Department of Pharmaceutics, Poona College of Pharmacy, Bharati Vidyapeeth Deemed University, Erandwane, Pune-411038, India.
Curr Drug Deliv. 2021;18(8):1056-1063. doi: 10.2174/1567201818999210120201252.
The cell's power house, mitochondrion, is a vital organelle for drug targeting in the treatment of many diseases due to its fundamental duties and function related to cell proliferation and death. The mitochondrial membrane comprises bilayer artifact and poses extremely negative potential, creating hurdles for therapeutic molecules in reaching mitochondria. To accomplish mitochondrial targeting, the scientific community has explored diverse pharmaceutical formulations like liposomes, polymeric nanoparticles (NPs), and inorganic NPs. However, the game changing technology was a modification of these carriers by mitochondriotropic moiety, dequalinium chloride (DQA) or delivering the chemotherapeutics by DQAsomes. The DQA represents a distinctive mitochondriotropic delocalized cation that displays their selectivity towards accumulation in mitochondria of carcinoma cells. Attributed to this characteristics, DQAsomes have been formulated using DQA and explored for successful mitochondrial targeting of bioactives. In this review, it is discussed the effectiveness of DQA nanocarriers which efficiently and selectively transmit the cytotoxic drug to the tumor cell. The DQA based nanoformulations have evidently displayed augmented pharmacological and therapeutic outcomes than their counterparts both in vitro and in vivo. Thus, DQAsomes symbolizes an ideal carrier with excellent potential as mitochondrial targeting agent.
细胞的动力工厂——线粒体，由于其与细胞增殖和死亡相关的基本职责和功能，成为许多疾病药物靶向治疗的重要细胞器。线粒体膜由双层人工制品组成，具有极其负的电势，为治疗分子到达线粒体设置了障碍。为了实现线粒体靶向，科学界探索了多种药物制剂，如脂质体、聚合物纳米颗粒 (NPs) 和无机 NPs。然而，改变游戏规则的技术是通过靶向线粒体的部分，即盐酸癸氧喹啉 (DQA) 对这些载体进行修饰，或通过 DQA 囊泡来递送化疗药物。DQA 代表一种独特的靶向线粒体的离域阳离子，显示其对癌细胞线粒体积累的选择性。由于这一特性，已经使用 DQA 来制备 DQA 囊泡，并探索其对生物活性物质的成功线粒体靶向。在这篇综述中，讨论了 DQA 纳米载体的有效性，这些载体能够有效地、选择性地将细胞毒性药物输送到肿瘤细胞。基于 DQA 的纳米制剂在体外和体内都明显显示出比其对应物更高的药理学和治疗效果。因此，DQA 囊泡是一种理想的载体，具有作为线粒体靶向剂的巨大潜力。
