Characterization of Nanodiamond-based anti-HIV drug Delivery to the Brain

Sci Rep. 2018 Jan 25;8(1):1603. doi: 10.1038/s41598-017-16703-9.


Human Immunodeficiency Virus Type 1 (HIV-1) remains one of the leading causes of death worldwide. Present combination antiretroviral therapy has substantially improved HIV-1 related pathology. However, delivery of therapeutic agents to the HIV reservoir organ like Central nervous system (CNS) remains a major challenge primarily due to the ineffective transmigration of drugs through Blood Brain Barrier (BBB). The recent advent of nanomedicine-based drug delivery has stimulated the development of innovative systems for drug delivery. In this regard, particular focus has been given to nanodiamond due to its natural biocompatibility and non-toxic nature-making it a more efficient drug carrier than other carbon-based materials. Considering its potential and importance, we have characterized unmodified and surface-modified (-COOH and -NH2) nanodiamond for its capacity to load the anti-HIV-1 drug efavirenz and cytotoxicity, in vitro. Overall, our study has established that unmodified nanodiamond conjugated drug formulation has significantly higher drug loading capacity than surface-modified nanodiamond with minimum toxicity. Further, this nanodrug formulation was characterized by its drug dissolution profile, transmigration through the BBB, and its therapeutic efficacy. The present biological characterizations provide a foundation for further study of in-vivo pharmacokinetics and pharmacodynamics of nanodiamond-based anti-HIV drugs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkynes
  • Anti-HIV Agents / pharmacokinetics*
  • Anti-HIV Agents / pharmacology*
  • Astrocytes / drug effects
  • Astrocytes / metabolism
  • Benzoxazines / pharmacokinetics*
  • Benzoxazines / pharmacology*
  • Cell Survival / drug effects
  • Cells, Cultured
  • Cyclopropanes
  • Drug Carriers / metabolism*
  • Drug Carriers / toxicity
  • Endothelial Cells / drug effects
  • Endothelial Cells / metabolism
  • Humans
  • Macrophages / drug effects
  • Macrophages / virology
  • Nanodiamonds*
  • Neurons / drug effects
  • Neurons / physiology


  • Alkynes
  • Anti-HIV Agents
  • Benzoxazines
  • Cyclopropanes
  • Drug Carriers
  • Nanodiamonds
  • efavirenz