science and Technology, Hanyang University, Ansan, Republic of Korea *These authors contributed equally to this work Background: Blending micellar systems of different types of polymers has been proposed as an efficient approach for tailor-made drug formulations. The lamellar structure of hydrophobic polymers may provide a high drug loading capacity, and hydrophilic polymers may provide good colloidal stability. Methods: In this study, the anticancer model drug docetaxel was loaded onto a nanosized blending micellar system with two pluronics (L121/F127). To achieve increased antitumor activity, the cyclic arginine-glycine-aspartic acid tripeptide (cRGD) as an active tumor targeting ligand was conjugated to the blending system.Results: The docetaxel-loaded Pluronic blending system exhibited a higher drug loading capacity than that of F127 and showed high colloidal stability with a spherical structure. cRGD conjugates demonstrated enhanced drug cellular uptake and anticancer activity against αvβ3 integrin-overexpressing U87MG cancer cells. In vivo animal imaging also revealed that the prepared cRGD-conjugated nanoparticles effectively accumulated at the targeted tumor site through an active and passive targeting strategy. Conclusion: Accordingly, the prepared nanosized system shows potential as a tailor-made, active targeting, nanomedicinal platform for anticancer therapy. We believe that this novel nanoplatform will provide insights for advancement of tumor therapy. Keywords: blending micellar system, docetaxel, cyclic RGD, Pluronic L121/F127, active targeting, nanomedicine |
| format |
article |
| author |
Lim C Moon J Sim T Hoang NH Won WR Lee ES Youn YS Choi HG Oh K Oh KT |
| author_facet |
Lim C Moon J Sim T Hoang NH Won WR Lee ES Youn YS Choi HG Oh K Oh KT |
| author_sort |
Lim C |
| title |
Cyclic RGD-conjugated Pluronic® blending system for active, targeted drug delivery |
| title_short |
Cyclic RGD-conjugated Pluronic® blending system for active, targeted drug delivery |
| title_full |
Cyclic RGD-conjugated Pluronic® blending system for active, targeted drug delivery |
| title_fullStr |
Cyclic RGD-conjugated Pluronic® blending system for active, targeted drug delivery |
| title_full_unstemmed |
Cyclic RGD-conjugated Pluronic® blending system for active, targeted drug delivery |
| title_sort |
cyclic rgd-conjugated pluronic® blending system for active, targeted drug delivery |
| publisher |
Dove Medical Press |
| publishDate |
2018 |
| url |
https://doaj.org/article/b891443d671f4964aa6224e2dedcb617 |
| work_keys_str_mv |
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1718403578387759104 |