Riphah Institute of Pharmaceutical Sciences, Riphah International University, Lahore Campus, 54000, Lahore, Pakistan.
Riphah Institute of Pharmaceutical Sciences, Riphah International University, Lahore Campus, 54000, Lahore, Pakistan.
J Pharm Sci. 2024 Oct;113(10):3078-3087. doi: 10.1016/j.xphs.2024.08.011. Epub 2024 Aug 16.
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).
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.
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/cm/hr. Additionally, histopathological assessment of vital organs in rabbits attested to the safety profile of the formulated microneedle patches.
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.
微针(MNs)是一种微创透皮给药系统,能够穿透角质层,克服屏障特性。本研究的主要目的是制备载有喹硫平(QTP)的溶解微针贴片(DMNP)。
采用溶剂浇铸技术制备 DMNP,使用不同的聚合物进料比,包括聚乙烯醇(PVA)、聚乙烯吡咯烷酮 K30(PVP-K30)和聚乳酸-共-羟基乙酸(PLGA)聚合物。载有 QTP 的负载 DMNP 进行了全面的表征过程,包括对其相容性、厚度、插入潜力、形态、热行为、X 射线衍射、体外渗透、皮肤刺激性和组织病理学变化进行评估。
FTIR 研究证实 QTP 与微针贴片复合材料具有相容性。载药 DMNP 的厚度在 0.67 毫米至 0.97 毫米之间。这些微针的穿透深度达到了 480 微米,超过 80%的微针在刺穿 Parafilm-M 后仍保持原来的形状。对优化后的 DMNP-2 进行 SEM 分析表明,形成了尖锐尖端和均匀表面的针,长度为 570 微米。值得注意的是,应用制备的 DMNP 时,微针没有引起任何刺激迹象。DMNP-2 显示出 QTP 的令人印象深刻的累积体外渗透,达到 17.82 µg/cm/hr。此外,对兔子重要器官的组织病理学评估证明了所制定的微针贴片的安全概况。
总之,所开发的微针贴片代表了增强 QTP 经皮传递的有前途的策略。这种创新方法有可能提高患者的依从性,提供一种更有效、更适合患者的 QTP 给药方法。