PLA-PCL microsphere formulation to deter abuse of prescription opioids by smoking.
PLA-PCL microsphere formulation to deter abuse of prescription opioids by smoking.
复制标题
PLA-PCL 微球制剂可防止通过吸烟滥用处方阿片类药物。
DOI：
10.1016/j.ijpharm.2022.122151
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发表时间：
2022
影响因子：
5.8
通讯作者：
Solorio,Luis
中科院分区：
文献类型：
--
作者：
Vasiukhina,Anastasiia;Gad,SheryhanF;Wellington,ElyssiaN;Wilmes,DanielleM;Yeo,Yoon;Solorio,Luis
阿片类药物通常在美国（US）用于缓解疼痛，尽管它们具有高度成瘾性，经常导致滥用和过量死亡。处方阿片类药物的滥用威慑制剂（ADF）使这些药物的非治疗性使用更加困难和不太令人满意。尽管在美国接受调查的滥用者中，约有三分之一报告吸食阿片类药物，但据我们所知，没有商业化的ADF能有效预防阿片类药物的吸食。在这里，我们报告了一种新的方法来阻止吸烟的模型处方阿片类药物，蒂巴因（THB），通过使用聚合物共混物微球（MS）包括聚乳酸（PLA）和聚己内酯（PCL）。我们利用高效液相色谱（HPLC）和热重分析（TGA）来测试PLA-PCL MS限制蒸发THB逃逸的能力。此外，我们比较了PLA-PCL MS与活性炭（AC）和介孔二氧化硅（MPS）这两种具有优异药物吸附性能的材料的滥用威慑潜力。我们的MS制剂在减少THB加热时产生的蒸气中活性药物和热降解产物的量方面是有效的。这些结果支持PLA-PCL微球可以与普通处方阿片类药物共同配制在片剂中，以阻止其通过吸烟途径滥用。
Opioids are commonly prescribed across the United States (US) for pain relief, despite their highly addictive nature that often leads to abuse and overdose deaths. Abuse deterrent formulations (ADFs) for prescription opioids make the non-therapeutic use of these drugs more difficult and less satisfying. Although approximately one-third of surveyed abusers in the US reported smoking opioids, to our knowledge, no commercialized ADF effectively prevents opioid smoking. Here, we report a novel approach to deter smoking of a model prescription opioid drug, thebaine (THB), by using polymer blend microspheres (MS) comprising polylactic acid (PLA) and polycaprolactone (PCL). We utilized high-performance liquid chromatography (HPLC) and thermogravimetric analysis (TGA) to test the ability of PLA-PCL MS to limit the escape of vaporized THB. Additionally, we compared the abuse-deterrent potential of PLA-PCL MS to that of activated carbon (AC) and mesoporous silica (MPS), two materials with excellent drug-adsorbing properties. Our MS formulation was effective in reducing the amount of both active drug and thermal degradation products in the vapor generated upon heating of THB. These results support that PLA-PCL microspheres can be co-formulated in a tablet with common prescription opioids to deter their abuse via the smoking route.