Practical liposomal formulation for taxanes with polyethoxylated castor oil and ethanol with complete encapsulation efficiency and high loading efficiency

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

Research output: Contribution to journalArticle

3 Citations (Scopus)

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.

Original languageEnglish
Article number290
JournalNanomaterials
Volume7
Issue number10
DOIs
Publication statusPublished - Oct 1 2017

Fingerprint

Taxoids
docetaxel
Liposomes
Encapsulation
Ethanol
Paclitaxel
Hydrophobicity
polyethoxylated castor oil
Oils
Drug delivery
Antineoplastic Agents
Peptides
Phosphates
Pharmaceutical Preparations

Keywords

  • Cremophor EL
  • HER2
  • Liposomal drug delivery
  • Targeted drug delivery
  • Taxanes

ASJC Scopus subject areas

  • Materials Science(all)
  • Chemical Engineering(all)

Cite this

Practical liposomal formulation for taxanes with polyethoxylated castor oil and ethanol with complete encapsulation efficiency and high loading efficiency. / Shigehiro, Tsukasa; Masuda, Junko; Saito, Shoki; Khayrani, Apriliana C.; Jinno, Kazumasa; Seno, Akimasa; Vaidyanath, Arun; Mizutani, Akifumi; Kasai, Tomonari; Murakami, Hiroshi; Satoh, Ayano; Ito, Tetsuya; Hamada, Hiroki; Seno, Yuhki; Mandai, Tadakatsu; Seno, Masaharu.

In: Nanomaterials, Vol. 7, No. 10, 290, 01.10.2017.

Research output: Contribution to journalArticle

Shigehiro, Tsukasa ; Masuda, Junko ; Saito, Shoki ; Khayrani, Apriliana C. ; Jinno, Kazumasa ; Seno, Akimasa ; Vaidyanath, Arun ; Mizutani, Akifumi ; Kasai, Tomonari ; Murakami, Hiroshi ; Satoh, Ayano ; Ito, Tetsuya ; Hamada, Hiroki ; Seno, Yuhki ; Mandai, Tadakatsu ; Seno, Masaharu. / Practical liposomal formulation for taxanes with polyethoxylated castor oil and ethanol with complete encapsulation efficiency and high loading efficiency. In: Nanomaterials. 2017 ; Vol. 7, No. 10.
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