Shakeel Faiyaz, Haq Nazrul, Alanazi Fars K, Alsarra Ibrahim A
a Center of Excellence in Biotechnology Research, College of Science, King Saud University , Riyadh , Saudi Arabia .
b Department of Pharmaceutics , College of Pharmacy, King Saud University , Riyadh , Saudi Arabia , and.
Pharm Dev Technol. 2016 Mar;21(2):131-9. doi: 10.3109/10837450.2014.971379. Epub 2014 Oct 16.
The aim of present investigation was to develop surface-adsorbed reverse-micelle-loaded solid self-nanoemulsifying drug delivery system (SNEDDS) of talinolol in order to enhance its in vitro dissolution rate, which in turn enhance the bioavailability. SNEDDS were prepared using aqueous phase titration method. Thermodynamically stable formulations were characterized in terms of droplet size, viscosity, % transmittance, drug content and surface morphology. Low cost acid-treated coffee husk was used as an effective biosorbent for preparation of solid SNEDDS. Developed SNEDDS were subjected to in vitro drug release/dissolution studies. In vitro drug release studies showed 99.6% release of talinolol from optimized solid SNEDDS TS3 after 120 min of study. The results of solubility studies showed 4849.5-folds enhancement in solubility of talinolol from optimized SNEDDS as compared to its aqueous solubility.
本研究的目的是开发他尼洛尔的表面吸附反胶束负载固体自纳米乳化药物递送系统(SNEDDS),以提高其体外溶出速率,进而提高生物利用度。采用水相滴定法制备SNEDDS。从粒径、粘度、透光率、药物含量和表面形态等方面对热力学稳定的制剂进行了表征。低成本的酸处理咖啡壳被用作制备固体SNEDDS的有效生物吸附剂。对所开发的SNEDDS进行体外药物释放/溶出研究。体外药物释放研究表明,在120分钟的研究后,优化后的固体SNEDDS TS3中他尼洛尔的释放率为99.6%。溶解度研究结果表明,与水溶解度相比,优化后的SNEDDS中他尼洛尔的溶解度提高了4849.5倍。