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用于洛索洛芬有效透皮递送的醇质体的制备与评估。

Fabrication and assessment of ethosomes for effective transdermal delivery of loxoprofen.

作者信息

Alhur Sarah Jabbar Abd, Mahmood Hasanain Shakir

机构信息

Department of Pharmaceutics, College of Pharmacy, Mustansiriyah University, Baghdad, Iraq.

Department of Pharmaceutics, College of Pharmacy, University of Kerbala, Kerbala, Iraq.

出版信息

Iran J Basic Med Sci. 2025;28(6):728-738. doi: 10.22038/ijbms.2025.84183.18206.

DOI:10.22038/ijbms.2025.84183.18206
PMID:40343291
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12057754/
Abstract

OBJECTIVES

To formulate and evaluate ethosomes for the transdermal delivery of loxoprofen, a potent non-steroidal anti-inflammatory drug (NSAID).

MATERIALS AND METHODS

Fifteen ethosomal formulations were created via thin-film hydration and probe sonication techniques, with variations in the amounts of egg yolk lecithin, ethanol, cholesterol (CHOL), Tween 80 (TW80), and propylene glycol (PG). The formulations were assessed for their particle size (PS), zeta potential (ZP), polydispersity index (PDI), pH, and entrapment efficiency (EE). Field scanning electron microscopy (FSEM) was utilized to evaluate their morphology. The drug release and permeability of the ethosomal formulations were evaluated against those in a hydroethanolic drug solution.

RESULTS

The formulation labeled F14, comprising 1% loxoprofen, 1% egg yolk lecithin, 30% ethanol, 5% propylene glycol, and phosphate-buffered saline (PBS) up to 25 ml, was recognized as an optimized ethosomal formulation. These ethosomes demonstrated an average size of 164.2±19 nm, a PDI of 0.280±0.028, a ZP of +45.1±4.5 mV, and an EE of 96.8±0.43%. and tests demonstrated that the ethosomal formulation (F14) showed superior drug release and penetration rates compared to a conventional hydroalcoholic solution. The differential scanning calorimetry (DSC) study showed that loxoprofen was completely trapped within ethosomes. On the other hand, the Fourier transform infrared (FTIR) study confirmed that the drug and the additives did not interact.

CONCLUSION

The current study revealed that loxoprofen can be effectively delivered transdermally via the ethosomal system.

摘要

目的

制备并评估用于透皮递送洛索洛芬(一种强效非甾体抗炎药)的醇质体。

材料与方法

通过薄膜水化和探头超声技术制备了15种醇质体制剂,其中蛋黄卵磷脂、乙醇、胆固醇(CHOL)、吐温80(TW80)和丙二醇(PG)的用量有所不同。对这些制剂的粒径(PS)、zeta电位(ZP)、多分散指数(PDI)、pH值和包封率(EE)进行了评估。利用场扫描电子显微镜(FSEM)评估其形态。将醇质体制剂的药物释放和渗透性与氢乙醇药物溶液中的情况进行了比较评估。

结果

标记为F14的制剂,包含1%洛索洛芬、1%蛋黄卵磷脂、30%乙醇、5%丙二醇和至25 ml的磷酸盐缓冲盐水(PBS),被认为是优化后的醇质体制剂。这些醇质体的平均粒径为164.2±19 nm,PDI为0.280±0.028,ZP为+45.1±4.5 mV,EE为96.8±0.43%。 测试表明,与传统氢乙醇溶液相比,醇质体制剂(F14)显示出更高的药物释放和渗透速率。差示扫描量热法(DSC)研究表明,洛索洛芬完全包封在醇质体内。另一方面,傅里叶变换红外光谱(FTIR)研究证实药物与添加剂之间没有相互作用。

结论

当前研究表明,洛索洛芬可通过醇质体系统有效实现透皮递送。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f8e1/12057754/48f56a9c903e/ijbms-28-728-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f8e1/12057754/48f56a9c903e/ijbms-28-728-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f8e1/12057754/48f56a9c903e/ijbms-28-728-g009.jpg

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