title: Preparation of a paclitaxel-loaded cationic nanoemulsome and its biodistribution via direct intratumoral injection.
abstract: In this study, a nano-preparation based on nanoemulsome (NES) modified with cetyltrimethylammonium bromide (CTAB) loading paclitaxel (PTX) was designed, and its biodistribution were explored after intratumoral (i.t.) administration on Heps tumor-bearing mice. The PTX-loaded nanoemulsome (PTX-NES) was prepared by using a solvent evaporation method and CTAB, chosen as a cationic material, was absorbed onto the surface of the NES via electrostatic interaction to yield paclitaxel-loaded cationic nanoemulsome (PTX-CTAB-NES). The MTT results exhibited that PTX-CTAB-NES (IC50: 0.50±0.035μg/mL in MCF-7 cells and 0.13±0.048μg/mL in SMMC-7721 cells) had the strongest cytotoxicity compared to Taxol (IC50: 0.88±0.054μg/mL in MCF-7 and 0.15±0.011μg/mL in SMMC-7721) and PTX-NES (IC50: 1.93±0.062μg/mL in MCF-7 and 0.32±0.027μg/mL in SMMC-7721). Body distribution of PTX revealed that the percent of PTX retained in the tumor after i.t. administration of PTX-CTAB-NES (approximately 92.99% at 0.167h and 15.35% at 48h) was higher when compared to that after i.t. injection of Taxol (approximately 58.94% at 0.167h and 0.83% at 48h) or PTX-NES (approximately 83.63% at 0.167h and 6.52% at 48h). Moreover, less PTX accumulated in liver, spleen, kidney, lung and heart after i.t. administration of PTX-CTAB-NES when compared with that after i.v. administration of PTX-CTAB-NES. In conclusion, PTX-CTAB-NES was a prospective in-situ delivery system for the therapy of tumor.
authors.affiliation: Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, PR China.
authors.forename: Yurui
authors.initials: Y
authors.lastname: Xu
authors.affiliation: Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, PR China; Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Faisalabad, Pakistan.
authors.forename: Sajid
authors.initials: S
authors.lastname: Asghar
authors.affiliation: Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, PR China; Affiliated Hospital of Weifang Medical University, Weifang 261031, PR China.
authors.forename: Hongying
authors.initials: H
authors.lastname: Li
authors.affiliation: Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, PR China.
authors.forename: Minglei
authors.initials: M
authors.lastname: Chen
authors.affiliation: Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, PR China.
authors.forename: Zhigui
authors.initials: Z
authors.lastname: Su
authors.affiliation: Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, PR China.
authors.forename: Yangfan
authors.initials: Y
authors.lastname: Xu
authors.affiliation: Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, PR China.
authors.forename: Qineng
authors.initials: Q
authors.lastname: Ping
authors.affiliation: Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, PR China. Electronic address: cpuyanyuxiao@163.com.
authors.forename: Yanyu
authors.initials: Y
authors.lastname: Xiao
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000493:pharmacokinetics* / Q000494:pharmacology; D019540:Area Under Curve; D000077286:Cetrimonium; D002593:Cetrimonium Compounds / Q000737:chemistry*; D004337:Drug Carriers; D004339:Drug Compounding; D006801:Humans; D020128:Inhibitory Concentration 50; D015552:Injections, Intralesional; D008055:Lipids / Q000737:chemistry*; D061986:MCF-7 Cells; D008297:Male; D051379:Mice; D008823:Micelles; D017239:Paclitaxel / Q000493:pharmacokinetics* / Q000494:pharmacology; D010316:Particle Size; D013499:Surface Properties; D014018:Tissue Distribution; D023041:Xenograft Model Antitumor Assays
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D002593:Cetrimonium Compounds; D004337:Drug Carriers; D008055:Lipids; D008823:Micelles; D017239:Paclitaxel; D000077286:Cetrimonium
keywords: Body distribution; Cetyltrimethylammonium bromide; Intratumoral drug delivery; Nanoemulsome; Pharmacokinetics