Details

Autor(en) / Beteiligte

• Qian, Jin
• Meng, Houjun
• Xin, Lei
• Xia, Mengxin
• Shen, Hongyi
• Li, Guowen
• Xie, Yan

Titel

Self-nanoemulsifying drug delivery systems of myricetin: Formulation development, characterization, and in vitro and in vivo evaluation

Ist Teil von

• Colloids and surfaces, B, Biointerfaces, 2017-12, Vol.160, p.101-109

Ort / Verlag

Netherlands: Elsevier B.V

Erscheinungsjahr

2017

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• [Display omitted] •Four Myr-SNEDDS with different characteristics were successfully prepared and evaluated.•The components and ratios of each component had influence on the properties of each SNEDDS formulation.•Myr-SNEDDS can improve the solubility and permeability of Myr.•The SNEDDS can improve the bioavailability of insoluble herbal drugs like Myr. Despite various pharmacological effects, myricetin (Myr) shows low oral bioavailability (<10%) due to its poor solubility, which limits its applications. To address this problem, self-nanoemulsifying drug delivery systems (SNEDDS) were developed by investigating the solubility of Myr in various excipients, constructing pseudo-ternary phase diagrams, and optimizing based on droplet size and emulsification efficacy after drug loading. The obtained Myr-SNEDDS were F04 (Capryol 90/Cremophor RH 40/PEG 400 4:3:3), F08 (Capryol 90/CremophorRH40/1,2-propanediol 4:3:3), F13 (Capryol 90/Cremophor EL/Transcutol HP 4:3:3) and F15 (Capryol 90/Cremephor RH 40/Transcutol HP 2:7:1), with droplet sizes less than 200nm. Additional evaluations showed that these Myr-SNEDDS formulations had fast release properties (over 90% in 1min), low cytotoxicity, and improved permeability and solubility compared with the free drug. Consequently, the oral bioavailabilities of Myr were 5.13, 6.33, 4.69 and 2.53-fold for F04, F08, F13 and F15, respectively, relative to Myr alone. The present study demonstrated that SNEDDS is a viable platform for the oral delivery of insoluble drugs such as Myr.