Taymouri Somayeh, Varshosaz Jaleh
Department of Pharmaceutics, School of Pharmacy and Novel Drug Delivery Systems Research Centre, Isfahan University of Medical Sciences, Isfahan, Iran.
Adv Biomed Res. 2016 Mar 16;5:48. doi: 10.4103/2277-9175.178781. eCollection 2016.
Niosomes are non-ionic surfactant vesicles used as drug carriers for encapsulating both hydrophobic and hydrophilic drugs. The aim of this study is to evaluate the effect of different surfactants on the physical properties and stability of carvedilol niosomes designed to improve oral bioavailability.
Different niosomal formulations were prepared using a film hydration method, with various mixtures of different non-ionic surfactants including Span 20, 40, and 60, and also Tween 20, 40, and 60, along with cholesterol. The physicochemical characteristics of the formulations were evaluated in vitro.
The drug encapsulation efficiency was reduced by using lauryl (C12) chain containing surfactants, that is, Span/Tween. Cholesterol content and drug entrapment were the main factors affecting the mean particle size of the niosomes. The drug release profiles from most of the formulations were fitted well with the Baker-Lonsdale model, indicating a diffusion-based drug release mechanism. Niosomes prepared from 50 and 40% of the cholesterol with 25 or 30% of Span/Tween 60 showed the highest stability due to their high transition temperature and solid state feature of these surfactants.
From the results obtained, it may be concluded that nanoniosomes are promising stable carriers for the oral delivery of carvedilol.
非离子表面活性剂囊泡用作药物载体，可包封疏水性和亲水性药物。本研究的目的是评估不同表面活性剂对旨在提高口服生物利用度的卡维地洛脂质体物理性质和稳定性的影响。
采用薄膜水化法制备不同的脂质体制剂，使用不同非离子表面活性剂的各种混合物，包括司盘20、40和60，以及吐温20、40和60，还有胆固醇。对制剂的理化特性进行体外评估。
使用含月桂基（C12）链的表面活性剂（即司盘/吐温）会降低药物包封效率。胆固醇含量和药物包封率是影响脂质体平均粒径的主要因素。大多数制剂的药物释放曲线与贝克-朗斯代尔模型拟合良好，表明药物释放机制基于扩散。由50%和40%的胆固醇与25%或30%的司盘/吐温60制备的脂质体由于其高转变温度和这些表面活性剂的固态特性而表现出最高的稳定性。
从所得结果可以得出结论，纳米脂质体是卡维地洛口服给药有前景的稳定载体。
