Dual combination of resveratrol and pterostilbene aqueous core nanocapsules for integrated prostate cancer targeting

Ther Deliv. 2024;15(9):685-698. doi: 10.1080/20415990.2024.2380239. Epub 2024 Aug 12.

Abstract

Aim: Development and evaluation of aqueous core nanocapsules (ACNs) of BCS-II-class drug like resveratrol (RSV) and pterostilbene (PTE) for prostate cancer.Materials & methods: Identify synergistic effects of molar ratios of RSV and PTE against PC-3 cell. Selected ratio of drugs was added to ACNs by double-emulsification-method using Box-Behnken design. Further, assessed for physicochemical characterization, release kinetics, compatibility, in vitro cytotoxicity, in vivo pharmacokinetic and biodistribution studies.Results: Selected 1:1 ratio of RSV and PTE had greatest synergy potential have smaller particle-size (128.1 ± 3.21 nm), zeta-potential (-22.12 ± 0.2 mV), 0.53 PDI, improved encapsulation (87% for RSV, 72% for PTE), stable, no systemic toxicity, high biodistributed/accumulated in prostate cells.Conclusion: ACNs exhibited high t1/2 (12.42 ± 1.92 hs) and 8.20 ± 8.21 hs Mean Residence Time and lower clearance, proving the high effectiveness for prostate cancer.

Keywords: Box–Behnken design; aqueous core nanocapsules; combination therapy; pterostilbene; resveratrol.

Plain language summary

[Box: see text].

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Drug Liberation
  • Humans
  • Male
  • Nanocapsules* / chemistry
  • PC-3 Cells
  • Particle Size
  • Prostatic Neoplasms* / drug therapy
  • Prostatic Neoplasms* / pathology
  • Resveratrol* / administration & dosage
  • Resveratrol* / chemistry
  • Resveratrol* / pharmacokinetics
  • Resveratrol* / pharmacology
  • Stilbenes* / administration & dosage
  • Stilbenes* / chemistry
  • Stilbenes* / pharmacokinetics
  • Stilbenes* / pharmacology
  • Tissue Distribution

Substances

  • Resveratrol
  • pterostilbene
  • Stilbenes
  • Nanocapsules