Biodegradable Kojic Acid-Based Polymers: Controlled Delivery of Bioactives for Melanogenesis Inhibition.
Biodegradable Kojic Acid-Based Polymers: Controlled Delivery of Bioactives for Melanogenesis Inhibition.
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DOI：
10.1021/acs.biomac.6b01353
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发表时间：
2017-02-13
影响因子：
6.2
通讯作者：
Uhrich KE
中科院分区：
文献类型：
--
作者：
Faig JJ;Moretti A;Joseph LB;Zhang Y;Nova MJ;Smith K;Uhrich KE
曲酸（KA）是一种天然存在的真菌代谢产物，由于其有效的酪氨酸酶抑制活性而被用作皮肤增白剂和抗褐变剂。虽然有效，但KA倾向于经历pH介导的、热和光降解，这降低了其功效，需要稳定载体。为了使降解最小化，通过溶液聚合方法制备由KA和天然二酸组成的聚（碳酸酯）和聚酯。体外水解降解分析显示KA释放受聚合物主链组成（例如，聚（碳酸酯-酯）对聚酯）、连接分子（脂肪族对含杂原子的）和释放条件（生理对皮肤）。酪氨酸酶抑制试验表明，脂肪族KA二烯醇，在皮肤条件下的主要降解产物，是更有效的，然后KA本身。在所有测试浓度下，发现所有二烯醇的毒性低于KA。此外，在抑制细胞中黑色素生物合成方面，最亲脂的二烯醇在统计学上比KA更有效。这些基于KA的聚合物系统提供具有改善的功效和细胞相容性的KA类似物，使其成为医疗和个人护理产品中持续局部治疗的理想候选物。
Kojic acid (KA) is a naturally occurring fungal metabolite that is utilized as a skin-lightener and antibrowning agent owing to its potent tyrosinase inhibition activity. While efficacious, KA’s inclination to undergo pH-mediated, thermal-, and photodegradation reduces its efficacy, necessitating stabilizing vehicles. To minimize degradation, poly(carbonate-esters) and polyesters comprised of KA and natural diacids were prepared via solution polymerization methods. In vitro hydrolytic degradation analyses revealed KA release was drastically influenced by polymer backbone composition (e.g., poly(carbonate-ester) vs polyester), linker molecule (aliphatic vs heteroatom-containing), and release conditions (physiological vs skin). Tyrosinase inhibition assays demonstrated that aliphatic KA dienols, the major degradation product under skin conditions, were more potent then KA itself. All dienols were found to be less toxic than KA at all tested concentrations. Additionally, the most lipophilic dienols were statistically more effective than KA at inhibiting melanin biosynthesis in cells. These KA-based polymer systems deliver KA analogues with improved efficacy and cytocompatible profiles, making them ideal candidates for sustained topical treatments in both medical and personal care products.
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影响因子：
1.7
作者：
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影响因子：
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影响因子：
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作者：
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通讯作者：
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