L-抗坏血酸(AA)是一种高度不稳定的化合物,因此,限制其在药品和化妆品中的使用,特别是在较高的浓度。
本研究旨在通过将高度敏感的分子(AA)封装在β-环糊精纳米海绵(β-CDNS)中,可以进一步用于制备具有较高AA浓度和增强稳定性的药妆产品。
NS是通过熔融法合成的。通过冷冻干燥方法将AA包封在β-CDNS中。用红外光谱对所制备的NS进行了表征,SEM,原子力显微镜(AFM),zetasizer,差示扫描量热法(DSC),并对其物理流动特性进行了研究。使用两种方法的组合在Franz装置上进行体外药物释放:样品&分离和透析膜。使用经验证的光谱测定方法进行测定。
AA在β-CDNS中的包封率表明良好的负载能力(83.57±6.35%)。FTIR,SEM,AFM,DSC结果证实了AA在β-CDNS中的包封。颗粒大小,多分散指数,和zeta电位结果确定了稳定的单分散纳米颗粒的形成。物理流动特性显示出良好的流动特性。在Korsmeyer-Peppas模型之后的4小时内,约有84%的AA从NS中释放。当在30±2℃/65±5%RH下储存时,负载AA的NS保持稳定9个月。
结论是制备的NS可以保护高度敏感的AA免于降解并提供维生素的延长释放。所制备的载AAβ-CDNS可用于配制其他具有较好稳定性和效果的药妆剂型。
BACKGROUND: L-Ascorbic acid (AA) is a highly unstable compound, thus, limiting its use in pharmaceutical and cosmetic products, particularly at higher concentrations.
OBJECTIVE: This study aimed to stabilize the highly sensitive molecule (AA) by encapsulating it in β- cyclodextrin nanosponges (β-CD NS) that can be used further in preparing cosmeceuticals products with higher AA concentrations and enhanced stability.
METHODS: The NS has been synthesized by the melting method. The AA was encapsulated in β-CD NS by the freeze-drying process. The prepared NS were characterized by FTIR spectrometry, SEM, Atomic Force Microscopy (AFM), zeta sizer, Differential Scanning Calorimetry (DSC), and the physical flow characteristics were also studied. The in vitro drug release was carried out on the Franz apparatus using a combination of two methods: sample & separate and dialysis membrane. The assay was performed using a validated spectrometric method.
RESULTS: The entrapment efficiency of AA in β-CD NS indicated a good loading capacity (83.57±6.35%). The FTIR, SEM, AFM, and DSC results confirmed the encapsulation of AA in β-CD NS. The particle size, polydispersity index, and zeta potential results ascertained the formation of stabilized monodisperse nanoparticles. The physical flow characteristics showed good flow properties. Around 84% AA has been released from the NS in 4 h following the Korsmeyer-Peppas model. The AA-loaded NS remained stable for nine months when stored at 30±2°C/65±5% RH.
CONCLUSIONS: It is concluded that the prepared NS can protect the highly sensitive AA from degradation and provide an extended-release of the vitamin. The prepared AA-loaded β-CD NS can be used to formulate other cosmeceutical dosage forms with better stability and effect.