Drug Delivery Research Unit, Research Institute for Medicines, iMed-ULisboa, Faculty of Pharmacy, Universidade de Lisboa, 1649-003 Lisboa, Portugal.
Host-Pathogen Interactions Unit, Research Institute for Medicines, iMed-ULisboa, Faculty of Pharmacy, Universidade de Lisboa, 1649-003 Lisboa, Portugal.
Molecules. 2021 Aug 31;26(17):5305. doi: 10.3390/molecules26175305.
When the first cases of HIV infection appeared in the 1980s, AIDS was a deadly disease without any therapeutic alternatives. Currently, there is still no cure for most cases mainly due to the multiple tissues that act as a reservoir for this virus besides the high viral mutagenesis that leads to an antiretroviral drug resistance. Throughout the years, multiple drugs with specific mechanisms of action on distinct targets have been approved. In this review, the most recent phase III clinical studies and other research therapies as advanced antiretroviral nanodelivery systems will be here discussed. Although the combined antiretroviral therapy is effective in reducing viral loading to undetectable levels, it also presents some disadvantages, such as usual side effects, high frequency of administration, and the possibility of drug resistance. Therefore, several new drugs, delivery systems, and vaccines have been tested in pre-clinical and clinical trials. Regarding drug delivery, an attempt to change the route of administration of some conventional antiretrovirals has proven to be successful and surpassed some issues related to patient compliance. Nanotechnology has brought a new approach to overcoming certain obstacles of formulation design including drug solubility and biodistribution. Overall, the encapsulation of antiretroviral drugs into nanosystems has shown improved drug release and pharmacokinetic profile.
当艾滋病病毒（HIV）感染的首例病例出现在 20 世纪 80 年代时，艾滋病是一种致命的疾病，没有任何治疗选择。目前，由于该病毒存在多个充当储库的组织，以及导致抗逆转录病毒药物耐药性的高病毒突变率，大多数病例仍然没有治愈方法。多年来，已经批准了多种具有针对不同靶点的特定作用机制的药物。在这篇综述中，将讨论最近的 III 期临床研究和其他研究治疗方法，如先进的抗逆转录病毒纳米递药系统。虽然联合抗逆转录病毒疗法在降低病毒载量至不可检测水平方面非常有效，但它也存在一些缺点，如常见的副作用、高给药频率以及发生耐药性的可能性。因此，已经在临床前和临床试验中测试了几种新的药物、递药系统和疫苗。关于药物递药，尝试改变一些常规抗逆转录病毒药物的给药途径已被证明是成功的，并克服了与患者依从性相关的一些问题。纳米技术为克服制剂设计中的某些障碍（包括药物溶解度和生物分布）提供了新的方法。总体而言，将抗逆转录病毒药物封装到纳米系统中已显示出改善的药物释放和药代动力学特征。
