The transdermal performance, pharmacokinetics, and anti-inflammatory pharmacodynamics evaluation of harmine-loaded ethosomes

Autor:	Jizong Jiang, Tingyun Ma, Liuhong Zhang, Xuemei Cheng, Changhong Wang
Rok vydání:	2020
Předmět:	medicine.drug_class Skin Absorption Anti-Inflammatory Agents Pharmaceutical Science 02 engineering and technology Pharmacology Administration Cutaneous 030226 pharmacology & pharmacy Anti-inflammatory Rats Sprague-Dawley 03 medical and health sciences chemistry.chemical_compound Drug Delivery Systems 0302 clinical medicine Harmine Pharmacokinetics Drug Discovery medicine Animals Edema Humans Skin Transdermal Inflammation Antipruritic Effect Alkaloid Organic Chemistry Fibroblasts 021001 nanoscience & nanotechnology Rats Bioavailability Disease Models Animal chemistry Area Under Curve Pharmacodynamics Liposomes sense organs 0210 nano-technology
Zdroj:	Drug Development and Industrial Pharmacy. 46:101-108
ISSN:	1520-5762 0363-9045
Popis:	Harmine (HAR) is a β-carboline alkaloid with anti-inflammatory and antipruritic effect. However, the low bioavailability and side effects of HAR severely limited its clinical application. The main objective of this study was to develop harmine-loaded ethosomes (HLE) drug delivery system for topical application to treat inflammation. HLE were obtained by ethanol injection method and characterized. The morphology of HLE was evaluated by transmission electron microscopy (TEM). HLE exhibited a good biocompatibility with human embryonic skin fibroblasts and rat skin. The in vitro skin penetration studies showed that HLE had the greatest skin deposition than harmine-loaded liposomes (HLL) and harmine solution (HS). In vivo pharmacokinetic study demonstrated that AUC(0–∞) and Cmax of HLE in subcutaneous tissues were much higher than that of in blood. Moreover, for convenience of fixing on skin, HLE were mixed with gel. HLE gel significantly inhibited the overexpression of inflammation cytokines prostaglandin E2, interleuking (IL)-1β, nitric oxide, and tumor necrosis factor-alpha (TNF-α) in the inflammation model of rat paw edema compared with HS gel. In short, HLE was promising formulation for topical delivery in treatment of inflammatory diseases.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::17c90311b4e8824efda712b6436b266b https://doi.org/10.1080/03639045.2019.1706549 Zobrazit plný text záznamu Plný text ve formátu PDF Plný text ve formátu HTML
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