Development of Safe and Potent Oil-in-Water Emulsion of Paclitaxel to Treat Peritoneal Dissemination

Ken ichi Ogawara, Yoshiko Fukuoka, Yuta Yoshizawa, Toshikiro Kimura, Kazutaka Higaki

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

To develop a safer and more potent paclitaxel (PTX) formulation, we prepared various oil-in-water emulsions by using egg phosphatidylcholine, Tween 80, and a mixture of triglycerides with different fatty acid chain lengths as the cosurfactant, surfactant, and oil phase component, respectively. The mean particle diameters of the PTX-emulsions prepared were around 100 nm. The PTX-emulsions did not provoke histamine release from rat mast cells and did not show any significant hemolytic activity, suggesting that PTX-emulsions are biocompatible. In vivo antitumor activity after single intraperitoneal injection of PTX-emulsions to ascites tumor-bearing mice revealed that the formulation containing tricaproin and triacetin (3:1, wt/wt, PTX-emulsion B) significantly prolonged the survival time and suppressed the accumulation of ascites fluid. Two distinct in vitro release studies showed that the release of PTX from emulsion B was significantly faster than those from other preparations. These results indicate that the adequately sustained PTX release would lead to potent in vivo antitumor activity and that PTX-emulsion B would offer an alternative approach to treat peritoneal dissemination.

Original languageEnglish
Pages (from-to)1143-1148
Number of pages6
JournalJournal of Pharmaceutical Sciences
Volume106
Issue number4
DOIs
Publication statusPublished - Apr 1 2017

Fingerprint

Paclitaxel
Emulsions
Oils
Water
Ascites
Triacetin
Polysorbates
Histamine Release
Intraperitoneal Injections
Phosphatidylcholines
Mast Cells
Surface-Active Agents
Ovum
Triglycerides
Fatty Acids

Keywords

  • biocompatibility
  • cancer
  • controlled release/delivery
  • drug delivery
  • emulsion/microemulsion
  • surfactants

ASJC Scopus subject areas

  • Medicine(all)
  • Pharmaceutical Science

Cite this

Development of Safe and Potent Oil-in-Water Emulsion of Paclitaxel to Treat Peritoneal Dissemination. / Ogawara, Ken ichi; Fukuoka, Yoshiko; Yoshizawa, Yuta; Kimura, Toshikiro; Higaki, Kazutaka.

In: Journal of Pharmaceutical Sciences, Vol. 106, No. 4, 01.04.2017, p. 1143-1148.

Research output: Contribution to journalArticle

Ogawara, Ken ichi ; Fukuoka, Yoshiko ; Yoshizawa, Yuta ; Kimura, Toshikiro ; Higaki, Kazutaka. / Development of Safe and Potent Oil-in-Water Emulsion of Paclitaxel to Treat Peritoneal Dissemination. In: Journal of Pharmaceutical Sciences. 2017 ; Vol. 106, No. 4. pp. 1143-1148.
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