Sheikh Afsana, Alhakamy Nabil A, Md Shadab, Kesharwani Prashant
Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, India.
Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia.
Front Pharmacol. 2022 Jan 25;12:803304. doi: 10.3389/fphar.2021.803304. eCollection 2021.
Cancer is a life-threatening disease, contributing approximately 9.4 million deaths worldwide. To address this challenge, scientific researchers have investigated molecules that could act as speed-breakers for cancer. As an abiotic drug delivery system, liposomes can hold both hydrophilic and lipophilic drugs, which promote a controlled release, accumulate in the tumor microenvironment, and achieve elongated half-life with an enhanced safety profile. To further improve the safety and impair the off-target effect, the surface of liposomes could be modified in a way that is easily identified by cancer cells, promotes uptake, and facilitates angiogenesis. Integrins are overexpressed on cancer cells, which upon activation promote downstream cell signaling and eventually activate specific pathways, promoting cell growth, proliferation, and migration. RGD peptides are easily recognized by integrin over expressed cells. Just like a multistage rocket, ligand anchored liposomes can be selectively recognized by target cells, accumulate at the specific site, and finally, release the drug in a specific and desired way. This review highlights the role of integrin in cancer development, so gain more insights into the phenomenon of tumor initiation and survival. Since RGD is recognized by the integrin family, the fate of RGD has been demonstrated after its binding with the acceptor's family. The role of RGD based liposomes in targeting various cancer cells is also highlighted in the paper.
癌症是一种危及生命的疾病,在全球范围内导致约940万人死亡。为应对这一挑战,科研人员研究了可作为癌症“减速器”的分子。作为一种非生物药物递送系统,脂质体可以容纳亲水性和亲脂性药物,促进药物的控释,在肿瘤微环境中蓄积,并实现延长的半衰期以及更高的安全性。为进一步提高安全性并减少脱靶效应,脂质体表面可以进行修饰,使其易于被癌细胞识别,促进摄取,并促进血管生成。整合素在癌细胞上过度表达,激活后会促进下游细胞信号传导,并最终激活特定途径,促进细胞生长、增殖和迁移。RGD肽很容易被整合素过表达的细胞识别。就像多级火箭一样,配体锚定脂质体可以被靶细胞选择性识别,在特定部位蓄积,并最终以特定且理想的方式释放药物。本综述强调了整合素在癌症发展中的作用,以便更深入地了解肿瘤起始和存活现象。由于RGD被整合素家族识别,其与受体家族结合后的命运已得到证实。本文还强调了基于RGD的脂质体在靶向各种癌细胞中的作用。