Tuberculosis is one of the deadliest infectious diseases killing annually 1,5 million people worldwide. The major problems connected with the tuberculosis treatment are: strong side effects of the majority of the existent antituberculosis drugs, long duration of treatment, high dosage, unpleasant organoleptic properties and high frequency of administration. These factors very often cause the lack of compliance of the patient with treatment. The last fact in association with low bioavailability and insufficient enantiomeric purity of some antituberculosis drugs, all together lead to development of drug-resistant (DRTB), multiple drug-resistant (MDRTB), and extensively drug-resistant (XTRB) tuberculosis. We have proposed to obtain new nano-encapsulated anti-tuberculosis remedies with higher efficiency and fewer side effects as compared to the existing drugs [1]. The problem is resolved by nano-encapsulation of new active antituberculosis substances in cyclodextrins. As such, cyclodextrins play the roles of solubilization agents and promoters of the antimycobacterial substances penetration inside the mycobacterial cell. The nano-encapsulated drugs are then loaded into the alginate-chitosan microparticles that help them penetrate into macrophages infected with M. tuberculosis [2]. Preliminary results of the biological tests of antimycobacterial activity of the obtained substances and systems have demonstrated that antituberculosis efficiency of the studied substances changes in association with different cyclodextrins. Thus, β-cyclodextrin, one of the naturally occurring cyclodextrins, seems to enhance antituberculosis activity of the associated oxadiazole derivative, while sulfobutyl ether of β-cyclodextrin does not have this influence. This observation might be explained by the fact that sulfobutyl ether of β-cyclodextrin possesses certain level of charge of the molecule due to the presence of sulfobutyl ether groups, which makes it less suitable for cholesterol complexation than simple β-cyclodextrin. Namely cholesterol complexation is considered to be in the core of mechanism of cyclodextrins activity as promoters of antituberculosis compounds penetration through the mycobacterial cell wall.