Low‐Density Lipoprotein‐Mimicking Nanoparticles for Tumor‐Targeted Theranostic Applications |
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| Authors: | Jeong Yu Lee Jin‐Ho Kim Ki Hyun Bae Mi Hwa Oh Youngwook Kim Jee Seon Kim Tae Gwan Park Keunchil Park Jung Hee Lee Yoon Sung Nam |
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| Affiliation: | 1. Department of Materials Science and Engineering, Korea Advanced Institute of Science and Technology, Yuseung‐gu, Daejeon, Republic of Korea;2. Medical Nanoelement Development Center, Samsung Biomedical Research Institute, Gangnam‐gu, Seoul, Republic of Korea;3. Department of Health Sciences and Technology, Samsung Advanced Institute for Health Sciences and Technology, Sungkyunkwan University, Gangnam‐gu, Seoul, Republic of Korea;4. Department of Biological Sciences, Korea Advanced Institute of Science and Technology, Yuseung‐gu, Daejeon, Republic of Korea;5. Division of Hematology and Oncology, Department of Medicine, Samsung Medical Center, Sungkyunkwan University School of Medicine, Gangnam‐gu, Seoul, Republic of Korea;6. Department of Radiology, Samsung Medical Center, Sungkyunkwan University School of Medicine, Gangnam‐gu, Seoul, Republic of Korea;7. KAIST Institute of NanoCentury (KINC), KAIST Institute for BioCentury (KIB), Korea Advanced Institute of Science and Technology, Yuseung‐gu, Daejeon, Republic of Korea |
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| Abstract: | This study introduces multifunctional lipid nanoparticles (LNPs), mimicking the structure and compositions of low‐density lipoproteins, for the tumor‐targeted co‐delivery of anti‐cancer drugs and superparamagnetic nanocrystals. Paclitaxel (4.7 wt%) and iron oxide nanocrystals (6.8 wt%, 11 nm in diameter) are co‐encapsulated within folate‐functionalized LNPs, which contain a cluster of nanocrystals with an overall diameter of about 170 nm and a zeta potential of about ‐40 mV. The folate‐functionalized LNPs enable the targeted detection of MCF‐7, human breast adenocarcinoma expressing folate receptors, in T2‐weighted magnetic resonance images as well as the efficient intracellular delivery of paclitaxel. Paclitaxel‐free LNPs show no significant cytotoxicity up to 0.2 mg mL?1, indicating the excellent biocompatibility of the LNPs for intracellular drug delivery applications. The targeted anti‐tumor activities of the LNPs in a mouse tumor model suggest that the low‐density lipoprotein‐mimetic LNPs can be an effective theranostic platform with excellent biocompatibility for the tumor‐targeted co‐delivery of various anti‐cancer agents. |
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| Keywords: | low‐density lipoproteins nanoparticles anti‐cancer agents self‐assembly imaging |
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