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Shigehiro T, Masuda J, Saito S, et al. Practical Liposomal Formulation for Taxanes with Polyethoxylated Castor Oil and Ethanol with Complete Encapsulation Efficiency and High Loading Efficiency. Nanomaterials (Basel). 2017;7(10)doi: 10.3390/nano7100290.
Shigehiro, T., Masuda, J., Saito, S., Khayrani, A. C., Jinno, K., Seno, A., Vaidyanath, A., Mizutani, A., Kasai, T., Murakami, H., Satoh, A., Ito, T., Hamada, H., Seno, Y., Mandai, T., & Seno, M. (2017). Practical Liposomal Formulation for Taxanes with Polyethoxylated Castor Oil and Ethanol with Complete Encapsulation Efficiency and High Loading Efficiency. Nanomaterials (Basel, Switzerland), 7(10), . https://doi.org/10.3390/nano7100290
Shigehiro, Tsukasa, et al. "Practical Liposomal Formulation for Taxanes with Polyethoxylated Castor Oil and Ethanol with Complete Encapsulation Efficiency and High Loading Efficiency." Nanomaterials (Basel, Switzerland) vol. 7,10 (2017). doi: https://doi.org/10.3390/nano7100290
Shigehiro T, Masuda J, Saito S, Khayrani AC, Jinno K, Seno A, Vaidyanath A, Mizutani A, Kasai T, Murakami H, Satoh A, Ito T, Hamada H, Seno Y, Mandai T, Seno M. Practical Liposomal Formulation for Taxanes with Polyethoxylated Castor Oil and Ethanol with Complete Encapsulation Efficiency and High Loading Efficiency. Nanomaterials (Basel). 2017 Sep 23;7(10). doi: 10.3390/nano7100290. PMID: 28946623; PMCID: PMC5666455.
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Nanomaterials (Basel). 2017 Sep 23;7(10). doi: 10.3390/nano7100290.

Practical Liposomal Formulation for Taxanes with Polyethoxylated Castor Oil and Ethanol with Complete Encapsulation Efficiency and High Loading Efficiency.

Nanomaterials (Basel, Switzerland)

Tsukasa Shigehiro, Junko Masuda, Shoki Saito, Apriliana C Khayrani, Kazumasa Jinno, Akimasa Seno, Arun Vaidyanath, Akifumi Mizutani, Tomonari Kasai, Hiroshi Murakami, Ayano Satoh, Tetsuya Ito, Hiroki Hamada, Yuhki Seno, Tadakatsu Mandai, Masaharu Seno

Affiliations

  1. Department of Medical Bioengineering, Graduate School of Natural Science and Technology, Okayama University, Okayama 700-0082, Japan. [email protected].
  2. Japan Society for the Promotion of Science, Tokyo 102-0083, Japan. [email protected].
  3. Department of Medical Bioengineering, Graduate School of Natural Science and Technology, Okayama University, Okayama 700-0082, Japan. [email protected].
  4. Department of Medical Bioengineering, Graduate School of Natural Science and Technology, Okayama University, Okayama 700-0082, Japan. [email protected].
  5. Department of Medical Bioengineering, Graduate School of Natural Science and Technology, Okayama University, Okayama 700-0082, Japan. [email protected].
  6. Department of Medical Bioengineering, Graduate School of Natural Science and Technology, Okayama University, Okayama 700-0082, Japan. [email protected].
  7. Department of Medical Bioengineering, Graduate School of Natural Science and Technology, Okayama University, Okayama 700-0082, Japan. [email protected].
  8. Department of Medical Bioengineering, Graduate School of Natural Science and Technology, Okayama University, Okayama 700-0082, Japan. [email protected].
  9. Department of Medical Bioengineering, Graduate School of Natural Science and Technology, Okayama University, Okayama 700-0082, Japan. [email protected].
  10. Department of Medical Bioengineering, Graduate School of Natural Science and Technology, Okayama University, Okayama 700-0082, Japan. [email protected].
  11. Department of Medical Bioengineering, Graduate School of Natural Science and Technology, Okayama University, Okayama 700-0082, Japan. [email protected].
  12. Department of Medical Bioengineering, Graduate School of Natural Science and Technology, Okayama University, Okayama 700-0082, Japan. [email protected].
  13. Ensuiko Sugar Refining Co., Ltd., Tokyo 102-0083, Japan. [email protected].
  14. Faculty of Science, Okayama University of Science, Okayama 700-0082, Japan. [email protected].
  15. Faculty of Life Science, Kurashiki University of Science and the Arts, Kurashiki 712-8505, Japan. [email protected].
  16. Faculty of Life Science, Kurashiki University of Science and the Arts, Kurashiki 712-8505, Japan. [email protected].
  17. Department of Medical Bioengineering, Graduate School of Natural Science and Technology, Okayama University, Okayama 700-0082, Japan. [email protected].

PMID: 28946623 PMCID: PMC5666455 DOI: 10.3390/nano7100290

Abstract

Taxanes including paclitaxel and docetaxel are effective anticancer agents preferably sufficient for liposomal drug delivery. However, the encapsulation of these drugs with effective amounts into conventional liposomes is difficult due to their high hydrophobicity. Therefore, an effective encapsulation strategy for liposomal taxanes has been eagerly anticipated. In this study, the mixture of polyethoxylated castor oil (Cremophor EL) and ethanol containing phosphate buffered saline termed as CEP was employed as a solvent of the inner hydrophilic core of liposomes where taxanes should be incorporated. Docetaxel-, paclitaxel-, or 7-oxacetylglycosylated paclitaxel-encapsulating liposomes were successfully prepared with almost 100% of encapsulation efficiency and 29.9, 15.4, or 29.1 mol% of loading efficiency, respectively. We then applied the docetaxel-encapsulating liposomes for targeted drug delivery. Docetaxel-encapsulating liposomes were successfully developed HER2-targeted drug delivery by coupling HER2-specific binding peptide on liposome surface. The HER2-targeting liposomes exhibited HER2-specific internalization and enhanced anticancer activity in vitro. Therefore, we propose the sophisticated preparation of liposomal taxanes using CEP as a promising formulation for effective cancer therapies.

Keywords: Cremophor EL; HER2; liposomal drug delivery; targeted drug delivery; taxanes

Conflict of interest statement

One of the authors, Tetsuya Ito, is an employee of Ensuiko Sugar Refining Co., Ltd. Okayama University, Ensuiko Sugar Refining Co., Ltd., and Hiroki Hamada are the applicants of the Japanese Patent No

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