Enhanced oral bioavailability and in vivo antioxidant activity of chlorogenic acid via liposomal formulation

详细信息    查看全文

• 作者：Yingshu Feng¹ ; Congyong Sun¹ ; Yangyang Yuan¹ ; Yuan Zhu ; Jinyi Wan ; Caleb Kesse Firempong ; Emmanuel Omari-Siaw ; Yang Xu ; Zunqin Pu ; Jiangnan Yu ; ^{yjn@ujs.edu.cn" class="auth_mail" title="E-mail the corresponding author} ; Ximing Xu ; ^{xmxu@ujs.edu.cn" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Chlorogenic acid ; Liposome ; Bioavailability ; Antioxidant activity ; Hepatoprotective
• 刊名：International Journal of Pharmaceutics
• 出版年：2016
• 出版时间：30 March 2016
• 年：2016
• 卷：501
• 期：1-2
• 页码：342-349
• 全文大小：1071 K

文摘

In the present study, a formulation system consisting of cholesterol and phosphatidyl choline was used to prepare an effective chlorogenic acid-loaded liposome (CAL) with an improved oral bioavailability and an increased antioxidant activity. The developed liposomal formulation produced regular, spherical and multilamellar-shaped distribution nanoparticles. The pharmacokinetic analysis of CAL compared with chlorogenic acid (CA), showed a higher value of C_max(6.42 ± 1.49 min versus 3.97 ± 0.39 min) and a delayed T_max(15 min versus 10 min), with 1.29-fold increase in relative oral bioavailability. The tissue distribution in mice also demonstrated that CAL predominantly accumulated in the liver which indicated hepatic targeting potential of the drug. The increased activities of antioxidant enzymes (Total Superoxide Dismutase (T-SOD) and Glutathione Peroxidase (GSH-Px)) and total antioxidant capacity (T-AOC), in addition to decreased level of malondialdehyde (MDA) in CCl₄-induced hepatotoxicity study further revealed that CAL exhibited significant hepatoprotective and antioxidant effects. Collectively, these findings present a liposomal formulation with significantly improved oral bioavailability and an increased in vivo antioxidant activity of CA.