Multifunctional Cholesterol-modified Dendrimers for Targeted Drug Delivery to Cancer Cells Expressing Folate Receptors

Fan-Fan Fu; Ben-Qing Zhou; Zhi-Jun Ouyang; Yi-Lun Wu; Jing-Yi Zhu; Ming-Wu Shen; Jin-Dong Xia; Xiang-Yang Shi

doi:10.1007/s10118-019-2172-9

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Multifunctional Cholesterol-modified Dendrimers for Targeted Drug Delivery to Cancer Cells Expressing Folate Receptors

ARTICLE | Updated：2021-02-18

- Multifunctional Cholesterol-modified Dendrimers for Targeted Drug Delivery to Cancer Cells Expressing Folate Receptors
- Chinese Journal of Polymer Science Vol. 37, Issue 2, Pages: 129-135(2019)
- Affiliations：
  
  a.Key Laboratory of Science & Technology of Eco-Textile, Ministry of Education, College of Chemistry, Chemical Engineering and Biotechnology, Donghua University, Shanghai 201620, China
  b.Department of Radiology, Shanghai Songjiang District Central Hospital, Shanghai 201600, China
- Author bio：
  
  mwshen@dhu.edu.cn (M.W.S.)
  xiajd_21@163.com (J.D.X.)
  xshi@dhu.edu.cn (X.Y.S.)
- Funds：
- DOI：10.1007/s10118-019-2172-9
  CLC：
- Received：29 July 2018，
  
  Revised：2018-9-14，
  
  Accepted：18 September 2018，
  
  Online First：22 October 2018，
  
  Published：2019-02
- Accepted：
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Citation: Fu, F. F.; Zhou, B. Q.; Ouyang, Z. J.; Wu, Y. L.; Zhu, J. Y.; Shen, M. W.; Xia, J. D.; Shi, X. Y. Multifunctional cholesterol-modified dendrimers for targeted drug delivery to cancer cells expressing folate receptors. Chinese J. Polym. Sci. 2019, 37, 129–135

Fan-Fan Fu, Ben-Qing Zhou, Zhi-Jun Ouyang, et al. Multifunctional Cholesterol-modified Dendrimers for Targeted Drug Delivery to Cancer Cells Expressing Folate Receptors[J]. Chinese Journal of Polymer Science, 2019, 37(2): 129-135.
Citation: Fu, F. F.; Zhou, B. Q.; Ouyang, Z. J.; Wu, Y. L.; Zhu, J. Y.; Shen, M. W.; Xia, J. D.; Shi, X. Y. Multifunctional cholesterol-modified dendrimers for targeted drug delivery to cancer cells expressing folate receptors. Chinese J. Polym. Sci. 2019, 37, 129–135 DOI： 10.1007/s10118-019-2172-9.

Fan-Fan Fu, Ben-Qing Zhou, Zhi-Jun Ouyang, et al. Multifunctional Cholesterol-modified Dendrimers for Targeted Drug Delivery to Cancer Cells Expressing Folate Receptors[J]. Chinese Journal of Polymer Science, 2019, 37(2): 129-135. DOI： 10.1007/s10118-019-2172-9.

摘要

Abstract

We present here the development of cholesterol (Chol)-modified dendrimer system for targeted chemotherapy of folate (FA) receptor-expressing cancer cells. In our study

poly(amidoamine) (PAMAM) dendrimers of generation 5 (G5) were functionalized step-by-step with Chol

fluorescein isothiocyanate (FI)

and FA

via

a poly(ethylene glycol) (PEG) spacer (PEG-FA)

and then acetamide to shield their remaining surface amines. The synthesized G5.NHAc-Chol-FI-PEG-FA (for short

G5-CFPF) dendrimers were utilized to encapsulate 10-hydroxycamptothecin (HCP)

a hydrophobic anticancer drug. We find that each G5-CFPF dendrimer can encapsulate 13.8 HCP molecules. The complexes show a slower release profiles of HCP in a pH-dependent manner than the control complexes formed using the same dendrimers without Chol under the same conditions. Thanks to the targeting role played by FA

the complexes display a specific inhibition efficacy to FA receptor-expressing cervical cancer cells. The designed Chol-modified dendrimers may be adopted as a promising carrier for application in targeted cancer therapy.

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Keywords

references

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