title: Modulating Drug Release Rate from Partially Silica-Coated Bicellar Nanodisc by Incorporating PEGylated Phospholipid.
abstract: This article reports an effective method to regulate hydrophobic drug release rate from partially silica-coated bicellar nanodisc generated from proamphiphilic organoalkoxysilane and dihexanoylphosphatidylcholine by introducing different molar percentages of 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-PEG2000 (DSPE-PEG2000) into planar bilayers of hybrid bicelles. It was found that the drug release rate increased with increasing the molar percentages of DSPE-PEG2000, and 57.38%, 69.21%, 78.69%, 81.64%, and 82.23% of hydrophobic doxorubicin was released within 120 h from the nanodics incorporating with 0%, 2.5%, 5%, 10%, and 20% DSPE-PEG2000, respectively. Compared with the non-PEGylated nanodisc and free doxorubicin, the PEGylated nanodiscs showed good biocompatibility, high cellular uptake, and adhesion, as well as high local drug accumulation. In addition, both in vitro and in vivo results demonstrated significantly improved antitumor efficacy of the PEGylated nanodisc than its control groups. Thus, the PEGylated nanodisc with partial silica coating offers a facile and efficient strategy of drug delivery for chemotherapy with improved patient acceptance and compliance.
authors.forename: Li
authors.initials: L
authors.lastname: Lin
authors.affiliation: Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery System, College of Engineering, School of Pharmaceutical Sciences, Peking University , Beijing 100871, China.
authors.forename: Xiaoyou
authors.initials: X
authors.lastname: Wang
authors.forename: Xiaoda
authors.initials: X
authors.lastname: Li
authors.forename: Yongbo
authors.initials: Y
authors.lastname: Yang
authors.forename: Xiuli
authors.initials: X
authors.lastname: Yue
authors.affiliation: Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery System, College of Engineering, School of Pharmaceutical Sciences, Peking University , Beijing 100871, China.
authors.forename: Qiang
authors.initials: Q
authors.lastname: Zhang
authors.affiliation: Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery System, College of Engineering, School of Pharmaceutical Sciences, Peking University , Beijing 100871, China.
authors.forename: Zhifei
authors.initials: Z
authors.lastname: Dai
mesh_terms: D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use; D001672:Biocompatible Materials; D045744:Cell Line, Tumor; D002478:Cells, Cultured; D004317:Doxorubicin / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use; D004337:Drug Carriers; D065546:Drug Liberation; D005260:Female; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D051379:Mice; D008807:Mice, Inbred BALB C; D049329:Nanostructures; D010743:Phospholipids / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012822:Silicon Dioxide / Q000737:chemistry*; D014018:Tissue Distribution
chemical_list: D000903:Antibiotics, Antineoplastic; D001672:Biocompatible Materials; D004337:Drug Carriers; D010743:Phospholipids; D011092:Polyethylene Glycols; D012822:Silicon Dioxide; D004317:Doxorubicin