Formulation of Piperine Nanoparticles: In Vitro Breast Cancer Cell Line and In Vivo Evaluation

Abstract

Piperine (PPN), one of the most investigated phytochemicals, is known to have excellent therapeutic efficacy against a variety of ailments including breast cancer. However, its physicochemical properties such as poor aqueous solubility restrict its clinical application. Therefore, the present investigation was designed to develop PPN encapsulated lipid polymer hybrid nanoparticles (PPN-LPHNPs) to overcome the limitation. The developed PPN-LPHNPs were optimized by the three-factor, three-level Box–Behnken design (33-BBD). The optimized PPN-LPHNPs were then evaluated for their drug release profile, cytotoxicity assay against MDA-MB-231 and MCF-7 cells, and gastrointestinal stability as well as colloidal stability. In addition, the optimized PPN-LPHNPs were evaluated for ex vivo intestinal permeation and in vivo pharmacokinetic in albino Wistar rats. As per the results, the optimized PPN-LPHNPs showed a small average particles size of <160 nm with a low (<0.3) polydispersity index, and highly positive surface charge (>+20 mV). PPN-LPHNPs revealed excellent gastrointestinal as well as colloidal stability and sustained release profiles up to 24 h. Furthermore, PPN-LPHNPs revealed excellent cytotoxicity against both MDA-MB-231 and MCF-7 cancer cells compared to the free PPN. Moreover, animal studies revealed that the PPN-LPHNPs exhibited a 6.02- and 4.55-fold higher intestinal permeation and relative oral bioavailability, respectively, in comparison to the conventional PPN suspension. Thus, our developed LPHNPs present a strong potential for improved delivery of PPN.

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

“…In addition, the greater cytotoxicity was attributed to small size, spherical morphology, and cytosolic PPN delivery from the nanocarrier. , Our finding also corroborated a previously published report. Kazmi et al studied the anticancer effect of PPN-loaded polymeric nanoparticles on MCF-7 cells . The researcher reported that the developed NPs showed IC 50 values of 21.32 ± 2.17 and 9.46 ± 2.18 μg/mL at 48 and 72 h, respectively.…”

“…Kazmi et al studied the anticancer effect of PPN-loaded polymeric nanoparticles on MCF-7 cells. 21 The researcher reported that the developed NPs showed IC 50 values of 21.32 ± 2.17 and 9.46 ± 2.18 μg/mL at 48 and 72 h, respectively. Therefore, it can be inferred that the development of PPN-encapsulated PCL-NPs can enhance the therapeutic efficacy against BC.…”

“…Moreover, the developed PPN-loaded nanocarrier exhibited significantly higher cellular uptake and anticancer effects against MCF-7 cells than native PPN. Similarly, Kazmi et al prepared PPN-encapsulated lipid-polymer hybrid nanoparticles (PPN-LPHNPs) to achieve higher therapeutic efficacy against BC . The developed PPN-LPHNPs showed a PS, PDI, and % EE of 151.2 ± 4.12 nm, 0.213 ± 0.02, and 83.54 ± 2.88%, respectively.…”

“…Similarly, Kazmi et al prepared PPN-encapsulated lipid-polymer hybrid nanoparticles (PPN-LPHNPs) to achieve higher therapeutic efficacy against BC. 21 The developed PPN-LPHNPs showed a PS, PDI, and % EE of 151.2 ± 4.12 nm, 0.213 ± 0.02, and 83.54 ± 2.88%, respectively. Further, the nanocarrier showed a lower IC 50 value in the cell viability study using MCF-7 cells than pure PPN.…”

Bioinspired Folic Acid-ADH-PLGA Polymeric Nanoparticles Loaded with Mangiferin and Piperine: A Promising Strategy for Targeted Delivery in Multidrug-Resistant Lung Cancer Cells

“…After centrifuging the dispersion for 12 min at 10,000 rpm, the foreign polymeric substances was separated from the supernatant. The clear supernantant solution was examined by HPLC at 415 nm and 342 nm, respectively, to ascertain the amount of loaded mangiferin and piperine in the developed FAP nanoparticle system [18][19][20].…”