Department of Drugs and Medicines, School of Pharmaceutical Sciences, São Paulo State University (UNESP), Araraquara, Brazil.
Curr Med Chem. 2023;30(12):1351-1367. doi: 10.2174/0929867329666220707102912.
The anti-inflammatory 5-aminosalicylic acid (5-ASA) is the main therapeutic option used to prevent and treat inflammatory bowel diseases. The upper intestinal tract performs rapid and almost complete absorption of this drug when administered orally, making local therapeutic levels of the molecule in the inflamed colonic mucosa difficult to achieve. Micro and nanoparticle systems are promising for 5-ASA incorporation because the reduced dimensions of these structures can improve the drug's pharmacodynamics and contribute to more efficient and localized therapy. Together, the association of these systems with polymers will allow the release of 5-ASA through specific targeting mechanisms to the colon, as demonstrated in the mesalazine modified-release dosage form. This review will summarize and discuss the challenges for the oral administration of 5-ASA and the different colon-specific delivery strategies using polymers.
抗炎药 5-氨基水杨酸(5-ASA)是预防和治疗炎症性肠病的主要治疗选择。当口服给药时,上消化道对该药物进行快速且几乎完全吸收,使得在发炎的结肠黏膜中难以达到分子的局部治疗水平。微纳米颗粒系统是 5-ASA 掺入的有前途的方法,因为这些结构的减小尺寸可以改善药物的药效学,并有助于更有效和更局部的治疗。这些系统与聚合物的结合将允许通过特定的靶向机制将 5-ASA 释放到结肠中,正如在美沙拉嗪控释剂型中所证明的那样。这篇综述将总结和讨论 5-ASA 的口服给药以及使用聚合物的不同结肠特异性传递策略所面临的挑战。