Comparative study between high-pressure homogenisation and Shirasu porous glass membrane technique in sildenafil base-loaded solid SNEDDS: Effects on physicochemical properties and in vivo characteristics.
The purpose of this study was to compare two types of emulsification techniques in a solid self-nanoemulsifying drug delivery system (SNEDDS); high-pressure homogenisation (HPH) and Shirasu porous glass membrane (SPG). Those two emulsification processes enhanced the solubility, dissolution and oral bioavailability of poorly water-soluble sildenafil base (SB) by producing fine and well-dispersed nanoemulsion droplet. The liquid SNEDDS consisting of Labrasol/Transcutol HP/coconut oil at the weight of 72/18/10, gave the smallest emulsion droplet size among the prepared liquid SNEDDS formulations. Then, the SB-loaded liquid SNEDDS was dissolved in the deionised water and applied to HPH or SPG techniques. Aerosil 200 was suspended as a mesoporous carrier and spray-dried, producing an SB-loaded solid SNEDDS. The emulsion droplet size, solubility and dissolution of each emulsification process were compared to the solid SNEDDS fabricated without any treatment of additional emulsification. Moreover, the physicochemical properties of all formulations were compared. The crystalline state of the drug in all products was converted to the amorphous state. The solid SNEDDS, subjected to HPH technique, provided fine and well-dispersed nanoemulsion. Additionally, it increasingly improved the drug solubility and dissolution as compared to the others, including SB powder, non-treated (NT) and SPG. Furthermore, it gave improved Cmax and increased AUC compared to SB powder and SPG, indicating HPH enhanced the oral bioavailability of SB the most. Thus, this solid SNEDDS with HPH would be strongly suggested as an oral SB-loaded pharmaceutical product.
['Kim|Jung Suk|JS|', 'Ud Din|Fakhar|F|', 'Lee|Sang Min|SM|', 'Kim|Dong Shik|DS|', 'Choi|Yoo Jin|YJ|', 'Woo|Mi Ran|MR|', 'Kim|Jong Oh|JO|', 'Youn|Yu Seok|YS|', 'Jin|Sung Giu|SG|', 'Choi|Han-Gon|HG|']
D000284:Administration, Oral D001682:Biological Availability D016503:Drug Delivery Systems D004655:Emulsions D053758:Nanoparticles D010316:Particle Size D016062:Porosity D000068677:Sildenafil Citrate D012995:Solubility D013501:Surface-Active Agents
High-pressure homogenisation Shirasu porous glass membrane Solid self-nanoemulsifying drug delivery system Sildenafil base Nanoemulsion In vitro dissolution Pharmacokinetics in rats