Purpose: the aim of this study is to synthesize lipid-hybrid nanoparticles (LPHNs) loaded with a mixture of two antiretroviral drugs for the treatment of human immunodeficiency virus (HIV). This system which is composed of a polymeric core and a lipid shell, combines the advantages of both polymeric nanoparticles and liposomes, these advantages include the synthesis of nanoparticles from biodegradable materials with high drug loading, relatively small size and low polydispersity, adding ligands to the surface of the LPHNS for active targeting, the drug release can be easily be controlled and the produced particles have high stability. Method: nanoprecipitation method was used, where 1.5 mL of 2.5 mg/mL solution of poly (lactic-co-glycolic acid) (PLGA) in acetonitrile, is slowly added to a stirring preheated 4% ethanol solution of soybean lethicin (150 µg/ml), the mixture is then vortexed for 3 minutes and left stirring for 2 hours, the mixture is then freeze dried for further assessment. Results: The synthesis method is reproducible and the Z-average of the produced nanoparticles was around 120 nm with PDI of 0.3 before freeze drying, increasing the amount of the drug did not affect the size, even when the drug loading % increased from 0 % in case of the blank LPHNs to 50% in case of the drug-loaded LPHNs. Adding PEG (Mn 2050) as a cryoprotectant during freeze drying reduced the aggregation of the particles and made them easy to re-disperse. The drug loading and encapsulation efficiency were relatively high compared to other drug delivery systems. Discussion: new aspects include designing LPHNs system to treat HIV which hasn’t been mentioned in the literature before, using a mixture of two antiretroviral drugs, the lipid nature of the surface of the particles enhances the uptake of the particles by Peyer patches to reach HIV reservoir sites.

Synthesis and optimisation of lipid-hybrid nanoparticles loaded with a mixture of two antiretroviral drugs for the treatment of HIV: Application in nanomedicine

2019 Spring National Meeting

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