Preprint Article Version 2 Preserved in Portico This version is not peer-reviewed

Synergistic Effects of Chemotherapy and Phototherapy on Ovarian Cancer Using Follicle-Stimulating Hormone Receptor-Mediated Liposomes Co-Loaded with SN38 and IR820

Version 1 : Received: 5 February 2024 / Approved: 5 February 2024 / Online: 5 February 2024 (08:14:52 CET)
Version 2 : Received: 5 February 2024 / Approved: 6 February 2024 / Online: 6 February 2024 (05:18:17 CET)

A peer-reviewed article of this Preprint also exists.

Pian, L.; Zeng, B.; Wang, N.; Wang, S.; Wu, H.; Wan, H.; Chen, L.; Huang, W.; Gao, Z.; Jin, D.; Jin, M. Synergistic Effects of Chemotherapy and Phototherapy on Ovarian Cancer Using Follicle-Stimulating Hormone Receptor-Mediated Liposomes Co-Loaded with SN38 and IR820. Pharmaceutics 2024, 16, 490. Pian, L.; Zeng, B.; Wang, N.; Wang, S.; Wu, H.; Wan, H.; Chen, L.; Huang, W.; Gao, Z.; Jin, D.; Jin, M. Synergistic Effects of Chemotherapy and Phototherapy on Ovarian Cancer Using Follicle-Stimulating Hormone Receptor-Mediated Liposomes Co-Loaded with SN38 and IR820. Pharmaceutics 2024, 16, 490.

Abstract

We developed an ovarian cancer-targeted drug delivery system based on a follicle-stimulating hormone receptor (FSHR) peptide. The lipophilic chemotherapeutic drug SN38 and the photosensitizer IR820 were loaded into the phospholipid bilayer of liposomes. Near-infrared laser irradiation stimulated the generation of reactive oxygen species, causing short-term reactive molecular species and spatial-temporal restricted photodamage to the biological targets. The reactive molecular species and spatial-temporal restricted photodamage enhanced the release and uptake of chemotherapy drugs and increased the sensitivity to chemotherapy drugs in ovarian cancer cells. FSH liposomes loaded with SN38 and IR820 (SN38/IR820-Lipo@FSH) were prepared using thin-film hydration-sonication. FSH peptide binding was analyzed using 1H NMR spectrum and Maldi-Tof. The average size and zeta potential of SN38/IR820-Lipo@FSH were 105.1 ± 1.15 nm (PDI: 0.204 ± 0.03) and −27.8 ± 0.42 mV, respectively. SN38/IR820-Lipo@FSH exhibited good drug-loading properties and the in vitro release was slow. FSH significantly increased the uptake of liposomes, inhibited cell proliferation, and induced apoptosis in A2780 cells. Moreover, SN38/IR820-Lipo@FSH exhibited good tumor-targeting ability and anti-ovarian cancer activity in vivo. The SN38/IR820-Lipo@FSH exhibited specific targeting to A2780 ovarian cancer cells. The combination of chemotherapy and photodynamic treatment based on an FSH peptide-targeted delivery system may be an effective approach to treating ovarian cancer.

Keywords

FSHβ (33-53) peptide; Ovarian cancer; Targeting therapy; PDT; SN38

Subject

Medicine and Pharmacology, Obstetrics and Gynaecology

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