Impact of PEGylated liposomes on cytotoxicity of tamoxifen and piperine on MCF-7 human breast carcinoma cells

Tamoxifen (TMF) is an anticancer agent used for managing estrogen receptor-positive breast cancer. It has limited therapeutic efficacy against breast cancer, which could be enhanced by the coadministration of herbal drugs like piperine (PIP). However, the hydrophobic nature of TMF and PIP restricts their therapeutic application. Therefore, the present study focuses on the impact of the anticancer activity of TMF in combination with PIP and after entrapping them into liposomes (TMF-PIP-LPs and TMF-PIP-PEG-LPs). The liposomes were prepared using the thin film hydration method. In addition, the morphology of the prepared liposomes was found spherical after SEM and TEM analyses. Further, the in vitro cytotoxicity (IC50) study of pure PIP and TMF was found to be 90.3 ± 10.2 μg/mL and 40.9 ± 5.9 μg/mL, respectively. Interestingly, an improved cytotoxicity (IC50) was observed when the TMF and PIP were loaded into liposomes (TMF-PIP-LPs: 21 ± 1.6 μg/mL and TMF-PIP-PEG-LPs: 10 ± 0.5 μg/mL). Also, the PEGylated liposomes showed improvement in cellular uptake as compared to liposomes without PEGylation in MCF-7 human breast carcinoma cells. Thus, the enhanced cellular uptake and improved cytotoxicity of PEGylated liposomes can be a suitable strategy for delivering TMF with PIP for breast cancer treatment. [Display omitted] •The lipid soybean phosphatidylcholine was used to prepare tamoxifen-piperine liposomes (TMF-PIP-LPs).•The lipid DSPE-PEG2000 was utilized to prepare PEGylated liposomes (TMF-PIP-PEG-LPs).•The cytotoxicity of TMF was significantly increased when combined with PIP in MCF-7 cell lines.•TMF-PIP-PEG-LPs showed enhanced cellular uptake and improved cytotoxicity as compared to TMF-PIP-LPs.