Sama Hamzehlou, Elaheh Rahimpour, Anahita Fathi Azarbayjani, Abolghasem Jouyban
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Development of high-solubility amorphous sulfasalazine: effect of hydrogen bonding.
Introduction: Sulphasalazine (Sulf) is a class IV compound with low aqueous solubility and low permeability which limit its therapeutic activity. This work aims to apply choline chloride (CC) and choline hydroxide (CH) as a hydrogen bond acceptor with Sulf for the production of Sulf salt.
Materials and method: New compounds were prepared and characterized by XRD, DSC, and FT-IR. Drug solubility was evaluated in different media including pure water, and buffer pH 1.2, 4.5, and 6.8 were evaluated.
Results: The diffractogram pattern of the Sulf-CH shows a smooth and low-intensity diffraction which may indicate amorphization of the drug molecule. The FT-IR spectra confirm participation of the carboxyl group of Sulf in the formation of hydrogen bonding between Sulf and CH through salt formation which helps to enhance drug solubility. Solubility of Sulf-CH significantly increased up to 10,000-folds in pure water. Sulf-CC caused up to 2-folds enhancement in drug solubility.
Conclusion: The difference in the solubility of Sulf-CC and Sulf-CH may suggest that each of these compounds involve different intermolecular interactions which were also confirmed by FT-IR, XRD, and DSC results. This effect can influence drug bioavailability and enhance its therapeutic efficacy.
期刊介绍：
Delivering therapeutics in a way that is right for the patient - safe, painless, reliable, targeted, efficient and cost effective - is the fundamental aim of scientists working in this area. Correspondingly, this evolving field has already yielded a diversity of delivery methods, including injectors, controlled release formulations, drug eluting implants and transdermal patches. Rapid technological advances and the desire to improve the efficacy and safety profile of existing medications by specific targeting to the site of action, combined with the drive to improve patient compliance, continue to fuel rapid research progress. Furthermore, the emergence of cell-based therapeutics and biopharmaceuticals such as proteins, peptides and nucleotides presents scientists with new and exciting challenges for the application of therapeutic delivery science and technology. Successful delivery strategies increasingly rely upon collaboration across a diversity of fields, including biology, chemistry, pharmacology, nanotechnology, physiology, materials science and engineering. Therapeutic Delivery recognizes the importance of this diverse research platform and encourages the publication of articles that reflect the highly interdisciplinary nature of the field. In a highly competitive industry, Therapeutic Delivery provides the busy researcher with a forum for the rapid publication of original research and critical reviews of all the latest relevant and significant developments, and focuses on how the technological, pharmacological, clinical and physiological aspects come together to successfully deliver modern therapeutics to patients. The journal delivers this essential information in concise, at-a-glance article formats that are readily accessible to the full spectrum of therapeutic delivery researchers.
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