Alsuraifi Ali, Lin Paul Kong Thoo, Curtis Anthony, Lamprou Dimitrios A, Hoskins Clare
Institute of Science and Technology in Medicine, Keele University, Keele ST5 5BG, UK.
College of Dentistry, University of Basrah, Basrah 61004, Iraq.
Pharmaceuticals (Basel). 2018 Sep 22;11(4):91. doi: 10.3390/ph11040091.
Nanoparticles have been shown to be effective drug carriers in cancer therapy. Pancreatic cancer forms dense tumours which are often resistant to drug molecules. In order to overcome such multidrug resistance, new drug entities, novel delivery systems and combination therapy strategies are being explored. In this paper, we report the design and synthesis of a poly(allylamine)-based amphiphile modified with hydrophobic naphthalimido pendant groups. Bisnaphthalimide compounds have been shown to possess anticancer activity. The potential of this polymer to encapsulate, solubilize and enhance drug (5-fluorouricil and bis-(naphthalimidopropyl)-diaminooctane) cytotoxicity in BxPC-3 cells was evaluated. Our studies showed that the insoluble drugs could be formulated up to 4.3 mg mL and 2.4 mg mL inside the amphiphiles, respectively. Additionally, the novel poly(allylamine)-naphthalimide carrier resulted in an amplification of cytotoxic effect with drug treatment after 24 h, and was capable of reduction of 50% cell population at concentrations as low as 3 μg mL.
纳米颗粒已被证明是癌症治疗中有效的药物载体。胰腺癌会形成致密的肿瘤，这些肿瘤通常对药物分子具有抗性。为了克服这种多药耐药性，人们正在探索新的药物实体、新型给药系统和联合治疗策略。在本文中，我们报道了一种基于聚烯丙胺的两亲物的设计与合成，该两亲物用疏水性萘二甲酰亚胺侧基进行了修饰。双萘二甲酰亚胺化合物已被证明具有抗癌活性。评估了这种聚合物在BxPC-3细胞中包封、增溶和增强药物（5-氟尿嘧啶和双（萘二甲酰亚胺丙基）-二氨基辛烷）细胞毒性的潜力。我们的研究表明，两亲物中不溶性药物的配制浓度分别可达4.3 mg/mL和2.4 mg/mL。此外，新型聚烯丙胺-萘二甲酰亚胺载体在24小时药物处理后导致细胞毒性作用增强，并且在低至3 μg/mL的浓度下能够使细胞数量减少50%。
