Proliposomes for oral delivery of total biflavonoids extract from Selaginella doederleinii: formulation development, optimization, and in vitro–in vivo characterization
| Autor: | Chen, Bing, Wang, Xuewen, Lin, Dan, Xu, Dafen, Li, Shaoguang, Huang, Jianyong, Weng, Shaohuang, Lin, Zhen, Zheng, Yanjie, Yao, Hong, Lin, Xinhua |
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| Jazyk: | angličtina |
| Rok vydání: | 2019 |
| Předmět: |
Male
Selaginellaceae Mice Inbred BALB C Plant Extracts sodium deoxycholate Selaginella doederleinii Administration Oral Biological Availability Oligosaccharides Antineoplastic Agents Phytogenic Xenograft Model Antitumor Assays Bile Acids and Salts Rats Sprague-Dawley Mice oral bioavailability Solubility Liposomes Animals Biflavonoids Humans HT29 Cells proliposomes Original Research antitumor |
| Zdroj: | International Journal of Nanomedicine |
| ISSN: | 1178-2013 1176-9114 |
| Popis: | Purpose Amentoflavone, robustaflavone, 2’’,3’’-dihydro-3’,3’’’-biapigenin, 3’,3’’’-binaringenin and delicaflavone are five major active ingredients in the total biflavonoids extract from Selaginella doederleinii (TBESD) with favorable anticancer properties. However, the natural-derived potent antitumor agent of TBESD is undesirable due to its poor solubility. The present study was to develop and optimize a proliposomal formulation of TBESD (P-TBESD) to improve its solubility, oral bioavailability and efficacy. Materials and methods P-TBESD containing a bile salt, a protective hydrophilic isomalto-oligosaccharides (IMOs) coating, were successfully prepared by thin film dispersion-sonication method. The physicochemical and pharmacokinetic properties of P-TBESD were characterized, and the antitumor effect was evaluated using the HT-29 xenograft-bearing mice models in rats. Results Compared with TBESD, the relative bioavailability of amentoflavone, robustaflavone, 2’’,3’’-dihydro-3’,3’’’-biapigenin, 3’,3’’’-binaringenin and delicaflavone from P-TBESD were 669%, 523%, 761%, 955% and 191%, respectively. The results of pharmacodynamics demonstrated that both TBESD and P-TBESD groups afforded antitumor effect without systemic toxicity, and the antitumor effect of P-TBESD was significantly superior to that of raw TBESD, based on the tumor growth inhibition and histopathological examination. Conclusion Hence, IMOs-modified proliposomes have promising potential for TBESD solving the problem of its poor solubility and oral bioavailability, which can serve as a practical oral preparation for TBESD in the future cancer therapy. |
| Databáze: | OpenAIRE |
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