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Pharmaceutical and Biomedical Sciences Journal (PBSJ)Pharmaceutical and Biomedical Sciences Journal (PBSJ)

Aceclofenac is a non-steroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX) and suppresses prostaglandin synthesis. Its clinical utility, however, is limited by poor aqueous solubility and low bioavailability. This study evaluates the anti-inflammatory activity of a multicomponent crystal (MC) of aceclofenac with saccharin using a carrageenan-induced granuloma pouch model in mice. Male mice were divided into three groups (n = 3 per group): control, aceclofenac, and aceclofenac-saccharin multicomponent crystal, administered intraperitoneally. Inflammatory response was assessed via exudate volume and TNF-α levels. Both aceclofenac and MC significantly reduced exudate volume and TNF-α compared to the control (p < 0.05), with the MC group showing the greatest reduction. Although not statistically different from aceclofenac in TNF-α suppression, the MC demonstrated superior performance overall. The enhanced efficacy may be attributed to improved solubility and drug delivery. These outcomes support co-crystallization as a promising approach to optimize NSAID therapy.

The study concludes that the multicomponent crystal (MC) of aceclofenac with saccharin exhibits enhanced anti-inflammatory activity compared to the parent drug.This was demonstrated by greater reductions in both exudate volume and TNF-α levels in a carrageenan-induced granuloma pouch model in mice.The improvements are likely due to enhanced solubility and drug release characteristics conferred by the co-crystal structure, supporting co-crystallization as an effective strategy for optimizing NSAID therapy.

Penelitian lebih lanjut perlu dilakukan untuk mengeksplorasi mekanisme molekuler yang mendasari peningkatan efikasi anti-inflamasi dari kristal multikomponen aceclofenac-saccharin, termasuk studi tentang interaksi obat-pembawa dan efeknya pada permeabilitas membran sel. Selain itu, studi in vivo yang lebih komprehensif dengan model hewan yang berbeda dan durasi yang lebih panjang diperlukan untuk mengevaluasi potensi jangka panjang dan profil keamanan dari formulasi ini. Terakhir, penelitian dapat difokuskan pada pengembangan formulasi kristal multikomponen aceclofenac-saccharin yang ditargetkan, seperti sistem pengiriman nano, untuk meningkatkan bioavailabilitas dan efikasi terapeutik, serta mengurangi potensi efek samping gastrointestinal yang terkait dengan penggunaan NSAID konvensional.

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