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Multicomponent Amorphous Nanofibers Electrospun from Hot Aqueous Solutions of a Poorly Soluble Drug

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ABSTRACT

Purpose

To design and fabricate multicomponent amorphous electrospun nanofibers for synergistically improving the dissolution rate and permeation profiles of poorly water-soluble drugs.

Methods

Nanofibers were designed to be composed of a poorly water soluble drug, helicid, a hydrophilic polymer polyvinylpyrrolidone as filament-forming matrix, sodium dodecyl sulfate as transmembrane enhancer and mannitol as taste masking agent, and were prepared from hot aqueous co-dissolving solutions of them. An elevated temperature electrospinning process was developed to fabricate the composite nanofibers, which were characterized using FESEM, DSC, XRD, ATR-FTIR, in vitro dissolution and permeation tests.

Results

The composite nanofibers were homogeneous with smooth surfaces and uniform structure, and the components were combined together in an amorphous state because of the favorable interactions such as hydrogen bonding, electrostatic interaction and hydrophobic interactions among them. In vitro dissolution and permeation tests demonstrated that the composite nanofibers had a dissolution rate over 26-fold faster than that of crude helicid particles and a 10-fold higher permeation rate across sublingual mucosa.

Conclusions

A new type of amorphous material in the form of nanofibers was prepared from hot aqueous solutions of multiple ingredients using an electrospinning process. The amorphous nanofibers were able to improve the dissolution rate and permeation rate of helicid.

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ACKNOWLEDGEMENTS

This work was financially supported by China Postdoctoral Science Foundation Project (Special NO. 200902195) and UK-CHINA Joint Laboratory for Therapeutic Textiles.

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Authors and Affiliations

  1. College of Chemistry, Chemical Engineering and Biotechnology, Donghua University, Shanghai, 201620, China

    Deng-Guang Yu & Li-Min Zhu

  2. College of Information Science &Technology, Beijing University of Chemical Technology, Beijing, 100029, China

    Li-Dong Gao

  3. Institute for Health Research and Policy, London Metropolitan University, London, N7 8DB, UK

    Kenneth White & Christopher Branford-White

  4. School of Pharmacy, Fudan University, Shanghai, 201203, China

    Wei-Yue Lu

Authors
  1. Deng-Guang Yu
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  2. Li-Dong Gao
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  3. Kenneth White
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  4. Christopher Branford-White
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  5. Wei-Yue Lu
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  6. Li-Min Zhu
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Correspondence to Deng-Guang Yu or Li-Min Zhu.

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Yu, DG., Gao, LD., White, K. et al. Multicomponent Amorphous Nanofibers Electrospun from Hot Aqueous Solutions of a Poorly Soluble Drug. Pharm Res 27, 2466–2477 (2010). https://doi.org/10.1007/s11095-010-0239-y

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  • DOI: https://doi.org/10.1007/s11095-010-0239-y

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