Engineering Lipusu with lysophosphatidylcholine for improved tumor cellular uptake and anticancer efficacy. Issue 11 (25th February 2022)

• Record Type: Journal Article
• Authors: Li, Lijie; Zhan, Qi; Yi, Kaikai; Chen, Ning; Li, Xueping; Yang, Shixue; Hou, Xin; Zhao, Jin; Yuan, Xubo; Kang, Chunsheng
• Is Part Of: Journal of materials chemistry. Volume 10:Issue 11(2022)
• Page Start: 1833
• Page End: 1842
• Publication Date: 2022-02-25
• Subjects: Materials -- Periodicals; Chemistry, Analytic -- Periodicals; Biomedical materials -- Research -- Periodicals; 543.0284
• DOI: 10.1039/d1tb02823e
• Languages: English
• ISSNs: 2050-750X

Abstract

Abstract : This work provides a new idea that, by engineering the lipids of Lipusu, enhanced tumor cellular uptake and antitumor efficacy can be achieved. Abstract : Liposomes have been developed as drug delivery carriers to enhance the antitumor efficiency of therapeutic agents. Lipusu® (Lip), a paclitaxel (PTX) liposome, has been widely used in the treatment of breast cancer. Compared with PTX, Lip could change the biodistribution and reduce the systemic toxicity. However, there was no positive effect on the entry of PTX into tumor cells, and thus the therapeutic effect was not significantly improved. Therefore, it is meaningful to engineer Lip for improving tumor cellular uptake efficiency. Here, lysophosphatidylcholine (LPC)-engineered Lip (LPC-Lip) was constructed via inserting single chain lipid tails into liposomal lipid bilayers, which was realized by simple incubation. Compared with Lip, the better cellular uptake of liposomes modified with LPC resulted in enhanced cytotoxic activity of LPC-Lip in 4T1 cells. Furthermore, stronger tumor growth inhibition was observed in LPC-Lip treated 4T1 tumor-bearing mice without significant side effects. In conclusion, by modulating the lipid composition of Lip, the antitumor efficacy can be improved, and LPC engineered Lip may serve as a promising formulation of PTX for future cancer therapy.