Preparation and Characterization of SN-38-Encapsulated Phytantriol Cubosomes Containing α-Monoglyceride Additives

• Ali Md Ashraf

  Laboratory of Pharmaceutical Engineering & Drug Delivery Science, Graduate School of Integrated Pharmaceutical & Nutritional Sciences, University of Shizuoka Department of Pharmacy, Faculty of Life Science, Mawlana Bhashani Science and Technology University

• Noguchi Shuji

  Laboratory of Pharmaceutical Engineering & Drug Delivery Science, Graduate School of Integrated Pharmaceutical & Nutritional Sciences, University of Shizuoka

• Iwao Yasunori

  Laboratory of Pharmaceutical Engineering & Drug Delivery Science, Graduate School of Integrated Pharmaceutical & Nutritional Sciences, University of Shizuoka

• Oka Toshihiko

  Department of Physics, Faculty of Science and Nanomaterials Research Division, Research Institute of Electronics, Shizuoka University

• Itai Shigeru

  Laboratory of Pharmaceutical Engineering & Drug Delivery Science, Graduate School of Integrated Pharmaceutical & Nutritional Sciences, University of Shizuoka

抄録

SN-38 is a potent active metabolite of irinotecan that has been considered as an anticancer candidate. However, the clinical development of this compound has been hampered by its poor aqueous solubility and chemical instability. In this study, we developed SN-38-encapsulated cubosomes to resolve these problems. Six α-monoglyceride additives, comprising monocaprylin, monocaprin, monolaurin, monomyristin, monopalmitin, and monostearin, were used to prepare phytantriol (PHYT) cubosomes by probe sonication. The mean particle size, polydispersity index, and zeta potential values of these systems were around 190–230 nm, 0.19–0.25 and −17 to −22 mV, respectively. Small-angle X-ray scattering analyses confirmed that the SN-38-encapsulated cubosomes existed in the Pn̄3m space group both with and without the additives. The monoglyceride additives led to around a two-fold increase in the solubility of SN-38 compared with the PHYT cubosome. The drug entrapment efficiency of PHYT cubosomes with additives was greater than 97%. The results of a stability study at 25°C showed no dramatic changes in the particle size or polydispersity index characteristics, with at least 85% of the SN-38 existing in its active lactone form after 10 d, demonstrating the high stability of the cubosome nanoparticles. Furthermore, approximately 55% of SN-38 was slowly released from the cubosomes with additives over 96 h in vitro under physiological conditions. Taken together, these results show that the SN-38-encapsulated PHYT cubosome particles are promising drug carriers that should be considered for further in vivo experiments, including drug delivery to tumor cells using the enhanced permeability and retention effect.

収録刊行物

• ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ

  ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ 64 (6), 577-584, 2016

  公益社団法人 日本薬学会

キーワード

• cubosome
• drug carrier
• 7-ethyl-10-hydroxyl camptothecin
• phytantriol
• monoglyceride

詳細情報

• CRID: 1390282679155112704
• NII論文ID: 130005154404
• NII書誌ID: AA00602100
• DOI: 10.1248/cpb.c15-00984
• ISSN: 13475223
• ISSN: 00092363
• NDL書誌ID: 027324677
• PubMed: 27250792
• Web Site: http://id.ndl.go.jp/bib/027324677
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I027324677
• Web Site: https://www.jstage.jst.go.jp/article/cpb/64/6/64_c15-00984/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/2017021082
• 本文言語コード: en
• データソース種別:
  • JaLC
  • NDL
  • Crossref
  • PubMed
  • CiNii Articles
  • KAKEN
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