背景:类维生素A,定义为维生素A的合成或天然衍生物,作为广泛应用于化妆品中的抗衰老分子,已经被广泛研究。然而,由于它们的物理化学性质,类维生素A非常不稳定,对光极其敏感,氧气,和温度。此外,类维生素A的局部应用通常导致皮肤刺激。类维生素A的这些不稳定性和刺激性限制了它们在化妆品和药物产品中的应用。
目的:我们的研究旨在提供系统综述,以总结类维生素A的不稳定性和刺激性的潜在机制,以及应对这些挑战的最新发展。
方法:使用以下关键字进行了全面的PubMed搜索:类维生素A,化学不稳定性,皮肤刺激,类维生素A衍生物,基于纳米脂质的载体,脂质体,渗透增强囊泡,乙醇体,Niosomes,纳米乳液,固体脂质纳米粒,维生素,舒缓和保湿剂,抗氧化剂和金属螯合剂和视黄醇的组合。回顾了1968年至2023年之间发表的相关研究以及与这些报告相关的研究。
结果:开发新的类维生素A衍生物,利用新的递送系统,如基于纳米脂质的载体,以及与其他化合物如维生素的组合,舒缓剂,抗氧化剂和金属螯合剂已被探索,以提高稳定性,生物利用度,和类维生素A家族的毒性。
结论:通过配方技术的进步,类维生素A衍生物的结构修饰和新型纳米脂质基载体的开发,类维生素A的化学不稳定性和皮肤刺激已得到缓解,确保其长期的功效和效力。
BACKGROUND: Retinoids, defined as synthetic or natural derivatives of vitamin A, have been extensively studied as anti-aging molecules that are widely applied in cosmetics. However, due to their physicochemical property, retinoids are highly unstable and extremely sensitive to light, oxygen, and temperature. Moreover, topical application of retinoids often leads to cutaneous irritation. These instabilities and irritant properties of retinoids limit their application in cosmetic and pharmaceutical products.
OBJECTIVE: Our study aimed to provide a systematic review to summarize the mechanisms underlying the instability and irritant properties of retinoids, as well as recent developments in addressing these challenges.
METHODS: A comprehensive PubMed search was conducted using the following keywords: retinoids, chemical instability, skin irritation, retinoid derivatives, nano lipid-based carriers, liposomes, penetration-enhancer vesicles, ethosomes, niosomes, nanoemulsions, solid lipid nanoparticles, vitamins, soothing and hydrating agents, antioxidants and metal chelator and retinol combinations. Relevant researches published between 1968 and 2023 and studies related to these reports were reviewed.
RESULTS: The development of new retinoid derivatives, the utilization of new delivery systems like nano lipid-based carriers and the combination with other compounds like vitamins, soothing agents, antioxidants and metal chelator have been explored to improve the stability, bioavailability, and toxicity of the retinoid family.
CONCLUSIONS: Through advancements in formulation techniques, structure modification of retinoid derivatives and development of novel nano lipid-based carriers, the chemical instability and skin irritation of retinoids has been mitigated, ensuring their efficacy and potency over extended periods.