Anjani Qonita Kurnia, Moreno-Castellanos Natalia, Adhami Masoud, Ramadon Delly, Jangga Jangga, Donnelly Ryan F
School of Pharmacy, Medical Biology Centre, Queen's University Belfast, 97 Lisburn Road, Belfast, Northern Ireland, BT9 7BL, UK.
Fakultas Farmasi, Universitas Megarezky, Jl. Antang Raya No. 43, Makassar, 90234, Indonesia.
Drug Deliv Transl Res. 2025 Jan;15(1):355-371. doi: 10.1007/s13346-024-01616-8. Epub 2024 May 9.
Quercetin, a natural compound, shows promising potential in wound healing by reducing fibrosis, limiting scar formation, and boosting fibroblast proliferation. However, its effectiveness is hindered by poor solubility, resulting in low bioavailability and necessitating high doses for therapeutic efficacy. This study presents a novel approach, fabricating quercetin-loaded microarray patches (MAPs) using widely employed solubility enhancement strategies. Fabricated MAPs exhibited favourable mechanical strength and could be inserted into excised porcine skin to a depth of 650 μm. Furthermore, formulations containing Soluplus significantly increased the drug loading capacity, achieving up to 2.5 mg per patch and complete dissolution within an hour of application on excised porcine skin. In vitro studies on full-thickness neonatal porcine skin demonstrated that Soluplus-enhanced MAPs effectively delivered quercetin across various skin layers, achieving a delivery efficiency exceeding 80% over 24 h. Additionally, these prototype MAPs displayed anti-inflammatory properties and demonstrated biocompatibility with human keratinocyte skin cells. Therefore, quercetin-loaded MAPs employing Soluplus as a solubility enhancer present a promising alternative strategy for wound healing and anti-inflammatory therapy applications.
槲皮素是一种天然化合物,在伤口愈合方面显示出有前景的潜力,它可以减少纤维化、限制疤痕形成并促进成纤维细胞增殖。然而,其溶解性差阻碍了其有效性,导致生物利用度低,需要高剂量才能达到治疗效果。本研究提出了一种新方法,即使用广泛采用的溶解度增强策略制备载槲皮素微阵列贴片(MAPs)。制备的MAPs表现出良好的机械强度,可插入切除的猪皮肤中达650μm深度。此外,含有Sol uplus的制剂显著提高了载药量,每片可达2.5mg,在应用于切除的猪皮肤一小时内完全溶解。对新生猪全层皮肤的体外研究表明,Sol uplus增强的MAPs能有效地将槲皮素输送穿过各皮肤层,在24小时内实现超过80%的输送效率。此外,这些原型MAPs具有抗炎特性,并与人角质形成皮肤细胞具有生物相容性。因此,以Sol uplus作为溶解度增强剂的载槲皮素MAPs为伤口愈合和抗炎治疗应用提供了一种有前景的替代策略。