| Summary: | Yumeng Wei,1 Jing Liang,1 Xiaoli Zheng,2 Chao Pi,1 Hao Liu,1 Hongru Yang,3 Yonggen Zou,4 Yun Ye,1,5 Ling Zhao1 1Department of Pharmaceutics, School of Pharmacy, Southwest Medical University, 2Department of Biochemistry, The Institute of Basic Medical Sciences, Southwest Medical University, Jiangyang District, 3Department of Oncology, The Affiliated Hospital of Southwest Medical University, 4Department of Orthopedics, The Affiliated Hospital of Traditional Chinese Medicine of Southwest Medical University, Longma Tan District, 5Department of Pharmacy, The Affiliated Hospital of Southwest Medical University, Luzhou City, Sichuan Province, People’s Republic of China Abstract: The present study aims to develop a kind of novel nanoliposomes for the lung-targeting delivery system of baicalin as a Chinese medicine monomer. Baicalin-loaded nanoliposomes were prepared by the effervescent dispersion and lyophilized techniques. Baicalin-loaded nanoliposomes had an average particle size of 131.7±11.7 nm with 0.19±0.02 polydispersity index, 82.8%±1.24% entrapment efficiency and 90.47%±0.93% of yield and sustaining drug release effect over 24 h and were stable for 12 months at least. In vitro no hemolytic activity was observed for the experimental drug concentration. After intravenous administration of baicalin-loaded nanoliposomes to rabbits, drug concentration in the lungs was the highest among the tested organs at all time points and was significantly higher than that of its solution. For the targeting parameters, the relative intake rate and the ratio of peak concentration of lung were 4.837 and 2.789, respectively. Compared with plasma, liver, spleen, and kidney, the ratios of targeting efficacy (Te)liposomes to (Te)injection of lung were increased by a factor of 14.131, 1.893, 3.357, and 3.470, respectively. Furthermore, the results showed that the baicalin-loaded nanoliposomes did not induce lung injury. Importantly, baicalin-loaded nanoliposomes showed better antitumor therapeutic efficacy in the nude mice bearing orthotopic human lung cancer with the median survival time of blank liposomes (11.40±0.16 days), baicalin solution (17.30±0.47 days), and baicalin-loaded nanoliposomes (25.90±0.53 days). Therefore, the liposome is a promising drug carrier with an excellent lung-targeting property and therapeutic effect for the treatment of lung disease, such as lung cancer. Keywords: liposomes, biodistribution, lung-targeting drug delivery, cancer therapy, baicalin
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