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Targeted thermosensitive liposomes: An attractive novel approach for increased drug delivery to solid tumors

机译:靶向热敏脂质体:增加药物向实体瘤的递送的有吸引力的新颖方法

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Introduction: Currently available chemotherapy is hampered by a lack in tumor specificity and resulting toxicity. Small and long-circulating liposomes can preferentially deliver chemotherapeutic drugs to tumors upon extravasation from tumor vasculature. Although clinically used liposomal formulations demonstrated significant reduction in toxicity, enhancement of therapeutic activity has not fully met expectations. Areas covered: Low drug bioavailability from liposomal formulations and limited tumor accumulation remain major challenges to further improve therapeutic activity of liposomal chemotherapy. The aim of this review is to highlight strategies addressing these challenges. A first strategy uses hyperthermia and thermosensitive liposomes to improve tumor accumulation and trigger liposomal drug bioavailability. Image-guidance can aid online monitoring of heat and drug delivery and further personalize the treatment. A second strategy involves tumor-specific targeting to enhance drug delivery specificity and drug internalization. In addition, we review the potential of combinations of the two in one targeted thermosensitive-triggered drug delivery system. Expert opinion: Heat-triggered drug delivery using thermosensitive liposomes as well as the use of tumor vasculature or tumor cell-targeted liposomes are both promising strategies to improve liposomal chemotherapy. Preclinical evidence has been encouraging and both strategies are currently undergoing clinical evaluation. A combination of both strategies rendering targeted thermosensitive liposomes (TTSL) may appear as a new and attractive approach promoting tumor drug delivery.
机译:简介:目前可用的化疗方法因缺乏肿瘤特异性和毒性而受到阻碍。当从肿瘤脉管系统渗出时,小而长循环的脂质体可以优先向肿瘤递送化疗药物。尽管临床上使用的脂质体制剂显示出毒性的显着降低,但治疗活性的提高仍未完全达到预期。涵盖领域:脂质体制剂的药物生物利用度低和有限的肿瘤积累仍然是进一步改善脂质体化学疗法治疗活性的主要挑战。这次审查的目的是强调解决这些挑战的策略。第一种策略使用热疗和热敏脂质体来改善肿瘤蓄积并触发脂质体药物的生物利用度。图像引导可以帮助在线监测热量和药物的输送,并进一步个性化治疗。第二种策略涉及肿瘤特异性靶向,以增强药物递送特异性和药物内在化。此外,我们回顾了在一个有针对性的热敏触发药物递送系统中将两者结合的潜力。专家意见:使用热敏脂质体进行热触发给药以及使用肿瘤脉管系统或靶向肿瘤细胞的脂质体都是改善脂质体化学疗法的有前途的策略。临床前证据令人鼓舞,两种策略目前都在进行临床评估。两种提供靶向热敏脂质体(TTSL)的策略的组合可能会作为一种新的,有吸引力的促进肿瘤药物递送的方法出现。

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