1447146-88-4Relevant articles and documents
Dimeric Drug Polymeric Nanoparticles with Exceptionally High Drug Loading and Quantitative Loading Efficiency
Cai, Kaimin,He, Xi,Song, Ziyuan,Yin, Qian,Zhang, Yanfeng,Uckun, Fatih M.,Jiang, Chen,Cheng, Jianjun
, p. 3458 - 3461 (2015)
Encapsulation of small-molecule drugs in hydrophobic polymers or amphiphilic copolymers has been extensively used for preparing polymeric nanoparticles (NPs). The loadings and loading efficiencies of a wide range of drugs in polymeric NPs, however, tend to be very low. In this Communication, we report a strategy to prepare polymeric NPs with exceptionally high drug loading (>50%) and quantitative loading efficiency. Specifically, a dimeric drug conjugate bearing a trigger-responsive domain was designed and used as the core-constructing unit of the NPs. Upon co-precipitation of the dimeric drug and methoxypoly(ethylene glycol)-block-polylactide (mPEG-PLA), NPs with a dimeric drug core and a polymer shell were formed. The high-drug-loading NPs showed excellent stability in physiological conditions. No premature drug or prodrug release was observed in PBS solution without triggering, while external triggering led to controlled release of drug in its authentic form.
A high drug loaded polymer nanoparticle based on a dimer prodrug structure and a preparing method thereof
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Paragraph 0034-0035, (2018/11/26)
The invention belongs to the field of medicinal preparation, and relates to a high drug loaded polymer nanoparticle and a preparing method thereof based on a dimer prodrug structure. A high drug loaded polymer nanoparticle preparation is prepared from a sulfur containing dimer camptothecin prodrug, a prodrug-polyethylene glycol amphiphilic polymeric material and the prodrug-polyethylene glycol amphiphilic polymeric material modified by polypeptide to prepare a sulfur containing dimer prodrug high drug loaded polymer nanometer administration system. Amphiphilic polymeric material is synthetizedby directly chemically bonding the sulfur containing dimer camptothecin prodrug with hydrophilic PEG, through a dimer special structure and a drug-cover-drug strategy, and the high drug loaded polymer nanoparticle is prepared. A disulfide bond is introduced in synthetizing the dimer prodrug, the stability of a carrier can be effectively improved, controllability releasing of a drug in a target cell can be realized, breast cancer targeting of the nanoparticle is improved, accumulation of the drug is increased, and the antineoplastic curative effect of the drug is improved.
A two-photon-activated prodrug for therapy and drug release monitoring
Liu, Peilian,Li, Bowen,Zhan, Chenyue,Zeng, Fang,Wu, Shuizhu
, p. 7538 - 7546 (2017/09/27)
A light-activated cleavage strategy for the concomitant release of active drugs and generation of fluorescence changes is highly desirable. Herein a molecular prodrug featuring real-time monitoring of drug localization and release by manipulating fluorophores has been created by constructing a cleavable structure which comprises a photoremovable coumarinyl, an anticancer drug camptothecin, a cleavable linker and a near infrared fluorescent dye dicyanomethylene-4H-pyran (DCM). The fluorescence of coumarinyl and CPT is completely quenched by the DCM moiety via fluorescence resonance energy transfer (FRET). The internalization of the prodrug by cells and its subsequent intracellular location can be tracked by collecting the red fluorescence of DCM; while the release of active CPT as a result of one- or two-photon irradiation can be monitored by observing the newly emerged fluorescence of CPT under one- or two-photon excitation. The prodrug also shows highly controllable cytotoxicity toward HeLa cells and A549 cells, with low IC50 values of 4.01 and 2.53 μM, respectively, upon light irradiation and with much higher IC50 values (>40 μM) without light irradiation. This strategy may provide an approach for the development of light-activatable theranostic anticancer therapeutics.
