Nanotransfersomes of carvedilol for intranasal delivery: formulation, characterization and in vivo evaluation
Nanotransfersomes of carvedilol for intranasal delivery: formulation, characterization and in vivo evaluation
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DOI：
10.3109/10717544.2015.1013587
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发表时间：
2016-09-01
期刊：
影响因子：
6
通讯作者：
Abd Elbary, Ahmed
中科院分区：
文献类型：
--
作者：
Aboud, Heba M.;Ali, Adel Ahmed;Abd Elbary, Ahmed
目的：研制卡维地洛转移体，并评价其在兔体内的行为。方法：将Span 20、Span 60、Tween20、Tween80和脱氧胆酸钠(SDC)等不同类型的转移体按95：5%、85：15%、95：5%、85：15%三种不同比例分别与磷脂酰胆碱(PC)混合制备成囊泡75：25%w/w(PC：EA)。对转移体的形状、大小、包封率、体外释放、体外渗透、激光共聚焦扫描显微镜(CLSM)和稳定性进行了评价。结果：微囊平均直径为295~443 nm。以95：5%(w/w)(PC：EA)的比例制备的转铁体具有最高的EE%，其中Span 60的值最高。而以85：15%w/w制备的缓释剂释药百分率最高，其中SDC的释药效果优于其他EA。所开发的转移体显示出显著更高的卡维地洛通过鼻黏膜的量。含85：15%(PC：EA)(PC：EA)的SDC的T14处方的CLSM具有较高的鼻黏膜渗透性。结论：卡维地洛的鼻腔给药效率较高，绝对生物利用度为63.4%。
Context: Development of carvedilol-loaded transfersomes for intranasal administration to overcome poor nasal permeability and hepatic first pass effect so as to enhance its bioavailability.Objective: The purpose of this study was to develop carvedilol-loaded transfersomes containing different edge activators (EAs) then evaluating the in vivo behavior of the optimized formula in rabbits.Methods: The vesicles were prepared by incorporating different EAs including Span 20, Span 60, Tween 20, Tween 80, and sodium deoxycholate (SDC) in the lipid bilayer and each EA was used in three different ratios with respect to phosphatidylcholine (PC) including 95:5%, 85:15%, and 75:25% w/w (PC:EA). Evaluation of transfersomes was carried out in terms of shape, size, entrapment efficiency (EE), in vitro release, ex vivo permeation, confocal laser scanning microscopy (CLSM), and stability studies. The pharmacokinetic study of the optimized formula was conducted in rabbits.Results: The mean diameter of the vesicles was in the range of 295-443nm. Transfersomes prepared with 95:5% (w/w) (PC:EA) ratio showed highest EE% where Span 60 gave the highest values. Whereas those prepared using 85:15% w/w ratio showed highest percentages of drug release where SDC was superior to other EAs. The developed transfersomes exhibited significantly higher amounts of carvedilol permeated through nasal mucosa. CLSM of formula T14 containing SDC with 85:15% (w/w) (PC:EA) ratio revealed high permeation across the nasal mucosa.Conclusion: The nanotransfersomal vesicles were significantly more efficient in nasal delivery of carvedilol with absolute bioavailability of 63.4%.