Departamento De Produtos Farmacêuticos, Faculdade De Farmácia, Universidade Federal De Minas Gerais, Belo Horizonte, Brazil.
Departamento De Farmácia, Faculdade De Ciências Biológicas E Da Saúde, Universidade Federal Dos Vales Do Jequitinhonha E Mucuri, Diamantina, Brazil.
Expert Opin Drug Deliv. 2021 Oct;18(10):1335-1354. doi: 10.1080/17425247.2021.1919619. Epub 2021 May 19.
: All- retinoic acid (ATRA, tretinoin) is the main drug used in the treatment of acute promyelocytic leukemia (APL). Despite its impressive activity against APL, the same could not be clinically observed in other types of cancer. Nanotechnology can be a tool to enhance ATRA anticancer efficacy and resolve its drawbacks in APL as well as in other malignancies.: This review covers ATRA use in APL and non-APL cancers, the problems that were found in ATRA therapy and how nanoencapsulation can aid to circumvent them. Pre-clinical results obtained with nanoencapsulated ATRA are shown as well as the two ATRA products based on nanotechnology that were clinically tested: ATRA-IV® and Apealea®.: ATRA presents interesting properties to be used in anticancer therapy with a notorious differentiation and antimetastatic activity. Bioavailability and resistance limitations impair the use of ATRA in non-APL cancers. Nanotechnology can circumvent these issues and provide tools to enhance its anticancer activities, such as co-loading of multiple drug and active targeting to tumor site.
全反式维甲酸(ATRA,维甲酸)是治疗急性早幼粒细胞白血病(APL)的主要药物。尽管它对 APL 具有令人印象深刻的活性,但在其他类型的癌症中却无法在临床上观察到。纳米技术可以成为增强 ATRA 抗癌疗效的工具,并解决 APL 以及其他恶性肿瘤中存在的问题。
本文综述了 ATRA 在 APL 和非 APL 癌症中的应用,以及在 ATRA 治疗中发现的问题,以及纳米封装如何帮助克服这些问题。还展示了用纳米封装 ATRA 获得的临床前结果,以及两种基于纳米技术的临床测试的 ATRA 产品:ATRA-IV®和 Apealea®。
ATRA 具有用于癌症治疗的有趣特性,具有明显的分化和抗转移活性。生物利用度和耐药性限制了 ATRA 在非 APL 癌症中的应用。纳米技术可以克服这些问题,并提供增强其抗癌活性的工具,例如多种药物的共同负载和主动靶向肿瘤部位。