Issue 3, 2012

Nanoparticledrug delivery enhances the cytotoxicity of hydrophobic–hydrophilic drug conjugates

Abstract

We report a drug conjugation approach to concurrently load both hydrophobic and hydrophilic drugs into the same drug delivery nanocarrier in a precisely controllable manner. Using paclitaxel as a model hydrophobic drug and cisplatin as a model hydrophilic drug, we demonstrate the synthesis and characterization of a paclitaxel–cisplatin conjugate via a hydrolysable linker and its easy encapsulation by a lipidpolymer hybrid nanoparticle with controllable drug loading yield and drug release profile. The cytotoxicity of the resulting drug conjugate loaded nanoparticles against human ovarian cancer cells is investigated and compared to that of unencapsulated free drug conjugates. It is found that the cellular cytotoxicity of the hydrophobic–hydrophilic drug conjugates is significantly improved after being encapsulated into the nanoparticles. This is likely because the nanoparticles facilitate the intracellular entry of the amphiphilic drug conjugates and thus overcome their poor transport ability across the lipid bilayer structured cellular membranes.

Graphical abstract: Nanoparticle drug delivery enhances the cytotoxicity of hydrophobic–hydrophilic drug conjugates

Supplementary files

Article information

Article type
Paper
Submitted
08 Aug 2011
Accepted
04 Oct 2011
First published
10 Nov 2011

J. Mater. Chem., 2012,22, 994-999

Nanoparticle drug delivery enhances the cytotoxicity of hydrophobic–hydrophilic drug conjugates

S. Aryal, C. Jack Hu, V. Fu and L. Zhang, J. Mater. Chem., 2012, 22, 994 DOI: 10.1039/C1JM13834K

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