Nanoemulsion-based delivery system for enhanced oral bioavailability and Caco-2 cell monolayers permeability of berberine hydrochloride
| Autor: | De-Hua Liao, Xiong-Bin Hu, Tian-Tian Tang, Yong-Jiang Li, Da-Xiong Xiang, Xiu-Ling Lu, Jun-Yong Wu |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
Berberine
nanoemulsion Administration Oral Biological Availability Pharmaceutical Science RM1-950 02 engineering and technology Permeability Glycerides Polyethylene Glycols Berberine hydrochloride Surface-Active Agents 03 medical and health sciences Drug Delivery Systems 0302 clinical medicine Pulmonary surfactant Cell Line Tumor medicine Humans Intestinal permeability Chromatography Chemistry Aqueous two-phase system Water General Medicine 021001 nanoscience & nanotechnology medicine.disease Antimicrobial Bioavailability Intestinal Absorption Solubility Caco-2 Permeability (electromagnetism) 030220 oncology & carcinogenesis transport Nanoparticles Emulsions Therapeutics. Pharmacology Efflux Caco-2 Cells bioavailability 0210 nano-technology Research Article |
| Zdroj: | Drug Delivery article-version (VoR) Version of Record Drug Delivery, Vol 24, Iss 1, Pp 1868-1873 (2017) |
| ISSN: | 1521-0464 1071-7544 |
| DOI: | 10.1080/10717544.2017.1410257 |
| Popis: | Berberine hydrochloride (BBH) has a variety of pharmacological activities such as antitumor, antimicrobial, anti-inflammation, and reduce irritable bowel syndrome. However, poor stability and low oral bioavailability limited its usage. Herein, an oil-in-water nanoemulsion system of BBH was developed to improve its stability and oral bioavailability. The pseudoternary phase diagrams were constructed for the determination of composition of various nanoemulsions. The nanoemulsions of BBH composed of Labrafil M 1944 CS (oil phase), RH-40 (surfactant), glycerin (co-surfactant), and water (aqueous phase). The O/W nanoemulsion of BBH showed a relative bioavailability of 440.40% compared with unencapsulated BBH and was stable in our 6-month stability study. Further, there was a significant increase in intestinal permeability of BBH as assessed by Caco-2 cell monolayers and a significant reduction in efflux of BBH by the multidrug efflux pump P-glycoprotein. This study confirmed that the nanoemulsion formulation could be used as an alternative oral formulation of BBH to improve its stability, oral bioavailability and permeability. |
| Databáze: | OpenAIRE |
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