Department of Industrial and Molecular Pharmaceutics, Purdue University, 575 West Stadium Avenue, West Lafayette, IN 47907, USA; Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt.
Weldon School of Biomedical Engineering, Purdue University, 206 S Martin Jischke Dr., West Lafayette, IN 47907, USA.
J Control Release. 2024 Jun;370:490-500. doi: 10.1016/j.jconrel.2024.04.046. Epub 2024 May 8.
Misuse of prescription opioid drugs is the leading cause of the opioid crisis and overdose-related death. Abuse deterrent formulations (ADFs) have been developed to discourage attempts to tamper with the formulation and alter the ingestion methods. However, abusers develop complex extraction strategies to circumvent the ADF technologies. For comprehensive deterrence of drug abuse, we develop tannic acid nanoparticles (NPs) that protect encapsulated opioids from solvent extraction and thermal challenge (crisping), complementing the existing formulation strategy to deter injection abuse. Here, we develop a hybrid ADF tablet (NP-Tab), consisting of iron-crosslinked tannic acid NPs encapsulating thebaine (model opioid compound), xanthan gum, and chitosan (gel-forming polymers), and evaluate its performance in common abuse conditions. NP-Tab tampered by crushing and suspended in aqueous solvents forms an instantaneous gel, which is difficult to pull or push through a 21-gauge needle. NPs insulate the drug from organic solvents, deterring solvent extraction. NPs also promote thermal destruction of the drug to make crisping less rewarding. However, NP-Tab releases thebaine in the simulated gastric fluid without delay, suggesting that its analgesic effect may be unaffected if consumed orally as prescribed. These results demonstrate that NP-Tab can provide comprehensive drug abuse deterrence, resisting aqueous/organic solvent extraction, injection, and crisping, while retaining its therapeutic effect upon regular usage.
处方类阿片类药物的滥用是阿片类药物危机和与过量用药相关的死亡的主要原因。为了阻止尝试篡改制剂和改变摄入方法,已经开发了滥用阻止制剂(Abuse Deterrent Formulations,ADFs)。然而,滥用者会开发出复杂的提取策略来规避 ADF 技术。为了全面阻止药物滥用,我们开发了单宁酸纳米颗粒(NPs),以保护包裹的阿片类药物免受溶剂提取和热挑战(脆化),补充现有的制剂策略以阻止注射滥用。在这里,我们开发了一种混合 ADF 片剂(NP-Tab),由铁交联的单宁酸 NPs 包裹可待因(模型阿片类化合物)、黄原胶和壳聚糖(凝胶形成聚合物)组成,并评估其在常见滥用条件下的性能。NP-Tab 经粉碎和悬浮在水性溶剂中形成瞬时凝胶,难以通过 21 号针拉动或推动。 NPs 使药物与有机溶剂隔离,阻止溶剂提取。 NPs 还促进药物的热破坏,使脆化的回报降低。然而,NP-Tab 在模拟胃液中没有延迟释放可待因,这表明如果按照规定口服,其镇痛效果可能不受影响。这些结果表明,NP-Tab 可以提供全面的药物滥用阻止,抵抗水性/有机溶剂提取、注射和脆化,同时在常规使用时保留其治疗效果。