PDMS-b-PMOXA polymersomes for hepatocyte targeting and assessment of toxicity

Kiene, Klara and Schenk, Susanne H. and Porta, Fabiola and Ernst, Alexandra and Witzigmann, Dominik and Grossen, Philip and Huwyler, Jörg. (2017) PDMS-b-PMOXA polymersomes for hepatocyte targeting and assessment of toxicity. European Journal of Pharmaceutics and Biopharmaceutics, 119. pp. 322-332.

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Official URL: http://edoc.unibas.ch/55721/

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Nanoparticles, such as polymersomes, can be directed to the hepatic asialoglycoprotein receptor to achieve targeted drug delivery. In this study, we prepared asialofetuin conjugated polymersomes based on the amphiphilic di-block copolymer poly(dimethylsiloxane)-b-poly(2-methyloxazoline) (PDMS-b-PMOXA). They had an average diameter of 150nm and formed monodisperse vesicles. Drug encapsulation and sustained release was monitored using the hydrophilic model compound carboxyfluorescein. Asialoglycoprotein receptor specific uptake by HepG2 cells in vitro was energy dependent and could be competitively inhibited by the free targeting ligand. Mechanistic uptake studies revealed intracellular trafficking of asialofetuin conjugated polymersomes from early endosomes and to the lysosomal compartment. Polymersomes showed no toxicity in the MTT assay up to concentrations of 500μg/mL. In addition, acute toxicity and tolerability of our PDMS-b-PMOXA polymersome formulations was assessed in vivo using zebrafish embryos as a vertebrate screening model. In conclusion, a hepatocyte specific drug delivery system was designed, which is safe and biocompatible and which can be used to implement liver-specific targeting strategies.
Faculties and Departments:05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Pharmazie > Pharmaceutical Technology (Huwyler)
UniBasel Contributors:Huwyler, Jörg and Kiene, Klara and Schenk, Susanne and Porta, Fabiola and Witzigmann, Dominik and Grossen, Philip
Item Type:Article, refereed
Article Subtype:Research Article
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:20 Oct 2017 09:17
Deposited On:20 Oct 2017 09:17

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