Polymeric nanoparticles containing combination antiretroviral drugs for HIV type 1 treatment

Annemarie Shibata, Emily McMullen, Alex Pham, Michael Belshan, Bridget Sanford, You Zhou, Michael Goede, Abjijit A. Date, Christopher J. Destache

Research output: Contribution to journalArticlepeer-review

68 Scopus citations


The use of combination antiretroviral nanoparticles (cART NPs) was investigated as a novel treatment approach for the inhibition of HIV-1 replication. We developed nanoparticles of biodegradable polymer, poly-(dl-lactide-co-glycolic acid; PLGA) containing efavirenz (EFV) and boosted lopinavir (lopinavir/ritonavir; LPV/r) by a high-pressure homogenization method. The method resulted in >79% drug entrapment efficiency for each of the three drugs. The average size of cART NPs was 138.3±55.4 nm as measured by dynamic light scanning, confirmed by scanning electron microscopy (SEM) with an average surface charge of-13.7±4.5. Lissamine-rhodamine-labeled fluorescent PLGA NPs exhibited efficient uptake in nonimmune (HeLa cells) and immune (H9 T cells) cells as measured by confocal microscopy. Cells treated with cART NPs resulted in minimal loss of cell viability over 28 days. Subcellular fractionation studies demonstrated that HIV-1-infected H9 monocytic cells treated with cART NPs contained significantly (p<0.05) higher nuclear, cytoskeleton, and membrane antiretroviral drug levels compared to cells treated with drug solutions alone. Finally, cART NPs efficiently inhibited HIV-1 infection and transduction. The IC50 for each of the three drugs in the cART NPs was <31 nM. These experiments demonstrate the efficacy of a novel PLGA NPs formulation for the delivery of cART to inhibit HIV-1 replication.

Original languageEnglish (US)
Pages (from-to)746-754
Number of pages9
JournalAIDS Research and Human Retroviruses
Issue number5
StatePublished - 2013

ASJC Scopus subject areas

  • Infectious Diseases
  • Virology
  • Immunology


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