Merck
  • Blended nanoparticle system based on miscible structurally similar polymers: a safe, simple, targeted, and surprisingly high efficiency vehicle for cancer therapy.

Blended nanoparticle system based on miscible structurally similar polymers: a safe, simple, targeted, and surprisingly high efficiency vehicle for cancer therapy.

Advanced healthcare materials (2015-03-25)
Wei Tao, Jinxie Zhang, Xiaowei Zeng, Danny Liu, Gan Liu, Xi Zhu, Yanlan Liu, Qingtong Yu, Laiqiang Huang, Lin Mei
ABSTRACT

A novel blended nanoparticle (NP) system for the delivery of anticancer drugs and its surprisingly high efficacy for cancer chemotherapy by blending a targeting polymer folic acid-poly(ethylene glycol)-b-poly(lactide-co-glycolide) (FA-PEG-b-PLGA) and a miscible structurally similar polymer D-α-tocopheryl polyethylene glycol 1000 succinate-poly(lactide-co-glycolide) (TPGS-PLGA) is reported. This blended NP system can be achieved through a simple and effective nanoprecipitation technique, and possesses unique properties: i) improved long-term compatibility brought by PEG-based polymers; ii) reduced multidrug resistance mediated by P-glycoprotein (P-gp) in tumor cells and increased bioavailability of anticancer drugs by incorporation of TPGS; iii) the regulation of controlled release through polymer ratios and active targeting by FA. Both in vitro cell experiments and in vivo antitumor assays demonstrated the reported blended NP system can achieve the best therapeutic efficiency in an extremely safe, simple and highly efficient process for cancer therapy. Moreover, this NP system is highly efficient in forming NPs with multiple functions, without repeated chemical modification of polymers, which is sometimes complex, inefficient and high cost. Therefore, the development of this novel blended NP concept is extremely meaningful for the application of pharmaceutical nanotechnology in recent studies.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Diisopropylcarbodiimide solution, 1 M in THF
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Diisopropylcarbodiimide solution, 1 M in dichloromethane
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Acetonitrile
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Acetonitrile, for chromatography
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Acetonitrile, SAJ first grade, ≥99.0%
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L-Lysine monohydrochloride, SAJ special grade, ≥99.0%
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Methanol-12C, 99.95 atom % 12C
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Acetonitrile, JIS special grade, ≥99.5%
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Acetonitrile, electronic grade, 99.999% trace metals basis
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L-Lysine monohydrochloride, from non-animal source, meets EP, JP, USP testing specifications, suitable for cell culture, 98.5-101.0%
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L-Lysine monohydrochloride, reagent grade, ≥98% (HPLC)
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N-Hydroxysuccinimide, 98%
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DCC, 1.0 M in methylene chloride
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Folic acid, meets USP testing specifications
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Folic acid, ≥97%
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DCC, 99%
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DIC, 99%
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L-Lysine monohydrochloride, BioUltra, ≥99.5% (AT)
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Folic acid, BioReagent, suitable for cell culture, suitable for insect cell culture, suitable for plant cell culture, ≥97%
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Methanol solution, contains 0.10 % (v/v) formic acid, UHPLC, suitable for mass spectrometry (MS), ≥99.5%
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Acetonitrile, anhydrous, 99.8%
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Acetonitrile, ≥99.5%, ACS reagent
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Methanol, NMR reference standard
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Acetonitrile solution, contains 0.05 % (w/v) ammonium formate, 5 % (v/v) water, 0.1 % (v/v) formic acid, suitable for HPLC
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Methanol, JIS 300, ≥99.8%, for residue analysis