Solubility and Bioavailability Enhancement of Oridonin: A Review

Zhang, Yuanyuan; Wang, Shaohua; Dai, Mengmeng; Nai, Jijuan; Zhu, Lei; Hua-gang, Sheng

doi:10.3390/molecules25020332

Cited by 46 publications

(33 citation statements)

References 144 publications

(174 reference statements)

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“…SLN formulations of oridonin were prepared using different lipid compositions to improve the in vitro release behavior, in vivo pharmacokinetics, and tissue distribution profile [ 92 , 93 , 94 ]. In cell culture studies, oridonin-containing SLNs inhibited the proliferation of cancer cells (MCF-7, HepG 2, and A549) more effectively compared to the free drug and, promisingly, did not exhibit any significant toxicity enhancement on human mammary epithelial cells [ 93 ].…”

Section: Nddss In the Delivery Of Nrf2 Modulators For Cancer Therapymentioning

confidence: 99%

Nanotechnology-Based Drug Delivery to Improve the Therapeutic Benefits of NRF2 Modulators in Cancer Therapy

et al. 2021

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The disadvantages of conventional anticancer drugs, such as their low bioavailability, poor targeting efficacy, and serious side effects, have led to the discovery of new therapeutic agents and potential drug delivery systems. In particular, the introduction of nano-sized drug delivery systems (NDDSs) has opened new horizons for effective cancer treatment. These are considered potential systems that provide deep tissue penetration and specific drug targeting. On the other hand, nuclear factor erythroid 2-related factor 2 (NRF2)-based anticancer treatment approaches have attracted tremendous attention and produced encouraging results. However, the lack of effective formulation strategies is one of the factors that hinder the clinical application of NRF2 modulators. In this review, we initially focus on the critical role of NRF2 in cancer cells and NRF2-based anticancer treatment. Subsequently, we review the preparation and characterization of NDDSs encapsulating NRF2 modulators and discuss their potential for cancer therapy.

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Section: Nddss In the Delivery Of Nrf2 Modulators For Cancer Therapymentioning

confidence: 99%

Nanotechnology-Based Drug Delivery to Improve the Therapeutic Benefits of NRF2 Modulators in Cancer Therapy

et al. 2021

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“…Generally, I. rubescens (Hemsl.) H.Hara is frequently utilized in the treatment of acute and chronic pharyngitis, tonsillitis and bronchitis in clinic ( Zhang et al, 2020 ). As the main bioactive chemical component of I. rubescens (Hemsl.)…”

Section: Introductionmentioning

confidence: 99%

Oridonin: A Review of Its Pharmacology, Pharmacokinetics and Toxicity

Zhang

et al. 2021

Front. Pharmacol.

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Oridonin, as a natural terpenoids found in traditional Chinese herbal medicine Isodon rubescens (Hemsl.) H.Hara, is widely present in numerous Chinese medicine preparations. The purpose of this review focuses on providing the latest and comprehensive information on the pharmacology, pharmacokinetics and toxicity of oridonin, to excavate the therapeutic potential and explore promising ways to balance toxicity and efficacy of this natural compound. Information concerning oridonin was systematically collected from the authoritative internet database of PubMed, Elsevier, Web of Science, Wiley Online Library and Europe PMC applying a combination of keywords involving “pharmacology,” “pharmacokinetics,” and “toxicology”. New evidence shows that oridonin possesses a wide range of pharmacological properties, including anticancer, anti-inflammatory, hepatorenal activities as well as cardioprotective protective activities and so on. Although significant advancement has been witnessed in this field, some basic and intricate issues still exist such as the specific mechanism of oridonin against related diseases not being clear. Moreover, several lines of evidence indicated that oridonin may exhibit adverse effects, even toxicity under specific circumstances, which sparked intense debate and concern about security of oridonin. Based on the current progress, future research directions should emphasize on 1) investigating the interrelationship between concentration and pharmacological effects as well as toxicity, 2) reducing pharmacological toxicity, and 3) modifying the structure of oridonin—one of the pivotal approaches to strengthen pharmacological activity and bioavailability. We hope that this review can provide some inspiration for the research of oridonin in the future.

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“…It has been widely used to treat a variety of diseases, including throat swelling, alzheimer’s disease, inflammation of tonsils ( Mir et al, 2020 ). In recent years, lines of evidence have proved that ORI inhibits growth of tumor cells and induces cell apoptosis in some solid tumor types, such as leukemia, lung cancer, colorectal cancer and so on ( Zhang et al, 2020 ). Oridonin inhibits breast cancer cell migration, invasion and adhesion, as well as tumor angiogenesis, which are mediated by suppressing EMT and the HIF-1α/VEGF signaling pathway ( Li et al, 2018 ).…”

Section: Introductionmentioning

confidence: 99%

Oridonin-Loaded Nanoparticles Inhibit Breast Cancer Progression Through Regulation of ROS-Related Nrf2 Signaling Pathway

Zhao

Xiao

Peng

et al. 2021

Front. Bioeng. Biotechnol.

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Oridonin (ORI) has been shown to inhibit tumor cell growth and proliferation in vitro, while its optimum anti-tumor activity in vivo is limited due to the poor aqueous solubility and bioavailability. In this study, to improve the bioavailability, we developed a nanoparticle-based drug delivery system to facilitate delivery of ORI to breast tumor. ORI was encapsulated in biodegradable nanoparticles (NPs) based on poly-lactic-co-glycolic acid (PLGA) and polyethylene glycol (PEG) to form ORI NPs (ORI-NPs). The resulting ORI-NPs exhibited a mean particle diameter of 100 nm and displayed an efficient cellular uptake by human breast cancer MCF-7 cells. Compared to free ORI that showed no effects on tumor cell proliferation, the ORI-NPs showed significant cytotoxicity and delayed endothelial cell migration, tube formation and angiogenesis. Pharmacokinetics studies showed that ORI-NPs significantly increased the half-life of ORI in the blood circulation. In the nude mouse xenograft model, ORI-NPs markedly inhibited tumor growth and angiogenesis, while ORI did not show any inhibitory effects on the growth of tumor xenografts. The mechanism experiments showed that the antitumor activity of ORI-NPs against breast cancer might be through ROS related Nrf2/HO-1 signaling pathway. Together, these results demonstrated that ORI-loaded PEG-PLGA NPs enhanced bioactivity and bioavailability in vivo over ORI, indicating that ORI-NPs may represent a promisingly effective candidate against breast cancer.

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Solubility and Bioavailability Enhancement of Oridonin: A Review

Cited by 46 publications

References 144 publications

Nanotechnology-Based Drug Delivery to Improve the Therapeutic Benefits of NRF2 Modulators in Cancer Therapy

Nanotechnology-Based Drug Delivery to Improve the Therapeutic Benefits of NRF2 Modulators in Cancer Therapy

Oridonin: A Review of Its Pharmacology, Pharmacokinetics and Toxicity

Oridonin-Loaded Nanoparticles Inhibit Breast Cancer Progression Through Regulation of ROS-Related Nrf2 Signaling Pathway

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