Surface modified kokum butter lipid nanoparticles for the brain targeted delivery of nevirapine

J Microencapsul. 2018 Nov-Dec;35(7-8):680-694. doi: 10.1080/02652048.2019.1573857.

Abstract

Aim: The present work investigates the efficacy of Polysorbate 80(P80) coated Kokum butter (KB) solid lipid nanoparticles (P80NvKLNs) for the brain targeted delivery of Nevirapine (Nv).

Methods: Solid lipid nanoparticles (SLNs) were prepared by nanoprecipitation technique and evaluated for drug excipient compatibility studies, z- average particle size (nm), zeta potential (mv), percentage drug entrapment efficiency (%EE), surface morphology and in-vitro drug release properties. The in-vivo biodistribution and brain targeting efficiency of nanoparticles were studied in healthy male Wistar rat (150-200 g).

Results: P80NvKLNs were found to be smooth surfaced, spherical shaped having average particle size of 177.80 ± 0.82 nm, zeta potential of -8.91 ± 4.36 mv and %EE of 31.32 ± 0.42%. P80NvKLNs remained in blood circulation for 48 h maintaining a sustained release in brain for 24 h (p < 0.05).

Conclusion: The study proves the efficacy of Polysorbate 80 coated Kokum butter nanoparticles for brain-targeted delivery of drugs providing ample opportunities for further study.

Keywords: biodistribution; Blood-brain barrier (BBB); SLNs; kokum butter; nanoprecipitation; nevirapine.

MeSH terms

  • AIDS Dementia Complex / drug therapy
  • AIDS Dementia Complex / etiology
  • AIDS Dementia Complex / metabolism
  • Acquired Immunodeficiency Syndrome / complications
  • Acquired Immunodeficiency Syndrome / drug therapy
  • Acquired Immunodeficiency Syndrome / metabolism
  • Animals
  • Anti-HIV Agents / administration & dosage
  • Anti-HIV Agents / pharmacokinetics*
  • Brain / metabolism*
  • Delayed-Action Preparations / chemistry*
  • Delayed-Action Preparations / metabolism
  • Drug Delivery Systems
  • Garcinia / chemistry*
  • Lipid Metabolism
  • Lipids / chemistry*
  • Male
  • Nanoparticles / chemistry*
  • Nanoparticles / metabolism
  • Neurocognitive Disorders / drug therapy
  • Neurocognitive Disorders / etiology
  • Neurocognitive Disorders / metabolism
  • Nevirapine / administration & dosage
  • Nevirapine / pharmacokinetics*
  • Polysorbates / chemistry
  • Polysorbates / metabolism
  • Rats, Wistar
  • Surface Properties
  • Tissue Distribution

Substances

  • Anti-HIV Agents
  • Delayed-Action Preparations
  • Lipids
  • Polysorbates
  • Nevirapine