Enhanced Solubility and Bioactivity of Pharmaceuticals

  • Author: ChemistryViews
  • Published: 20 April 2012
  • Copyright: WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
  • Source / Publisher: Nature Chemistry
thumbnail image: Enhanced Solubility and Bioactivity of Pharmaceuticals

Methods for increasing drug solubility are highly prized, as the solubility characteristics of 40–70 % of new drug candidates are so poor that they cannot be formulated on their own.

Volker Briken, Lyle Isaacs, and colleagues, University of Maryland, USA, describe a new class of general-purpose solubilizing agents which increase the solubility of ten insoluble drugs by a factor of between 23 and 2,750. Their acyclic cucurbit[n]uril molecular container complexes exhibit low in vitro toxicity in human liver, kidney and monocyte cell lines. They outbred Swiss Webster mice tolerate high doses of the container without sickness or weight loss.
The acyclic cucurbituril-type containers preferentially bind cationic and aromatic drugs. They also solubilize neutral drugs such as paclitaxel, a mitotic inhibitor used in cancer chemotherapy. Paclitaxel solubilized by the acyclic cucurbituril-type containers kills cervical and ovarian cancer cells more efficiently than paclitaxel alone.

The acyclic cucurbituril-type containers represent an attractive extension of cyclodextrin-based technology for drug solubilization and delivery.

Article Views: 3000

Sign in Area

Please sign in below

Additional Sign In options

Please note that to comment on an article you must be registered and logged in.
Registration is for free, you may already be registered to receive, e.g., the newsletter. When you register on this website, please ensure you view our terms and conditions. All comments are subject to moderation.

Article Comments - To add a comment please sign in

If you would like to reuse any content, in print or online, from ChemistryViews.org, please contact us first for permission and consult our permission guidance prior to making your request

Follow on Facebook Follow on Twitter Follow on YouTube Follow on LinkedIn Follow on Instagram RSS Sign up for newsletters

Magazine of Chemistry Europe (16 European Chemical Societies) published by Wiley-VCH