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New Class of Polymers for the Delivery of Macromolecular Therapeutics

Gonzalez, Hector and Hwang, Sue Jean and Davis, M. E. (1999) New Class of Polymers for the Delivery of Macromolecular Therapeutics. Bioconjugate Chemistry, 10 (6). pp. 1068-1074. ISSN 1043-1802. doi:10.1021/bc990072j.

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Cationic polymers show promise for the in vitro and in vivo delivery of macromolecular therapeutics. Known cationic polymers, e.g., poly(L)lysine (PLL) and polyethylenimine (PEI), have been employed in native and modified forms for the delivery of plasmid DNA (pDNA) and reveal varying levels of toxicity. Here, we report the preparation of a new class of cationic polymers that are specifically designed to deliver macromolecular therapeutics. Linear, cationic, β-cyclodextrin (β-CD)-containing polymers (CD-polymers) are synthesized by copolymerizing difunctionalized β-CD monomers (AA) with other difunctionalized comonomers (BB) such that an AABBAABB product is formed. The β-CD polymers are able to bind ∼5 kbp pDNA above polymer to DNA (+/−) charge ratios of 1.5, compact the bound pDNA into particles of approximately 100−150 nm in size at charge ratios above 5+/−, and transfect cultured cells at charge ratios above 10+/−. In vitro transfections with the new β-CD-polymers are comparable to the best results obtained in our hands with PEI and Lipofectamine. Some cell line-dependent toxicities are observed for serum-free transfections; however, no toxicity is revealed at charge ratios as high as 70+/− in transfections conducted in 10% serum. Single IV and IP doses as high as 200 mg/kg in mice showed no mortalities.

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Davis, M. E.0000-0001-8294-1477
Additional Information:© 1999 American Chemical Society. Received June 9, 1999; Revised Manuscript Received August 6, 1999. Publication Date (Web): September 24, 1999. This work was partially supported by the Colvin Foundation and S.J.H. thanks the Whitaker Foundation for a doctoral fellowship. We also thank Pat Koen for his assistance with the transmission electron microscope.
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Colvin FoundationUNSPECIFIED
Whitaker FoundationUNSPECIFIED
Issue or Number:6
Record Number:CaltechAUTHORS:20171107-083706407
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Official Citation:New Class of Polymers for the Delivery of Macromolecular Therapeutics. Hector Gonzalez, Sue Jean Hwang, and M. E. Davis. Bioconjugate Chemistry 1999 10 (6), 1068-1074. DOI: 10.1021/bc990072j
Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:83021
Deposited By: Tony Diaz
Deposited On:07 Nov 2017 18:44
Last Modified:15 Nov 2021 19:54

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