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Preparation Nanocrystals of Poorly Soluble Plant Compounds Using an Ultra-Small-Scale Approach

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Abstract

The usage of downscaling technology for producing nanosuspensions/nanocrystals can be beneficial for formulation development, which has attracted increased attention recently. An ultra-small bead milling method (5 mg compound per batch, smallest scale to date) was tested to produce nanocrystals of four poorly soluble plant compounds, i.e., quercetin, rutin, resveratrol, and hesperidin. A particle size of ranged from 200 to 500 nm was obtained for nanosuspensions of four compounds and the stabilizer selection could be achieved within 2 h by using this ultra-small bead milling method. Six months stability was observed for selected samples. In addition, the scalability of the ultra-small lab-scale milling was confirmed when it was conducted under optimal conditions. A simple and fast ultra-small-scale approach for nanosuspension production was established. Freeze-drying was applied to convert nanosuspensions into solid forms. Finally, freeze-dried intermediates with good redispersity and physical stability were obtained, which could be used for further application.

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Acknowledgements

We are grateful for financial support from the Shandong Provincial Natural Science Foundation, China (No. ZR2014HP023).

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Authors and Affiliations

  1. Department of Pharmaceutical Engineering, Qingdao University of Science and Technology, Qingdao, China

    Tao Liu, Guili Yao & Xiaotian Liu

  2. Department of Internal Medicine, Qingdao Shibei District People Hospital, Qingdao, China

    Haipeng Yin

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  1. Tao Liu
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  2. Guili Yao
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  3. Xiaotian Liu
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Correspondence to Tao Liu.

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Liu, T., Yao, G., Liu, X. et al. Preparation Nanocrystals of Poorly Soluble Plant Compounds Using an Ultra-Small-Scale Approach. AAPS PharmSciTech 18, 2610–2617 (2017). https://doi.org/10.1208/s12249-017-0742-0

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