Delivery of Ursolic Acid by Polyhydroxybutyrate Nanoparticles for Cancer Therapy: in silico and in vitro Studies.
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.
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