Abstract
The present research work is designed to prepare and evaluate piperine liposomes and piperine–chitosan-coated liposomes for oral delivery. Piperine (PPN) is a water-insoluble bioactive compound used for different diseases. The prepared formulations were evaluated for physicochemical study, mucoadhesive study, permeation study and in vitro cytotoxic study using the MCF7 breast cancer cell line. Piperine-loaded liposomes (PLF) were prepared by the thin-film evaporation method. The selected liposomes were coated with chitosan (PLFC) by electrostatic deposition to enhance the mucoadhesive property and in vitro therapeutic efficacy. Based on the findings of the study, the prepared PPN liposomes (PLF3) and chitosan coated PPN liposomes (PLF3C1) showed a nanometric size range of 165.7 ± 7.4 to 243.4 ± 7.5, a narrow polydispersity index (>0.3) and zeta potential (−7.1 to 29.8 mV). The average encapsulation efficiency was found to be between 60 and 80% for all prepared formulations. The drug release and permeation study profile showed biphasic release behavior and enhanced PPN permeation. The in vitro antioxidant study results showed a comparable antioxidant activity with pure PPN. The anticancer study depicted that the cell viability assay of tested PLF3C2 has significantly (p < 0.001)) reduced the IC50 when compared with pure PPN. The study revealed that oral chitosan-coated liposomes are a promising delivery system for the PPN and can increase the therapeutic efficacy against the breast cancer cell line.
Highlights
Piperine (PPN) is the major bioactive compound found in black pepper
The permeation study was performed for PLF3 and PLF3C1 formulations, and the results were compared with pure PPN
Data reveal that lower concentrations of both pure PPN and PPN liposome formulaData reveal that lower concentrations of both pure PPN and PPN liposome formulations have minimal effects on the cell viability of MCF7, which is reduced with increasing tions have minimal effects on the cell viability of MCF7, which is reduced with increasing concentration (Figure 6)
Summary
Piperine (PPN) is the major bioactive compound found in black pepper. It has been widely used as a food supplement and has many therapeutic properties in different diseases. Using natural bioactive compounds with an anticancer property is a useful alternative to breast cancer chemotherapy treatment. Jain et al reported that PIP increased the generation of the intracellular ROS level in HeLa and MCF-7, which arrest the cell cycle at the G2/M phase with decreased cell viability [12] It inhibits the spouting process of rat aorta in angiogenesis induced by breast cancer cells [13]. A number of nanosized delivery systems have been reported for the anticancer activity of PPN, such as piperine with paclitaxel liposomes [15], apamycin and piperine polymeric nanoparticles [16], piperine micelles [17], PIP hydroxyapatite nanoparticles [18], curcumin and piperine emulsomes [19] and protopanaxadiol-piperine nanoparticles [20]. The selected chitosan-coated PPN liposomes were evaluated for cytotoxic effects in the MF7 breast cancer cell line
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