Department of Pharmaceutics and Pharmaceutical Technology, School of Pharmacy, The University of Jordan, Amman 11942, Jordan.
Department of Pharmaceutics and Pharmaceutical Technology, School of Pharmacy, The University of Jordan, Amman 11942, Jordan.
Int J Pharm. 2023 Apr 5;636:122781. doi: 10.1016/j.ijpharm.2023.122781. Epub 2023 Feb 26.
Long-term exposure to solar radiation can lead to skin damage such as photoageing, and photocarcinogenesis. This can be prevented by topically applying α-tocopherol phosphate (α-TP). The major challenge is that a significant amount of α-TP needs to reach viable skin layers for effective photoprotection. This study aims to develop candidate formulations of α-TP (gel-like, solution, lotion, and gel), and investigate formulation characteristics' effect on membrane diffusion and human skin permeation. All the formulations developed in the study had an appealing appearance and no signs of separation. All formulations had low viscosity and high spreadability except the gel. The flux of α-TP through the polyethersulfone membrane was the highest for lotion (6.63 ± 0.86 mg/cm/h), followed by control gel-like (6.14 ± 1.76 mg/cm/h), solution (4.65 ± 0.86 mg/cm/h), and gel (1.02 ± 0.22 mg/cm/h). The flux of α-TP through the human skin membrane was numerically higher for lotion compared to the gel-like (328.6 vs.175.2 µg/cm/h). The lotion delivered 3-fold and 5-fold higher α-TP in viable skin layers at 3 h and 24 h, respectively, compared to that of the gel-like. The low skin membrane penetration rate and deposition of α-TP in viable skin layers were observed for the solution and gel. Our study demonstrated that dermal penetration of α-TP was influenced by characteristics of formulation such as formulation type, pH, and viscosity. The α-TP in the lotion scavenged higher DPPH free radicals compared to that of gel-like (almost 73% vs. 46%). The IC of α-TP in lotion was significantly lower than that of gel-like (397.2 vs. 626.0 µg/mL). The preservative challenge test specifications were fulfilled by Geogard 221 and suggested that the combination of benzyl alcohol and Dehydroacetic Acid effectively preserved 2% α-TP lotion. This result confirms the suitability of the α-TP cosmeceutical lotion formulation employed in the present work for effective photoprotection.
长期暴露在太阳辐射下会导致皮肤损伤，如光老化和光致癌。通过局部涂抹α-生育酚磷酸酯（α-TP）可以预防这种情况。主要的挑战是需要有大量的α-TP 到达有活力的皮肤层以实现有效的光保护。本研究旨在开发 α-TP 的候选配方（凝胶状、溶液、乳液和凝胶），并研究配方特性对膜扩散和人体皮肤渗透的影响。本研究中开发的所有配方都具有吸引人的外观，没有分离的迹象。除了凝胶外，所有配方的粘度都很低，扩展性都很高。α-TP 通过聚醚砜膜的通量以乳液最高（6.63±0.86mg/cm/h），其次是对照凝胶状（6.14±1.76mg/cm/h）、溶液（4.65±0.86mg/cm/h）和凝胶（1.02±0.22mg/cm/h）。α-TP 通过人体皮肤膜的通量以乳液比凝胶状高（328.6 比 175.2µg/cm/h）。与凝胶状相比，乳液在 3 小时和 24 小时时，在有活力的皮肤层中输送的α-TP 分别高出 3 倍和 5 倍。在有活力的皮肤层中，溶液和凝胶的α-TP 皮肤穿透率低，沉积量低。本研究表明，α-TP 的真皮渗透受到配方特性的影响，如配方类型、pH 值和粘度。与凝胶状相比，乳液中的α-TP 清除了更高的 DPPH 自由基（近 73%比 46%）。乳液中 α-TP 的 IC 明显低于凝胶状（397.2 比 626.0µg/mL）。Geogard 221 通过了防腐剂挑战测试规范，表明苯氧乙醇和脱氢乙酸的组合有效地保存了 2%α-TP 乳液。该结果证实了本工作中使用的 α-TP 化妆品乳液配方用于有效光保护的适宜性。
