Abstract
In recent decades, several types of anticancer drugs that inhibit cancer cell growth and cause cell death have been developed for chemotherapeutic application. However, these agents are usually associated with side effects resulting from nonspecific delivery, which may induce cytotoxicity in healthy cells. To reduce the nonspecific delivery issue, nanoparticles have been successfully used for the delivery of anticancer drugs to specific target sites. In this study, a functional polymeric lipid, PEG-GLFG-K(C16)2 (PEG-GLFG, polyethylene glycol-Gly-Leu-Phe-Gly-Lys(C16)2), was synthesized to enable controlled anticancer drug delivery using cathepsin B enzyme-responsive liposomes. The liposomes composed of PEG-GLFG/DOTAP (1,2-dioleoyl-3-trimethylammonium-propane (chloride salt))/DPPC (dipalmitoylphosphatidylcholine)/cholesterol were prepared and characterized at various ratios. The GLFG liposomes formed were stable liposomes and were degraded when acted upon by cathepsin B enzyme. Doxorubicin (Dox) loaded GLFG liposomes (GLFG/Dox) were observed to exert an effective anticancer effect on Hep G2 cells in vitro and inhibit cancer cell proliferation in a zebrafish model.
Highlights
Cancer is a disease involving the abnormal proliferation of cells with deleterious effects on human health
GLFG liposomes were prepared at 2 mg/mL in a 5 mM HEPES buffer
Free Dox and liposomes/Dox were treated in Hep G2 cells at 2.5 and 5 μM of Dox
Summary
Cancer is a disease involving the abnormal proliferation of cells with deleterious effects on human health. Chemotherapy and radiation are associated with high levels of cytotoxicity and risk of injury to normal cells [1] Conventional anticancer drugs such as doxorubicin, cisplatin, docetaxel, and gemcitabine, are used to treat cancer by inhibiting the growth and proliferation of cancer cells [2,3,4]. Nanoparticles can increase the water solubility of non-soluble drugs, protect genes from cellular enzymes, target specific cells, and regulate the release of therapeutic drugs Owing to these properties, nanoparticles have the potential to be used in medical devices for enhanced diagnosis and treatment of diseases [6,7,8]. 1S.cheSmchaetmic aptriecsenptraetisoenntoaftGioLnFGo/Df oxGlLipFoGso/Dmoexs liposomes (doxorubicin (doxorubicin loaded GLFG loaded GLFG (Gly-Leu-Phe-Gly) l(iGploys-oLmeue-sP) hfoer-Genlyz)ylmipeo-storimggeesr)efdordernuzgydmeeli-vtreirgyg. ered drug delivery
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