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 language | English |
|---|---|
| Article number | 290 |
| Journal | Nanomaterials |
| Volume | 7 |
| Issue number | 10 |
| DOIs | |
| Publication status | Published - Oct 1 2017 |
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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 journal › Article
}
TY - JOUR
T1 - Practical liposomal formulation for taxanes with polyethoxylated castor oil and ethanol with complete encapsulation efficiency and high loading efficiency
AU - Shigehiro, Tsukasa
AU - Masuda, Junko
AU - Saito, Shoki
AU - Khayrani, Apriliana C.
AU - Jinno, Kazumasa
AU - Seno, Akimasa
AU - Vaidyanath, Arun
AU - Mizutani, Akifumi
AU - Kasai, Tomonari
AU - Murakami, Hiroshi
AU - Satoh, Ayano
AU - Ito, Tetsuya
AU - Hamada, Hiroki
AU - Seno, Yuhki
AU - Mandai, Tadakatsu
AU - Seno, Masaharu
PY - 2017/10/1
Y1 - 2017/10/1
N2 - 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.
AB - 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.
KW - Cremophor EL
KW - HER2
KW - Liposomal drug delivery
KW - Targeted drug delivery
KW - Taxanes
UR - http://www.scopus.com/inward/record.url?scp=85031432560&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=85031432560&partnerID=8YFLogxK
U2 - 10.3390/nano7100290
DO - 10.3390/nano7100290
M3 - Article
VL - 7
JO - Nanomaterials
JF - Nanomaterials
SN - 2079-4991
IS - 10
M1 - 290
ER -