Strategy for Increasing Drug Solubility and Efficacy through Covalent Attachment to Polyvalent DNA–Nanoparticle Conjugates

Paclitaxel, a potent chemotherapeutic utilized in a variety of cancers, can be limited in its effectiveness due to inherent insolubility in aqueous media and acquired chemoresistance within certain cells. An approach has been developed for increasing Paclitaxel solubility and effectiveness by covale...

Full description

Saved in:
Bibliographic Details
Published in:ACS nano 2011-09, Vol.5 (9), p.6962-6970
Main Authors: Zhang, Xue-Qing, Xu, Xiaoyang, Lam, Robert, Giljohann, David, Ho, Dean, Mirkin, Chad A
Format: Article
Language:English
Subjects:
Antineoplastic Agents, Phytogenic - chemistry
Attachment
Cell Line, Tumor
Chemical compounds
Conjugates
Covalence
Deoxyribonucleic acid
DNA - chemistry
Drugs
Fluorescent Dyes - chemistry
Gold - chemistry
Humans
In Situ Nick-End Labeling
Media
Metal Nanoparticles
Paclitaxel - chemistry
Solubility
Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
Strategy
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Paclitaxel, a potent chemotherapeutic utilized in a variety of cancers, can be limited in its effectiveness due to inherent insolubility in aqueous media and acquired chemoresistance within certain cells. An approach has been developed for increasing Paclitaxel solubility and effectiveness by covalent attachment to gold nanoparticles via DNA linkers. The resulting conjugates are highly soluble in aqueous buffer, exhibiting greater than a 50-fold increase in solubility over the unconjugated drug. DNA linkers are labeled with a fluorophore, which affords a convenient means of visualizing resultant conjugates within cells. Internalized conjugates demonstrate increased activity as compared with free drug across a variety of cell types, including a Paclitaxel-resistant cell line. Attachment to DNA–nanoparticle conjugates may become a general strategy for solubilizing and enhancing a wide variety of therapeutic agents in aqueous media.
ISSN:1936-0851
1936-086X
DOI:10.1021/nn201446c