title: Efficacy of dual-functional liposomes containing paclitaxel for treatment of lung cancer.
abstract: This study was mainly focused on the development of a dual-ligand liposomal delivery system for targeting the delivery of paclitaxel (PTX) to lung cancer. The specific ligand peptide HAIYPRH (T7) and the cationic cell-penetrating peptide TAT were connected with phospholipid via a polyethylene glycol (PEG) spacer to prepare the dual-ligand liposomes (T7/TAT-LP-PTX). Physicochemical characterizations of T7/TAT-LP-PTX, such as particle size, ζ potential, morphology, encapsulation efficiency, and in vitro PTX release, were also evaluated. In the cellular uptake study, the T7/TAT-LP endocytosed by the A549 cells was 2.26-, 3.48- and 8.56-fold higher than TAT-LP, T7-LP and LP, respectively. The IC50 values of TAT-LP-PTX, T7-LP-PTX and LP-PTX were much higher than those of T7/TAT-LP-PTX, respectively. The homing specificity of T7/TAT-LP was evaluated on the tumor spheroids, which revealed that T7/TAT-LP was more efficaciously internalized in tumor cells than TAT-LP, T7-LP and LP, respectively. Compared to LP, TAT-LP and T7-LP, T7/TAT-LP showed the strongest cell uptake property, and the highest accumulation ability in tumor spheroids in vitro. In the in vivo study, the T7/TAT-LP-PTX exhibited the best inhibitory effect of tumor growth for A549-bearing mice. Collectively, these results suggested that T7/TAT-LP-PTX is a promising drug delivery system for the treatment of lung cancer.
authors.affiliation: Department of Cardiothoracic Surgery, People's Hospital of Zhangqiu, Zhangqiu, Shandong 250200, P.R. China.
authors.forename: Rong-Hua
authors.initials: RH
authors.lastname: Wang
authors.affiliation: Pharmacy Intravenous Admixture Services, People's Hospital of Zhangqiu, Zhangqiu, Shandong 250200, P.R. China.
authors.forename: Hong-Mei
authors.initials: HM
authors.lastname: Cao
authors.affiliation: Pharmacy Intravenous Admixture Services, People's Hospital of Zhangqiu, Zhangqiu, Shandong 250200, P.R. China.
authors.forename: Zhi-Ju
authors.initials: ZJ
authors.lastname: Tian
authors.affiliation: Department of Cardiothoracic Surgery, People's Hospital of Zhangqiu, Zhangqiu, Shandong 250200, P.R. China.
authors.forename: Bo
authors.initials: B
authors.lastname: Jin
authors.affiliation: Department of Orthopedic Surgery, People's Hospital of Zhangqiu, Zhangqiu, Shandong 250200, P.R. China.
authors.forename: Qing
authors.initials: Q
authors.lastname: Wang
authors.affiliation: Department of Oral Pendulum Medicine, People's Hospital of Zhangqiu, Zhangqiu, Shandong 250200, P.R. China.
authors.forename: Hong
authors.initials: H
authors.lastname: Ma
authors.affiliation: Pharmacy Intravenous Admixture Services, The Second Hospital of Shandong University, Jinan, Shandong 250033, P.R. China.
authors.forename: Jing
authors.initials: J
authors.lastname: Wu
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D057846:Cell-Penetrating Peptides / Q000737:chemistry*; D016503:Drug Delivery Systems; D006801:Humans; D008081:Liposomes / Q000008:administration & dosage / Q000737:chemistry*; D008175:Lung Neoplasms / Q000188:drug therapy*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D017239:Paclitaxel / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry*; D015398:Signal Transduction / Q000187:drug effects; D023041:Xenograft Model Antitumor Assays
chemical_list: D057846:Cell-Penetrating Peptides; D008081:Liposomes; D011092:Polyethylene Glycols; D017239:Paclitaxel