丁香素负载丙二醇二元醇醚的设计制备：稳定性、经皮渗透性和抗氧化活性。

Designed Fabrication of Phloretin-Loaded Propylene Glycol Binary Ethosomes: Stability, Skin Permeability and Antioxidant Activity.

机构信息

College of Pharmacy, Jiamusi University, Jiamusi 154007, China.

Heilongjiang Provincial Key Laboratory of New Drug Development and Pharmacotoxicological Evaluation, Jiamusi University, Jiamusi 154007, China.

出版信息

Molecules. 2023 Dec 21;29(1):66. doi: 10.3390/molecules29010066.

DOI:10.3390/molecules29010066

PMID:38202649

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10780158/

Abstract

Binary ethosome vesicles have been developed as flexible lipid vesicles for the enhanced physicochemical stability and skin delivery of drugs. This work aimed to prepare phloretin-loaded propylene glycol ethosomes (PHL-PGEs) to improve their stability, skin permeability and antioxidant activity. PHL-PGEs were prepared via the ethanol injection method and optimized using different weight ratios of ethanol to propylene glycol (PG). When the ethanol/PG mass ratio changed from 10:0 to 0:10, the encapsulation efficiency and stability of ethosomes increased. At a PHL concentration of 1mg/mL, the EE% was 89.42 ± 2.42 and the DL% was 4.21 ± 0.04, which exhibited their highest values. The encapsulation of the PHL in the PHL-PGEs was strengthened via XRD analysis and FTIR analysis. The results of the in vitro percutaneous permeability test demonstrated that the combined use of ethanol and PG exhibited a notable enhancement in skin permeability, and the skin retention of PHL-PGEs was 1.06 times that of PHL-ethosomes (PHL-Es) and 2.24 times that of the PHL solution. An in vitro antioxidant activity study indicated that solubility and antioxidant activity was potentiated via the nanoencapsulation of phloretin. Therefore, these results confirm the potential of this nanocarrier to enhance physicochemical stability, skin permeability and antioxidant activity.

摘要

双元醇质体囊泡已被开发为灵活的脂质体，用于增强药物的物理化学稳定性和皮肤传递。本工作旨在制备装载根皮素的丙二醇醇质体（PHL-PGE），以提高其稳定性、皮肤渗透性和抗氧化活性。通过乙醇注入法制备 PHL-PGE，并使用不同的乙醇与丙二醇（PG）重量比进行优化。当乙醇/PG 质量比从 10:0 变为 0:10 时，醇质体的包封效率和稳定性增加。在 PHL 浓度为 1mg/mL 时，EE%为 89.42±2.42%，DL%为 4.21±0.04%，表现出最高值。通过 XRD 分析和 FTIR 分析，证实了 PHL 在 PHL-PGE 中的包封作用得到了加强。体外透皮渗透试验结果表明，乙醇和 PG 的联合使用显著增强了皮肤渗透性，并且 PHL-PGE 的皮肤滞留量是 PHL-醇质体（PHL-Es）的 1.06 倍，是 PHL 溶液的 2.24 倍。体外抗氧化活性研究表明，通过根皮素的纳米封装，提高了其溶解度和抗氧化活性。因此，这些结果证实了这种纳米载体在增强物理化学稳定性、皮肤渗透性和抗氧化活性方面的潜力。