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Enhancing the Delivery of Anti Retroviral Drug “Saquinavir” Across the Blood Brain Barrier Using Nanoparticles

Authors: Supriya D. Mahajan1, Indrajit Roy2, GaiXia Xu2, Ken-Tye Yong3, Hong Ding2, Ravikumar Aalinkeel1, Jessica L. Reynolds1, Donald E. Sykes1, Bindukumar B. Nair1, Elaine Y. Lin1, Paras N. Prasad2 and Stanley A. Schwartz1

Online: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2904057/

Issue: Current HIV Research 2010 Jul; 8(5): 396–404.


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.

Keywords: HIV-1, antiretroviral drugs, saquinavir, protease inhibitor, quantum rods (QR), blood brain barrier, transferrin receptor, multimodal nanoparticles and bioconjugation



  1. Department of Medicine, Division of Allergy, Immunology, and Rheumatology, State University of New York at Buffalo, 100 High street, Buffalo General Hospital, Buffalo, USA
  2. Institute for Lasers Photonics and Biophotonics, 428 Natural Science Complex, State University of New York at Buffalo, North campus, Buffalo, New York, NY 14260, USA
  3. School of Electrical and Electronic Engineering, Nanyang Technological University, Singapore 639798, Singapore