Delivery of Ursolic Acid by Polyhydroxybutyrate Nanoparticles for Cancer Therapy: in silico and in vitro Studies.
Sureshbabu Ram Kumar PandianKunjiappan SelvarajParasuraman PavadaiVelmurugan SundarapandianVivek ChandramohanKrishnan SundarPublished in: Drug research (2021)
Ursolic acid (UA), a pentacyclic triterpenoid and a phytochemical, is a potent inhibitory agent against proliferation of various tumors. Polyhydroxybutyrate nanoparticles (PHB NPs) are preferred in therapeutics due to their drug-stabilizing property and enhanced biological activity. In this study, PHB NPs were utilized to deliver and enhance the bioavailability of UA against cancer cells (HeLa). Further, molecular docking and dynamic studies were conducted to calculate the binding affinity and stability of UA at the active site of target protein (epidermal growth factor receptor-EGFR). The PHB NPs revealed the average size as 150-200 nm in TEM, which were used in subsequent experiments. The cytoplasmic uptake of nanoparticles was confirmed by florescent microscopy. The encapsulation potential of PHB NPs with UA was assessed by UV-visible spectrophotometer as 54%. Besides, the drug release behavior, cytotoxicity and the regulation of apoptosis were investigated in vitro. The cytotoxicity results revealed that the maximum efficiency of drug delivery was at 96th hour.
Keyphrases
- epidermal growth factor receptor
- molecular docking
- drug delivery
- drug release
- cancer therapy
- tyrosine kinase
- advanced non small cell lung cancer
- oxide nanoparticles
- molecular dynamics simulations
- cell cycle arrest
- small cell lung cancer
- single cell
- case control
- cell death
- single molecule
- blood pressure
- oxidative stress
- signaling pathway
- small molecule
- high throughput
- emergency department
- high speed
- walled carbon nanotubes
- climate change
- amino acid
- atomic force microscopy
- optical coherence tomography
- mass spectrometry
- protein protein