RGD-Conjugated Resveratrol HSA Nanoparticles as a Novel Delivery System in Ovarian Cancer Therapy

Drug Des Devel Ther. 2020 Dec 30:14:5747-5756. doi: 10.2147/DDDT.S248950. eCollection 2020.

Abstract

Background: To establish a novel delivery system of RGD-conjugated resveratrol human serum albumin (HAS) nanoparticles in ovarian cancer therapy.

Methods: The nanoparticles system was characterized for physicochemical properties, the stability in the serum and in vitro release. The comparison between RVT injection, HSA-RVT NPs and RGD-HSA-RVT NPs regarding tissue distributions and pharmacokinetics was also carried out using mice as the animal models.

Results: The results showed that RGD-HSA-RVT NPs were characterized of small particle size about 128.2 nm and negative zeta potential about -21.42 mV, and drug controlled to release slowly on a biphasic pattern. Compared with control groups, RGD-HSA-RVT NPs showed the higher cellular uptake and cell inhibition rates. In vivo data showed that RGD-HSA-RVT NPs have good tumor enrichment characteristics and a significant difference in tumor inhibition, compared with the control group.

Conclusion: RGD-conjugated resveratrol HSA nanoparticles are an ideal drug delivery system, which can play a role in the treatment of ovarian cancer.

Keywords: HAS; cell viability; cellular uptake; nanoparticle; pharmacokinetics; resveratrol; tissue distributions.

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Drug Carriers / chemistry
  • Drug Delivery Systems*
  • Drug Screening Assays, Antitumor
  • Female
  • Humans
  • Mice
  • Mice, Inbred BALB C
  • Mice, Nude
  • Nanoparticles / chemistry*
  • Neoplasms, Experimental / drug therapy
  • Neoplasms, Experimental / pathology
  • Oligopeptides / chemistry
  • Oligopeptides / pharmacology*
  • Ovarian Neoplasms / drug therapy*
  • Ovarian Neoplasms / pathology
  • Resveratrol / chemistry
  • Resveratrol / pharmacology*
  • Serum Albumin, Human / chemistry*

Substances

  • Antineoplastic Agents
  • Drug Carriers
  • Oligopeptides
  • arginyl-glycyl-aspartic acid
  • Resveratrol
  • Serum Albumin, Human