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A nanosystem for water-insoluble drugs prepared by a new technology, nanoparticulation using a solid lipid and supercritical fluid

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Abstract

While the number and diversity of lead compounds has increased with the development of science technologies, ca. 90 % of new chemical entities under development have shown low aqueous solubility, classified as class II or IV of the biopharmaceutics classification system (BCS). The low aqueous solubility hinders their clinical translations due to low bioavailability and dissolution-limited absorption of orally-administered drugs. Several technologies have been employed to improve the solubility of poorly water-soluble drugs. In this paper, a new method of nanoparticulation using fat and a supercritical fluid (NUFS) for the formulation of hydrophobic drugs was applied to solve the low solubility problem. A typical BCS class II drug, itraconazole, was selected and formulated with hydroxypropyl methylcellulose, emulsification, and anticoagulating agents for NUFS. The non-spherical itraconazole nanoparticles prepared by NUFS were ~300–500 nm in size with a ~15-fold improved dissolution rate compared to non-nanoparticles of itraconazole (i.e., raw itraconazole). In addition, a high drug content of ~46 % by weight and a drug loading efficiency greater than 85 % were achieved. Therefore, the new technology for nano-platforms could be a promising solution for solubilization of poorly water-soluble drugs, resulting in improved bioavailability.

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Acknowledgments

This research was supported by Chung-Ang University Research scholarship grants in 2009–2010.

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Authors and Affiliations

  1. College of Pharmacy, Chung-Ang University, Seoul, 155-756, Korea

    Joo Won Park, Jeong Min Yun & Kyung Teak Oh

  2. Bio-Synectics, Inc., Seoul, 153-803, Korea

    Joo Won Park & Kab Sig Kim

  3. Division of Biotechnology, The Catholic University of Korea, Gyeonggi-do, Seoul, 420-743, Korea

    Eun Seong Lee

  4. College of Pharmacy, SungKyunKwan University, Suwon, 440-746, Korea

    Yu Seok Youn

  5. College of Medicine, Department of Radiology and Research Institute of Radiological Science, Yonsei University, Seoul, 120-752, Korea

    Young Taik Oh

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  1. Joo Won Park
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Correspondence to Young Taik Oh or Kyung Teak Oh.

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Park, J.W., Yun, J.M., Lee, E.S. et al. A nanosystem for water-insoluble drugs prepared by a new technology, nanoparticulation using a solid lipid and supercritical fluid. Arch. Pharm. Res. 36, 1369–1376 (2013). https://doi.org/10.1007/s12272-013-0187-2

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