i3S-Instituto de Investigação e Inovação em Saúde, Universidade do Porto, Porto, Portugal; INEB-Instituto de Engenharia Biomédica, Universidade do Porto, Porto, Portugal; CESPU, Instituto de Investigação e Formação Avançada em Ciências e Tecnologias da Saúde & Instituto Universitário de Ciências da Saúde, Gandra, Portugal.
i3S-Instituto de Investigação e Inovação em Saúde, Universidade do Porto, Porto, Portugal; INEB-Instituto de Engenharia Biomédica, Universidade do Porto, Porto, Portugal; ICBAS-Instituto de Ciências Biomédicas Abel Salazar, Universidade do Porto, Porto, Portugal.
Adv Drug Deliv Rev. 2016 Aug 1;103:57-75. doi: 10.1016/j.addr.2016.01.017. Epub 2016 Jan 30.
Prevention plays an invaluable role in the fight against HIV/AIDS. The use of microbicides is considered an interesting potential approach for topical pre-exposure prophylaxis of HIV sexual transmission. The prospects of having an effective product available are expected to be fulfilled in the near future as driven by recent and forthcoming results of clinical trials. Different dosage forms and delivery strategies have been proposed and tested for multiple microbicide drug candidates presently at different stages of the development pipeline. One particularly interesting approach comprises the application of nanomedicine principles to the development of novel anti-HIV microbicides, but its implications to efficacy and safety are not yet fully understood. Nanotechnology-based systems, either presenting inherent anti-HIV activity or acting as drug nanocarriers, may significantly influence features such as drug solubility, stability of active payloads, drug release, interactions between active moieties and virus/cells, intracellular drug delivery, drug targeting, safety, antiviral activity, mucoadhesive behavior, drug distribution and tissue penetration, and pharmacokinetics. The present manuscript provides a comprehensive and holistic overview of these topics as relevant to the development of vaginal and rectal microbicides. In particular, recent advances pertaining inherently active microbicide nanosystems and microbicide drug nanocarriers are discussed.
预防在抗击艾滋病病毒/艾滋病方面发挥着不可估量的作用。杀微生物剂的使用被认为是一种有前途的方法，可以局部用于预防艾滋病毒的性传播。由于最近和即将到来的临床试验结果，预计在不久的将来就会有有效的产品问世。目前有多种不同的剂型和给药策略被提出并用于多种杀微生物候选药物，这些药物目前处于不同的研发阶段。一种特别有趣的方法是将纳米医学原理应用于新型抗 HIV 杀微生物剂的开发，但它对疗效和安全性的影响尚不完全清楚。基于纳米技术的系统，无论是具有固有抗 HIV 活性还是作为药物纳米载体，都可能显著影响药物的溶解度、活性有效成分的稳定性、药物释放、活性基团与病毒/细胞之间的相互作用、细胞内药物递送、药物靶向、安全性、抗病毒活性、黏膜黏附性、药物分布和组织穿透性以及药代动力学等特征。本文全面概述了这些与阴道和直肠杀微生物剂开发相关的主题。特别是，讨论了具有固有活性的杀微生物纳米系统和杀微生物药物纳米载体的最新进展。
