Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok, Thailand.
AAPS PharmSciTech. 2012 Mar;13(1):336-43. doi: 10.1208/s12249-011-9749-0. Epub 2012 Jan 25.
The topical application of all-trans retinoic acid (ATRA) is an effective treatment for several skin disorders, including photo-aging. Unfortunately, ATRA is susceptible to light, heat, and oxidizing agents. Thus, this study aimed to investigate the ability of polymeric micelles prepared from polyethylene glycol conjugated phosphatidylethanolamine (PEG-PE) to stabilize ATRA under various storage conditions. ATRA entrapped in polymeric micelles with various PEG and PE structures was prepared. The critical micelle concentrations were 97-243 μM, depending on the structures of the PEG and PE molecules. All of the micelles had particle diameters of 6-20 nm and neutral charges. The highest entrapment efficiency (82.7%) of the tested micelles was exhibited by ATRA in PEG with a molecular weight of 750 Da conjugated to dipalmitoyl phosphatidylethanolamine (PEG(750)-DPPE) micelles. The PEG(750)-DPPE micelle could significantly retard ATRA oxidation compared to ATRA in 75% methanol/HBS solution. Up to 87% of ATRA remained in the PEG(750)-DPPE micelle solution after storage in ambient air for 28 days. This result suggests that PEG(750)-DPPE micelle can improve ATRA stability. Therefore, ATRA in PEG(750)-DPPE micelle is an interesting alternative structure for the development of cosmeceutical formulations.
全反式维甲酸（ATRA）的局部应用是治疗多种皮肤疾病的有效方法，包括光老化。不幸的是，ATRA 容易受到光、热和氧化剂的影响。因此，本研究旨在探讨聚乙二醇接枝磷脂酰乙醇胺（PEG-PE）制备的聚合物胶束在各种储存条件下稳定 ATRA 的能力。制备了具有不同 PEG 和 PE 结构的聚合物胶束包封的 ATRA。临界胶束浓度取决于 PEG 和 PE 分子的结构，范围为 97-243 μM。所有胶束的粒径为 6-20nm，带中性电荷。用分子量为 750Da 的聚乙二醇（PEG（750））与二棕榈酰磷脂酰乙醇胺（DPPE）偶联的聚乙二醇（PEG（750）-DPPE）胶束包封的 ATRA 的包封效率最高（82.7%）。与 75%甲醇/HBS 溶液中的 ATRA 相比，PEG（750）-DPPE 胶束能显著延缓 ATRA 的氧化。在环境空气中储存 28 天后，PEG（750）-DPPE 胶束溶液中仍有 87%的 ATRA 保持不变。这一结果表明，PEG（750）-DPPE 胶束可以提高 ATRA 的稳定性。因此，PEG（750）-DPPE 胶束中的 ATRA 是开发美容化妆品制剂的一种有趣的替代结构。
