Enhancing the delivery of anti retroviral drug "saquinavir" across the blood brain barrier using nanoparticles

Supriya D. Mahajan, Indrajit Roy, Gai Xia Xu, Ken Tye Yong, Hong Ding, Ravikumar Aalinkeel, Jessica L. Reynolds, Donald E. Sykes, Bindukumar B. Nair, Elaine Y. Lin, Paras N. Prasad, Stanley A. Schwartz

Research output: Contribution to journalArticlepeer-review

92 Scopus citations


Antiretroviral drugs are ineffective at treating viral infection in the brain because they cannot freely diffuse across the blood-brain barrier (BBB). Therefore, HIV-1 viral replication persists in the central nervous system (CNS) and continues to augment the neuropathogenesis process. Nanotechnology can play a pivotal role in HIV-1 therapeutics as it can increase drug solubility, enhance systemic bioavailability, and at the same time offer multifunctionality. Moreover, following conjugation with transferrin (Tf), these drug-loaded nanoformulations can permeate across biological barriers such as the blood brain barrier (BBB) via a receptor mediated transport mechanism. In the current study, we have stably incorporated the antiviral drug, Saquinavir, within Tf-conjugated quantum rods (QRs), which are novel nanoparticles with unique optical properties. We have evaluated the transversing ability of the QR-Tf-Saquinavir nanoformulation across an in vitro model of BBB. In addition, we have analyzed the subsequent antiviral efficacy of this targeted nanoformulation in HIV-1 infected peripheral blood mononuclear cells (PBMCs), which are cultured on the basolateral end of the in vitro BBB model. Our results show a significant uptake of QR-Tf-Saquinavir by brain microvascular endothelial cells (BMVECs), which constitute the BBB. In addition, we observed a significant enhancement in the transversing capability of QR-Tf-Saquinavir across the BBB, along with a marked decrease in HIV-1 viral replication in the PBMCs. These observations indicate that drug-loaded nanoparticles can deliver therapeutics across the BBB. These results highlight the potential of this nanoformulation in the treatment of Neuro-AIDS and other neurological disorders.

Original languageEnglish (US)
Pages (from-to)396-404
Number of pages9
JournalCurrent HIV Research
Issue number5
StatePublished - 2010
Externally publishedYes


  • Antiretroviral drugs
  • Blood brain barrier
  • Hiv-1
  • Multimodal nanoparticles and bioconjugation
  • Protease inhibitor
  • Quantum rods (qr)
  • Saquinavir
  • Transferrin receptor

ASJC Scopus subject areas

  • Infectious Diseases
  • Virology


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