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含姜黄素的自纳米乳化药物递送系统局部剂型的体外和体内疗效

In Vitro and In Vivo Efficacy of Topical Dosage Forms Containing Self-Nanoemulsifying Drug Delivery System Loaded with Curcumin.

作者信息

Frei Gréta, Haimhoffer Ádám, Csapó Enikő, Bodnár Krisztina, Vasvári Gábor, Nemes Dániel, Lekli István, Gyöngyösi Alexandra, Bácskay Ildikó, Fehér Pálma, Józsa Liza

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, 4032 Debrecen, Hungary.

Healthcare Industry Institute, University of Debrecen, 4032 Debrecen, Hungary.

出版信息

Pharmaceutics. 2023 Jul 31;15(8):2054. doi: 10.3390/pharmaceutics15082054.

DOI:10.3390/pharmaceutics15082054
PMID:37631267
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10459893/
Abstract

The external use of curcumin is rare, although it can be a valuable active ingredient in the treatment of certain inflammatory diseases. The aim of our experimental work was to formulate topical dosage forms containing curcumin for the treatment of atopic dermatitis. Curcumin has extremely poor solubility and bioavailability, so we have tried to increase it with the usage of self-emulsifying drug delivery systems. Creams and gels were formulated using penetration-enhancing surfactants and gelling agents. The release of the drug from the vehicle and its penetration through the membrane were determined using a Franz diffusion cell. An MTT cytotoxicity and in vitro antioxidant assays were performed on HaCaT cell line. The in vivo anti-inflammatory effect of the preparations was tested by measuring rat paw edema. In addition, we examined the degree of inflammation induced by UV radiation after pretreatment with the cream and the gel on rats. For the gels containing SNEDDS, the highest penetration was measured after half an hour, while for the cream, it took one hour to reach the maximum concentration. The gel containing Pemulen TR-1 showed the highest drug release. It was determined that the curcumin-containing preparations can be safely applied on the skin and have antioxidant effects. The animal experiments have proven the effectiveness of curcumin-containing topical preparations.

摘要

姜黄素的外用情况较为罕见,尽管它在某些炎症性疾病的治疗中可能是一种有价值的活性成分。我们实验工作的目的是制备含姜黄素的局部用剂型,用于治疗特应性皮炎。姜黄素的溶解度和生物利用度极低,因此我们尝试通过使用自乳化药物递送系统来提高其溶解度和生物利用度。使用渗透促进表面活性剂和胶凝剂制备了乳膏和凝胶。使用Franz扩散池测定药物从载体中的释放及其透过膜的渗透情况。对HaCaT细胞系进行了MTT细胞毒性和体外抗氧化测定。通过测量大鼠足爪水肿来测试制剂的体内抗炎作用。此外,我们还检测了在大鼠身上用乳膏和凝胶预处理后紫外线辐射诱导的炎症程度。对于含有自乳化药物递送系统的凝胶,半小时后测得的渗透率最高,而对于乳膏,达到最大浓度需要1小时。含有Pemulen TR-1的凝胶显示出最高的药物释放率。已确定含姜黄素的制剂可安全地应用于皮肤并具有抗氧化作用。动物实验证明了含姜黄素局部用制剂的有效性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ca29/10459893/ea0bbd474c8e/pharmaceutics-15-02054-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ca29/10459893/210f04a7cd63/pharmaceutics-15-02054-g001.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ca29/10459893/ee57c1d3ffd6/pharmaceutics-15-02054-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ca29/10459893/ea0bbd474c8e/pharmaceutics-15-02054-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ca29/10459893/210f04a7cd63/pharmaceutics-15-02054-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ca29/10459893/19d6790e88ea/pharmaceutics-15-02054-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ca29/10459893/6bbcc313f233/pharmaceutics-15-02054-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ca29/10459893/ded9c634ac43/pharmaceutics-15-02054-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ca29/10459893/36c52d7ab6ed/pharmaceutics-15-02054-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ca29/10459893/f2969a13f475/pharmaceutics-15-02054-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ca29/10459893/1d10137aae19/pharmaceutics-15-02054-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ca29/10459893/ee57c1d3ffd6/pharmaceutics-15-02054-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ca29/10459893/ea0bbd474c8e/pharmaceutics-15-02054-g009.jpg

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