Ojewole Elizabeth, Mackraj Irene, Naidoo Panjasaram, Govender Thirumala
School of Pharmacy and Pharmacology, University of KwaZulu-Natal, Durban, South Africa.
Eur J Pharm Biopharm. 2008 Nov;70(3):697-710. doi: 10.1016/j.ejpb.2008.06.020. Epub 2008 Jul 3.
Novel drug delivery systems present an opportunity for formulation scientists to overcome the many challenges associated with antiretroviral (ARV) drug therapy, thereby improving the management of patients with HIV/AIDS. This paper provides a comprehensive review of the various ARV delivery systems that have been developed for achieving sustained drug release kinetics, specifically targeting drugs to the macrophages, brain and gastric mucosa, and for addressing formulation difficulties such as poor solubility, stability and drug entrapment. Studies on the potential of systems for alternative routes of ARV drug administration, i.e., transdermal, buccal and rectal, are also highlighted. The physico-chemical properties and the in vitro/in vivo performances of various systems such as sustained release tablets, ceramic implants, nanoparticles, nanocontainers, liposomes, emulsomes, aspasomes, microemulsions, nanopowders and Pheroid(TM) are summarised. Further studies that remain to be undertaken for formulation optimisation are also identified. This review highlights the significant potential that novel drug delivery systems have for the future effective treatment of HIV/AIDS patients on ARV drug therapy.
新型药物递送系统为制剂科学家提供了一个机会,以克服与抗逆转录病毒(ARV)药物治疗相关的诸多挑战,从而改善对艾滋病毒/艾滋病患者的管理。本文全面综述了为实现药物持续释放动力学、将药物特异性靶向巨噬细胞、大脑和胃黏膜以及解决诸如溶解度差、稳定性和药物包封等制剂难题而开发的各种抗逆转录病毒药物递送系统。还重点介绍了抗逆转录病毒药物经皮、颊部和直肠等替代给药途径的系统潜力研究。总结了各种系统(如缓释片、陶瓷植入物、纳米颗粒、纳米容器、脂质体、乳剂体、阿帕体、微乳剂、纳米粉末和Pheroid(TM))的物理化学性质及体外/体内性能。还确定了有待进行的进一步制剂优化研究。本综述强调了新型药物递送系统在未来有效治疗接受抗逆转录病毒药物治疗的艾滋病毒/艾滋病患者方面的巨大潜力。