Self-Assembled Hydrophobic Honokiol Loaded MPEG-PCL Diblock Copolymer Micelles
Purpose Honokiol showed potential application in cancer treatment, but its poor water solubility restricts its clinical application greatly. So, we designed a self-assembled monomethoxy poly(ethylene glycol)-poly(ε-caprolactone) (MPEG-PCL) micelle to load honokiol to overcome its poor water solubili...
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Published in | Pharmaceutical research Vol. 26; no. 9; pp. 2164 - 2173 |
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Main Authors | , , , , , , , , , , , , |
Format | Journal Article |
Language | English |
Published |
Boston
Boston : Springer US
01.09.2009
Springer US Springer Springer Nature B.V |
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Abstract | Purpose Honokiol showed potential application in cancer treatment, but its poor water solubility restricts its clinical application greatly. So, we designed a self-assembled monomethoxy poly(ethylene glycol)-poly(ε-caprolactone) (MPEG-PCL) micelle to load honokiol to overcome its poor water solubility. Methods We synthesized MPEG-PCL diblock copolymer that could self-assemble into monodisperse micelles at the particle size of ca.18 nm in water. Honokiol was loaded into MPEG-PCL micelle by direct dissolution method assisted by ultrasound, without any surfactants, organic solvents, and vigorous stirring. Results The blank MPEG-PCL micelles (100 mg/mL) did not induce any hemolysis in vitro and showed very low toxicity ex vivo and in vivo. Honokiol could be molecularly incorporated into MPEG-PCL micelles at the drug loading of about 20% by direct dissolution method assisted by ultrasound. After loaded into MPEG-PCL micelles, honokiol maintained its molecular structure and anticancer activity in vitro. Honokiol could be sustained released from MPEG-PCL micelles in vitro. The honokiol loaded MPEG-PCL micelles could be lyophilized without any adjuvant. Conclusion The prepared honokiol formulation based on self-assembled MPEG-PCL micelle was stable, safe, effective, easy to produce and scale up, and showed potential clinical application. |
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AbstractList | Purpose
Honokiol showed potential application in cancer treatment, but its poor water solubility restricts its clinical application greatly. So, we designed a self-assembled monomethoxy poly(ethylene glycol)-poly(ε-caprolactone) (MPEG-PCL) micelle to load honokiol to overcome its poor water solubility.
Methods
We synthesized MPEG-PCL diblock copolymer that could self-assemble into monodisperse micelles at the particle size of ca.18 nm in water. Honokiol was loaded into MPEG-PCL micelle by direct dissolution method assisted by ultrasound, without any surfactants, organic solvents, and vigorous stirring.
Results
The blank MPEG-PCL micelles (100 mg/mL) did not induce any hemolysis
in vitro
and showed very low toxicity
ex vivo
and
in vivo
. Honokiol could be molecularly incorporated into MPEG-PCL micelles at the drug loading of about 20% by direct dissolution method assisted by ultrasound. After loaded into MPEG-PCL micelles, honokiol maintained its molecular structure and anticancer activity
in vitro
. Honokiol could be sustained released from MPEG-PCL micelles
in vitro
. The honokiol loaded MPEG-PCL micelles could be lyophilized without any adjuvant.
Conclusion
The prepared honokiol formulation based on self-assembled MPEG-PCL micelle was stable, safe, effective, easy to produce and scale up, and showed potential clinical application. Honokiol showed potential application in cancer treatment, but its poor water solubility restricts its clinical application greatly. So, we designed a self-assembled monomethoxy poly(ethylene glycol)-poly([epsilon]-caprolactone) (MPEG-PCL) micelle to load honokiol to overcome its poor water solubility. We synthesized MPEG-PCL diblock copolymer that could self-assemble into monodisperse micelles at the particle size of ca.18 nm in water. Honokiol was loaded into MPEG-PCL micelle by direct dissolution method assisted by ultrasound, without any surfactants, organic solvents, and vigorous stirring. The blank MPEG-PCL micelles (100 mg/mL) did not induce any hemolysis in vitro and showed very low toxicity ex vivo and in vivo. Honokiol could be molecularly incorporated into MPEG-PCL micelles at the drug loading of about 20% by direct dissolution method assisted by ultrasound. After loaded into MPEG-PCL micelles, honokiol maintained its molecular structure and anticancer activity in vitro. Honokiol could be sustained released from MPEG-PCL micelles in vitro. The honokiol loaded MPEG-PCL micelles could be lyophilized without any adjuvant. The prepared honokiol formulation based on self-assembled MPEG-PCL micelle was stable, safe, effective, easy to produce and scale up, and showed potential clinical application. [PUBLICATION ABSTRACT] Purpose Honokiol showed potential application in cancer treatment, but its poor water solubility restricts its clinical application greatly. So, we designed a self-assembled monomethoxy poly(ethylene glycol)-poly(ε-caprolactone) (MPEG-PCL) micelle to load honokiol to overcome its poor water solubility. Methods We synthesized MPEG-PCL diblock copolymer that could self-assemble into monodisperse micelles at the particle size of ca.18 nm in water. Honokiol was loaded into MPEG-PCL micelle by direct dissolution method assisted by ultrasound, without any surfactants, organic solvents, and vigorous stirring. Results The blank MPEG-PCL micelles (100 mg/mL) did not induce any hemolysis in vitro and showed very low toxicity ex vivo and in vivo. Honokiol could be molecularly incorporated into MPEG-PCL micelles at the drug loading of about 20% by direct dissolution method assisted by ultrasound. After loaded into MPEG-PCL micelles, honokiol maintained its molecular structure and anticancer activity in vitro. Honokiol could be sustained released from MPEG-PCL micelles in vitro. The honokiol loaded MPEG-PCL micelles could be lyophilized without any adjuvant. Conclusion The prepared honokiol formulation based on self-assembled MPEG-PCL micelle was stable, safe, effective, easy to produce and scale up, and showed potential clinical application. Honokiol showed potential application in cancer treatment, but its poor water solubility restricts its clinical application greatly. So, we designed a self-assembled monomethoxy poly(ethylene glycol)-poly(epsilon-caprolactone) (MPEG-PCL) micelle to load honokiol to overcome its poor water solubility. We synthesized MPEG-PCL diblock copolymer that could self-assemble into monodisperse micelles at the particle size of ca.18 nm in water. Honokiol was loaded into MPEG-PCL micelle by direct dissolution method assisted by ultrasound, without any surfactants, organic solvents, and vigorous stirring. The blank MPEG-PCL micelles (100 mg/mL) did not induce any hemolysis in vitro and showed very low toxicity ex vivo and in vivo. Honokiol could be molecularly incorporated into MPEG-PCL micelles at the drug loading of about 20% by direct dissolution method assisted by ultrasound. After loaded into MPEG-PCL micelles, honokiol maintained its molecular structure and anticancer activity in vitro. Honokiol could be sustained released from MPEG-PCL micelles in vitro. The honokiol loaded MPEG-PCL micelles could be lyophilized without any adjuvant. The prepared honokiol formulation based on self-assembled MPEG-PCL micelle was stable, safe, effective, easy to produce and scale up, and showed potential clinical application. PURPOSEHonokiol showed potential application in cancer treatment, but its poor water solubility restricts its clinical application greatly. So, we designed a self-assembled monomethoxy poly(ethylene glycol)-poly(epsilon-caprolactone) (MPEG-PCL) micelle to load honokiol to overcome its poor water solubility. METHODSWe synthesized MPEG-PCL diblock copolymer that could self-assemble into monodisperse micelles at the particle size of ca.18 nm in water. Honokiol was loaded into MPEG-PCL micelle by direct dissolution method assisted by ultrasound, without any surfactants, organic solvents, and vigorous stirring. RESULTSThe blank MPEG-PCL micelles (100 mg/mL) did not induce any hemolysis in vitro and showed very low toxicity ex vivo and in vivo. Honokiol could be molecularly incorporated into MPEG-PCL micelles at the drug loading of about 20% by direct dissolution method assisted by ultrasound. After loaded into MPEG-PCL micelles, honokiol maintained its molecular structure and anticancer activity in vitro. Honokiol could be sustained released from MPEG-PCL micelles in vitro. The honokiol loaded MPEG-PCL micelles could be lyophilized without any adjuvant. CONCLUSIONThe prepared honokiol formulation based on self-assembled MPEG-PCL micelle was stable, safe, effective, easy to produce and scale up, and showed potential clinical application. |
Author | Lv, Lei Chen, LiJuan Wei, YuQuan Zhao, Xia Gou, MaLing Zhang, Juan Luo, Feng Wang, BiLan Wang, XiuHong Zhao, YinLan Qian, ZhiYong Zheng, XiuLing Men, Ke |
Author_xml | – sequence: 1 fullname: Gou, MaLing – sequence: 2 fullname: Zheng, XiuLing – sequence: 3 fullname: Men, Ke – sequence: 4 fullname: Zhang, Juan – sequence: 5 fullname: Wang, BiLan – sequence: 6 fullname: Lv, Lei – sequence: 7 fullname: Wang, XiuHong – sequence: 8 fullname: Zhao, YinLan – sequence: 9 fullname: Luo, Feng – sequence: 10 fullname: Chen, LiJuan – sequence: 11 fullname: Zhao, Xia – sequence: 12 fullname: Wei, YuQuan – sequence: 13 fullname: Qian, ZhiYong |
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Keywords | Micelle MPEG-PCL self-assembly nanomedicine honokiol Performance evaluation Pharmaceutical technology Diblock copolymer Technique Nanotechnology |
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Snippet | Purpose Honokiol showed potential application in cancer treatment, but its poor water solubility restricts its clinical application greatly. So, we designed a... Purpose Honokiol showed potential application in cancer treatment, but its poor water solubility restricts its clinical application greatly. So, we designed a... Honokiol showed potential application in cancer treatment, but its poor water solubility restricts its clinical application greatly. So, we designed a... PURPOSEHonokiol showed potential application in cancer treatment, but its poor water solubility restricts its clinical application greatly. So, we designed a... |
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Title | Self-Assembled Hydrophobic Honokiol Loaded MPEG-PCL Diblock Copolymer Micelles |
URI | https://link.springer.com/article/10.1007/s11095-009-9929-8 https://www.ncbi.nlm.nih.gov/pubmed/19568695 https://www.proquest.com/docview/222683993/abstract/ https://search.proquest.com/docview/67548208 |
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