A multi-component paclitaxel -loaded β-elemene nanoemulsion by transferrin modification enhances anti-non-small-cell lung cancer treatment

Int J Pharm. 2024 Sep 30:663:124570. doi: 10.1016/j.ijpharm.2024.124570. Epub 2024 Aug 10.

Abstract

A multi-component paclitaxel (PTX) -loaded β-elemene nanoemulsion by transferrin modification (Tf-PE-MEs) was developed to enhance non-small-cell lung cancer (NSCLC) treatment. After transferrin modification, the particle size of Tf-PE-MEs was (14.87 ± 1.84) nm, and the zeta potential was (-10.19 ± 0.870) mV, respectively. In vitro experiments showed that Tf-PE-MEs induced massive apoptosis in A549 cells, indicating that it had significant cytotoxicity to A549 cells. Through transferrin modification, Tf-PE-MEs accumulated at the tumor site efficiently with overexpressed transferrin receptor (TfR) on the surface of A549 cells. This will allow increasing PTX and β-elemene concentration in the target cells, enhancing the therapeutic effect. Compared to PTX alone, Tf-PE-MEs displayed good anti-tumor efficacy and diminished systemic toxicity in vivo studies. With favourable therapeutic potential, this study provides a new strategy for the combined anticancer treatment of non-small cell lung cancer.

Keywords: Nanoemulsion; Non-small-cell lung cancer; Tumor target.

MeSH terms

  • A549 Cells
  • Animals
  • Antineoplastic Agents, Phytogenic* / administration & dosage
  • Antineoplastic Agents, Phytogenic* / chemistry
  • Antineoplastic Agents, Phytogenic* / pharmacology
  • Apoptosis* / drug effects
  • Carcinoma, Non-Small-Cell Lung* / drug therapy
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Drug Liberation
  • Emulsions*
  • Humans
  • Lung Neoplasms* / drug therapy
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Mice, Nude
  • Nanoparticles* / chemistry
  • Paclitaxel* / administration & dosage
  • Paclitaxel* / chemistry
  • Paclitaxel* / pharmacology
  • Particle Size
  • Receptors, Transferrin / metabolism
  • Sesquiterpenes* / administration & dosage
  • Sesquiterpenes* / chemistry
  • Sesquiterpenes* / pharmacology
  • Transferrin* / administration & dosage
  • Transferrin* / chemistry

Substances

  • Paclitaxel
  • beta-elemene
  • Transferrin
  • Emulsions
  • Sesquiterpenes
  • Antineoplastic Agents, Phytogenic
  • Receptors, Transferrin