Preparation and in vitro/in vivo Evaluation of Lacidipine by Adsorption onto Fumed Silica Using Supercritical Carbon Dioxide

• Published in: Current drug delivery Vol. 13; no. 7; p. 1053
• Main Authors: Geng, Yajie, Fu, Qiang, Guo, Bei, Li, Yun, Zhang, Xiangrong, Wang, Xianglin, Zhang, Tianhong
• Format: Journal Article
• Language: English
• Published: United Arab Emirates 01.11.2016
• Subjects: Adsorption; Animals; Antihypertensive Agents - administration & dosage; Antihypertensive Agents - blood; Antihypertensive Agents - chemistry; Antihypertensive Agents - pharmacokinetics; Biological Availability; Calcium Channel Blockers - administration & dosage; Calcium Channel Blockers - blood; Calcium Channel Blockers - chemistry; Calcium Channel Blockers - pharmacokinetics; Calorimetry, Differential Scanning; Carbon Dioxide - chemistry; Dihydropyridines - administration & dosage; Dihydropyridines - blood; Dihydropyridines - chemistry; Dihydropyridines - pharmacokinetics; Dogs; Drug Compounding; Drug Stability; Microscopy, Electron, Scanning; Powder Diffraction; Silicon Dioxide - administration & dosage; Silicon Dioxide - chemistry; Solubility; X-Ray Diffraction
• ISSN: 1875-5704
• DOI: 10.2174/1567201813666151203233232

The aim of this study was to design a silica-supported solid dispersion of lacidipine (LCDP) to enhance the dissolution rate and oral absorption using supercritical CO2 (scCO2) as a solvent. The formulation was characterized using differential scanning calorimetry, powder X-ray diffraction, scanning electron microscopy and fourier transformed infrared spectroscopy. In the dissolution test, LCDP-scCO2 formulation showed a significantly enhanced dissolution compared with LCDPsilica physical mixture and a faster dissolution rate than Lacipil® under different dissolution conditions. In an in vivo test, the area under concentration-time curve and Cmax of LCDP-scCO2 formulation was 9.23 and 23.78 fold greater than LCDP-silica physical mixture (1:15, w/w), respectively, whereas the corresponding values were 1.92 and 2.80 fold greater than Lacipil®, respectively. Our results showed that the solid dispersion prepared by supercritical fluids technology is a feasible method to enhance the oral bioavailability of LCDP.