Interaction of rifampicin embedded in phospholipid nanoparticles with blood plasma lipoproteins

The drug formulations of antituberculous remedy rifampicin in nanoparticles less than 30 nm based on soy phosphatidylcholine and sodium oleate was elaborated in Institute of Biomedical Chemistry. The distribution of rifampicin in blood plasma fractions after incubation with this formulation and with free rifampicin was studied. This goal was stimulated by the literature data about activation of macrophages LDL receptors in cases of M. tuberculosis infection. Plasma was incubated 30 min with free rifampicin or rifampicin encapsulated into the nanoformulation followed by ultracentrifugation and subsequent rifampicin determination by HPLC in lipoprotein fractions. In the case of free rifampicin it appeared mainly in the plasma protein fraction and in HDL (41% and 38%, correspondentely). But after incubation of rifampicin in nanoparticles the drug redistribution was observed. Its proportion in these factions decreased 2-3-fold, and it was found mainly in LDL (60% as compared with 21% for free rifampicin). The increased association of rifampicin encapsulated into phospholipid nanoparticles with LDL is considered as facilitating factor for macrophages delivery and thus for antituberculosis efficiency as well