Angiopep2-functionalized polymersomes for targeted doxorubicin delivery to glioblastoma cells

Figueiredo, Patricia and Balasubramanian, Vimalkumar and Shahbazi, Mohammad-Ali and Correia, Alexandra and Wu, Dalin and Palivan, Cornelia G. and Hirvonen, Jouni T. and Santos, Helder A.. (2016) Angiopep2-functionalized polymersomes for targeted doxorubicin delivery to glioblastoma cells. International Journal of Pharmaceutics, 511 (2). pp. 794-803.

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Official URL: http://edoc.unibas.ch/52593/

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A targeted drug delivery nanosystem for glioblastoma multiforme (GBM) based on polymersomes (Ps) made of poly(dimethylsiloxane)-poly(2-methyloxazoline) (PDMS-PMOXA) diblock copolymers was developed to evaluate their potential to actively target brain cancer cells and deliver anticancer drugs. Angiopep2 was conjugated to the surface of preformed Ps to target the low density lipoprotein receptor related protein I that are overexpressed in blood brain barrier (BBB) and glioma cells. The conjugation efficiency yield for angiopep2 was estimated to be 24%. The angiopep2-functionalized Ps showed no cellular toxicity after 24 h and enhanced the cellular uptake around 5 times more in U87MG glioblastoma cells compared to the non-targeted Ps. The encapsulation efficiency of doxorubicin (DOX) in Ps was 13% by co-solvent method, compared to a film rehydration method (4%). The release profiles of the DOX from Ps showed a release of 42% at pH 5.5 and 40% at pH 7.4 after 24 h, indicating that Ps can efficiently retain the DOX with a slow release rate. Furthermore, the in vitro antiproliferative activity of DOX-loaded Ps-Angiopep2 showed enhanced toxicity to U87MG glioblastoma cells, compared to non -targeted Ps. Overall, our in vitro results suggested that angiopep2-conjugated Ps can be used as nanocarriers for efficient targeted DOX delivery to glioblastoma cells.
Faculties and Departments:05 Faculty of Science > Departement Chemie > Chemie > Physikalische Chemie (Palivan)
UniBasel Contributors:Palivan, Cornelia G
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:14 Jun 2017 09:18
Deposited On:14 Jun 2017 09:18

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