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一种新型载有SabiWhite的乙醇胺脂质体凝胶用于治疗由多重耐药病原体引起的靶向性皮肤炎症的研发与优化

Development and optimization of a novel nanocarrier SabiWhite-loaded ethosomal gel for targeted skin inflammation complicated by multidrug-resistant pathogens.

作者信息

Shi Gaofeng, Guo Yun, Yang Minlie

机构信息

Burn and Trauma Treatment Center, Affiliated Hospital of Jiangnan University, Wuxi, Jiangsu, China.

出版信息

Front Cell Infect Microbiol. 2025 Jul 22;15:1640799. doi: 10.3389/fcimb.2025.1640799. eCollection 2025.

Abstract

BACKGROUND

This study aimed to develop and evaluate SabiWhite-loaded ethosomes (SW-ETH) for topical application, focusing on improving stability, biocompatibility, and therapeutic efficacy. Ethosomal formulations are known for their enhanced drug delivery properties, making them suitable for skin inflammation.

METHODS

The SW-ETH formulations were developed utilizing an adapted cold preparation technique. A 3² factorial design was used to optimize phospholipid concentration and ethanol content, and their impact on vesicle size and entrapment efficiency (EE%) was assessed. Structural characterization of SabiWhite was performed using melting point determination, Fourier-Transform Infrared Spectroscopy (FTIR), and X-ray Diffraction (XRD). drug release was assessed using a Franz diffusion cell, and anti-inflammatory and skin irritation studies were performed on Wistar rats.

RESULTS

SabiWhite exhibited a melting point of 96°C and characteristic FTIR peaks, confirming its identity and purity. XRD analysis revealed its crystalline nature, while ethosomal formulations showed a shift to an amorphous state. The optimized SW-ETH formulation (SW-ETH 6) had a vesicle size of 184.4 nm, an EE% of 92.5%, and a zeta potential of -13.50 mV, indicating stable and uniform vesicles. drug release from SW-ETH 6 showed a sustained release profile with 93.12% drug release over 24 hours. , SW-ETH demonstrated significant anti-inflammatory effects with 36.17% edema inhibition at 150 minutes, comparable to Diclofenac gel (41.92%). No skin irritation was observed, and the formulation was classified as non-irritant. Stability tests confirmed minimal changes in appearance, viscosity, and drug content over 120 days at different storage conditions.

CONCLUSION

SW-ETH demonstrated effective drug encapsulation, enhanced anti-inflammatory activity, and excellent biocompatibility, making it a promising candidate for topical therapy. Further clinical validation is warranted to confirm its therapeutic potential.

摘要

背景

本研究旨在开发并评估用于局部应用的载有萨比怀特(SabiWhite)的乙醇脂质体(SW-ETH),重点在于提高其稳定性、生物相容性和治疗效果。乙醇脂质体制剂以其增强的药物递送特性而闻名,使其适用于皮肤炎症。

方法

采用改良的冷制备技术开发SW-ETH制剂。使用3²析因设计优化磷脂浓度和乙醇含量,并评估它们对囊泡大小和包封率(EE%)的影响。通过熔点测定、傅里叶变换红外光谱(FTIR)和X射线衍射(XRD)对萨比怀特进行结构表征。使用Franz扩散池评估药物释放,并在Wistar大鼠上进行抗炎和皮肤刺激性研究。

结果

萨比怀特的熔点为96°C,并具有特征性的FTIR峰,证实了其身份和纯度。XRD分析揭示了其晶体性质,而乙醇脂质体制剂显示出向无定形状态的转变。优化后的SW-ETH制剂(SW-ETH 6)的囊泡大小为184.4 nm,EE%为92.5%,ζ电位为-13.50 mV,表明囊泡稳定且均匀。SW-ETH 6的药物释放显示出持续释放曲线,24小时内药物释放率为93.12%。此外,SW-ETH在150分钟时表现出显著的抗炎作用,水肿抑制率为36.17%,与双氯芬酸凝胶(41.92%)相当。未观察到皮肤刺激,该制剂被归类为无刺激性。稳定性测试证实,在不同储存条件下120天内,外观、粘度和药物含量的变化极小。

结论

SW-ETH显示出有效的药物包封、增强的抗炎活性和优异的生物相容性,使其成为局部治疗的有前景的候选者。需要进一步的临床验证来确认其治疗潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0402/12321823/8480ce07fc81/fcimb-15-1640799-g001.jpg

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