title: Synthesis and characterization of biotin modified cholesteryl pullulan as a novel anticancer drug carrier.
abstract: A series of biotin modified cholesteryl pullulan (Bio-CHSP) conjugates with different degrees of substitution (DS) of biotin moiety were synthesized and characterized by Fourier transform infrared (FT-IR), proton nuclear magnetic resonance ((1)H NMR) and X-ray diffraction (XRD). Bio-CHSP conjugates were amphiphilic in nature and their self-aggregation behavior in aqueous media was evaluated by the fluorescence probe technique. Bio-CHSP self-aggregated nanoparticles (Bio-CHSP NPs) were prepared and analyzed by dynamic light scattering (DLS), zeta potential and transmission electron microscopy (TEM) technologies. These novel nanoparticles were almost spherical in shape, and their size, ranging from 178.8 to 100.0 nm. The safety of Bio-CHSP NPs was studied through single dose toxicity test in mice, and the result showed that Bio-CHSP NPs were well tolerated at the intravenous dose of 200 mg/kg in mice. Moreover, as a model anticancer drug, mitoxantrone loaded Bio-CHSP NPs were also prepared and characterized in this study.
authors.affiliation: College of Pharmacy & Key Laboratory of Pharmaceutical Quality Control of Hebei Province, Hebei University, Baoding 071002, China. Electronic address: wenzhi_yang@sina.com.
authors.forename: Wenzhi
authors.initials: W
authors.lastname: Yang
authors.forename: Miaomiao
authors.initials: M
authors.lastname: Wang
authors.forename: Lilan
authors.initials: L
authors.lastname: Ma
authors.forename: Haiying
authors.initials: H
authors.lastname: Li
authors.forename: Le
authors.initials: L
authors.lastname: Huang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000378:metabolism; D001710:Biotin / Q000737:chemistry*; D002784:Cholesterol / Q000737:chemistry*; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000494:pharmacology; D004339:Drug Compounding; D005260:Female; D005936:Glucans / Q000737:chemistry*; D006001:Glycoconjugates / Q000138:chemical synthesis* / Q000494:pharmacology; D007700:Kinetics; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D008942:Mitoxantrone / Q000378:metabolism; D015394:Molecular Structure; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D017550:Spectroscopy, Fourier Transform Infrared; D014961:X-Ray Diffraction
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D005936:Glucans; D006001:Glycoconjugates; D001710:Biotin; C009109:pullulan; D002784:Cholesterol; D008942:Mitoxantrone
keywords: Biotin-modified cholesteryl pullulan; Drug delivery; Mitoxantrone; Self-aggregated nanoparticle