title: Sustained delivery of cytarabine-loaded vesicular phospholipid gels for treatment of xenografted glioma.
abstract: This study described the development of vesicular phospholipid gels (VPGs) for sustained delivery of cytarabine (Ara-C) for the treatment of xenografted glioma. Ara-C-loaded VPGs in the state of a semisolid phospholipid dispersion looked like numerous vesicles tightly packing together under the freeze-fracture electron microscopy (FF-TEM), their release profiles displayed sustained drug release up to 384 h in vitro. The biodistribution of Ara-C in the rat brain showed that Ara-C-loaded VPGs could maintain therapeutic concentrations up to 5mm distance from the implantation site in brain tissue within 28 days. At the same time, fluorescence micrograph confirmed drug distribution in brain tissue visually. Furthermore, after single administration, Ara-C-loaded VPGs group significantly inhibited the U87-MG glioma growth in right flank in comparison with Ara-C solution (p<0.01). It was explained that the entrapped drug in VPGs could avoid degradation from cytidine deaminase and sustained release of drug from Ara-C-loaded VPGs could maintain the effective therapeutic levels for a long time around the tumor. In conclusion, Ara-C-loaded VPGs, with the properties of sustained release, high penetration capacity, nontoxicity and no shape restriction of the surgical cavity, are promising local delivery systems for post-surgical sustained chemotherapy against glioma.
authors.affiliation: Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, PR China; Department of Pharmaceutics, Guilin Medical University, Guilin 541004, PR China.
authors.forename: Na
authors.initials: N
authors.lastname: Qi
authors.affiliation: Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Cuifang
authors.initials: C
authors.lastname: Cai
authors.affiliation: Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Wei
authors.initials: W
authors.lastname: Zhang
authors.affiliation: Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Yantao
authors.initials: Y
authors.lastname: Niu
authors.affiliation: Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Jingyu
authors.initials: J
authors.lastname: Yang
authors.affiliation: Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Lihui
authors.initials: L
authors.lastname: Wang
authors.affiliation: Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Bin
authors.initials: B
authors.lastname: Tian
authors.affiliation: Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Xiaona
authors.initials: X
authors.lastname: Liu
authors.affiliation: Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Xia
authors.initials: X
authors.lastname: Lin
authors.affiliation: Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Yu
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Haibing
authors.initials: H
authors.lastname: He
authors.affiliation: Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Kang
authors.initials: K
authors.lastname: Chen
authors.affiliation: Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, PR China. Electronic address: tanglab@126.com.
authors.forename: Xing
authors.initials: X
authors.lastname: Tang
mesh_terms: D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D001932:Brain Neoplasms / Q000188:drug therapy*; D045744:Cell Line, Tumor; D003561:Cytarabine / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D016503:Drug Delivery Systems; D005782:Gels; D005910:Glioma / Q000188:drug therapy*; D008819:Mice, Nude; D010743:Phospholipids / Q000737:chemistry; D017208:Rats, Wistar; D014018:Tissue Distribution; D023041:Xenograft Model Antitumor Assays
chemical_list: D000964:Antimetabolites, Antineoplastic; D003692:Delayed-Action Preparations; D005782:Gels; D010743:Phospholipids; D003561:Cytarabine
keywords: Cytarabine; Glioma; Local delivery; Sustained release; Vesicular phospholipids gels