One of the key obstacles encountered by the pharmaceutical industry is the deficient bioavailability of drugs due to poor aqueous solubility. One approach to address this problem is the development of molecular containers that encapsulate and thereby solubilize otherwise insoluble drugs in an aqueous environment. Ideally, such molecular container-drug complexes can be delivered in a targeted manner in the human body. Accordingly, water soluble molecular containers are highly desirable toward the formulation of a wide array of pharmaceutical drugs and agents. Currently, the most commonly used class of water soluble molecular containers for drug delivery applications are the cyclodextrins. Cyclodextrins however, have their drawbacks and cannot be considered as a universal container for all possible drugs. Therefore a great need exists for the invention of new classes of molecular containers that will provide an alternative to cyclodextrins as solubility enhancers and delivery agents.

Researchers at the University of Maryland have discovered a new cucurbit[n]uril-type molecular container that binds to a variety of FDA approved agents in water. For example the new CB[n]-type container binds to Rocuronium which is a widely used anesthetic during surgery. By sequestering Rocuronium post-operatively by the application of the new CB[n]-type container, the recovery time of the patient is decreased. The excellent aqueous solubility (≥ 100 mM) of this new CB[n]-type container makes it ideal for intravenous administration. The new CB[n]-type container has also been successfully tested for enhancing the aqueous solubility of a multitude of FDA approved pharmaceuticals including anti-cancer, anti-arrhythmic, anti-clotting and anti-histamine drugs and agents. Toxicity studies in human cell lines establish that the new CB[n]-type container is bio-compatible (e.g. non-toxic). A scalable, efficient, and cost effective synthetic route to this compound has also been developed by the same researchers.

File Number: LS-2010-039 

Web site: http://otc.umd.edu