Lei Yang1,2, Jin Xin1, Zhenhai Zhang1, Hongmei Yan1, Jing Wang1, E Sun1, Jian Hou1,2, Xiaobin Jia1,2, Huixia Lv3. 1. Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, Nanjing, Jiangsu, China. 2. College of Pharmacy, Jiangsu University, Zhenjiang, Jiangsu, China. 3. Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu, China.
Abstract
OBJECTIVE: This work aimed at preparing ginsenoside compound K (GCK)-loaded liposomes modified with TPGS (GCKT-liposomes) to enhance solubility and targeting capability of GCK, as well as inhibit the efflux of GCK from tumour cells. METHODS: GCKT-liposomes were prepared by the thin-film hydration method and characterized by particle size, polydispersity, zeta potential and drug encapsulation efficiency. A549 cells were used as antitumour cell model to access the cellular uptake of the GCK and perform its antitumour function. The enhancement of in vivo antitumour efficacy of GCKT-liposomes was evaluated by nude mice bearing tumour model. KEY FINDINGS: The results showed that GCKT-liposomes achieved a comparatively high drug loading efficiency and reasonable particle size at the ratio of 7 : 3 (phospholipid: TPGS). The in vitro release demonstrated that the dissolution of GCK was remarkably improved by entrapping it into liposomes. In addition, GCKT-liposomes exhibited a great hypersensitizing effect on A549 cells, and the cellular uptake was enhanced. Compared with free GCK, the IC50 of GCKT-liposomes was significantly reduced (16.3 ± 0.8 vs 24.9 ± 1.0 μg/ml). In vivo antitumour assay also indicated that GCKT-liposomes achieved higher antitumour efficacy (67.5 ± 0.5 vs 40.8 ± 0.7%). CONCLUSION: The novel GCKT-liposomes significantly improved the antitumour efficacy of GCK.
OBJECTIVE: This work aimed at preparing ginsenoside compound K (GCK)-loaded liposomes modified with TPGS (GCKT-liposomes) to enhance solubility and targeting capability of GCK, as well as inhibit the efflux of GCK from tumour cells. METHODS: GCKT-liposomes were prepared by the thin-film hydration method and characterized by particle size, polydispersity, zeta potential and drug encapsulation efficiency. A549 cells were used as antitumour cell model to access the cellular uptake of the GCK and perform its antitumour function. The enhancement of in vivo antitumour efficacy of GCKT-liposomes was evaluated by nude mice bearing tumour model. KEY FINDINGS: The results showed that GCKT-liposomes achieved a comparatively high drug loading efficiency and reasonable particle size at the ratio of 7 : 3 (phospholipid: TPGS). The in vitro release demonstrated that the dissolution of GCK was remarkably improved by entrapping it into liposomes. In addition, GCKT-liposomes exhibited a great hypersensitizing effect on A549 cells, and the cellular uptake was enhanced. Compared with free GCK, the IC50 of GCKT-liposomes was significantly reduced (16.3 ± 0.8 vs 24.9 ± 1.0 μg/ml). In vivo antitumour assay also indicated that GCKT-liposomes achieved higher antitumour efficacy (67.5 ± 0.5 vs 40.8 ± 0.7%). CONCLUSION: The novel GCKT-liposomes significantly improved the antitumour efficacy of GCK.
Authors: Lei Yang; Zhenghai Zhang; Jian Hou; Xin Jin; Zhongcheng Ke; Dan Liu; Mei Du; Xiaobing Jia; Huixia Lv Journal: Int J Nanomedicine Date: 2017-10-17