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Oral Delivery of DMAB-Modified Docetaxel-Loaded PLGA-TPGS Nanoparticles for Cancer Chemotherapy

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ABSTRACT

Three types of nanoparticle formulation from biodegradable PLGA-TPGS random copolymer were developed in this research for oral administration of anticancer drugs, which include DMAB-modified PLGA nanoparticles, unmodified PLGA-TPGS nanoparticles and DMAB-modified PLGA-TPGS nanoparticles. Firstly, the PLGA-TPGS random copolymer was synthesized and characterized. DMAB was used to increase retention time at the cell surface, thus increasing the chances of particle uptake and improving oral drug bioavailability. Nanoparticles were found to be of spherical shape with an average particle diameter of around 250 nm. The surface charge of PLGA-TPGS nanoparticles was changed to positive after DMAB modification. The results also showed that the DMAB-modified PLGA-TPGS nanoparticles have significantly higher level of the cellular uptake than that of DMAB-modified PLGA nanoparticles and unmodified PLGA-TPGS nanoparticles. In vitro, cytotoxicity experiment showed advantages of the DMAB-modified PLGA-TPGS nanoparticle formulation over commercial Taxotere® in terms of cytotoxicity against MCF-7 cells. In conclusion, oral chemotherapy by DMAB-modified PLGA-TPGS nanoparticle formulation is an attractive and promising treatment option for patients.

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Cellular uptake of coumarin-6-loaded 5% DMAB-modified PLGA nanoparticles (ANP), unmodified PLGA-TPGS nanoparticles (BNP) and 5% DMAB-modified PLGA-TPGS nanoparticles (CNP) by a Caco-2 and b MCF-7 cells after 2-h incubation.
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Figure 4: Cellular uptake of coumarin-6-loaded 5% DMAB-modified PLGA nanoparticles (ANP), unmodified PLGA-TPGS nanoparticles (BNP) and 5% DMAB-modified PLGA-TPGS nanoparticles (CNP) by a Caco-2 and b MCF-7 cells after 2-h incubation.

Mentions: Caco-2 cells are a widely accepted model to predict permeability and absorption of compounds in humans [30]. Taxoids have been extensively used to treat metastatic breast cancer. The fluorescence uptake by the MCF-7 cells could provide a useful model to assess the in vitro therapeutic effect of the Taxoids in the various formulations for breast cancer treatment [31,32]. The cellular uptake of coumarin-6-loaded 5% DMAB-modified PLGA nanoparticles (ANP), unmodified PLGA-TPGS nanoparticles (BNP) and 5% DMAB-modified PLGA-TPGS nanoparticles (CNP) was thus evaluated in this research using Caco-2 cell line as in vitro model of the GI barrier and MCF-7 cell line as model cancer cells. The cellular uptake efficiency of the coumarin-6-loaded nanoparticles by Caco-2 and MCF-7 cells was assayed upon 2-h incubation, and the results are shown in Figure 4.


Oral Delivery of DMAB-Modified Docetaxel-Loaded PLGA-TPGS Nanoparticles for Cancer Chemotherapy
Cellular uptake of coumarin-6-loaded 5% DMAB-modified PLGA nanoparticles (ANP), unmodified PLGA-TPGS nanoparticles (BNP) and 5% DMAB-modified PLGA-TPGS nanoparticles (CNP) by a Caco-2 and b MCF-7 cells after 2-h incubation.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC3102336&req=5

Figure 4: Cellular uptake of coumarin-6-loaded 5% DMAB-modified PLGA nanoparticles (ANP), unmodified PLGA-TPGS nanoparticles (BNP) and 5% DMAB-modified PLGA-TPGS nanoparticles (CNP) by a Caco-2 and b MCF-7 cells after 2-h incubation.
Mentions: Caco-2 cells are a widely accepted model to predict permeability and absorption of compounds in humans [30]. Taxoids have been extensively used to treat metastatic breast cancer. The fluorescence uptake by the MCF-7 cells could provide a useful model to assess the in vitro therapeutic effect of the Taxoids in the various formulations for breast cancer treatment [31,32]. The cellular uptake of coumarin-6-loaded 5% DMAB-modified PLGA nanoparticles (ANP), unmodified PLGA-TPGS nanoparticles (BNP) and 5% DMAB-modified PLGA-TPGS nanoparticles (CNP) was thus evaluated in this research using Caco-2 cell line as in vitro model of the GI barrier and MCF-7 cell line as model cancer cells. The cellular uptake efficiency of the coumarin-6-loaded nanoparticles by Caco-2 and MCF-7 cells was assayed upon 2-h incubation, and the results are shown in Figure 4.

View Article: PubMed Central - HTML

ABSTRACT

Three types of nanoparticle formulation from biodegradable PLGA-TPGS random copolymer were developed in this research for oral administration of anticancer drugs, which include DMAB-modified PLGA nanoparticles, unmodified PLGA-TPGS nanoparticles and DMAB-modified PLGA-TPGS nanoparticles. Firstly, the PLGA-TPGS random copolymer was synthesized and characterized. DMAB was used to increase retention time at the cell surface, thus increasing the chances of particle uptake and improving oral drug bioavailability. Nanoparticles were found to be of spherical shape with an average particle diameter of around 250 nm. The surface charge of PLGA-TPGS nanoparticles was changed to positive after DMAB modification. The results also showed that the DMAB-modified PLGA-TPGS nanoparticles have significantly higher level of the cellular uptake than that of DMAB-modified PLGA nanoparticles and unmodified PLGA-TPGS nanoparticles. In vitro, cytotoxicity experiment showed advantages of the DMAB-modified PLGA-TPGS nanoparticle formulation over commercial Taxotere® in terms of cytotoxicity against MCF-7 cells. In conclusion, oral chemotherapy by DMAB-modified PLGA-TPGS nanoparticle formulation is an attractive and promising treatment option for patients.

No MeSH data available.