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α-硫辛酸负载的纳米结构脂质载体的理化性质表征、鉴定及光稳定性改善。

Physicochemical characterization, identification and improved photo-stability of α-lipoic acid-loaded nanostructured lipid carrier.

机构信息

School of Biological Science and Medical Engineering, State Key Laboratory of Bioelectronics, Southeast University , Nanjing 210096 , China.

出版信息

Drug Dev Ind Pharm. 2014 Feb;40(2):201-10. doi: 10.3109/03639045.2012.753901. Epub 2013 Jan 22.

Abstract

OBJECTIVE

The ultimate goal of this research is to corroborate the physicochemical characterization of nanostructured lipid carrier (NLC) loading unstable lipophilic active ingredients with an antioxidant function, such as alpha-lipoic acid (ALA), and monitoring its photochemical stability of ALA-NLC against natural daylight. NLC is an innovative active compound delivery system in pharmaceutical and cosmetic fields. It has been recommended as active substance carriers to enhance the effectiveness of lipophilic compounds.

METHODS

ALA-NLC was manufactured using hot high pressure homogenization technique to increase the water solubility and photo-stability. The physicochemical characterization properties of ALA-NLC have been determined in terms of nanoparticle size, zeta potential, polydispersity index value and size distribution. Size analysis was implemented through photon correlation spectroscopy and laser diffractometry. Morphological profile of nanoparticles was observed via atomic force microscopy. The loading of NLC containing ALA was evaluated by high performance liquid chromatography. ALA-NLC was subjected to UV-Vis spectrophotometer to validate the existence of ALA. Water contact angle measurement was manipulated to determine the hydrophilicity of the sample. The photo-stability of ALA-NLC within 120 days was assessed by the retention of ALA.

RESULTS

The ALA-NLC provided maximum ALA retention of 93.9% in 30 days exposure to natural daylight, the retention of free ALA only 42.5%. About 88.5% of the initial ALA in NLC system remained after 120 days under the same conditions, while the retention of free ALA only 0.7% under natural daylight irradiation. The photo-stability of ALA was considerably enhanced by NLC formulation compared with free ALA itself. Therefore, the NLC formulation provided a reliable protection of ALA against natural daylight, enhancing its photochemical stability.

CONCLUSION

The present investigation elucidated that the NLC drastically improved the water solubility, particularly the facilitation of photo-stability of ALA exposure to natural daylight.

摘要

目的

本研究的最终目标是证实纳米结构脂质载体(NLC)负载具有抗氧化功能的不稳定脂溶性活性成分(如α-硫辛酸(ALA))的物理化学特性,并监测其在自然光下 ALA-NLC 的光化学稳定性。NLC 是制药和化妆品领域中创新的活性化合物输送系统。它已被推荐为增强脂溶性化合物功效的活性物质载体。

方法

使用高压均质热技术制造 ALA-NLC,以提高其水溶性和光稳定性。通过纳米颗粒粒径、Zeta 电位、多分散指数值和粒径分布来确定 ALA-NLC 的物理化学特性。通过光子相关光谱法和激光衍射法进行粒径分析。通过原子力显微镜观察纳米颗粒的形态。通过高效液相色谱法评估负载 NLC 的 ALA。通过紫外可见分光光度计验证 ALA-NLC 中 ALA 的存在。通过水接触角测量来确定样品的亲水性。通过保留率评估 120 天内 ALA-NLC 的光稳定性。

结果

ALA-NLC 在 30 天的自然光暴露下提供了最大的 ALA 保留率 93.9%,而游离 ALA 的保留率仅为 42.5%。在相同条件下,NLC 体系中初始 ALA 的 88.5%在 120 天后仍保留,而游离 ALA 的保留率仅为 0.7%。与游离 ALA 本身相比,NLC 配方显著增强了 ALA 的光稳定性。因此,NLC 配方为 ALA 提供了可靠的自然光保护,增强了其光化学稳定性。

结论

本研究表明,NLC 极大地提高了 ALA 的水溶性,特别是促进了 ALA 在自然光下的光稳定性。

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