Cyclic RGD-Decorated Liposomal Gossypol AT-101 Targeting for Enhanced Antitumor Effect

• DOI: 10.2147/ijn.s341824
• Publication Date: 2022-01-13T12:10:15Z
• Authors: Hao Liu; Ruirui Zhang; Dan Zhang; Chun Zhang; Zhuo Zhang; Xiujuan Fu; Yu Luo; Siwei Chen; Ailing Wu; Weiling Zeng; Kunyan Qu; Hao Zhang; Sijiao Wang; Houyin Shi
• Keywords: Gossypol; Nanogel; Biodistribution

(-)-Gossypol (AT-101), the (-)-enantiomer of natural compound gossypol, has shown significant inhibitory effects on various types cancers such as osteosarcoma, myeloma, glioma, lung cancer, and prostate cancer. However, clinical application (-)-gossypol was often hindered by its evident side low bioavailability via oral administration, which necessitated development suitable preparations to settle problems. In this study, injectable cyclic RGD (cRGD)-decorated liposome (cRGD-LP) prepared for tumor-targeted delivery (-)-gossypol.The cRGD-LP based cRGD-modified lipids. For comparison, a non-cRGD-containing (LP) with similar chemical composition specially designed. The physicochemical properties (-)-gossypol-loaded (Gos/cRGD-LP) were investigated in terms drug loading efficiency, particle size, morphology, release, so on. effect Gos/cRGD-LP proliferation tumor cells vitro evaluated using different cell lines. biodistribution vivo near-infrared (NIR) fluorescence imaging technique. antitumor PC-3 tumor-bearing nude mice.Gos/cRGD-LP had an average size about 62 nm narrow distribution, efficiency over 90%, sustained release 96 h. results NIR demonstrated enhanced targeting vivo. Moreover, showed significantly tumors mice, inhibition rate 74% good biocompatibility.The incorporation cRGD could enhance tumor-targeting liposomes improve liposomal vivo, indicated potential that warrants further investigation applications single-isomer drug.