title: Lung-targeting drug delivery system of baicalin-loaded nanoliposomes: development, biodistribution in rabbits, and pharmacodynamics in nude mice bearing orthotopic human lung cancer.
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)liposomesto (Te)injectionof 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.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Southwest Medical University.
authors.forename: Yumeng
authors.initials: Y
authors.lastname: Wei
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Southwest Medical University.
authors.forename: Jing
authors.initials: J
authors.lastname: Liang
authors.affiliation: Department of Biochemistry, The Institute of Basic Medical Sciences, Southwest Medical University, Jiangyang District.
authors.forename: Xiaoli
authors.initials: X
authors.lastname: Zheng
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Southwest Medical University.
authors.forename: Chao
authors.initials: C
authors.lastname: Pi
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Southwest Medical University.
authors.forename: Hao
authors.initials: H
authors.lastname: Liu
authors.affiliation: Department of Oncology, The Affiliated Hospital of Southwest Medical University.
authors.forename: Hongru
authors.initials: H
authors.lastname: Yang
authors.affiliation: Department of Orthopedics, The Affiliated Hospital of Traditional Chinese Medicine of Southwest Medical University, Longma Tan District.
authors.forename: Yonggen
authors.initials: Y
authors.lastname: Zou
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Southwest Medical University; Department of Pharmacy, The Affiliated Hospital of Southwest Medical University, Luzhou City, Sichuan Province, People's Republic of China.
authors.forename: Yun
authors.initials: Y
authors.lastname: Ye
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Southwest Medical University.
authors.forename: Ling
authors.initials: L
authors.lastname: Zhao
mesh_terms: D000818:Animals; D004337:Drug Carriers / Q000493:pharmacokinetics; D016503:Drug Delivery Systems / Q000379:methods*; D004355:Drug Stability; D005419:Flavonoids / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D006801:Humans; D008081:Liposomes / Q000008:administration & dosage* / Q000493:pharmacokinetics; D008175:Lung Neoplasms / Q000188:drug therapy*; D051379:Mice; D008819:Mice, Nude; D049329:Nanostructures / Q000008:administration & dosage / Q000737:chemistry; D010316:Particle Size; D011817:Rabbits; D017207:Rats, Sprague-Dawley; D000068936:Theranostic Nanomedicine / Q000379:methods; D014018:Tissue Distribution; D023041:Xenograft Model Antitumor Assays
chemical_list: D004337:Drug Carriers; D005419:Flavonoids; D008081:Liposomes; C038044:baicalin
keywords: baicalin; biodistribution; cancer therapy; liposomes; lung-targeting drug delivery