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姜烯酮增溶和生物利用度的制剂和纳米技术方法。

Formulation and Nanotechnology-Based Approaches for Solubility and Bioavailability Enhancement of Zerumbone.

机构信息

College of Pharmacy, Roseman University of Health Sciences, South Jordan, UT 84096, USA.

Department of Pharmaceutical Sciences, College of Pharmacy and Allied Health Professions, South Dakota State University, Brookings, SD 57007, USA.

出版信息

Medicina (Kaunas). 2020 Oct 23;56(11):557. doi: 10.3390/medicina56110557.

Abstract

About 40-70% of drug molecules in the clinical development pipeline suffer from one of either low aqueous solubility, poor absorption, or extremely low bioavailability. Approximately 75% of the world population relies on traditional therapies and therefore there has been a growing interest in the utilization of natural compounds. Zerumbone is one such natural compound, classified as a sesquiterpenoid that is extracted from the essential volatile oils of rhizomes from . It possesses strong antitumor, antioxidant, antimicrobial, and anti-inflammatory activity. However, despite promising preclinical studies demonstrating the therapeutic utility of zerumbone, its clinical development has been limited due to its low aqueous solubility, poor absorption, or associated low bioavailability. Multiple reviews demonstrating the pharmacological effects of zerumbone for various diseases have been published. However, to our knowledge, no review demonstrates the various formulation strategies developed to overcome the biopharmaceutical challenges of zerumbone. The purpose of this review is to provide a comprehensive perspective on zerumbone as a molecule for formulation development. A section related to pharmacokinetics, toxicity, and patents of zerumbone is included. This review provides the importance of developing novel formulations of zerumbone to overcome its biopharmaceutical challenges thereby advance its potential in the treatment of various diseases.

摘要

大约有 40-70%的药物分子在临床开发管道中由于低水溶性、吸收差或极低的生物利用度而受到影响。大约 75%的世界人口依赖于传统疗法,因此人们对利用天然化合物越来越感兴趣。姜烯酮是一种天然化合物,归类为倍半萜烯,从根茎的挥发油中提取。它具有很强的抗肿瘤、抗氧化、抗菌和抗炎活性。然而,尽管有有希望的临床前研究表明姜烯酮具有治疗用途,但由于其低水溶性、吸收差或相关的低生物利用度,其临床开发受到限制。已经发表了多篇综述,展示了姜烯酮在各种疾病中的药理学作用。然而,据我们所知,没有综述展示了为克服姜烯酮的生物制药挑战而开发的各种制剂策略。本文综述的目的是提供一个关于姜烯酮作为制剂开发分子的全面视角。本文还包括了与姜烯酮的药代动力学、毒性和专利相关的部分。本文综述提供了开发新型姜烯酮制剂的重要性,以克服其生物制药挑战,从而推进其在治疗各种疾病中的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dcb9/7690806/ed6838a3e666/medicina-56-00557-g001.jpg

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