Lopinavir is an antiretroviral drug that is important for the treatment of HIV. Unfortunately, it has a low bioavailability because it dissolves poorly in water.
The drug might be absorbed better if it was encased in a nanostructured lipid carrier (NLC). An NLC is a particle containing a mixture of solid and liquid lipids- which should deliver drugs better than solid-only lipid particles. Recently, researchers in Malaysia sought to do a proof-of-concept of an NLC to deliver lopinavir.
To determine optimal conditions for creating NLCs, they varied homogenization time and amounts of solid lipid, liquid lipid, and surfactant. They picked the most promising sets of conditions for further study.
The researchers tested the NLCs for drug release rate in simulated gastric fluid and in simulated intestinal fluid. The NLCs released drug better than straight lopinavir, which would not dissolve in either fluid. Next, they applied the NLCs to a cell line that is popular for studying intestinal epithelium. NLC lopinavir entered the cells faster than straight lopinavir.
Finally, the researchers fed an NLC lopinavir suspension to rats. The rats reached higher blood lopinavir concentrations than rats fed straight lopinavir.
Lopinavir is an antiretroviral drug with poor bioavailability. Nanostructured lipid carriers show potential for improved drug delivery of lopinavir.
Khan AA, Mudassir J, Akhtar S, et al. Freeze-dried lopinavir-loaded nanostructured lipid carriers for enhanced cellular uptake and bioavailability: statistical optimization, in vitro and in vivo evaluations. Pharmaceutics. 2019; 11(2):97. PMID: 30823545