Abstract
The novel methotrexate-loaded nanoparticles (MTX/PGD NPs) prepared with amphiphilic codendrimer PGD from polyamidoamine and oligothylene glycol dendrons were obtained via antisolvent precipitation method augmented by ultrasonication. Based on the excellent hydrophility of PGD, the drug-loaded nanoparticles could be investigated easily with the high drug-loading content (~85.2%, w/w). The MTX/PGD NPs possessed spherical morphology, nanoscaled particle size (approximately 182.4 nm), and narrow particle size distribution. Release of MTX from MTX/PGD NPs showed a sustained release manner and completed within 48 h. Hemolytic evaluation indicated MTX/PGD NPs presented good blood compatibility, and the cytotoxicity of nanoparticles against breast cancer cells in vitro, biodistribution in tumor tissue, and antitumor efficacy in vivo were enhanced significantly compared to MTX injection. According to the higher drug-loading content, enhanced antitumor efficacy, and appropriate particle size, MTX/PGD NPs as the drug delivery systems could have potential application for cancer chemotherapy in clinic.
Highlights
Inhibitory effect on the cell proliferation[23]
We report a novel strategy of preparation MTX nanoparticles (MTX/PGD NPs) based on amphiphilic codendrimer PGD via the antisolvent precipitation method augmented by ultrasonication (Fig. 1), and the drug-loaded content (DLC) of MTX/PGD NPs was improved to 85.2% (w/w)
The MTX-loaded PGD nanoparticles (MTX/PGD NPs) were prepared via the revised antisolvent precipitation method augmented by ultrasonication, the resultant nanoparticles were dispersed in deionized water with slight yellow color (Fig. 2a), and the DLC was approximately 85.2%
Summary
Inhibitory effect on the cell proliferation[23]. Baker et al researched the polyvalent dendrimer-MTX conjugate, which inhibited dihydrofolate reductase and induced cytotoxicity in KB cells[24]. The particle size and zeta potential of MTX/PGD NPs in aqueous solution were measured by dynamic light scattering (DLS).
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