Piperine-Loaded PLGA Nanoparticles as Cancer Drug Carriers

Abstract

Factors like oxidative stress, environmental risk factors, genetics, chemical treatments, and resistance to treatment strategies all have serious impediments in scientific progress for treating diseases. Naturally occurring bioactive compounds when associated with nanocarriers could provide a solution for tackling problems as therapeutic agents against cancer. This report investigates a facile method of using ultrasonic atomization for synthesizing piperine-loaded poly(d,l-lactide-co-glycolic acid) (PLGA) nanocomposites specialized for targeted drug delivery for their potential use against cancer. The nanoformulation was characterized using dynamic light scattering (DLS), microscopic techniques like scanning electron microscopy (SEM), transmission electron microscopy (TEM), and confocal laser scanning microscopy (CLSM), spectroscopic methods for determination of encapsulation efficiency, sustained-release kinetics, and cellular studies like cellular uptake study and in vitro antitumor activity against different cancer cell lines. The ultrasonic atomization led to the formation of NPs with a mean size of 95 ± 10 nm and a zeta (ζ) potential of -19.29 mV. In vitro release was sustained up to 312 h with about 28% cumulative release at pH 7.2 and 91% at pH 5.5. The tailored delivery of nanocarriers suppressed cancer cell growth and migration in a variety of cancer cell lines, indicating anticancer properties. This nanocarrier formulation showed low cytotoxicity towards HEK-293 in comparison to HeLa, A549, HT1080, PC-3, and MCF-7 cancer cell lines when analyzed for cell viability through 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide dye (MTT) assay. The results suggest that nanocarrier-mediated delivery of piperine (Pip) could prove to be efficient against cancer and aid in reaching inaccessible sites, overcome physiological barriers, and maintain the concentration of drugs, and has higher targeting capability and reduced cellular toxicity. ©