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Abstract

In an attempt to develop the tumor-targeted nanocarrier which can surmount major challenges for in vivo application, we prepared tumor microenvironment-specific nanoparticles which can be sequentially activated at the extracellular and intracellular levels of tumor tissue by stepwise transformation. This polymeric nanoparticle has been prepared using an amphiphilic polyethyleneimine derivative with the pH-responsive charge-convertible moiety and the reduction-responsive crosslink. Once reaching the tumor tissue in vivo after systemic administration, the surface charge of this nanoparticle can be converted from negative to positive by recognizing the mildly acidic extracellular matrix of tumor, allowing for the enhanced cellular uptake. After the cellular uptake, the nanoparticle can selectively release the drug at the intracellular level since it has the chemically crosslinked core by the disulfide bond which is cleaved in intracellular reductive environment. The tumor microenvironment-specific nanoparticle shows the high tumor targetability and dramatically improves the antitumor efficacy of the drug. 

Author information

Ko H1, Son S1, Jeon J2, Thambi T2, Kwon S2, Chae YS3, Kang YM3, Park JH4.​

1Department of Health Sciences and Technology, Samsung Advanced Institute for Health Sciences and Technology (SAIHST), Sungkyunkwan University, 2066, Seobu-ro, Jangan-gu, Suwon 440-746, Republic of Korea.

2School of Chemical Engineering, College of Engineering, Sungkyunkwan University, Suwon 440-746, Republic of Korea.

3School of Medicine, Kyungpook National University, 680, Gukchaebosang-ro, Jung-gu, Daegu 700-842, Republic of Korea.

4Department of Health Sciences and Technology, Samsung Advanced Institute for Health Sciences and Technology (SAIHST), Sungkyunkwan University, 2066, Seobu-ro, Jangan-gu, Suwon 440-746, Republic of Korea; School of Chemical Engineering, College of Engineering, Sungkyunkwan University, Suwon 440-746, Republic of Korea. Electronic address: jhpark1@skku.edu.