Our research aimed to enhance the oral bioavailability of doxorubicin hydrochloride (DOX·HCl) while minimizing the potential for myocardial toxicity. To achieve this goal, we developed a new method that utilizes a coating material to encapsulate the drug in liposomes, which can specifically target intestinal taurine transporter proteins. This coating material, TAU-CS, was created by combining taurine with chitosan. We characterized TAU-CS using various methods, including ¹H NMR, FT-IR, and scanning electron microscopy (SEM). The resulting liposomes exhibited a regular spherical morphology, with a particle size of 195.7 nm, an encapsulation efficiency of 91.23 %, and a zeta potential of +11.65 mV. Under simulated gastrointestinal conditions, TAU-CS/LIP@DOX·HCl exhibited good stability and slow release. Pharmacokinetic studies revealed that, compared with DOX·HCl, TAU-CS/LIP@DOX·HCl had a relative bioavailability of 342 %. Intracellular uptake, immunofluorescence imaging, and permeation assays confirmed that the taurine transporter protein mediates the intestinal uptake of these liposomes. Our study suggested that liposomes coated with TAU-CS could serve as an effective oral delivery system and that targeting the taurine transporter protein shows promise in enhancing drug absorption.

我们的研究旨在提高盐酸阿霉素（DOX·HCl）的口服生物利用度，同时最大限度地减少心肌毒性的可能性。为了实现这一目标，我们开发了一种新方法，利用涂层材料将药物封装在脂质体中，该脂质体可以特异性靶向肠道牛磺酸转运蛋白。这种涂层材料 TAU-CS 是通过将牛磺酸与壳聚糖结合而制成的。我们使用各种方法对 TAU-CS 进行了表征，包括¹ H NMR、FT-IR 和扫描电子显微镜 (SEM)。所得脂质体呈规则球形，粒径为195.7 nm，包封率为91.23%，zeta电位为+11.65 mV。在模拟胃肠道条件下，TAU-CS/LIP@DOX·HCl表现出良好的稳定性和缓慢的释放。药代动力学研究表明，与DOX·HCl相比，TAU-CS/LIP@DOX·HCl的相对生物利用度为342%。细胞内摄取、免疫荧光成像和渗透测定证实牛磺酸转运蛋白介导这些脂质体的肠道摄取。我们的研究表明，涂有 TAU-CS 的脂质体可以作为有效的口服递送系统，并且靶向牛磺酸转运蛋白有望增强药物吸收。