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The drug delivery potential of the molecular hosts cucurbit[n]uril (CB[n]) and CB[n]- type derivatives has been explored by a number of researchers worldwide. These hosts can act as drug delivery vehicles either in their simplest form as drug@host or in more complex forms such as nanoparticles, where the structural integrity of the nanoparticle is maintained and supported by secondary molecular interactions with molecular hosts, while the drug is held within the structure. A large number of drugs and bioactive molecules (>90) have been investigated, however, the primary interest discussed in this chapter relates to results from cell cultures and animal models. The usual protocol of initial evaluation of drug delivery through in vitro analysis for both diseased and healthy cells has revealed positive and encouraging outcomes. The progression of drug delivery studies to ex vivo and in vivo using only the free-hosts to evaluate their toxicology has demonstrated high biocompatibility with healthy tissue and animal models. Some pharmacokinetics is also discussed with and without drug association. Further to these studies positive pharmacological outcomes have also been reported in animal models, in particular for the reduction of toxicity, while maintaining pharmacological activity. Other features such as, increased bioavailability, drug retention and targeted delivery are also highlighted with reported examples. In contrast to examples of drug delivery, sequestration is also presented as a method of encapsulation, deactivation and excretion as an aid to anaesthesia recovery.

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