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약학대학
약학과
Journal papers
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Improved method for synthesis of low molecular weight protamine–siRNA conjugate
Title
Improved method for synthesis of low molecular weight protamine–siRNA conjugate
Authors
Yu Z.
;
Ye J.
;
Pei X.
;
Sun L.
;
Liu E.
;
Wang J.
;
Huang Y.
;
Lee S.J.
;
He H.
Ewha Authors
이승진
SCOPUS Author ID
이승진
Issue Date
2018
Journal Title
Acta Pharmaceutica Sinica B
ISSN
2211-3835
Citation
Acta Pharmaceutica Sinica B vol. 8, no. 1, pp. 116 - 126
Keywords
Biomimetic delivery
;
Cell penetrating peptide
;
Conjugate
;
Conjugation yield
;
Crosslinker
;
siRNA
Publisher
Chinese Academy of Medical Sciences
Indexed
SCOPUS
Document Type
Article
Abstract
RNAi technology has aroused wide public interest due to its high efficiency and specificity to treat multiple types of diseases. However, the effective delivery of siRNA remains a challenge due to its large molecular weight and strong anionic charge. Considering their remarkable functions in vivo and features that are often desired in drug delivery carriers, biomimetic systems for siRNA delivery become an effective and promising strategy. Based on this, covalent attachment of synthetic cell penetrating peptides (CPP) to siRNA has become of great interest. We developed a monomeric covalent conjugate of low molecular weight protamine (LMWP, a well-established CPP) and siRNA via a cytosol-cleavable disulfide linkage using PEG as a crosslinker. Results showed that the conjugates didn't generate coagulation, and exhibited much better RNAi potency and intracellular delivery compared with the conventional charge-complexed CPP/siRNA aggregates. Three different synthetic and purification methods were compared in order to optimize synthesis efficiency and product yield. The methodology using hetero-bifunctional NHS–PEG–OPSS as a crosslinker to synthesize LMWP–siRNA simplified the synthesis and purification process and produced the highest yield. These results pave the way towards siRNA biomimetic delivery and future clinical translation. © 2018 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences
DOI
10.1016/j.apsb.2017.11.011
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