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用于透皮给药的含秋水仙碱立方液晶纳米粒的制剂与评价

Formulation and evaluation of cubosomes containing colchicine for transdermal delivery.

作者信息

Nasr Mohamed, Younes Hassan, Abdel-Rashid Rania S

机构信息

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Helwan University, Cairo, 11790, Egypt.

Department of Pharmaceutics, Faculty of Pharmacy, Delta University for Science and Technology, Gamasa, Egypt.

出版信息

Drug Deliv Transl Res. 2020 Oct;10(5):1302-1313. doi: 10.1007/s13346-020-00785-6.

Abstract

Gout is a common inflammatory disease that is characterized by the deposition of serum urate crystals in the synovial fluids and joints. In spite of high efficiency of colchicine (COL) in treatment of gout, it has potential side effects associated with its oral administration. This study was aimed to enhance COL bioavailability and minimize associated side effects through transdermal delivery of COL-loaded cubosomes. Eight cubosomal dispersions were prepared according to Box-Behnken factorial design and the effect of COL, glyceryl monooleate (GMO), and surfactant (P407) concentrations on particle size distribution, zeta potential, and entrapment efficiency were assessed. The results revealed that the optimum formula exhibited a mean particle size of 73.07 ± 2.18 nm and entrapped 32.40 ± 2.33% of COL. The influence of transdermal application of COL cubosomal gel on the in vivo absorption of the drug was studied in rats compared with oral COL solution. The results of in vivo study showed that transdermal application of COL cubosomal gel significantly improves the drug absorption compared with oral COL solution, with evidence of a relative bioavailability of 4.6 times greater than that of oral COL solution. In conclusion, transdermal application of COL cubosomal gel may be a promising delivery system for enhancing the bioavailability of COL. Graphical abstract.

摘要

痛风是一种常见的炎症性疾病,其特征是血清尿酸盐晶体沉积在滑液和关节中。尽管秋水仙碱(COL)治疗痛风的效率很高,但口服给药会有潜在的副作用。本研究旨在通过经皮递送载有COL的立方液晶纳米粒来提高COL的生物利用度并将相关副作用降至最低。根据Box-Behnken析因设计制备了八种立方液晶纳米粒分散体,并评估了COL、单油酸甘油酯(GMO)和表面活性剂(P407)浓度对粒径分布、ζ电位和包封率的影响。结果显示,最佳配方的平均粒径为73.07±2.18nm,COL包封率为32.40±2.33%。与口服COL溶液相比,研究了大鼠经皮应用COL立方液晶纳米粒凝胶对药物体内吸收的影响。体内研究结果表明,与口服COL溶液相比,经皮应用COL立方液晶纳米粒凝胶显著提高了药物吸收,相对生物利用度比口服COL溶液高4.6倍。总之,经皮应用COL立方液晶纳米粒凝胶可能是一种提高COL生物利用度的有前景的给药系统。图形摘要。

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