Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2010 Jul 14;145(2):116-23.
doi: 10.1016/j.jconrel.2010.04.019. Epub 2010 Apr 24.

Hydrophobic pharmaceuticals mediated self-assembly of beta-cyclodextrin containing hydrophilic copolymers: novel chemical responsive nano-vehicles for drug delivery

Jianxiang Zhang  1 , Kristin Ellsworth, Peter X Ma
Affiliations

Hydrophobic pharmaceuticals mediated self-assembly of beta-cyclodextrin containing hydrophilic copolymers: novel chemical responsive nano-vehicles for drug delivery

Jianxiang Zhang et al. J Control Release. .

Abstract

Double hydrophilic copolymers with one polyethylene glycol (PEG) block and one beta-cyclodextrin (beta-CD) flanking block (PEG-b-PCDs) were synthesized through the post-modification of macromolecules. The self-assembly of PEG-b-PCDs in aqueous solutions was initially studied by a fluorescence technique. This measurement together with AFM and TEM characterizations demonstrated the formation of nanoparticles in the presence of lipophilic small molecules. The host-guest interaction between the beta-CD unit of a host copolymer and the hydrophobic group of a guest molecule was found to be the driving force for the observed self-assembly. This spontaneous assembly upon loading of guest molecules was also observed for hydrophobic drugs with various chemical structures. Relatively high drug loading was achieved by this approach. Desirable encapsulation was also achieved for the hydrophobic drugs that cannot efficiently interact with free beta-CD. In vitro release studies suggested that the payload in nano-assemblies could be released in a sustained manner. In addition, both the fluorescence measurement and the in vitro drug release studies suggested that these nano-assemblies mediated by the inclusion complexation exhibited a chemical sensitivity. The release of payload can be accelerated upon the triggering by hydrophobic guest molecules or free beta-CD molecules. These results support the potential applications of the synthesized copolymers for the delivery of hydrophobic drugs.

PubMed Disclaimer

Figures

Fig. 1
Fig. 1
TEM images of PEG-b-PCD-3 assemblies containing (a) IBU, (b) IND, (c) RAP, and (d) DEX. Dialysis method was employed to prepare drug containing assemblies. For all the drugs, the employed drug/polymer feed ratio was 2:20.
Fig. 1
Fig. 1
TEM images of PEG-b-PCD-3 assemblies containing (a) IBU, (b) IND, (c) RAP, and (d) DEX. Dialysis method was employed to prepare drug containing assemblies. For all the drugs, the employed drug/polymer feed ratio was 2:20.
Fig. 2
Fig. 2
RAP containing assemblies based on PEG-b-PCDs. TEM images of PEG-b-PCD-3 derived assemblies with feed ratios of (a) 3.5:20, (b) 5:20 and (c) 10:20. (d) SEM image of assemblies based on PEG-b-PCD-3 with a feed ratio of 5:20. Assemblies originated from PEG-b-PCD-1 (e) and PEG-b-PCD-2 (f) with a feed ratio of 5:20.
Fig. 2
Fig. 2
RAP containing assemblies based on PEG-b-PCDs. TEM images of PEG-b-PCD-3 derived assemblies with feed ratios of (a) 3.5:20, (b) 5:20 and (c) 10:20. (d) SEM image of assemblies based on PEG-b-PCD-3 with a feed ratio of 5:20. Assemblies originated from PEG-b-PCD-1 (e) and PEG-b-PCD-2 (f) with a feed ratio of 5:20.
Fig. 3
Fig. 3
Pyrene emission spectra in the aqueous solutions of PEG-b-PCD-3 in the presence of various additives (a) ADCA, polymer concentration was 2.0 mg/ml; and (b) β-CD, polymer concentration was 1.5 mg/ml.
Fig. 4
Fig. 4
In vitro release profiles of PEG-b-PCD-3 based assemblies containing various drugs (a) C102, (b) DEX, (c) IND, and (d) IBU.
Fig. 5
Fig. 5
In vitro release profiles of PEG-b-PCD-3 based assemblies in the presence of various chemicals.
See this image and copyright information in PMC

References

    1. Wu Y, Sefah K, Liu H, Wang R, Tan W. DNA aptamer–micelle as an efficient detection/delivery vehicle toward cancer cells. Proc Natl Acad Sci U S A. 2010;107:5–10. - PMC - PubMed
    1. Peters D, Kastantin M, Kotamraju VR, Karmali PP, Gujraty K, Tirrell M, Ruoslahti E. Targeting atherosclerosis by using modular, multifunctional micelles. Proc Natl Acad Sci U S A. 2009;106:9815–9819. - PMC - PubMed
    1. Ruenraroengsak P, Cook JM, Florence AT. Nanosystem drug targeting: Facing up to complex realities. J Control Release. 2010;141:265–276. - PubMed
    1. Kabanov AV, Gendelman HE. Nanomedicine in the diagnosis and therapy of neuro degenerative disorders. Prog Polym Sci. 2007;32:1054–1082. - PMC - PubMed
    1. Sethuraman VA, Lee MC, Bae YH. A biodegradable pH-sensitive micelle system for targeting acidic solid tumors. Pharm Res. 2008;25:657–666. - PubMed

Publication types

MeSH terms