Development of Statistically Optimized Piperine-Loaded Polymeric Nanoparticles for Breast Cancer: In Vitro Evaluation and Cell Culture Studies

High Resolution Image Download MS PowerPoint Slide Piperine (PPN) is a natural alkaloid derived from black pepper ( Piper nigrum L.) and has garnered substantial attention for its potential in breast cancer therapy due to its diverse pharmacological properties. However, its highly lipophilic characteristics and poor dissolution in biological fluids limit its clinical application. Therefore, to overcome this limitation, we formulate and evaluate PPN-encapsulated polycaprolactone (PCL) nanoparticles (PPN-PCL-NPs). The nanoparticles were prepared by a single-step nanoprecipitation method and further optimized by a formulation design approach. The influence of selected independent variables PCL ( X 1 ), poloxamer 188 (P-188; X 2 ), and stirring speed (SS; X 3 ) were investigated on the particle size (PS), polydispersity index (PDI), and % encapsulation efficiency (EE). The selected optimized nanoparticles were further assessed for stability, in vitro release, and in vitro antibreast cancer activity in the MCF-7 cancer cell line. The PS, PDI, zeta potential, and % EE of the optimized PPN-PCL-NPs were observed to be 107.61 ± 5.28 nm, 0.136 ± 0.011, −20.42 ± 1.82 mV, and 79.53 ± 5.22%, respectively. The developed PPN-PCL-NPs were stable under different temperature conditions with insignificant changes in their pharmaceutical attributes. The optimized PPN-PCL-NPs showed a burst release for the first 6 h and later showed sustained release for 48 h. The PPN-PCL-NPs exhibit exceptional cytotoxic effects in MCF-7 breast tumor cells in comparison with the native PPN. Thus, the formulation of PPN-loaded PCL-NPs can be a promising approach for better therapeutic efficacy against breast cancer.