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Effects of Structure of β-Cyclodextrin-Containing Polymers on Gene Delivery

Hwang, Suzie J. and Bellocq, Nathalie C. and Davis, Mark E. (2001) Effects of Structure of β-Cyclodextrin-Containing Polymers on Gene Delivery. Bioconjugate Chemistry, 12 (2). pp. 280-290. ISSN 1043-1802. doi:10.1021/bc0001084.

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Linear cationic β-cyclodextrin-based polymers (βCDPs) are capable of forming polyplexes with nucleic acids and transfecting cultured cells. The βCDPs are synthesized by the condensation of a diamino-cyclodextrin monomer A with a diimidate comonomer B. In this paper, the effects of polymer structure on polyplex formation, in vitro transfection efficiency and toxicity are elucidated. By comparison of the βCDPs to polyamidines lacking cyclodextrins, the inclusion of a cyclodextrin moiety in the comonomer A units reduces the IC50s of the polymer by up to 3 orders of magnitude. The spacing between the cationic amidine groups is also important. Different polymers with 4, 5, 6, 7, 8, and 10 methylene units (βCDP4, 5, 6, 7, 8, and 10) in the comonomer B molecule are synthesized. Transfection efficiency is dependent on comonomer B length with up to 20-fold difference between polymers. Optimum transfection is achieved with the βCDP6 polymer. In vitro toxicity varied by 1 order of magnitude and the lowest toxicity is observed with βCDP8. The LD40 of the βCDP6 to mice is 200 mg/kg, making this polymer a promising agent for in vivo gene delivery applications.

Item Type:Article
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Hwang, Suzie J.0000-0003-1443-4996
Davis, Mark E.0000-0001-8294-1477
Alternate Title:Effects of structure of beta-cyclodextrin-containing polymers on gene delivery.
Additional Information:© 2001 American Chemical Society. Received September 8, 2000; Revised Manuscript Received December 21, 2000. S.J.H. thanks the Whitaker Foundation for a doctoral fellowship.
Funding AgencyGrant Number
Whitaker FoundationUNSPECIFIED
Issue or Number:2
Record Number:CaltechAUTHORS:20170125-084653375
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Official Citation:Effects of Structure of β-Cyclodextrin-Containing Polymers on Gene Delivery Suzie J. Hwang,†, Nathalie C. Bellocq,† and, and Mark E. Davis* Bioconjugate Chemistry 2001 12 (2), 280-290 DOI: 10.1021/bc0001084
Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:73698
Deposited By: Ruth Sustaita
Deposited On:25 Jan 2017 19:10
Last Modified:11 Nov 2021 05:20

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