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pH-sensitive pHLIP® coated niosomes.
Molecular Membrane Biology ( IF 2.857 ) Pub Date : 2017-08-09 , DOI: 10.1080/09687688.2017.1342969
Mohan C Pereira 1 , Monica Pianella 2 , Da Wei 1 , Anna Moshnikova 1 , Carlotta Marianecci 2 , Maria Carafa 2 , Oleg A Andreev 1 , Yana K Reshetnyak 1
Affiliation  

Nanomedicine is becoming very popular over conventional methods due to the ability to tune physico-chemical properties of nano vectors, which are used for encapsulation of therapeutic and diagnostic agents. However, the success of nanomedicine primarily relies on how specifically and efficiently nanocarriers can target pathological sites to minimize undesirable side effects and enhance therapeutic efficacy. Here, we introduce a novel class of targeted nano drug delivery system, which can be used as an effective nano-theranostic for cancer. We formulated pH-sensitive niosomes (80–90 nm in diameter) using nonionic surfactants Span20 (43–45 mol%), cholesterol (50 mol%) and 5 mol% of pH (Low) insertion peptide (pHLIP) conjugated with DSPE lipids (DSPE-pHLIP) or hydrophobic fluorescent dye, pyrene, (Pyr-pHLIP). In coating of niosomes, pHLIP was used as an acidity sensitive targeting moiety. We have demonstrated that pHLIP coated niosomes sense the extracellular acidity of cancerous cells. Intravenous injection of fluorescently labeled (R18) pHLIP-coated niosomes into mice bearing tumors showed significant accumulation in tumors with minimal targeting of kidney, liver and muscles. Tumor-targeting niosomes coated with pHLIP exhibited 2–3 times higher tumor uptake compared to the non-targeted niosomes coated with PEG polymer. Long circulation time and uniform bio-distribution throughout the entire tumor make pHLIP-coated niosomes to be an attractive novel delivery system.



中文翻译:

对pH敏感的pHLIP®包覆的脂质体。

由于具有调节用于封装治疗剂和诊断剂的纳米载体的物理化学性质的能力,因此与常规方法相比,纳米药物变得非常受欢迎。然而,纳米药物的成功主要取决于纳米载体如何特异性和有效地靶向病理部位,以最大程度地减少不良副作用并增强治疗效果。在这里,我们介绍了一类新型的靶向纳米药物递送系统,可以将其用作有效的癌症纳米治疗剂。我们使用非离子表面活性剂Span20(43–45 mol%),胆固醇(50 mol%)和5 mol%与DSPE脂质偶联的pH(低)插入肽(pHLIP)配制了对pH敏感的脂质体(直径80-90 nm)。 (DSPE-pHLIP)或疏水性荧光染料,(Pyr-pHLIP)。在包覆脂质体时,pHLIP用作酸度敏感的靶向部分。我们已经证明,pHLIP包覆的脂质体可感知癌细胞的细胞外酸性。向携带有肿瘤的小鼠静脉内注射荧光标记(R18)pHLIP涂层的脂质体后,在肾脏中显着蓄积,而对肾脏,肝脏和肌肉的靶向作用却最小。与非PEG聚合物包被的靶向脂质体相比,pHLIP包被的靶向肿瘤的脂质体的肿瘤吸收率高2–3倍。较长的循环时间和在整个肿瘤中均匀的生物分布使pHLIP包覆的脂质体成为一种有吸引力的新型递送系统。向携带有肿瘤的小鼠静脉内注射荧光标记(R18)pHLIP涂层的脂质体,在肿瘤中显着积累,而对肾脏,肝脏和肌肉的靶向作用最小。pHLIP包被的靶向肿瘤的脂质体与PEG包被的未靶向的脂质体相比,其肿瘤吸收率高出2-3倍。较长的循环时间和在整个肿瘤中均匀的生物分布使pHLIP包覆的脂质体成为有吸引力的新型传递系统。向携带有肿瘤的小鼠静脉内注射荧光标记(R18)pHLIP涂层的脂质体后,在肾脏中显着蓄积,而对肾脏,肝脏和肌肉的靶向作用却最小。与非PEG聚合物包被的靶向脂质体相比,pHLIP包被的靶向肿瘤的脂质体的肿瘤吸收率高2–3倍。较长的循环时间和在整个肿瘤中均匀的生物分布使pHLIP包覆的脂质体成为一种有吸引力的新型递送系统。

更新日期:2017-08-09
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