TY - JOUR
T1 - A polymeric prodrug for non-invasive, real-time reporting drug release based on “turn-on” fluorescent probes
AU - Zhao, Xiaodan
AU - Lei, Hengxin
AU - Cheng, Yilong
AU - Wu, Youshen
AU - Zhang, Mingming
AU - He, Gang
AU - Pei, Dandan
AU - Dong, Zhen
AU - Li, Ang
AU - Zhang, Yanfeng
N1 - Publisher Copyright:
© 2020 Elsevier B.V.
PY - 2020/9
Y1 - 2020/9
N2 - Non-invasive monitoring of the in situ drug release in a real-time manner is crucial for the clinical cancer treatment. In this work, a polymeric prodrug, P(HPMA-co-(CPT-SS-CyN)), composed of N-(2-hydroxypropyl) methacrylamide (HPMA) and a functional monomer (a near-infrared fluorescent cyanine-amine dye (CyN) and camptothecin (CPT) linked by disulfide bond) was reported for the non-invasive and real-time reporting drug release. The cleavage of the disulfide bond intracellularly could lead to the release of free CPT as well as the blue shift of the dye (CyN conjugated polymer), enabling facile monitoring of the drug release. Moreover, the percentage of the released drug showed a linear correlation with the normalized increase in the fluorescence intensity, which can be further used for the quantification of the local drug concentration. In vitro cell study showed that the fluorescence intensity gradually increased with the prolongation of incubation time, and P(HPMA-co-(CPT-SS-CyN)) exhibited the same inhibition efficiency of tumor cell proliferation as CPT. This work may guide researchers for the precise design and development of various pharmaceutical formulations.
AB - Non-invasive monitoring of the in situ drug release in a real-time manner is crucial for the clinical cancer treatment. In this work, a polymeric prodrug, P(HPMA-co-(CPT-SS-CyN)), composed of N-(2-hydroxypropyl) methacrylamide (HPMA) and a functional monomer (a near-infrared fluorescent cyanine-amine dye (CyN) and camptothecin (CPT) linked by disulfide bond) was reported for the non-invasive and real-time reporting drug release. The cleavage of the disulfide bond intracellularly could lead to the release of free CPT as well as the blue shift of the dye (CyN conjugated polymer), enabling facile monitoring of the drug release. Moreover, the percentage of the released drug showed a linear correlation with the normalized increase in the fluorescence intensity, which can be further used for the quantification of the local drug concentration. In vitro cell study showed that the fluorescence intensity gradually increased with the prolongation of incubation time, and P(HPMA-co-(CPT-SS-CyN)) exhibited the same inhibition efficiency of tumor cell proliferation as CPT. This work may guide researchers for the precise design and development of various pharmaceutical formulations.
KW - In situ monitoring and qualification
KW - NIR imaging
KW - Polymer-drug delivery system
KW - Reduction-sensitivity
UR - https://www.scopus.com/pages/publications/85085637992
U2 - 10.1016/j.reactfunctpolym.2020.104649
DO - 10.1016/j.reactfunctpolym.2020.104649
M3 - 文章
AN - SCOPUS:85085637992
SN - 1381-5148
VL - 154
JO - Reactive and Functional Polymers
JF - Reactive and Functional Polymers
M1 - 104649
ER -
