Researchers have made notable strides in improving the solubility of mesalazine, a drug widely used to treat inflammatory bowel diseases, by analyzing its behavior in supercritical carbon dioxide (scCO2). Conducted at Tabriz University of Medical Sciences, this study is groundbreaking as it marks the first time the solubility of mesalazine has been investigated under these unique conditions.
The research team studied mesalazine's solubility at various temperatures ranging from 308 K to 338 K and pressures between 12 and 30 MPa, aiming to address challenges related to poor drug solubility—a common impediment to effective treatment. By employing scCO2, known for its low toxicity and distinctive properties, they reported findings showing how the addition of dimethyl sulfoxide (DMSO) as a cosolvent significantly enhances solubility.
Experimental results indicated molar solubility values of mesalazine without DMSO varied considerably, ranging from 4.41 × 10–5 to 9.97 × 10–5 under the lowest temperature conditions, to as high as 18.4 × 10–5 at 338 K. Conversely, using 2% DMSO as a cosolvent raised its solubility dramatically, with measurements reaching from 28.22 × 10–5 to as high as 82.6 × 10–5 across the temperature spectrum assessed.
What’s more, researchers reported the new association model they developed along with existing semiempirical models effectively predicted these solubility behaviors. Remarkably, the novel model achieved average absolute relative deviations of just 4.13% without DMSO and 3.36% with the cosolvent—a significant improvement over existing predictive models.
“The determined experimental molar solubilities of mesalazine were significantly increased when 2% DMSO was utilized as cosolvent, demonstrating the potential of using scCO2 for pharmaceutical applications,” stated the authors.
Historically, drug particle solubility and the ensuing absorption have been streamlined through methods such as spray drying and milling, but these conventional techniques carry risks of altering drug composition due to thermal and mechanical stress. The study advocates for supercritical fluid technology as a more innovative and effective method, leveraging scCO2’s ability to dissolve certain solutes more efficiently than traditional solvents.
The corollary effects of pressure on solubility denote intriguing potential for pharmaceutical purposes. The analysis indicated increased pressure led to enhanced solubility—underlying principles linked to the rise of density within the supercritical solution. The research tied these observations back to previous studies affirming the association, enhancing the reliability of their findings.
Through rigorous experimentation and application of advanced modeling strategies, researchers unveiled the strong capability of scCO2 systems blended with cosolvents to potentially revolutionize the micronization processes for mesalazine, yielding micro and nanoparticles with remarkable performance.
The cumulative insights from this research suggest promising future avenues for optimizing drug delivery mechanisms not only for mesalazine but potentially for various other pharmaceuticals constrained by low solubility. “The new association model outperformed other semiempirical correlations, achieving lower average absolute relative deviations, which reflects the accuracy of our predictions,” the team concluded. The results reaffirm the advantageous prospects of supercritical carbon dioxide technology, urging for its wider adoption within the pharmaceutical field.