Lipase-catalyzed transesterification of vitamin C by natural triglycerides is promising approach for cost-efficient synthesis of liposoluble food and cosmetic antioxidants. Nevertheless, application of these alternative acyl donors is insufficiently explored, despite of their low price, wide abundance and possibility for obtaining versatile products. Within current study, fatty acid ascorbyl esters were synthesized from vitamin C and natural triglycerides (lard, sunflower, coconut and linseed oil) in a process catalyzed by immobilized lipase Novozym® 435 and their controlled release was examined. High conversions were achieved at optimized conditions, even at high substrate concentrations, thus high concentrations of acsorbyl-ester were synthesized using these natural lipids. All ester mixtures exhibited very high capacity for scavenging of DPPH radicals, among which linseed oil derived esters, with ascorbyl linolenate as prevailing compound, were the most efficient (IC₅₀ 0.663 μM), while coconut oil derived ester mixture (IC₅₀ 0.739 μM), composed predominantly of molecules with medium side chains, was second best. Coconut oil derived esters were successfully incorporated in typical cosmetic formulations for controlled release of bioactive compounds - O/W emulsion and gel-emulsion. Franz cell diffusion study demonstrated that esters release from mixture and two carrier systems was formulation dependent and revealed decrease of effective diffusivities with ester side acyl chain length increase. According to calculated effective diffusivity coefficients, faster trans-membrane delivery of the same molecule was achieved from gel-emulsion comparing to O/W emulsion. Applied approach enabled highly efficient cost-saving production of fatty acid ascorbyl esters, which could find direct application in various lipophilic products.

天然甘油三酸酯经脂肪酶催化的维生素C酯交换反应是一种经济有效的合成脂溶性食品和化妆品抗氧化剂的方法。然而，尽管价格低廉，种类繁多且有可能获得通用产品，但仍未充分探索这些替代性酰基供体的应用。在当前的研究中，在固定化脂肪酶435催化下的过程中，由维生素C和天然甘油三酸酯（猪油，向日葵，椰子和亚麻籽油）合成了脂肪酸抗坏血酸酯，并检查了它们的控制释放。即使在高底物浓度下，也可以在最佳条件下实现高转化率，因此使用这些天然脂质合成了高浓度的乙酰基酯。₅₀ 0.663μM），而椰子油衍生的酯混合物（IC ₅₀次优是0.739μM），主要由具有中等侧链的分子组成。椰子油衍生的酯已成功掺入典型的化妆品配方中，以控制释放生物活性化合物-O / W乳液和凝胶乳液。Franz细胞扩散研究表明，混合物和两种载体体系中的酯释放取决于制剂，并揭示了随着酯侧酰基链长度的增加，有效扩散率降低。根据计算出的有效扩散系数，与O / W乳剂相比，凝胶乳剂可实现相同分子更快的跨膜递送。应用方法使脂肪酸抗坏血酸酯的生产得以高效节约，这可以直接应用于各种亲脂性产品中。