El-Badry Mahmoud, Haq Nazrul, Fetih Gihan, Shakeel Faiyaz
Department of Pharmaceutics, College of Pharmacy, King Saud University.
J Oleo Sci. 2014;63(6):567-76. doi: 10.5650/jos.ess13236. Epub 2014 Apr 25.
The aim of this study was to develop and evaluate self-nanoemulsifying drug delivery system (SNEDDS) of tadalafil (TDL) in order to enhance its aqueous solubility and dissolution rate. TDL SNEDDS were developed by aqueous phase titration method via construction of pseudo-ternary phase diagrams. The formulations which passed thermodynamic stability and self-nanoemulsification tests were further characterized in terms of droplet size, viscosity, % transmittance and drug content. Selected SNEDDS and drug suspension were subjected to in vitro drug release studies via dialysis membrane in phosphate buffer (pH 6.8). In vitro drug release studies showed 96.6% release of TDL from optimized SNEDDS F5 as compared to only 12.4% from drug suspension after 24 h of study. The results of solubility studies showed 1434 folds enhancement in TDL solubility from optimized SNEDDS F5 as compared to its aqueous solubility. Overall, these results indicated that developed SNEDDS could be successfully used to enhance solubility and dissolution rate of poorly soluble drugs such as TDL.
本研究的目的是开发并评估他达拉非（TDL）的自纳米乳化药物递送系统（SNEDDS），以提高其水溶性和溶解速率。通过构建伪三元相图，采用水相滴定法制备了TDL SNEDDS。对通过热力学稳定性和自纳米乳化测试的制剂，进一步在粒径、粘度、透光率和药物含量方面进行了表征。选用的SNEDDS和药物混悬液通过透析膜在磷酸盐缓冲液（pH 6.8）中进行体外药物释放研究。体外药物释放研究表明，在研究24小时后，优化后的SNEDDS F5中TDL的释放率为96.6%，而药物混悬液中的释放率仅为12.4%。溶解度研究结果表明，与TDL的水溶性相比，优化后的SNEDDS F5使TDL的溶解度提高了1434倍。总体而言，这些结果表明，所开发的SNEDDS可成功用于提高难溶性药物（如TDL）的溶解度和溶解速率。
