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Article

Encapsulation of Paclitaxel in Macromolecular Nanoshells

Supporting Info

Alisar S. Zahr^† and Michael V. Pishko*^‡

Departments of Chemical Engineering, Materials Science and Engineering, and Chemistry, The Pennsylvania State University, University Park, Pennsylvania 16802

Biomacromolecules, 2007, 8 (6), pp 2004–2010

DOI: 10.1021/bm070177m

Publication Date (Web): May 19, 2007

†

Department of Chemical Engineering.

Author to whom correspondence should be addressed. E-mail: mpishko@engr.psu.edu.

‡

Departments of Chemical Engineering, Materials Science and Engineering, and Chemistry.

Abstract

An electrostatic layer-by-layer self-assembly technique was used to encapsulate solid core paclitaxel nanoparticles within a polymeric nanometer-scale shell. This approach provides a new strategy for the development of polymeric vehicles that control drug release and target diseased tissues and cells specific to the ailment, such as breast cancer. Core paclitaxel nanoparticles, 153 ± 28 nm in diameter, were prepared using a modified nanoprecipitation technique. A nanoshell composed of multilayered polyelectrolytes, poly(allylamine hydrochloride) and poly(styrene-4-sulfonate) was assembled stepwise onto core charged drug nanoparticles. In vitro studies were performed to determine the anticancer activity of paclitaxel core−shell nanoparticles. Paclitaxel core−shell nanoparticles induced cell cycle arrest in the G2/M phase after 24 and 48 h of incubation with a human breast carcinoma cell line, MCF-7. Changes in MCF-7 cell morphology, fragmentation of the nucleus, and loss of cell−cell contacts indicated that the cells responded to paclitaxel core nanoparticles upon treatment for 24 and 48 h. Cells arrested in G2/M phase illustrated abnormal microtubule and actin cytoskeleton morphology. The core−shell drug nanoparticles fabricated using this procedure provide a new approach in the delivery of paclitaxel devoid of Cremophor EL, a solvent that causes adverse side effects in patients undergoing chemotherapy for treatment of metastasized mammary cancers.

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