Bayan Mohammad F, Marji Saeed M, Salem Mutaz S, Begum M Yasmin, Chidambaram Kumarappan, Chandrasekaran Balakumar
Faculty of Pharmacy, Philadelphia University, P.O. Box 1, Amman 19392, Jordan.
Faculty of Pharmacy, Jordan University of Science and Technology, P.O. Box 3030, Irbid 22110, Jordan.
Polymers (Basel). 2022 Sep 5;14(17):3697. doi: 10.3390/polym14173697.
Conventional oral formulations are mainly absorbed in the small intestine. This limits their use in the treatment of some diseases associated with the colon, where the drug has to act topically at the inflammation site. This paved the way for the development of a smart colonic drug delivery system, thereby improving the therapeutic efficacy, reducing the dosing frequency and potential side effects, as well as improving patient acceptance, especially in cases where enemas or other topical preparations may not be effective alone in treating the inflammation. In healthy individuals, it takes an oral medication delivery system about 5 to 6 h to reach the colon. A colonic drug delivery system should delay or prohibit the medication release during these five to six hours while permitting its release afterward. The main aim of this study was to develop a smart drug delivery system based on pH-sensitive polymeric formulations, synthesized by a free-radical bulk polymerization method, using different monomer and crosslinker concentrations. The formulations were loaded with 5-amino salicylic acid as a model drug and Capmul MCM C8 as a bioavailability enhancer. The glass transition temperature (Tg), tensile strength, Young's modulus, and tensile elongation at break were all measured as a part of the dried films' characterization. In vitro swelling and release studies were performed to assess the behavior of the produced formulations. The in vitro swelling and release evaluation demonstrated the potential ability of the developed system to retard the drug release at conditions mimicking the stomach and small intestine while triggering its release at conditions mimicking the colon, which indicates its promising applicability as a potential smart colonic drug delivery system.
传统口服制剂主要在小肠吸收。这限制了它们在治疗某些与结肠相关疾病中的应用，因为药物必须在炎症部位局部起作用。这为智能结肠给药系统的开发铺平了道路，从而提高了治疗效果，降低了给药频率和潜在副作用，同时提高了患者的接受度，特别是在灌肠剂或其他局部制剂单独治疗炎症可能无效的情况下。在健康个体中，口服药物递送系统大约需要5到6小时才能到达结肠。结肠给药系统应在这五到六个小时内延迟或阻止药物释放，同时允许其在之后释放。本研究的主要目的是开发一种基于pH敏感聚合物制剂的智能给药系统，该制剂通过自由基本体聚合法合成，使用不同的单体和交联剂浓度。制剂中负载了5-氨基水杨酸作为模型药物和Capmul MCM C8作为生物利用度增强剂。作为干燥膜表征的一部分，测量了玻璃化转变温度（Tg）、拉伸强度、杨氏模量和断裂伸长率。进行了体外溶胀和释放研究，以评估所制备制剂的行为。体外溶胀和释放评估表明，所开发的系统具有在模拟胃和小肠的条件下延迟药物释放，同时在模拟结肠的条件下触发药物释放的潜在能力，这表明其作为潜在的智能结肠给药系统具有广阔的应用前景。
