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载有大豆异黄酮的海藻酸钠微球在温敏凝胶基质中的应用:改善创伤愈合效果的尝试。

Soy isoflavone-loaded alginate microspheres in thermosensitive gel base: attempts to improve wound-healing efficacy.

机构信息

Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka, Saudi Arabia.

Department of Pharmaceutics and Ind. Pharmacy, Faculty of Pharmacy (Boys), Al-Azhar University, Nasr City, Cairo, Egypt.

出版信息

J Pharm Pharmacol. 2019 May;71(5):774-787. doi: 10.1111/jphp.13066. Epub 2019 Jan 14.

Abstract

OBJECTIVES

This study aims to develop thermosensitive gel containing soy isoflavone (antioxidant and anti-inflammatory natural agent) alginate microspheres for enhancement of wound-healing performance.

METHODS

Soy isoflavone microspheres were prepared by ionic cross-linking method and optimized using the Box-Behnken optimization design. Formulations were characterized in terms of particle size, encapsulation efficiency and equilibrium swelling degree. The optimized formula was incorporated in Pluronic F127 gel base and examined for in vivo wound-healing efficacy.

KEY FINDINGS

Results showed mean particle size between 18 and 25 μm, encapsulation efficiency of over 75% and equilibrium swelling degree over 1.9. Thermal analysis indicated interaction between alginate and CaCl and embedding of soy isoflavone in microspheres. In vivo wound-healing efficacy showed significant advance in re-epithelization, mature collagen synthesis and proangiogenesis. Immunohistochemical investigation exhibited promising alpha-smooth muscle actin immunopositive cells expression, fibroblast activation and expression of proliferating cell nuclear antigen (proliferation marker) in the epidermis and in the dermis.

CONCLUSIONS

The developed formulation would appear to be a promising topical preparation for accelerating healing process.

摘要

目的

本研究旨在开发一种含有大豆异黄酮(抗氧化和抗炎天然剂)海藻酸钠微球的温敏凝胶,以增强伤口愈合性能。

方法

采用离子交联法制备大豆异黄酮微球,并采用 Box-Behnken 优化设计进行优化。从粒径、包封率和平衡溶胀度等方面对配方进行了表征。将优化后的配方加入泊洛沙姆 F127 凝胶基质中,考察其体内伤口愈合效果。

主要发现

结果表明,平均粒径在 18 到 25 微米之间,包封率超过 75%,平衡溶胀度超过 1.9。热分析表明海藻酸钠与 CaCl2 之间存在相互作用,并且大豆异黄酮嵌入微球中。体内伤口愈合效果表明,上皮再上皮化、成熟胶原蛋白合成和促血管生成有显著进展。免疫组织化学研究显示,表皮和真皮中α-平滑肌肌动蛋白免疫阳性细胞表达、成纤维细胞激活和增殖细胞核抗原(增殖标志物)表达有很大改善。

结论

所开发的制剂似乎是一种有前途的加速愈合过程的局部制剂。

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