肝靶向载药缓释毫微粒的研究进展
作者：徐颖 周世文
单位：第三军医大学新桥医院临床药理基地(400037)
关键词：
重庆医学000460 临床用药后药物的体内分布和代谢是影响其治疗效果的重要因素。改变药物在体内分布和代谢的途径之一是将其包封于亚微粒药物载体中。在这些载体中，脂质体、毫微粒(NP)及药质体己得到广泛研究。目前，人用脂质体的发展仍受到限制，主要问题是其不稳定，泄漏快及贮存期变质。为克服这些缺点，自70年代末以来研究了聚合物毫微粒(纳米级的颗粒)的制备。毫微粒是毫微球和毫微囊的统称，其粒径大小为10～1000nm之间，由大分子物质构成并可作为药物载体[1]。本文就肝靶向载药缓释毫微粒的研究进展综述如下。……
参考文献：
[1]Sherer D, Robinson JR and Kreuter J. Influencd of enzymes on the stability of polyhutylcyanoaerylate nanopartides.Int J Pharm, 1994,101(2):165
, http://www.100md.com
[2]Gallardo M, Cowarraze G, Denizot B. Study of the mechanisms of formation of nanoparticles and nanocapsales of polyisobutyl-2-cyanoacrylate.Int J Pharm,1994,190(1):55
[3]修志龙，齐冬建，苏志国.肽和蛋白类药物的给药系统.中国生化药物杂志，1996，17(4)：172
[4]陈庆华.高新技术在药物新制剂开发与研究中的应用.中国药学杂志，1997，32(11)：681
[5]Li JK, Wang N, Wu XS. A novel biodegradable system based on gelatin nanoparticles and poly(lactic-co-glycolic acid)microspheres for protein and peptide drug delivery. J Pharm Sci, 1997,86(8):891
, 百拇医药
[6]Muller RH, Lherm C, Herbort J, et al. Alkylcyanoacrylate drug carties: I Physicochemical characterization of nanoparticles with different alkyl chain length. Int J. Pharm, 1992,84(1):1
[7]Cartherine L, Lherm C, Muller RH, et al. Alkylcyanoacrylate drug carries 2 cytotoxicity of cyanoacrylate nanoparticles with different alkyl chain length. Int J Pharm, 1992, 84(1):13
[8]Molpeceres J, Guzman M, Aberturas MR, et al. Application of central composite designs to the preparation of polystyrene nanoparticles by solvent displacement. J Pharm Sci, 1997, 85(2):206
, http://www.100md.com
[9]Couvreur P, Dubemet C. Controlled drug delivery with nanoparticles.Fur J Pharm Biopharm, 1995, 41(1):2
[10]Gasco MP, Morel S, Trotta M et al. Doxorubieine englobed in polybutylcyanocatylate nanocapsules: behavior in vitro and in vivo.Pharm Acta Helv, 1991,66(1):47
[11]Cleland JL, Duenas E, Daugherty A, et al. Recombinant human growth hormane poly(lactic-co-glycolic acid) (PLGA) microspheres provide a long lasting effect. J Controlled Release, 1997, 49(2): 193
, 百拇医药
[12]Guterres SS, Fessi H, Barratt JP, et al Poly(DL-lactide) nanocapsule containing diclofenac; I. Formulation and stability study. Int J Pharm, 1995, 113(1):57
[13]Niwa T, Takeuchi H, Hino T et al. Preparations of biodegradable nanospherea of water-soluble and insolube dngs with DL-lactide/glycolide copolymer by a novel spontaneous emulsification solvent diffusion method and the drug release behavior. J Controlled Release, 1993, 25(1):89
, 百拇医药
[14]Scholas PD, Coombes AGG, lllum L, et al. The preparation of sub-200 nm poly(lacide-co-glycolide)microspheres for sitespecific drug deliveay. J Controlled Release, 1993, 25(1):145
[15]Niwa T, Takeuchi H, Hino T, et al. Biodegradable submicron carriers for peptide drugs:preparation of DL-lactide/glycdide copolymer(PLGA) nanospheres with nafarelin acetate by a novel emulsion-phase separation method in an oil system. Int. J Pharm, 1995,121(1):45
, http://www.100md.com
[16]Anderson JM, Shire MS. Biodegradation and biocornpatibility of PLGA microspere. Adv Drug Del Rev, 1997,28(1):5
[17]Johnson OL, Jaworowicz W, Cleland JL, et al. The stabilization and encapsulation of human growth hormone into biodegradable microspheres. Pharm Res, 1997, 14(5):730
[18]Marchal-Heclssier L, Maincent P, Hoffman M, et al. Antiglancomatous activity of bataxolol chlorhydrate sorbed onto different isobutyl cyanoacrylate nanoparticles preparation. Int J Pharm,1990,58(2):115
, http://www.100md.com
[19]Niwa T, Takeuchi H, Hino T, et al. In vitro drug release behavior of DLlactide/glycolide copolymer(PLGA) nanospheres with nafarelin acetate prepared by a novel spontaneous emulsification sovent diffusion method. J Pharm Sci, 1994,83(7):727
[20]Thomasin C, Nam-Tran H, Merkle HP, et al. Drug Microencapsulation by PLA/PLGA coacervation in the light of thermodynamics.1. Overview and theoretical considerations. J Pharm Sci, 1998, 87(3):259, http://www.100md.com
单位：第三军医大学新桥医院临床药理基地(400037)
关键词：
重庆医学000460 临床用药后药物的体内分布和代谢是影响其治疗效果的重要因素。改变药物在体内分布和代谢的途径之一是将其包封于亚微粒药物载体中。在这些载体中，脂质体、毫微粒(NP)及药质体己得到广泛研究。目前，人用脂质体的发展仍受到限制，主要问题是其不稳定，泄漏快及贮存期变质。为克服这些缺点，自70年代末以来研究了聚合物毫微粒(纳米级的颗粒)的制备。毫微粒是毫微球和毫微囊的统称，其粒径大小为10～1000nm之间，由大分子物质构成并可作为药物载体[1]。本文就肝靶向载药缓释毫微粒的研究进展综述如下。……
参考文献：
[1]Sherer D, Robinson JR and Kreuter J. Influencd of enzymes on the stability of polyhutylcyanoaerylate nanopartides.Int J Pharm, 1994,101(2):165
, http://www.100md.com
[2]Gallardo M, Cowarraze G, Denizot B. Study of the mechanisms of formation of nanoparticles and nanocapsales of polyisobutyl-2-cyanoacrylate.Int J Pharm,1994,190(1):55
[3]修志龙，齐冬建，苏志国.肽和蛋白类药物的给药系统.中国生化药物杂志，1996，17(4)：172
[4]陈庆华.高新技术在药物新制剂开发与研究中的应用.中国药学杂志，1997，32(11)：681
[5]Li JK, Wang N, Wu XS. A novel biodegradable system based on gelatin nanoparticles and poly(lactic-co-glycolic acid)microspheres for protein and peptide drug delivery. J Pharm Sci, 1997,86(8):891
, 百拇医药
[6]Muller RH, Lherm C, Herbort J, et al. Alkylcyanoacrylate drug carties: I Physicochemical characterization of nanoparticles with different alkyl chain length. Int J. Pharm, 1992,84(1):1
[7]Cartherine L, Lherm C, Muller RH, et al. Alkylcyanoacrylate drug carries 2 cytotoxicity of cyanoacrylate nanoparticles with different alkyl chain length. Int J Pharm, 1992, 84(1):13
[8]Molpeceres J, Guzman M, Aberturas MR, et al. Application of central composite designs to the preparation of polystyrene nanoparticles by solvent displacement. J Pharm Sci, 1997, 85(2):206
, http://www.100md.com
[9]Couvreur P, Dubemet C. Controlled drug delivery with nanoparticles.Fur J Pharm Biopharm, 1995, 41(1):2
[10]Gasco MP, Morel S, Trotta M et al. Doxorubieine englobed in polybutylcyanocatylate nanocapsules: behavior in vitro and in vivo.Pharm Acta Helv, 1991,66(1):47
[11]Cleland JL, Duenas E, Daugherty A, et al. Recombinant human growth hormane poly(lactic-co-glycolic acid) (PLGA) microspheres provide a long lasting effect. J Controlled Release, 1997, 49(2): 193
, 百拇医药
[12]Guterres SS, Fessi H, Barratt JP, et al Poly(DL-lactide) nanocapsule containing diclofenac; I. Formulation and stability study. Int J Pharm, 1995, 113(1):57
[13]Niwa T, Takeuchi H, Hino T et al. Preparations of biodegradable nanospherea of water-soluble and insolube dngs with DL-lactide/glycolide copolymer by a novel spontaneous emulsification solvent diffusion method and the drug release behavior. J Controlled Release, 1993, 25(1):89
, 百拇医药
[14]Scholas PD, Coombes AGG, lllum L, et al. The preparation of sub-200 nm poly(lacide-co-glycolide)microspheres for sitespecific drug deliveay. J Controlled Release, 1993, 25(1):145
[15]Niwa T, Takeuchi H, Hino T, et al. Biodegradable submicron carriers for peptide drugs:preparation of DL-lactide/glycdide copolymer(PLGA) nanospheres with nafarelin acetate by a novel emulsion-phase separation method in an oil system. Int. J Pharm, 1995,121(1):45
, http://www.100md.com
[16]Anderson JM, Shire MS. Biodegradation and biocornpatibility of PLGA microspere. Adv Drug Del Rev, 1997,28(1):5
[17]Johnson OL, Jaworowicz W, Cleland JL, et al. The stabilization and encapsulation of human growth hormone into biodegradable microspheres. Pharm Res, 1997, 14(5):730
[18]Marchal-Heclssier L, Maincent P, Hoffman M, et al. Antiglancomatous activity of bataxolol chlorhydrate sorbed onto different isobutyl cyanoacrylate nanoparticles preparation. Int J Pharm,1990,58(2):115
, http://www.100md.com
[19]Niwa T, Takeuchi H, Hino T, et al. In vitro drug release behavior of DLlactide/glycolide copolymer(PLGA) nanospheres with nafarelin acetate prepared by a novel spontaneous emulsification sovent diffusion method. J Pharm Sci, 1994,83(7):727
[20]Thomasin C, Nam-Tran H, Merkle HP, et al. Drug Microencapsulation by PLA/PLGA coacervation in the light of thermodynamics.1. Overview and theoretical considerations. J Pharm Sci, 1998, 87(3):259, http://www.100md.com