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자료유형
학술저널
저자정보
Dong, Qing (Key Laboratory of Smart Drug Delivery [Fudan University], Ministry of Education, Department of Pharmaceutics, School of Pharmacy, Fudan University) Xie, Zuo-Xu (Key Laboratory of Smart Drug Delivery [Fudan University], Ministry of Education, Department of Pharmaceutics, School of Pharmacy, Fudan University) Xie, Cao (Key Laboratory of Smart Drug Delivery [Fudan University], Ministry of Education, Department of Pharmaceutics, School of Pharmacy, Fudan University) Lu, Wei-Yue (Key Laboratory of Smart Drug Delivery [Fudan University], Ministry of Education, Department of Pharmaceutics, School of Pharmacy, Fudan University) Zhang, Qian (Department of Medicinal Chemistry, School of Pharmacy, Fudan University) Li, Xue (Key Laboratory of Smart Drug Delivery [Fudan University], Ministry of Education, Department of Pharmaceutics, School of Pharmacy, Fudan University) Liu, Min (Key Laboratory of Smart Drug Delivery [Fudan University], Ministry of Education, Department of Pharmaceutics, School of Pharmacy, Fudan University)
저널정보
아시아태평양암예방학회 Asian Pacific journal of cancer prevention : APJCP Asian Pacific journal of cancer prevention : APJCP 제15권 제17호
발행연도
2014.1
수록면
7,363 - 7,369 (7page)

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The present study aimed to prepare and evaluate polymeric micelles conjugated with folic acid through ${\alpha}$- or ${\gamma}$-carboxyl groups for antitumor efficacy. The isomeric block copolymers, ${\alpha}$- and ${\gamma}$-folate-polyethyleneglycol-distearoyl phosphatidylethanolamine (${\alpha}$- and ${\gamma}$-Fol-PEG-DSPE), were produced by solid phase peptide synthesis. Three types of doxorubicin (DOX)-loaded polymeric micelles (MPEG-DSPE-DOX and ${\alpha}$- / ${\gamma}$-Fol-PEG-DSPEDOX micelles) were prepared via the film formation method. Compared with MPEG-DSPE-DOX micelles, the ${\alpha}$- / ${\gamma}$-Fol-PEG-DSPE-DOX micelles presented a higher cellular uptake behavior in the live cell study. Cell viability percentages were 81.8%, 57.3%, 56.6% at 2 hours for MPEG-DSPE-DOX, ${\alpha}$- and ${\gamma}$-Fol-PEG-DSPE-DOX micelles, respectively (p<0.05). Using the KB xenograft tumor model, both ${\alpha}$- and ${\gamma}$-folate-conjugated micelles were found to have better antitumor effects with lower toxicity in comparison with MPEG-DSPE-DOX micelles. No difference in in vivo antitumor efficacy was found between ${\alpha}$- and ${\gamma}$-Fol-PEG-DSPE-DOX micelles. The folate-conjugated micelles might be a potentially useful strategy for tumor targeting of therapeutic agents, whether grafting with folic acid through ${\alpha}$- or ${\gamma}$-carboxyl groups.

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