Sustained-release nanoART formulation for the treatment of neuroAIDS.
Sustained-release nanoART formulation for the treatment of neuroAIDS.
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DOI：
10.2147/ijn.s76517
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发表时间：
2015
影响因子：
8
通讯作者：
Nair M
中科院分区：
文献类型：
--
作者：
Jayant RD;Atluri VS;Agudelo M;Sagar V;Kaushik A;Nair M
开发了一种新方法，使用磁性引导逐层（LbL）组装纳米载体来共封装抗 HIV 药物（替诺福韦）和潜伏期破坏剂（伏立诺他）来治疗神经艾滋病。合成并表征了超小的氧化铁（Fe3O4）纳米颗粒（10±3 nm）。 LbL技术用于实现缓释特性，将2个双层（[替诺福韦+硫酸葡聚糖]2+伏立诺他）应用于磁性纳米粒子，导致药物（替诺福韦）载量增加2.8倍，并且还导致药物释放期增加30倍，在5天的时间内以持续的方式100%药物释放，同时刺激潜在的HIV表达。纳米制剂表现出良好的血脑屏障迁移能力（37.95%±1.5%），在原代人星形胶质细胞感染HIV后5天内具有良好的体外抗病毒功效（p24水平降低约33%），并且具有良好的细胞活力（>90%）。因此，药物在磁性纳米颗粒上的 LbL 排列提供了持续释放，因此可以提高患者对治疗的依从性并带来更好的依从性。
A novel approach was developed for the coencapsulation of an anti-HIV drug (tenofovir) and a latency-breaking agent (vorinostat), using magnetically guided layer-by-layer (LbL) assembled nanocarriers for the treatment of neuroAIDS. Ultrasmall iron oxide (Fe3O4) nanoparticles (10±3 nm) were synthesized and characterized. The LbL technique was used to achieve a sustained release profile, and application of 2 bilayers ([tenofovir+dextran sulphate]2+vorinostat) to magnetic nanoparticles resulted in a 2.8 times increase in drug (tenofovir) loading and also resulted in an increase in the drug release period by 30-fold, with 100% drug release in sustained manner over a period of 5 days with the simultaneous stimulation of latent HIV expression. Nanoformulation showed a good blood–brain barrier transmigration ability (37.95%±1.5%) with good in vitro antiviral efficacy (~33% reduction of p24 level) over a period of 5 days after HIV infection in primary human astrocytes, with good cell viability (>90%). Hence, LbL arrangements of drugs on magnetic nanoparticles provides sustained release and, therefore, may improve the patient’s adherence to therapy and lead to better compliance.