Injectable long-acting human immunodeficiency virus antiretroviral prodrugs with improved pharmacokinetic profiles
作者: Sai Archana KroviMatthew D. GallovicAustin M. KellerMenakshi BhatPamela TietNaihan ChenMichael A. CollierElizabeth G. GuryshErica N. PinoMonica M. JohnsonM. Shamim Hasan ZahidMackenzie L. CottrellJason R. PironeAngela D. KashubaJesse J. KwiekEric M. BachelderKristy M. Ainslie
作者单位: 1Division of Pharmacoengineering and Molecular Pharmaceutics, University of North Carolina Eshelman School of Pharmacy, Chapel Hill, NC 27599, USA
2Department of Microbiology, Ohio State University, Columbus, OH 43210, USA
3United Therapeutics, Durham, NC 27709, USA
4Avanti Polar Lipids, Alabaster, AL 35007, USA
5Division of Pharmacotherapy and Experimental Therapeutics, University of North Carolina Eshelman School of Pharmacy, Chapel Hill, NC 27599, USA
6Department of Microbiology and Immunology, University of North Carolina, Chapel Hill, NC, USA
刊名: International Journal of Pharmaceutics, 2018, Vol.552 (1-2), pp.371-377
来源数据库: Elsevier Journal
DOI: 10.1016/j.ijpharm.2018.10.017
关键词: EmtricitabineElvitegravirSustained release formulationsAntiretroviral therapyLipid drug conjugate
英文摘要: Abstract(#br)While highly active antiretroviral therapy (HAART) has significantly reduced mortality rates in patients with human immunodeficiency virus type 1 (HIV-1), its efficacy may be impeded by emergence of drug resistance caused by lack of patient adherence. A therapeutic strategy that requires infrequent drug administration as a result of sustained release of antiretroviral drugs would put less burden on the patient. Long-acting antiretroviral prodrugs for HIV therapy were synthesized through modification of the active drugs, emtricitabine (FTC) and elvitegravir (EVG), with docosahexaenoic acid (DHA) in one-step, one-pot, high-yielding reactions. The in vitro drug release profiles of these synthetic conjugates demonstrated sustained and controlled release of the active drug over a...
全文获取路径: Elsevier  (合作)
影响因子:3.458 (2012)

  • acting 动作
  • conjugate 共轭的
  • improved 改进
  • human 人的
  • release 释放
  • virus 病毒
  • therapy 治疗