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Photoactive Liposomal Formulation of PVP-Conjugated Chlorin e6 for Photodynamic Reduction of Atherosclerotic Plaque

机译:PVP缀合氯e6的光活性脂质体制物,用于牙动粥样硬化斑块的光动力学减少

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摘要

Background: Liposomes serve as delivery systems for biologically active compounds. Existing technologies inefficiently encapsulate large hydrophilic macromolecules, such as PVP-conjugated chlorin e6 (Photolon). This photoactive drug has been widely tested for therapeutic applications, including photodynamic reduction of atherosclerotic plaque. Methods: A novel formulation of Photolon was produced using “gel hydration technology”. Its pharmacokinetics was tested in Sus scrofa f. domestica. Its cellular uptake, cytotoxicity, and ability to induce a phototoxic reaction were demonstrated in J774A.1, RAW264.7 macrophages, and vascular smooth muscle (T/G HA-VSMC) as well as in vascular endothelial (HUVEC) cells. Results: Developed liposomes had an average diameter of 124.7 ± 0.6 nm (polydispersity index (PDI) = 0.055) and contained >80% of Photolon). The half-life of formulation in S. scrofa was 20 min with area under the curve (AUC) equal to 14.7. The formulation was noncytotoxic in vitro and was rapidly (10 min) and efficiently accumulated by macrophages, but not T/G HA-VSMC or HUVEC. The accumulated quantity of photosensitizer was sufficient for induction of phototoxicity in J774A.1, but not in T/G HA-VSMC. Conclusions: Due to the excellent physical and pharmacokinetic properties and selectivity for macrophages, the novel liposomal formulation of Photolon is a promising therapeutic candidate for use in arteriosclerosis treatment when targeting macrophages but not accompanying vascular tissue is critical for effective and safe therapy.
机译:背景:脂质体用作生物活性化合物的递送系统。现有技术效率低下封装了大型亲水性大分子,例如PVP缀合的氯e6(光学)。这种光活性药物已被广泛测试治疗应用,包括热动力减少动脉粥样硬化斑块。方法:采用“凝胶水合技术”制备了一种新型的光学制剂。其药代动力学在SUS Scrofa F中进行了测试。国内。在J774A.1,Raw264.7巨噬细胞和血管平滑肌(T / G HA-VSMC)以及血管内皮(HUVEC)细胞中,证明了其细胞吸收,细胞毒性和诱导光毒反应的能力。结果:开发的脂质体的平均直径为124.7±0.6nm(多分散性指数(PDI)= 0.055),并含有> 80%的光子)。在S. scrofa中的制剂的半衰期为20分钟,曲线下(AUC)等于14.7。该配方在体外是非胞间毒性的,并且迅速(10分钟)并通过巨噬细胞有效累积,但不是T / G Ha-VSMC或HUVEC。光敏剂的累积量足以诱导J774A.1中的光毒性,但不含T / G Ha-VSMC。结论:由于巨噬细胞的优异物理和药代动力学性能和选择性,光学的新型脂质体制素是在靶向巨噬细胞的动脉硬化治疗中使用的有前途的治疗候选者,但不伴随血管组织对于有效和安全的治疗至关重要。

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