长效注射性布普伦诺芬PLGA微粒配方的长效注射性布普伦诺芬
Andrew Otte1, Chad Johnson2, John Garner2
1Purdue University, Weldon School of Biomedical Engineering, West Lafayette, IN 47907, USA.
International journal of pharmaceutics
|July 29, 2025
概括
研究人员开发了一种长期作用的注射性布普伦诺芬微粒配方,用于治疗阿片类药物使用障碍 (OUD). 这种新配方提供了持续释放超过三个月,为OUD管理提供了一个有前途的治疗选择.
科学领域:
- 药理学 药理学是指药理学的学科.
- 材料科学 材料科学 材料科学
- 药物输送系统 药物输送系统
背景情况:
- 阿片类药物使用障碍 (OUD) 构成了全球重大健康挑战,导致高发病率和死亡率.
- 对OUD的药物,如布普伦诺芬,在减少非法阿片类药物使用,过量死亡和医疗保健费用方面是有效的.
- 布普伦诺啡因的特性使其适合开发长效配方,以改善治疗坚持和结果.
研究的目的:
- 开发一种新的3个月长效注射性布普伦诺芬微粒配方,用于治疗OUD.
- 为了达到35-40%的目标药物负载和至少3个月的体内药物释放.
主要方法:
- 使用固体-在-油-在-水 (S/O/W) 乳液技术进行微粒制造.
- 在油阶段使用的具有特定材料属性的 (85:15,MW=108kDa) 聚乳糖酸 (PLGA) 含量为15.2% w/v.
- 优化了关键处理参数,包括以乙酸乙烯作为溶剂和用25%乙醇溶液进行8小时的后处理.
主要成果:
- 在大鼠模型中进行的一项药理动力学研究表明,布普伦诺芬持续释放.
- 药物度在60多天内保持在2 ng/mL以上,并在另外40天内保持在1 ng/mL以上.
- 该配方在很长一段时间内保持了治疗性布普伦诺芬水平 (≥1 ng/mL),与现有的商业选择相美.
结论:
- 通过S/O/W乳液方法成功开发了一种可行的长效注射布普伦诺芬微粒配方.
- 该配方显示持续释放药物≥3个月,符合目标产品配置文件.
- 这种长效配方具有改善OUD治疗管理和患者坚持治疗的潜力.
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