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丹皮酚的化学、药代动力学、药理学及近期新型药物传递系统。

Chemistry, pharmacokinetics, pharmacology and recent novel drug delivery systems of paeonol.

机构信息

Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKM'S NMIMS, V.L. Mehta Road, Vile Parle (West), Mumbai 400056, India.

Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKM'S NMIMS, V.L. Mehta Road, Vile Parle (West), Mumbai 400056, India.

出版信息

Life Sci. 2020 Jun 1;250:117544. doi: 10.1016/j.lfs.2020.117544. Epub 2020 Mar 13.

Abstract

UNLABELLED

Paeonol is a bioactive phenol present in Dioscorea japonica, Paeonia suffruticosa and Paeonia lactiflora. It is reported for various pharmacological activities.

AIM

To review chemistry, pharmacokinetics, pharmacological activities as well as various formulations of paeonol.

MATERIALS AND METHODS

A literature search was done using different search terms for paeonol by using different scientific databases like PubMed, Scopus and ProQuest. Scientific papers published during the period 1969 to 2019 were comprehensively reviewed.

KEY FINDINGS

Researchers have synthesized methoxy, ethoxy, piperazine, chromonylthiazolidine, phenol-phenylsulfonyl, alkyl ether, aminothiazole, tryptamine hybrids and paeononlsilatie derivatives to enhance the stability of paeonol. These derivatives were synthesized and evaluated for in vitro series of biological activities like anti-inflammatory, tyrosinase inhibitory, neuroprotective, anticancer and antiviral activity. Regardless of valuable therapeutic potential, the clinical use of paeonol is restricted due to poor water solubility, low oral bioavailability, low stability and high volatility at room temperature. To enhance the bioavailability of paeonol various formulations are prepared and evaluated for its activity. Paeonol formulations can be categorized as conventional-tablets, topical gel and hydrogel; polymeric delivery system-microparticles, microsponges, dendrimers, nanocapsules, polymeric nanoparticles, nanospheres; lipid-based delivery systems-microemulsion, self-micro-emulsifying drug delivery, liposome, transethosomes, ethosomes, niosomes, proniosomes, lipid-based nanoparticles and nanoemulsion of paeonol.

SIGNIFICANCE

Paeonol has a potential to be developed as a techno-commercial product with respect to its multi-faceted pharmacological properties. Even though in vitro and in vivo studies have been reported the important activities of paeonol, its commercial utilization requires extensive safety and efficacy data.

摘要

未加标签

丹皮酚是存在于山药、牡丹和芍药中的一种生物活性酚类物质。它具有多种药理活性。

目的

综述丹皮酚的化学、药代动力学、药理活性以及各种制剂形式。

材料和方法

使用不同的搜索词,通过 PubMed、Scopus 和 ProQuest 等不同的科学数据库对丹皮酚进行了文献检索。全面综述了 1969 年至 2019 年期间发表的科学论文。

主要发现

研究人员合成了甲氧基、乙氧基、哌嗪、色酮噻唑烷、苯酚-苯磺酰基、烷基醚、氨基噻唑、色胺杂合体和丹皮酚硅烷衍生物,以提高丹皮酚的稳定性。这些衍生物被合成并评估了一系列体外生物活性,如抗炎、酪氨酸酶抑制、神经保护、抗癌和抗病毒活性。尽管具有有价值的治疗潜力,但由于丹皮酚的水溶性差、口服生物利用度低、室温下稳定性和挥发性高,其临床应用受到限制。为了提高丹皮酚的生物利用度,制备了各种制剂并评估了其活性。丹皮酚制剂可分为常规片剂、局部凝胶和水凝胶;聚合物给药系统-微粒、微海绵、树枝状大分子、纳米囊、聚合物纳米粒、纳米球;基于脂质的给药系统-微乳液、自微乳给药系统、脂质体、转胞吞体、传递体、非离子型脂质体、普罗尼奥斯、纳米脂质体和丹皮酚纳米乳液。

意义

丹皮酚具有多方面的药理特性,有可能开发成为一种技术商业产品。尽管已经报道了丹皮酚的体外和体内研究,但要将其商业化,需要广泛的安全性和疗效数据。

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