Department of Pharmaceutics, Faculty of Pharmacy, Ahram Canadian University, Cairo, Egypt.
Department of Clinical Pharmacy, Faculty of Pharmacy, Ahram Canadian University, Cairo, Egypt.
Drug Deliv. 2021 Dec;28(1):445-453. doi: 10.1080/10717544.2021.1886377.
l-Ascorbic acid (LAA) is considered a powerful antioxidant that protects skin from premature aging. Maintaining the stability of vitamin C remains the biggest challenge in cosmeceuticals. Our main aim is the entrapment of high dose of vitamin C in spanlastic vesicles to provide maximum stability and efficacy. LAA-loaded spanlastics were prepared by ethanol injection method and were characterized for entrapment efficiency (EE%), particles size (PS), polydispersity index (PDI), zeta potential, deformability index (DI) and skin permeation. Selected spanlastics formula composed of span 60 and tween 60 (5:1) showed highest EE% of 89.77 ± 3.61% (w/w), high deformability of 11.13 ± 1.145 as well as good physical and chemical stability for 6 months. Improved drug penetration into stratum corneum (SC) was obtained from spanlastics compared to topical LAA solution. Quantitative real time PCR revealed that MMP2 and MMP9 levels were significantly suppressed in response to LAA spanlastics treated rats by 30.4% and 65.3%, respectively, when compared to the control group after exposure to UV irradiation. Results were confirmed by western blot analysis. Histopathological study of rat skin after UV irradiation revealed that application of LAA-loaded spanlastics provided the highest skin protection compared to UVB and LAA solution treated group which was evident by the normal thick epidermal morphology and the densely arranged dermal collagen fibers. LAA-loaded spanlastics successfully improved LAA stability, skin permeation and antioxidant protection against skin photodamage.
抗坏血酸(LAA)被认为是一种强大的抗氧化剂,可保护皮肤免受过早衰老。保持维生素 C 的稳定性仍然是化妆品领域的最大挑战。我们的主要目标是将高剂量的维生素 C 包封在spanlastic 泡囊中,以提供最大的稳定性和功效。通过乙醇注入法制备 LAA 加载的 spanlastics,并对包封效率(EE%)、颗粒大小(PS)、多分散指数(PDI)、Zeta 电位、变形指数(DI)和皮肤渗透进行了表征。由 span 60 和 tween 60(5:1)组成的选定 spanlastics 配方显示出最高的 EE%为 89.77±3.61%(w/w)、高变形性为 11.13±1.145,并且在 6 个月内具有良好的物理化学稳定性。与局部 LAA 溶液相比,spanlastics 可改善药物渗透进入角质层(SC)。定量实时 PCR 显示,与对照组相比,LAA spanlastics 处理的大鼠 MMP2 和 MMP9 水平分别显著降低了 30.4%和 65.3%,而对照组在暴露于 UV 照射后。Western blot 分析证实了这一点。UV 照射后大鼠皮肤的组织病理学研究表明,与 UVB 和 LAA 溶液处理组相比,LAA 负载的 spanlastics 提供了最高的皮肤保护,这可以通过正常的厚表皮形态和密集排列的真皮胶原纤维来证明。LAA 负载的 spanlastics 成功提高了 LAA 的稳定性、皮肤渗透和抗氧化保护作用,防止皮肤光损伤。