The design of new drug delivery systems has been widely sought after. The stability, solubility, and difficulty of targeting active sites for new drugs have always been challenging and remain one of the major drawbacks to the efficiency of certain drugs. Liposomes are phospholipid vesicles enclosing one or more aqueous compartments. Depending on its properties, a drug is embedded in the lipid bilayer or the aqueous medium. Thus, liposomes can act as drug carriers for both lipo- and hydrophilic compounds. New strategies such as “drug-in-cyclodextrin-in liposomes” (DCLs) have been developed as safe and effective carriers for exploiting the inclusion properties of water-soluble cyclodextrins known to form host–guest complexes with lipophilic molecules. Once inclusion complexes are formed, they can be inserted into a liposome aqueous core in order to stabilize it and better control the drug release. Our review will provide an update on the use of DCLs in the field of drug delivery for various kinds of active compounds. While previous reviews focused on the interesting advantages of using this method, such as enhancing the solubility and stability of a drug or controlling and improving drug release, the authors intend to highlight the impact of these nanocarriers on the pharmacokinetic and/or pharmacodynamic properties of drugs.

The synthesis of a contrast agent based on a β-cyclodextrin is reported. An enhancement of relaxivity in the presence of an intramolecular inclusion complex is observed.

Two new imaging tools using polydentate cyclodextrins were obtained using an innovative synthetic strategy. For the first time the influence of hydrogen bonding interactions of the cyclodextrin free rim was studied by MRI. The positive second coordination sphere effect was then quantified.