Kumar Ajay, Ahmad Anas, Vyawahare Akshay, Khan Rehan
Department of Nano-Therapeutics, Institute of Nano Science and Technology, Mohali, India.
Front Pharmacol. 2020 May 27;11:629. doi: 10.3389/fphar.2020.00629. eCollection 2020.
The movement of micro and macro molecules into and within a cell significantly governs several of their pharmacokinetic and pharmacodynamic parameters, thus regulating the cellular response to exogenous and endogenous stimuli. Trafficking of various pharmacological agents and other bioactive molecules throughout and within the cell is necessary for the fidelity of the cells but has been poorly investigated. Novel strategies against cancer and microbial infections need a deeper understanding of membrane as well as subcellular trafficking pathways and essentially regulate several aspects of the initiation and spread of anti-microbial and anti-cancer drug resistance. Furthermore, in order to avail the maximum possible bioavailability and therapeutic efficacy and to restrict the unwanted toxicity of pharmacological bioactives, these sometimes need to be functionalized with targeting ligands to regulate the subcellular trafficking and to enhance the localization. In the recent past the scenario drug targeting has primarily focused on targeting tissue components and cell vicinities, however, it is the membranous and subcellular trafficking system that directs the molecules to plausible locations. The effectiveness of the delivery platforms largely depends on their physicochemical nature, intracellular barriers, and biodistribution of the drugs, pharmacokinetics and pharmacodynamic paradigms. Most subcellular organelles possess some peculiar characteristics by which membranous and subcellular targeting can be manipulated, such as negative transmembrane potential in mitochondria, intraluminal delta pH in a lysosome, and many others. Many specialized methods, which positively promote the subcellular targeting and restrict the off-targeting of the bioactive molecules, exist. Recent advancements in designing the carrier molecules enable the handling of membrane trafficking to facilitate the delivery of active compounds to subcellular localizations. This review aims to cover membrane trafficking pathways which promote the delivery of the active molecule in to the subcellular locations, the associated pathways of the subcellular drug delivery system, and the role of the carrier system in drug delivery techniques.
微观和宏观分子进出细胞以及在细胞内的移动,在很大程度上决定了它们的几个药代动力学和药效学参数,从而调节细胞对外源性和内源性刺激的反应。各种药理剂和其他生物活性分子在细胞内外的运输对于细胞的功能完整性是必要的,但目前对此研究甚少。针对癌症和微生物感染的新策略需要更深入地了解膜以及亚细胞运输途径,并从根本上调节抗菌和抗癌药物耐药性的起始和传播的几个方面。此外,为了获得最大可能的生物利用度和治疗效果,并限制药理生物活性物质的不良毒性,有时需要用靶向配体对其进行功能化,以调节亚细胞运输并增强定位。在最近,药物靶向主要集中在靶向组织成分和细胞周边区域,然而,正是膜性和亚细胞运输系统将分子引导到合理的位置。递送平台的有效性在很大程度上取决于其物理化学性质、细胞内屏障、药物的生物分布、药代动力学和药效学模式。大多数亚细胞器具有一些独特的特征,通过这些特征可以操纵膜性和亚细胞靶向,例如线粒体中的负跨膜电位、溶酶体中的腔内pH值差等等。存在许多积极促进亚细胞靶向并限制生物活性分子脱靶的专门方法。设计载体分子的最新进展使得能够处理膜运输,以促进活性化合物向亚细胞定位的递送。本综述旨在涵盖促进活性分子递送至亚细胞位置的膜运输途径、亚细胞药物递送系统的相关途径以及载体系统在药物递送技术中的作用。