Synthesis of Loureirin B-Loaded Nanoliposomes for Pharmacokinetics in Rat Plasma

Loureirin B (LB) is the most radioactive compound of dragon's blood, but its poor pharmacokinetics due to its hydrophobic nature limits its clinical applications. Owing to the excellent biocompatibility of liposomes with body fluid, here phospholipids and cholesterol-based nanoliposomes (NLs) were synthesized using the thin-film evaporation technique as a nanocarrier for LB to overcome associated clinical issues. The NLs exhibited overall vesicular shape, which is favorable for enhanced drug uptake (up to 74.5%), while the particle size of NLs was found to be strongly dependent on lipid concentration that ranges from 58 to 94 nm. Further, a high zeta-potential of -51.2 mV shown by the LB-loaded NLs confirms their high stability and better dispersion in designated solvents/cell plasma as well as proves their ability for homogeneous drug delivery. In vitro flow cytometry results revealed that LB-loaded NLs recover the radiation injury in viable cell from 79.4 to 89.9%, early apoptosis from 3.5 to 0.2%, necrosis from 14.8 to 9.8%, and late apoptosis from 2.3 to 0.0%. In vivo assay showed that LB-loaded NLs successfully improved the pharmacokinetic parameters such as maximum concentration of LB-loaded NLs formulation, elimination rate half-life, area under the curve, and plasma clearance to 3.247 +/- 0.631 ng/mL h, 14.765 +/- 10.780 min, 2.957 +/- 0.201 ng/mL h, and 0.132 +/- 0.901 ng/mL h, respectively. Thus, we believe that designing such unique LB-loaded NLs composite not only improved the antiradiation characteristics of LB but also make it suitable for other biomedical applications like drug delivery by enhancing its solubility and dispersion.