mPEG-PCL from PolySciTech used in development of docetaxel/osthol dual-drug delivery system for treatment of cancer

 

The treatment of cancer requires delivery of medicinal compounds to the site of cancer itself. However, often, the drugs used for cancer therapy have very poor water solubility and bad bioavailability (poor absorption). One means to rectify this is to utilize block copolymers to form micelles with interior hydrophobic portions (often degradable polyesters such as PLA, PCL, or PLGA) surrounded by hydrophilic exterior (often polyethylene glycol). In this case the hydrophobic drugs can be loaded into the oil-soluble interior and the micelle as a whole can circulate more freely in the bloodstream for improved uptake. Recently, Researchers at Chungbuk National University and Sookmyung Women’s University (Korea) used mPEG-PCL (AK073) from PolySciTech (www.polyscitech.com) to create micelles loaded with docetaxel and osthol for cancer therapy uses. This research holds promise to provide for improved cancer therapies in the future. Read More: Jo, Min Jeong, Yu Jin Lee, Chun-Woong Park, Youn Bok Chung, Jin-Seok Kim, Mi Kyeong Lee, and Dae Hwan Shin. "Evaluation of the Physicochemical Properties, Pharmacokinetics, and In Vitro Anticancer Effects of Docetaxel and Osthol Encapsulated in Methoxy Poly (ethylene glycol)-b-Poly (caprolactone) Polymeric Micelles." International Journal of Molecular Sciences 22, no. 1 (2021): 231. https://www.mdpi.com/1422-0067/22/1/231

“Docetaxel (DTX), a taxane-based anticancer drug, and osthol (OTH), a coumarin-derivative compound, have shown anticancer effects against different types of cancers through various mechanisms. However, these drugs have low solubility in water and low oral bioavailability, and thus their clinical application is difficult. To overcome these problems, we encapsulated DTX and OTH in methoxy poly(ethylene glycol)-b-poly(caprolactone) (mPEG-b-PCL) and conducted studies in vitro and in vivo. We selected a 1:4 ratio as the optimal ratio of DTX and OTH, through combination index analysis in A549 cancer cells, and prepared micelles to evaluate the encapsulation efficiency, drug loading, particle size, and zeta potential. The in vitro drug-release profile showed that DTX/OTH-loaded mPEG-b-PCL micelles could slowly release DTX and OTH. In the clonogenic assay, DTX/OTH-loaded mPEG-b-PCL micelles showed 3.7 times higher inhibitory effect than the DTX/OTH solution. Pharmacokinetic studies demonstrated that micelles in combination with DTX and OTH exhibited increased area under curve and decreased clearance values, as compared with single micelles. Keywords: docetaxel; osthol; mPEG-b-PCL polymeric micelles; combination therapy; pharmacokinetics”