title: Biodegradable self-assembled PEG-PCL-PEG micelles for hydrophobic honokiol delivery: I. Preparation and characterization.
abstract: This study aims to develop self-assembled poly(ethylene glycol)-poly(epsilon-caprolactone)-poly(ethylene glycol) (PEG-PCL-PEG, PECE) micelles to encapsulate hydrophobic honokiol (HK) in order to overcome its poor water solubility and to meet the requirement of intravenous administration. Honokiol loaded micelles (HK-micelles) were prepared by self-assembly of PECE copolymer in aqueous solution, triggered by its amphiphilic characteristic assisted by ultrasonication without any organic solvents, surfactants and vigorous stirring. The particle size of the prepared HK-micelles measured by Malvern laser particle size analyzer were 58 nm, which is small enough to be a candidate for an intravenous drug delivery system. Furthermore, the HK-micelles could be lyophilized into powder without any adjuvant, and the re-dissolved HK-micelles are stable and homogeneous with particle size about 61 nm. Furthermore, the in vitro release profile showed a significant difference between the rapid release of free HK and the much slower and sustained release of HK-micelles. Moreover, the cytotoxicity results of blank micelles and HK-micelles showed that the PECE micelle was a safe carrier and the encapsulated HK retained its potent antitumor effect. In short, the HK-micelles were successfully prepared by an improved method and might be promising carriers for intravenous delivery of HK in cancer chemotherapy, being effective, stable, safe (organic solvent and surfactant free), and easy to produce and scale up.
authors.affiliation: State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, and School of Life Sciences, Sichuan University, Chengdu, 610041, People's Republic of China.
authors.forename: ChangYang
authors.initials: C
authors.lastname: Gong
authors.forename: XiaWei
authors.initials: X
authors.lastname: Wei
authors.forename: XiuHong
authors.initials: X
authors.lastname: Wang
authors.forename: YuJun
authors.initials: Y
authors.lastname: Wang
authors.forename: Gang
authors.initials: G
authors.lastname: Guo
authors.forename: YongQiu
authors.initials: Y
authors.lastname: Mao
authors.forename: Feng
authors.initials: F
authors.lastname: Luo
authors.forename: ZhiYong
authors.initials: Z
authors.lastname: Qian
mesh_terms: D000230:Adenocarcinoma / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry*; D001713:Biphenyl Compounds / Q000008:administration & dosage / Q000737:chemistry*; D048708:Cell Growth Processes / Q000187:drug effects; D045744:Cell Line, Tumor; D003110:Colonic Neoplasms / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D016503:Drug Delivery Systems / Q000379:methods*; D004354:Drug Screening Assays, Antitumor; D004355:Drug Stability; D004365:Drugs, Chinese Herbal / Q000008:administration & dosage / Q000737:chemistry; D006801:Humans; D017705:Lignans / Q000008:administration & dosage / Q000737:chemistry*; D008175:Lung Neoplasms / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D051379:Mice; D008823:Micelles; D046529:Microscopy, Electron, Transmission; D010316:Particle Size; D011091:Polyesters / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry*; D012995:Solubility; D013010:Sonication; D014961:X-Ray Diffraction; D000498:Allyl Compounds; D010636:Phenols
chemical_list: D000970:Antineoplastic Agents; D001713:Biphenyl Compounds; D004365:Drugs, Chinese Herbal; D017705:Lignans; D008823:Micelles; D011091:Polyesters; D011092:Polyethylene Glycols; C502908:poly(ethylene glycol)-poly(caprolactone)-poly(ethylene glycol); C005499:honokiol; D000498:Allyl Compounds; D010636:Phenols