The assessment of pharmacokinetics and neuroprotective effect of berberine hydrochloride-embedded albumin nanoparticles via various administration routes: comparative in-vivo studies in rats

J Microencapsul. 2024 Nov;41(7):576-600. doi: 10.1080/02652048.2024.2395976. Epub 2024 Sep 4.

Abstract

The current study aimed to evaluate the pharmacokinetics and neuroprotective effect of well-characterised berberine-bovine serum albumin (BBR-BSA) nanoparticles. BBR-BSA nanoparticles were generated by desolvation method. Entrapment efficiency, loading capacity, particle size, polydispersity index, surface morphology, thermal stability, and in-vitro release were estimated. In-vitro pharmacokinetic and tissue distribution were conducted. Their neuroprotection was evaluated against lipopolysaccharides-induced neurodegeneration. BBR-BSA nanoparticles showed satisfactory particle size (202.60 ± 1.20 nm) and entrapment efficiency (57.00 ± 1.56%). Results confirmed the formation of spheroid-thermal stable nanoparticles with a sustained drug release over 48 h. Sublingual and intranasal routes had higher pharmacokinetic plasma profiles than other routes, with Cmax values at 0.75 h (444 ± 77.79 and 259 ± 42.41 ng/mL, respectively). BBR and its metabolite distribution in the liver and kidney were higher than in plasma. Intranasal and sublingual treatment improves antioxidants, proinflammatory, amyloidogenic biomarkers, and brain architecture, protecting the brain. In conclusion, neuroinflammation and neurodegeneration may be prevented by intranasal and sublingual BBR-BSA nanoparticles.

Keywords: BBR-BSA nanoparticles; LPS-neuroinflammation and neurodegeneration; intranasal; pharmacokinetic study; sublingual; tissue distribution.

Publication types

  • Comparative Study

MeSH terms

  • Administration, Intranasal
  • Animals
  • Berberine* / administration & dosage
  • Berberine* / pharmacokinetics
  • Berberine* / pharmacology
  • Male
  • Nanoparticles* / chemistry
  • Neuroprotective Agents* / administration & dosage
  • Neuroprotective Agents* / pharmacokinetics
  • Neuroprotective Agents* / pharmacology
  • Particle Size
  • Rats
  • Rats, Wistar
  • Serum Albumin, Bovine* / chemistry
  • Serum Albumin, Bovine* / pharmacokinetics
  • Tissue Distribution

Substances

  • Berberine
  • Serum Albumin, Bovine
  • Neuroprotective Agents