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

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.

SUBMITTER: Zhang J

PROVIDER: S-EPMC2902716 | biostudies-other | 2010 Jul

REPOSITORIES: biostudies-other

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

Zhang Jianxiang J Ellsworth Kristin K Ma Peter X PX

Journal of controlled release : official journal of the Controlled Release Society 20100424 2

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 ...[more]

PMID: 20417674

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Project description:Tailor-made and designed micro- and nanocarriers can bring significant benefits over their traditional macroscopic counterparts in drug delivery applications. For the successful loading and subsequent release of bioactive compounds, carriers should present a high loading capacity, trigger release mechanisms, biodegradability and biocompatibility. Hydrophobic drug molecules can accumulate in fat tissues, resulting in drawbacks for the patient's recovery. To address these issues, we propose to combine the advantageous features of both host molecules (cyclodextrin) and calcium carbonate (CaCO3) particles in order to load hydrophobic chemicals. Herein, hybrid cyclodextrin-CaCO3 micro- to nano-particles have been fabricated by combining Na2CO3 solution and CaCl2 solution in the presence of an additive, namely poly (vinylsulfonic acid) (PVSA) or glycerol (gly). By investigating experimental parameters and keeping the Na2CO3 and CaCl2 concentrations constant (0.33 M), we have evidenced that the PVSA or gly concentration and mixing time have a direct impact on the final cyclodextrine-CaCO3 particle size. Indeed, by increasing the concentration of PVSA (5 mM to 30 mM) or gly (0.7 mM to 4 mM) or the reaction time (from 10 min to 4 h), particles with a size of 200 nm could be reached. Interestingly, the vaterite or calcite form could also be selected, according to the experimental conditions. We hypothesised that the incorporation of PVSA or gly into the precipitation reaction might reduce the nucleation rate by sequestering Ca2+. The obtained particles have been found to keep their crystal structure and surface charge after storage in aqueous media for at least 6 months. In the context of improving the therapeutic benefit of hydrophobic drugs, the developed particles were used to load the hydrophobic drug tocopherol acetate. The resulting particles are biocompatible and highly stable in a physiological environment (pH 7.4, 0.15 M NaCl). A selective release of the cargo is observed in acidic media (pH lower than 5).

Dataset Information

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

Publications

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

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