Ndesendo Valence M K, Pillay Viness, Choonara Yahya E, Buchmann Eckhart, Bayever David N, Meyer Leith C R
Department of Pharmacy and Pharmacology, University of the Witwatersrand, 7 York Road, Parktown 2193, Johannesburg, South Africa.
AAPS PharmSciTech. 2008;9(2):505-20. doi: 10.1208/s12249-008-9073-5. Epub 2008 Apr 2.
The objective of this review is to describe the current status of several intravaginal anti-HIV microbicidal delivery systems these delivery systems and microbicidal compounds in the context of their stage within clinical trials and their potential cervicovaginal defence successes. The global Human Immuno-Deficiency Virus (HIV) pandemic continues to spread at a rate of more than 15,000 new infections daily and sexually transmitted infections (STIs) can predispose people to acquiring HIV infection. Male-to-female transmission is eight times more likely to occur than female-to-male transmission due to the anatomical structure of the vagina as well as socio-economic factors and the disempowerment of women that renders them unable to refuse unsafe sexual practices in some communities. The increased incidence of HIV in women has identified the urgent need for efficacious and safe intravaginal delivery of anti-HIV agents that can be used and controlled by women. To meet this challenge, several intravaginal anti-HIV microbicidal delivery systems are in the process of been developed. The outcomes of three main categories are discussed in this review: namely, dual-function polymeric systems, non-polymeric systems and nanotechnology-based systems. These delivery systems include formulations that modify the genital environment (e.g. polyacrylic acid gels and lactobacillus gels), surfactants (e.g. sodium lauryl sulfate), polyanionic therapeutic polymers (e.g. carageenan and carbomer/lactic acid gels), proteins (e.g. cyanovirin-N, monoclonal antibodies and thromspondin-1 peptides), protease inhibitors and other molecules (e.g. dendrimer based-gels and the molecular condom). Intravaginal microbicide delivery systems are providing a new option for preventing the transmission of STIs and HIV.
本综述的目的是描述几种阴道内抗HIV杀微生物剂递送系统的现状,这些递送系统和杀微生物化合物处于临床试验阶段,以及它们在宫颈阴道防御方面可能取得的成功。全球人类免疫缺陷病毒(HIV)大流行仍在以每天超过15000例新感染的速度蔓延,性传播感染(STIs)会使人更容易感染HIV。由于阴道的解剖结构以及社会经济因素和妇女赋权不足,导致在某些社区她们无法拒绝不安全的性行为,所以男性向女性的传播比女性向男性的传播可能性高八倍。女性中HIV发病率的上升表明迫切需要一种有效且安全的可由女性使用和控制的抗HIV药物阴道内递送方法。为应对这一挑战,几种阴道内抗HIV杀微生物剂递送系统正在研发中。本综述讨论了三大类的成果:即双功能聚合物系统、非聚合物系统和基于纳米技术的系统。这些递送系统包括改变生殖环境的制剂(如聚丙烯酸凝胶和乳酸杆菌凝胶)、表面活性剂(如十二烷基硫酸钠)、聚阴离子治疗聚合物(如角叉菜胶和卡波姆/乳酸凝胶)、蛋白质(如氰苷 - N、单克隆抗体和血小板反应蛋白 - 1肽)、蛋白酶抑制剂和其他分子(如基于树枝状聚合物的凝胶和分子避孕套)。阴道内杀微生物剂递送系统为预防性传播感染和HIV传播提供了新的选择。