Cyclic RGD-conjugated Pluronic (R) blending system for active, targeted drug delivery
- Authors
- Lim, Chaemin; Moon, Junseong; Sim, Taehoon; Hoang, Ngoc Ha; Won, Woong Roeck; Lee, Eun Seong; Youn, Yu Seok; Choi, Han-Gon; Oh, Kyungsoo; Oh, Kyung Taek
- Issue Date
- 2018
- Publisher
- DOVE MEDICAL PRESS LTD
- Keywords
- blending micellar system; docetaxel; cyclic RGD; Pluronic L121/F127; active targeting; nanomedicine
- Citation
- INTERNATIONAL JOURNAL OF NANOMEDICINE, v.13, pp 4627 - 4639
- Pages
- 13
- Journal Title
- INTERNATIONAL JOURNAL OF NANOMEDICINE
- Volume
- 13
- Start Page
- 4627
- End Page
- 4639
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/1523
- DOI
- 10.2147/IJN.S171794
- ISSN
- 1178-2013
1178-2013
- Abstract
- 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 alpha v beta 3 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.
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