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Harnessing the therapeutic potential of anticancer drugs through amorphous solid dispersions.
Biochimica et Biophysica Acta (BBA) - Reviews on Cancer ( IF 9.7 ) Pub Date : 2019-10-31 , DOI: 10.1016/j.bbcan.2019.188319
Urvi H Gala 1 , Dave A Miller 2 , Robert O Williams 3
Affiliation  

The treatment of cancer is still a major challenge. But tremendous progress in anticancer drug discovery and development has occurred in the last few decades. However, this progress has resulted in few effective oncology products due to challenges associated with anticancer drug delivery. Oral administration is the most preferred route for anticancer drug delivery, but the majority of anticancer drugs currently in product pipelines and the majority of those that have been commercially approved have inherently poor water solubility, and this cannot be mitigated without compromising their potency and stability. The poor water solubility of anticancer drugs, in conjunction with other factors, leads to suboptimal pharmacokinetic performance. Thus, these drugs have limited efficacy and safety when administered orally. The amorphous solid dispersion (ASD) is a promising formulation technology that primarily enhances the aqueous solubility of poorly water-soluble drugs. In this review, we discuss the challenges associated with the oral administration of anticancer drugs and the use of ASD technology in alleviating these challenges. We emphasize the ability of ASDs to improve not only the pharmacokinetics of poorly water-soluble anticancer drugs, but also their efficacy and safety. The goal of this paper is to rationalize the application of ASD technology in the formulation of anticancer drugs, thereby creating superior oncology products that lead to improved therapeutic outcomes.

中文翻译:

通过无定形固体分散体利用抗癌药的治疗潜力。

癌症的治疗仍然是主要挑战。但是在过去的几十年中,抗癌药物的发现和开发取得了巨大的进步。然而,由于与抗癌药物递送相关的挑战,该进展导致有效的肿瘤学产品很少。口服给药是抗癌药物递送的最优选途径,但是目前产品线中的大多数抗癌药物和大多数已被商业批准的药物固有地具有较差的水溶性,并且这在不损害其效力和稳定性的情况下不能得到缓解。抗癌药的水溶性差,再加上其他因素,导致药代动力学性能欠佳。因此,这些药物口服时疗效和安全性有限。无定形固体分散体(ASD)是一种很有前途的配制技术,主要可提高水溶性差的药物的水溶性。在这篇综述中,我们讨论了与口服抗癌药物相关的挑战以及在缓解这些挑战中使用ASD技术的问题。我们强调ASD不仅可以改善水溶性差的抗癌药的药代动力学,而且还可以改善其功效和安全性。本文的目的是使ASD技术在抗癌药物配方中的应用合理化,从而创造出可改善治疗效果的优质肿瘤学产品。我们将讨论与口服抗癌药物相关的挑战以及在缓解这些挑战中使用ASD技术的问题。我们强调ASD不仅可以改善水溶性差的抗癌药的药代动力学,而且还可以改善其功效和安全性。本文的目的是使ASD技术在抗癌药物配方中的应用合理化,从而创造出可改善治疗效果的优质肿瘤学产品。我们将讨论与口服抗癌药物相关的挑战以及在缓解这些挑战中使用ASD技术的问题。我们强调ASD不仅可以改善水溶性差的抗癌药的药代动力学,而且还可以改善其功效和安全性。本文的目的是使ASD技术在抗癌药物配方中的应用合理化,从而创造出可改善治疗效果的优质肿瘤学产品。
更新日期:2019-10-31
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