title: Development of lipid-shell and polymer core nanoparticles with water-soluble salidroside for anti-cancer therapy.
abstract: Salidroside (Sal) is a potent antitumor drug with high water-solubility. The clinic application of Sal in cancer therapy has been significantly restricted by poor oral absorption and low tumor cell uptake. To solve this problem, lipid-shell and polymer-core nanoparticles (Sal-LPNPs) loaded with Sal were developed by a double emulsification method. The processing parameters including the polymer types, organic phase, PVA types and amount were systemically investigated. The obtained optimal Sal-LPNPs, composed of PLGA-PEG-PLGA triblock copolymers and lipids, had high entrapment efficiency (65%), submicron size (150 nm) and negatively charged surface (-23 mV). DSC analysis demonstrated the successful encapsulation of Sal into LPNPs. The core-shell structure of Sal-LPNPs was verified by TEM. Sal released slowly from the LPNPs without apparent burst release. MTT assay revealed that 4T1 and PANC-1 cancer cell lines were sensitive to Sal treatment. Sal-LPNPs had significantly higher antitumor activities than free Sal in 4T1 and PANC-1 cells. The data indicate that LPNPs are a promising Sal vehicle for anti-cancer therapy and worthy of further investigation.
authors.affiliation: State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China. fangdailongtwozero@126.com.
authors.forename: Dai-Long
authors.initials: DL
authors.lastname: Fang
authors.affiliation: State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China. yanzai1112@sina.com.
authors.forename: Yan
authors.initials: Y
authors.lastname: Chen
authors.affiliation: State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China. xb1990625@126.com.
authors.forename: Bei
authors.initials: B
authors.lastname: Xu
authors.affiliation: Department of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, NE 68198, USA. renkemallee@gmail.com.
authors.forename: Ke
authors.initials: K
authors.lastname: Ren
authors.affiliation: State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China. heyaode@163.com.
authors.forename: Zhi-Yao
authors.initials: ZY
authors.lastname: He
authors.affiliation: College of Chemistry and Environment Protection Engineering, Southwest University for Nationalities, Chengdu 610041, Sichuan, China. lilihes@163.com.
authors.forename: Li-Li
authors.initials: LL
authors.lastname: He
authors.affiliation: State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China. 13981836037@139.com.
authors.forename: Yi
authors.initials: Y
authors.lastname: Lei
authors.affiliation: State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China. fanchunmeiok@163.com.
authors.forename: Chun-Mei
authors.initials: CM
authors.lastname: Fan
authors.affiliation: State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China. songxr@scu.edu.cn.
authors.forename: Xiang-Rong
authors.initials: XR
authors.lastname: Song
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004339:Drug Compounding; D005960:Glucosides / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D008055:Lipids / Q000737:chemistry*; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles / Q000737:chemistry* / Q000633:toxicity / Q000648:ultrastructure; D010636:Phenols / Q000737:chemistry* / Q000494:pharmacology; D011092:Polyethylene Glycols / Q000737:chemistry; D011098:Polyglactin 910 / Q000737:chemistry; D011108:Polymers / Q000737:chemistry*; D012995:Solubility; D012997:Solvents / Q000737:chemistry; D014867:Water / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D005960:Glucosides; D008055:Lipids; D010636:Phenols; D011108:Polymers; D012997:Solvents; C528571:poly(lactic-co-glycolic acid)-polyethylene glycol-poly(lactic-co-glycolic acid); D014867:Water; D011098:Polyglactin 910; D011092:Polyethylene Glycols; C009172:rhodioloside