title: Drug nanoparticles by emulsion-freeze-drying via the employment of branched block copolymer nanoparticles.
abstract: A large percentage of drug compounds exhibit low water solubility and hence low bioavailability and therapeutic efficacy. This may be addressed by preparation of drug nanoparticles, leading to enhanced dissolution rate and direct use for treatment. Various methods have been developed to produce drug nanocrystals, including wet milling, homogenization, solution precipitation, emulsion diffusion, and the recently developed emulsion freeze-drying. The drawback for these methods may include difficult control in particles size, use of surfactants & polymer, and low ratio of drug to stabilizer. Here, biocompatible branched block copolymer nanoparticles with lightly-crosslinked hydrophobic core and hydrophilic surface groups are synthesized by the direct monomer-to-particle methodology, characterized, and then used as scaffold polymer/surfactant to produce drug nanoparticles via the emulsion-freeze-drying approach. This method can be used for model organic dye and different poorly water-soluble drugs. Aqueous drug nanoparticle dispersions can be obtained with high ratio of drug to stabilizer and relatively uniform nanoparticle sizes.
authors.affiliation: Department of Chemistry, University of Liverpool, Liverpool L69 7ZD, UK; Institute of Chemical and Engineering Science, 1 Pesek Road, Jurong Island 627833, Singapore.
authors.forename: Ulrike
authors.initials: U
authors.lastname: Wais
authors.affiliation: Institute of Chemical and Engineering Science, 1 Pesek Road, Jurong Island 627833, Singapore.
authors.forename: Alexander W
authors.initials: AW
authors.lastname: Jackson
authors.affiliation: School of Chemistry and Chemical Engineering, Hefei University of Technology, Hefei, China.
authors.forename: Yanming
authors.initials: Y
authors.lastname: Zuo
authors.affiliation: School of Chemistry and Chemical Engineering, Hefei University of Technology, Hefei, China.
authors.forename: Yu
authors.initials: Y
authors.lastname: Xiang
authors.affiliation: School of Chemistry and Chemical Engineering, Hefei University of Technology, Hefei, China. Electronic address: taohe@hfut.edu.cn.
authors.forename: Tao
authors.initials: T
authors.lastname: He
authors.affiliation: Department of Chemistry, University of Liverpool, Liverpool L69 7ZD, UK. Electronic address: zhanghf@liv.ac.uk.
authors.forename: Haifei
authors.initials: H
authors.lastname: Zhang
mesh_terms: D000180:Acrylic Resins / Q000737:chemistry*; D001391:Azo Compounds / Q000737:chemistry; D004396:Coloring Agents / Q000737:chemistry*; D004339:Drug Compounding; D004655:Emulsions; D005612:Freeze Drying; D057927:Hydrophobic and Hydrophilic Interactions; D007213:Indomethacin / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*
chemical_list: D000180:Acrylic Resins; D001391:Azo Compounds; D004396:Coloring Agents; D004655:Emulsions; C052970:poly-N-isopropylacrylamide; D011092:Polyethylene Glycols; C011049:oil red O; D007213:Indomethacin
keywords: Block copolymer; Drug nanoparticles; Emulsion; Freeze drying; Nanoparticles; Poorly water-soluble drugs