目的:微针(MN)是微创经皮药物递送系统,能够穿透角质层以克服屏障特性。本研究的主要目的是制备负载喹硫平(QTP)的溶解微针贴片(DMNP)。
方法:DMNP采用溶剂浇铸技术制备,利用各种聚合物进料比,包括聚乙烯醇(PVA),聚乙烯吡咯烷酮K30(PVP-K30),和聚丙交酯-共-乙交酯(PLGA)聚合物。带有QTP的加载DMNP经历了全面的表征过程,包括兼容性评估,厚度,插入电位,形态学,热行为,X射线衍射,离体渗透,皮肤刺激,和组织病理学变化。
结果:FTIR研究证实了QTP与微针贴片复合材料的相容性。载药DMNP的厚度范围为0.67mm至0.97mm。这些微针显示出令人印象深刻的480μm的穿透深度,超过80%的针头在刺穿Parafilm-M后保持其原始形状。优化的DMNP-2的SEM分析显示形成尖锐的尖端和均匀的表面针,测量长度为570μm。值得注意的是,在施用制备的DMNP时,微针没有引起任何刺激迹象。DMNP-2展示了令人印象深刻的QTP体外累积渗透,达到17.82微克/平方厘米/小时。此外,兔重要器官的组织病理学评估证明了配制的微针贴片的安全性。
结论:结论:开发的微针贴片代表了增强QTP透皮给药的有希望的策略。这种创新的方法有可能提高患者的依从性,提供了一种更有效和对患者友好的QTP管理方法。
OBJECTIVE: Microneedles (MNs) are minimally invasive transdermal drug delivery systems capable of penetrating the stratum corneum to overcome the barrier properties. The primary objective of this research was to prepare dissolving microneedle patches (DMNP) loaded with quetiapine (QTP).
METHODS: DMNP were fabricated employing the solvent casting technique, utilizing various polymer feed ratios including polyvinyl alcohol (PVA), polyvinylpyrrolidone K30 (PVP-K30), and polylactide-co-glycolide (PLGA) polymers. The loaded DMNP with QTP underwent a comprehensive characterization process encompassing assessments for compatibility, thickness, insertion potential, morphology, thermal behavior, X-ray diffraction, ex-vivo permeation, skin irritation, and histopathological changes.
RESULTS: FTIR studies confirmed the compatibility of QTP with the microneedle patch composites. The thickness of the drug-loaded DMNP ranged from 0.67 mm to 0.97 mm. These microneedles exhibited an impressive penetration depth of 480 μm, with over 80% of the needles maintaining their original shape after piercing Parafilm-M. SEM analysis of the optimized DMNP-2 revealed the formation of sharp-tipped and uniformly surfaced needles, measuring 570 μm in length. Remarkably, the microneedles did not elicit any signs of irritation upon application of the prepared DMNP. The DMNP-2 showcased an impressive cumulative ex-vivo permeation of QTP, reaching 17.82 µg/cm2/hr. Additionally, histopathological assessment of vital organs in rabbits attested to the safety profile of the formulated microneedle patches.
CONCLUSIONS: In conclusion, the developed microneedle patch represents a promising strategy for enhancing the transdermal delivery of QTP. This innovative approach has the potential to increase patient compliance, offering a more efficient and patient-friendly method of administering QTP.