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Mol Pharm. 2017 Oct 2;14(10):3598-3608. doi: 10.1021/acs.molpharmaceut.7b00612. Epub 2017 Sep 20.

Poly(vinyl methyl ether/maleic anhydride)-Doped PEG-PLA Nanoparticles for Oral Paclitaxel Delivery To Improve Bioadhesive Efficiency.

Wang Q1,2,3,4, Li C2,3,4, Ren T1, Chen S2,3,4, Ye X2,3,4,5, Guo H2,3,4, He H1, Zhang Y1, Yin T1, Liang XJ2,3,4, Tang X1.

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School of Pharmacy, Shenyang Pharmaceutical University , Shenyang 110016, P. R. China.
Chinese Academy of Sciences (CAS) Center for Excellence in Nanoscience, National Center for Nanoscience and Technology , Beijing 100190, P. R. China.
Laboratory of Controllable Nanopharmaceuticals, CAS Key Laboratory for Biomedical Effects of Nanomaterials and Nanosafety, National Center for Nanoscience and Technology , Beijing 100190, P. R. China.
University of Chinese Academy of Sciences , Beijing 100049, P. R. China.
Department of Pharmacology, Shenyang Pharmaceutical University , Shenyang 110016, P. R. China.


Bioadhesive nanoparticles based on poly(vinyl methyl ether/maleic anhydride) (PVMMA) and poly(ethylene glycol) methyl ether-b-poly(d,l-lactic acid) (mPEG-b-PLA) were produced by the emulsification solvent evaporation method. Paclitaxel was utilized as the model drug, with an encapsulation efficiency of up to 90.2 ± 4.0%. The nanoparticles were uniform and spherical in shape and exhibited a sustained drug release compared with Taxol. m-NPs also exhibited favorable bioadhesive efficiency at the same time. Coumarin 6 or DiR-loaded nanoparticles with/without PVMMA (C6-m-NPs/DiR-m-NPs or C6-p-NPs/DiR-p-NPs) were used for cellular uptake and intestinal adhesion experiments, respectively. C6-m-NPs were shown to enhance cellular uptake, and caveolae/lipid raft mediated endocytosis was the primary route for the uptake of the nanoparticles. Favorable bioadhesive efficiency led to prolonged retention in the intestine reflected by the fluorescence in isolated intestines ex vivo. In a ligated intestinal loops model, C6-m-NPs showed a clear advantage for transporting NPs across the mucus layer over C6-p-NPs and free C6. The apparent permeability coefficient (Papp) of PTX-m-NPs through Caco-2/HT29 monolayers was 1.3- and 1.6-fold higher than PTX-p-NPs and Taxol, respectively, which was consistent with the AUC0-t of different PTX formulations after oral administration in rats. PTX-m-NPs also exhibited a more effective anticancer efficacy, with an IC50 of 0.2 ± 1.4 μg/mL for A549 cell lines, further demonstrating the advantage of bioadhesive nanoparticles. The bioadhesive nanoparticles m-NPs demonstrated both mucus permeation and epithelial absorption, and thus, this bioadhesive drug delivery system has the potential to improve the bioavailability of drugs that are insoluble in the gastrointestinal environment.


anticancer efficacy; bioadhesive nanoparticles; epithelial absorption; mucus permeation; oral delivery

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