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Open AccessArticle

Development of ErbB2-Targeting Liposomes for Enhancing Drug Delivery to ErbB2-Positive Breast Cancer

by 1,†, 2,†, 3, 3, 4,* and 2,*
1
Graduate School of Science and Technology (GSST), Kumamoto University, Kumamoto 860-8555, Japan
2
International Research Organization for Advanced Science and Technology (IROAST), Kumamoto University, Kumamoto 860-8555, Japan
3
School of Chemical Engineering, Chonnam National University, Gwangju 61186, Korea
4
Faculty of Advanced Science and Technology, Kumamoto University, Kumamoto 860-8555, Japan
*
Authors to whom correspondence should be addressed.
These authors have contributed equally to this work.
Pharmaceutics 2020, 12(6), 585; https://doi.org/10.3390/pharmaceutics12060585
Received: 26 May 2020 / Revised: 19 June 2020 / Accepted: 22 June 2020 / Published: 24 June 2020
(This article belongs to the Special Issue Biodegradable Nanoparticulate Drug Delivery Systems)
ErbB2 is a type of receptor tyrosine kinase, which is known to be involved in tumorigenesis, tumor aggressiveness, and clinical outcome. ErbB2-targeting therapy using therapeutic antibodies has been successful in breast cancer treatment. However, the need for repeated treatments and the high cost are major disadvantages with monoclonal antibody therapies. Compared with antibodies, peptides are cheap, relatively stable, and have low immunogenicity. We have developed a highly specific cancer-targeting drug delivery system using a targeting peptide to maximize the therapeutic efficiency of rapamycin and to help prevent drug resistance in ErbB2-positive breast cancer. Physicochemical characterization confirmed the successful construction of ErbB2-targeting liposomes (ErbB2Lipo). A comparison of a scrambled peptide (ScrErbB2) with the ErbB2-targeting peptide confirmed that these peptides had similar properties except for the targeting ability. The ErbB2Lipo exhibited higher delivery efficiency in ErbB2 positive BT-474 cells than non-targeting liposomes conjugated with ScrErbB2 (ScrErbB2Lipo). This peptide-targeting strategy has the potential to improve the efficacy of chemotherapy in ErbB2-positive cancers. View Full-Text
Keywords: targeted therapy; targeting peptide; mTOR inhibitor; immunoliposome; drug delivery system; breast cancer therapy targeted therapy; targeting peptide; mTOR inhibitor; immunoliposome; drug delivery system; breast cancer therapy
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    Doi: 10.5281/zenodo.3854982
    Description: Table S1. Fmoc determination. Figure S1. Synthetic chemical structure of DSPE-PEG-ErbB2. Figure S2. Characterization of ErbB2Lipo. A. Size of ErbB2Lipo under PBS (pH 7.4, 6.5 and 5.0, respectively) for 5 days. B. PdI of ErbB2Lipo under PBS (pH 7.4, 6.5 and 5.0, respectively) for 5 days. C. Encapsulation efficiency (red) and loading efficiency (black) of Rapa in the ErbB2Lipo. D. Cumulative release of Rapa at 37 °C in PBS pH 6.5 and pH 7.4. Figure S3. MDA-MB-231 and BT-474 cellular level of ErbB2 (185 kDa). GAPDH was used as an internal control (37 kDa). Figure S4. Representative images of BT-474 incubated with ErbB2lipo under pre-treated or non-treated anti-ErbB2 antibody (5 μg, 3 h). Scale bar, 10 μm.
MDPI and ACS Style

Ueno, S.; Kim, M.W.; Lee, G.; Park, Y.I.; Niidome, T.; Lee, R. Development of ErbB2-Targeting Liposomes for Enhancing Drug Delivery to ErbB2-Positive Breast Cancer. Pharmaceutics 2020, 12, 585. https://doi.org/10.3390/pharmaceutics12060585

AMA Style

Ueno S, Kim MW, Lee G, Park YI, Niidome T, Lee R. Development of ErbB2-Targeting Liposomes for Enhancing Drug Delivery to ErbB2-Positive Breast Cancer. Pharmaceutics. 2020; 12(6):585. https://doi.org/10.3390/pharmaceutics12060585

Chicago/Turabian Style

Ueno, Sho; Kim, Min W.; Lee, Gibok; Park, Yong I.; Niidome, Takuro; Lee, Ruda. 2020. "Development of ErbB2-Targeting Liposomes for Enhancing Drug Delivery to ErbB2-Positive Breast Cancer" Pharmaceutics 12, no. 6: 585. https://doi.org/10.3390/pharmaceutics12060585

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