Work

Multicomponent Crystal of Aceclofenac with Saccharin to Improve Solubility and Dissolution Rate

Year: 2025

Type: article

Abstract: Aceclofenac is a Non-Steroidal Anti-Inflammatory Drug (NSAID) frequently prescribed for managing osteoarthritis and rheumatoid arthritis. It is categorized under the Biopharmaceutics Classification System (BCS) as a Class II compound, characterized by low water solubility but high membrane permeability. This poor solubility presents challenges in dissolution and absorption in gastrointestinal fluid. The objective of this study was to improve the solubility and dissolution behavior of aceclofenac by formulating a multicomponent crystal with saccharin as the selected coformer. The multicomponent crystal was prepared through a solvent-drop grinding technique using a 1:1 molar ratio. To confirm the formation and evaluate the physicochemical properties of the multicomponent system, solid-state characterization was performed using differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and Fourier-transform infrared spectroscopy (FTIR). Additionally, solubility and in vitro dissolution tests were carried out and compared with those of the unmodified drug. Results from DSC and PXRD demonstrated a substantial decrease in crystallinity, evident by the loss of distinct melting peaks and diffraction signals, indicative of eutectic formation. This structural alteration is associated with a reduction in lattice energy, which contributes to enhanced dissolution. FTIR spectra verified the absence of covalent interactions between the drug and coformer. The optimized multicomponent crystal exhibited a 2.49-fold increase in solubility and a 2.6-fold enhancement in dissolution rate relative to pure aceclofenac. Overall, this study supports the use of multicomponent crystal engineering with saccharin as a feasible approach to improve the biopharmaceutical performance of aceclofenac.

Source: International Journal of Drug Delivery Technology

DOI: 10.25258/ijddt.15.2.32

Authors: Hendrizal Usman, Yufri Aldi, Salman Umar, Muhammad Nasrul Siregar, Erizal Zaini

Institution: Andalas University

Language: English

Topic: Drug Solubulity and Delivery Systems

Subfield: Pharmaceutical Science

Field: Pharmacology, Toxicology and Pharmaceutics

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: bronze

Funder: Universitas Andalas