Solubility of Dexamethasone in Supercritical Carbon Dioxide

Abstract

Dexamethasone (DXMT) is a glucocorticoid that belongs to an important class of synthetic steroid hormones with potential to treat chronic immune and inflammatory diseases. In this work, the solid solubility of dexamethasone in supercritical carbon dioxide (scCO2) was measured using a static method. Experimental data were measured at (308.2, 318.2, and 328.2) K in the pressure range from (15.1 to 35.7) MPa. The solubility in scCO2 was found to be low and between (1.25·10–6 or 9.1·10–3) kg·m–3 (at 308.2 K and 15.1 MPa) and (2.81·10–6 or 22.0·10–3) kg·m–3 (at 328.2 K and 34.8 MPa) in terms of mole fraction or mass of drug per volume of solvent, respectively. Experimental data were correlated using semiempirical density based models (Méndez-Santiago–Teja, Bartle, and Chrastil). Obtained average absolute relative deviation [AARD (%)] values were lower than 13 %.

Solubility of Dexamethasone in Supercritical Carbon Dioxide with and without a Cosolvent

“…The solubility of Dex in pure SC-CO 2 is in the range of 1.19·10 −6 to 1.52·10 −6 , and the minimum and maximum solubility data were measured at 323.2 K, 10 MPa and 323.2 K, 25 MPa, respectively. Compared with Dex solubility data at Figure 2, three isothermal curves intersected each other at the pressure region around (14.0 to 16.0) MPa, and this phenomenon was also pointed out by Chim et al 18 As expected, the Dex solubility increased with the elevation of pressure for each isotherm. Generally, the increase of pressure leads to the increase of the density of SC-CO 2 which is beneficial to the interactions between the molecules of solute and solvent.…”

“…Solubility of Dex in Pure SC-CO 2 . The experimental solubility data in pure SC-CO 2 are presented in Table 2 and Figure 2, and the solubility of Dex in SC-CO 2 from the literature 18 is also illustrated in Figure 2 for a reference. As shown in Table 2, the solubility of Dex obtained in this work is low.…”

Dexamethasone-loaded poly(ɛ-caprolactone)/silica nanoparticles composites prepared by supercritical CO2 foaming/mixing and deposition

“…The DXMT solubility in scCO 2 at 35 • C was found to be low and not dependent on pressure: 9.07 × 10 −2 g cm −3 at 15 MPa, and 10.14 × 10 −2 g cm −3 at 25 MPa (Chim et al, 2012). Therefore, the loading yield should be mostly controlled by the balance between the DXMT/scCO 2 interactions (hydrophobic methyl/CO 2 and Lewis basic-type carbonyl/CO 2 ) (Kazarian, 2000;Kikic, 2009;Kikic and Vecchione, 2003) and the DXMT/SNPs specific interactions (hydrogen bonds between the silanol moieties of silica and the hydroxyl groups of the DXMT molecule), which determines the final DXMT "solubility" and partitioning into SNPs.…”

“…SNPs (16 mg) were placed inside four sealed dialysis membranes which were introduced in a high pressure cell placed in a temperaturecontrolled water bath. The cell was loaded with 9 mg of DXMT (i.e., an amount 8-9 times greater than that needed to saturate scCO 2 under the operational conditions (Chim et al, 2012)) and CO 2 was then introduced. Experiments were performed under magnetic stirring (700 rpm) at 35 • C and at 14.0 MPa or 25.0 MPa (which corresponds to scCO 2 densities of 0.801 g cm −3 and 0.901 g cm −3 , respectively) (NIST, 2013).…”

Solubility of cefuroxime axetil in supercritical CO2: Measurement and modeling

“…Generally, the solubility of antibiotics or of anti-inflammatory drugs in CO 2 is very low. Indeed, it is the case of nimesulide [4][5][6], gatifloxacin [7], penicillin G [8], penicillin V [9], cefixime trihydrate [10], dexamethasone [11], azithromycin [12], erythromycin [12], clindamycin [12] and clarithromycin [12]. The values of their solubility vary between 10 −7 and 10 −5 (in mole fraction).…”