| 論文名 |
Acyclic cucurbit[n]uril-type molecular containers: influence of aromatic walls on their function as solubilizing excipients for insoluble drugs. |
| 著者 |
Ben Zhang
Lyle Isaacs
|
| キーワード |
|
| 出版年月 |
1970年1月 |
| 発表先 |
J Med Chem. 2014 Nov 26;57(22):9554-63. doi: 10.1021/jm501276u. Epub 2014 Nov 17. |
| WEBサイト |
|
| 論文概要（和文） |
非環状ククルビット[n]ウリル型分子容器：不溶性薬物の可溶化賦形剤としてのそれらの機能に対する芳香族壁の影響 |
| 論文概要（英文） |
We studied the influence of the aromatic sidewalls on the ability of acyclic CB[n]-type molecular containers (1a-1e) to act as solubilizing agents for 19 insoluble drugs including the developmental anticancer agent PBS-1086. All five containers exhibit good water solubility and weak self-association (Ks ? 624 M(-1)). We constructed phase solubility diagrams to extract Krel and Ka values for the container?drug complexes. The acyclic CB[n]-type containers generally display significantly higher Ka values than HP-β-CD toward drugs. Containers 1a-1e bind the steroidal ring system and aromatic moieties of insoluble drugs. Compound 1b displays highest affinity toward most of the drugs studied. Containers 1a and 1b are broadly applicable and can be used to formulate a wider variety of insoluble drugs than was previously possible with cyclodextrin technology. For drugs that are solubilized by both HP-β-CD and 1a-1e, lower concentrations of 1a-1e are required to achieve identical [drug]. |
