Journal
JOURNAL OF CONTROLLED RELEASE
Volume 276, Issue -, Pages 42-49Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.jconrel.2018.02.028
Keywords
Surfactant-free solubilization; Systemic drug delivery; Low molecular weight methylcellulose; Anti-cancer drug
Funding
- National Research Foundation of Korea [NRF-2015R1A2A1A09003019]
- Bio & Medical Technology Development Program [NRF-2017M3A9F5029655]
- Brain Korea 21 Plus Program [22A20130011095]
- Korean Health Technology R&D project through the Ministry of Health and Welfare [HI17C0888]
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Docetaxel, an advanced taxoid, has been widely used as an anti-mitotic agent, but further augmentation of its properties is still required, including improvement in low aqueous solubility. Herein, we report the development of bio-eliminable low molecular weight methylcellulose-based surfactant-free injectable formulation for the delivery of docetaxel. Crude methylcellulose, a hydrophobically modified cellulose derivative, was hydrolyzed by an enzymatic degradation method to obtain low molecular weight methylcellulose (LMwMC). Docetaxel was successfully loaded in micelles with small particle sizes high drug loading and sustained release profile. The in vivo anti-cancer effects of intravenously injected nanoparticle systems in B16F10 melanoma xenograft mice were evaluated and demonstrated a significantly enhanced therapeutic effect with the docetaxel-LMwMC micellar aggregates compared to a commercially available docetaxel, Taxotere (R). Surfactant-free solubilization of docetaxel could be a promising delivery method for effective insoluble drug delivery for anti-tumor efficacy.
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