Nanoformulation and Evaluation of Oral Berberine-Loaded Liposomes.
Nanoformulation and Evaluation of Oral Berberine-Loaded Liposomes.
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DOI：
10.3390/molecules26092591
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发表时间：
2021-04-29
期刊：
影响因子：
--
通讯作者：
Pham TM
中科院分区：
文献类型：
--
作者：
Duong TT;Isomäki A;Paaver U;Laidmäe I;Tõnisoo A;Yen TTH;Kogermann K;Raal A;Heinämäki J;Pham TM
黄连素（BBR）是一种植物来源的水溶性较差的季铵异喹啉生物碱，在高胆固醇血症的药物治疗中具有潜在用途。为了解决与BBR口服治疗使用相关的局限性（如首过代谢和吸收不良），采用乙醇注入法和薄膜水化法制备了载有BBR的脂质体。对脂质体的大小和粒径分布、多分散指数（PDI）、固态性质、包封率（EE）以及体外药物释放进行了研究。通过乙醇注入法和薄膜水化法制备的载BBR脂质体的平均脂质体大小分别在50纳米至244纳米和111纳米至449纳米之间。脂质体的PDI值小于0.3，表明粒径分布较窄。脂质体的EE在56%至92%之间。发现水溶性较差的BBR在薄膜水化法制备的脂质体的双层磷脂膜中积累。两种纳米制备方法所制备的载BBR脂质体在体外均呈现出缓释行为。总之，乙醇注入法和薄膜水化纳米制备方法均可用于制备具有均匀粒径、高EE以及体外药物释放特性得到改善的载BBR口服脂质体。
Berberine (BBR) is a poorly water-soluble quaternary isoquinoline alkaloid of plant origin with potential uses in the drug therapy of hypercholesterolemia. To tackle the limitations associated with the oral therapeutic use of BBR (such as a first-pass metabolism and poor absorption), BBR-loaded liposomes were fabricated by ethanol-injection and thin-film hydration methods. The size and size distribution, polydispersity index (PDI), solid-state properties, entrapment efficiency (EE) and in vitro drug release of liposomes were investigated. The BBR-loaded liposomes prepared by ethanol-injection and thin-film hydration methods presented an average liposome size ranging from 50 nm to 244 nm and from 111 nm to 449 nm, respectively. The PDI values for the liposomes were less than 0.3, suggesting a narrow size distribution. The EE of liposomes ranged from 56% to 92%. Poorly water-soluble BBR was found to accumulate in the bi-layered phospholipid membrane of the liposomes prepared by the thin-film hydration method. The BBR-loaded liposomes generated by both nanofabrication methods presented extended drug release behavior in vitro. In conclusion, both ethanol-injection and thin-film hydration nanofabrication methods are feasible for generating BBR-loaded oral liposomes with a uniform size, high EE and modified drug release behavior in vitro.
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影响因子：
8
作者：
Guan, Peipei;Lu, Yi;Wu, Wei
通讯作者：
Wu, Wei
影响因子：
10.2
作者：
Luo, Xiang;Li, Jing;Deng, Yihui
通讯作者：
Deng, Yihui
影响因子：
10.8
作者：
Quinn, Peter J.
通讯作者：
Quinn, Peter J.
影响因子：
--
作者：
Akbarzadeh A;Rezaei-Sadabady R;Davaran S;Joo SW;Zarghami N;Hanifehpour Y;Samiei M;Kouhi M;Nejati-Koshki K
通讯作者：
Nejati-Koshki K
影响因子：
5.6
作者：
BANGHAM, AD;STANDISH, MM;WATKINS, JC
通讯作者：
WATKINS, JC