以缩水甘油为单体，采用阴离子聚合法一步合成分子量为5 000的超支化聚缩水甘油醚（HPG），将其作为药物载体负载盐酸阿霉素（DOX）。向载体中投入不同量的DOX，用扫描电子显微镜对载药纳米粒子进行表征，用荧光标准曲线测定法研究HPG对DOX的负载及释放性能。结果表明：HPG对DOX有较好的负载性能，载药量可达到7.25%，且具有一定的缓释性和靶向释放性，药物释放时间可持续20 h以上。用HPG作为药物载体具有很大的优势，为药物载体的应用提供了很好的依据。
Hyperbranched polyglycerol (HPG) with the molecular weight of 5 000 was synthesized from the glycide monomer via anionic polymerization. HPG nanoparticles loaded with different amounts of doxorubicin (DOX) were evaluated by fluorescence and scanning electron microscope. The results showed that HPG had good loading ability for DOX. The drug loading capacity reaches 7.25%. The doxorubicin-loaded HPG nanoparticle also showed slow-releasing and target-releasing behavior. The sustained release was kept on over 20 h. All these properties of HPG nanoparticle suggest its promising potential as an effective controlled anticancer drug-delivery system.
[1] Svenson S, Tomalia D A. Dendrimers in biomedical applications:reflections on the field[J]. Advanced Drug Delivery Reviews, 2005,57(15):2106-2129.
[2] Torchilin V P. Multifunctional nanocarriers[J]. Advanced Drug Delivery Reviews, 2006, 58(14):1532-1555.
[3] Calderón M, Quadir M A, Sharma S K, et al. Dendritic polyglycerols for biomedical applications[J]. Advanced Materials, 2010, 22(2):190-218.
[4] Zarrabi A, Shokrgozar M A, Vossoughi M, et al. In vitro biocompatibility evaluations of hyperbranched polyglycerol hybrid nanostructure as a candidate for nanomedicine applications[J]. Journal of Materials Science:Materials in Medicine, 2014, 25(2):499-506.
[5] Naahidi S, Jafari M, Edalat F, et al. Biocompatibility of engineered nanoparticles for drug delivery[J]. Journal of Controlled Release, 2013, 166(2):182-194.
[6] Jin H, Huang W, Zhu X, et al. Biocompatible or biodegradable hyperbranched polymers:from self-assembly to cytomimetic applications[J]. Chemical Society Reviews, 2012, 41(18):5986-5997.
[7] Siegers C, Biesalski M, Haag R. Self-assembled monolayers of dendritic polyglycerol derivatives on gold that resist the adsorption of proteins[J]. Chemistry (Weinheiman der Bergstrasse, Germany), 2004, 10(11):2831-2838.
[8] Bian Q, Xiao Y, Zhou C, et al. Synthesis, self-assembly, and pH-responsive behavior of (photo-crosslinked) star amphiphilic triblock copolymer[J]. Journal of Colloid & Interface Science, 2013, 392(4):141-150.
[9] Knop K, Pretzel D, Urbanek A, et al. Star-shaped drug carriers for doxorubicin with POEGMA and POEtOxMA brush-like shells:a structural, physical, and biological comparison[J]. Biomacromolecules, 2013, 14(8):2536-2548.
[10] Duncan R. Designing polymer conjugates as lysosomotropic nanomedicines[J]. Biochemical Society Transactions, 2007, 35(1):56-60.
[11] Huang H, Li J, Liao L, et al. Poly(-glutamic acid)-based star-block copolymers as pH-responsive nanocarriers for cationic drugs[J]. European Polymer Journal, 2012, 48(4):696-704.
[12] Kainthan R K, Brooks D E. In vivo biological evaluation of high molecular weight hyperbranchedpolyglycerols[J]. Biomaterials, 2007, 28(32):4779-4787.
[13] Kainthan R K, Hester S R, Levin E, et al. In vitro biological evaluation of high molecular weight hyperbranched polyglycerols[J]. Biomaterials, 2007, 28(31):4581-4590.
[14] Sunder A, Hanselmann R, Holger Frey A, et al. Controlled synthesis of hyperbranched polyglycerols by ring-opening multibranching polymerization[J]. Macromolecules, 1999, 32(13):4240-4246.
[15] Wang Y, Grayson S M. Approaches for the preparation of non-linear amphiphilic polymers and their applications to drug delivery[J]. Advanced Drug Delivery Reviews, 2012, 64(9):852-865.
[16] Jeong Y I, Nah J W, Lee H C, et al. Adriamycin release from flower-type polymeric micelle based on star-block copolymer composed of poly(gamma-benzyl L-glutamate) as the hydrophobic part and poly(ethylene oxide) as the hydrophilic part[J]. Int J Pharm, 1999, 188(1):49-58.
