Tavano Lorena, de Cindio Bruno, Picci Nevio, Ioele Giuseppina, Muzzalupo Rita
Dipartimento di Farmacia e Scienze della Salute e della Nutrizione, Università della Calabria, Edificio Polifunzionale, 87036, Arcavacata di Rende, CS, Italy.
Biomed Microdevices. 2014 Dec;16(6):851-8. doi: 10.1007/s10544-014-9889-6.
The objective of this research was to study the effect of diclofenac sodium compartmentalization on the physico-chemical properties (such as size, drug entrapment efficiency and percutaneous permeation across rabbit skin) of niosomal vesicles used as carriers. Niosomes were prepared starting from nonionic commercial surfactants belonging to the class of Polysorbates and Pluronics: mixtures of Span 60/F127 and Tween 60/F127 at different ratios were used to obtain vesicles and all formulations were compared in terms of dimensions, morphology, polydispersity index and entrapment efficiency. Moreover, the enhancing effect of niosomes on the ex vivo percutaneous penetration of diclofenac sodium was investigated using Franz-type diffusion chambers and compared to that obtained by using the corresponding drug solution. Results demonstrated that niosomes were spherical and homogeneous in shape. Their size was found to be dependent on the hydrophile-lipophile balance of the surfactant mixture: increasing hydrophobicity resulted in smaller vesicles. Drug incorporation led to a significant variation in vesicle size dependently from the compartment in which the drug was located. The permeation of diclofenac from free solution used as control was found to be lower respect to that obtained for all niosomal formulations, that can be considered as percutaneous permeation enhancers. In particular, the results indicated that the highest cumulative amounts of diclofenac permeated across rabbit skin after 24 h were obtained by formulations in which the drug was located in the aqueous core.
本研究的目的是研究双氯芬酸钠分隔对用作载体的脂质体囊泡的物理化学性质（如大小、药物包封率和经兔皮的透皮渗透率）的影响。脂质体由属于聚山梨酯类和普朗尼克类的非离子商业表面活性剂制备：使用不同比例的司盘60/泊洛沙姆F127和吐温60/泊洛沙姆F127混合物来获得囊泡，并在尺寸、形态、多分散指数和包封率方面对所有制剂进行比较。此外，使用弗兰兹型扩散池研究了脂质体对双氯芬酸钠离体透皮渗透的增强作用，并与使用相应药物溶液获得的结果进行比较。结果表明，脂质体呈球形且形状均匀。发现它们的大小取决于表面活性剂混合物的亲水亲脂平衡：疏水性增加导致囊泡变小。药物包封导致囊泡大小因药物所在的隔室而有显著变化。用作对照的游离溶液中双氯芬酸的渗透率低于所有脂质体制剂的渗透率，这些脂质体制剂可被视为透皮渗透促进剂。特别是，结果表明，在24小时后，药物位于水相核心的制剂经兔皮渗透的双氯芬酸累积量最高。
