持续释放的三类微球的开发和优化
Hui-Lin Zeng1, Qian Qiu1, Ting-Xiong Fu1
1Department of Pharmacy, Central Hospital of Wuhan, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, Hubei, China.
PloS one
|October 19, 2023
概括
为了改善类风湿性关节炎的治疗,开发了托利德的持续释放微球. 这种配方提供了更好的生物可用性和患者遵守的潜力,尽管最初的突发释放需要进一步调查.
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
- 药物运输 药物运输 药物运输
背景情况:
- 类风湿性关节炎是一种慢性自身免疫性疾病,导致关节的破坏.
- 特里普托利德显示治疗潜力,但面临治疗窗口狭窄和生物可用性差等局限性.
- 目前的三类药物治疗有副作用,由于频繁服用,患者不适应药物.
研究的目的:
- 开发和优化持续释放的三类微球,使用聚酸乳酸-co-glycolide (PLGA).
- 解决传统三类配方的局限性,包括低生物利用率和患者不良遵守.
主要方法:
- 使用油在水乳液溶剂蒸发技术与PLGA和聚乙烯醇 (PVA) 制备微球.
- 响应表面方法 (RSM) 与中央复合设计 (CCD) 用于配方优化.
- 关键变量包括PVA度,PLGA度和理论药物含量;反应是药物含量,封装效率,平均直径和初始释放.
主要成果:
- 优化的配方实现了42.36微米的平均直径,7.96%的药物含量和80.16%的封装效率.
- 试验室研究表明,在4周内,托利的持续释放概况符合科尔斯迈耶-佩帕斯模型.
- 观察到一个显著的初始突发释放约14%,需要进一步调查.
结论:
- 持续释放的三类微球是一种可行的策略,可以提高口服生物可用性和患者对类风湿关节炎治疗的遵从性.
- 需要进一步的研究来调查最初的爆发释放现象,并进行体内评估.
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