Khaing Ei Mon, Intaraphairot Torsak, Mahadlek Jongjan, Okonogi Siriporn, Pichayakorn Wiwat, Phaechamud Thawatchai
Programme of Pharmaceutical Engineering, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand.
Department of Biopharmacy, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand.
Gels. 2022 Aug 23;8(9):526. doi: 10.3390/gels8090526.
Localized delivery systems have been typically designed to enhance drug concentration at a target site and minimize systemic drug toxicity. A rosin/cinnamon oil (CO) in situ forming gel (ISG) was developed for the sustainable delivery of imatinib mesylate (IM) against colorectal cancer cells. CO has been claimed to express a potent anticancer effect against various cancer cells, as well as a synergistic effect with IM on colorectal cancer cells; however, poor aqueous solubility limits its application. The effect of rosin with the adding CO was assessed on physicochemical properties and in vitro drug release from developed IM-loaded rosin/CO-based ISG. Moreover, in vitro cytotoxicity tests were conducted against two colorectal cancer cells. All formulations exhibited Newtonian flow behavior with viscosity less than 266.9 cP with easier injectability. The adding of CO decreased the hardness and increased the adhesive force of the obtained rosin gel. The gel formation increased over time under microscopic observation. CO-added ISG had a particle-like gel appearance, and it promoted a higher release of IM over a period of 28 days. All tested ISG formulations revealed cytotoxicity against HCT-116 and HT-29 cell lines at different incubation times. Thus, CO-loaded rosin-based ISG can act as a potentially sustainable IM delivery system for chemotherapy against colorectal cancer cells.
局部给药系统通常旨在提高靶部位的药物浓度并使全身药物毒性最小化。开发了一种用于甲磺酸伊马替尼(IM)对结肠癌细胞进行可持续给药的松香/肉桂油(CO)原位形成凝胶(ISG)。据称CO对各种癌细胞具有强大的抗癌作用,并且与IM对结肠癌细胞具有协同作用;然而,其水溶性差限制了其应用。评估了添加CO的松香对所开发的载IM的松香/CO基ISG的物理化学性质和体外药物释放的影响。此外,对两种结肠癌细胞进行了体外细胞毒性试验。所有制剂均表现出牛顿流体行为,粘度小于266.9厘泊,易于注射。添加CO降低了所得松香凝胶的硬度并增加了粘附力。在显微镜观察下,凝胶形成随时间增加。添加CO的ISG具有颗粒状凝胶外观,并且在28天内促进了IM的更高释放。所有测试的ISG制剂在不同孵育时间对HCT-116和HT-29细胞系均显示出细胞毒性。因此,载CO的松香基ISG可作为一种潜在的可持续IM给药系统用于结肠癌细胞的化疗。