Harmine-loaded galactosylated pluronic F68-gelucire 44/14 mixed micelles for liver targeting

Kushwaha, Jeetendra; Baidya, Debjani; Patil, Sharvil

doi:10.1080/03639045.2019.1620267

Cited by 20 publications

(5 citation statements)

References 21 publications

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“…According to modern pharmacological studies, P. harmala L has been proven to possess therapeutic effects against malignant tumors, and harmine maybe the key active component for its anti-cancer effect [7]. It is reported that harmine inhibits the progression of various malignant tumors, such as breast cancer [8], lung cancer [9], gastric cancer [10] and liver cancer [11]. Hamsa et al demonstrated that harmine could act as a strong angiogenesis inhibitor by suppressing key factors such as vascular endothelial growth factor and matrix metalloproteinases [12].…”

Section: Introductionmentioning

confidence: 99%

Harmine suppresses the malignant phenotypes and PI3K activity in breast cancer

Yao

et al. 2022

Anti-Cancer Drugs

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Breast cancer remains a serious threaten to the women’s health, discovery of potent treatment would help to improve the outcomes of breast cancer patients. Harmine extracted from Peganum harmala L, has been reported to exert tumor suppressive activity in several malignancies. Our objective was to demonstrate the effects of harmine on the malignant phenotypes of breast cancer cells. Breast cancer cell lines (MDA-MB-231, SKBR3, and MCF-7) and human normal breast cell line MCF-10A were employed in the present study. The MTT and colony formation assays were applied to the detection of cell viability and proliferation. Wound healing and transwell assays were performed to evaluate the alterations of cell migration and invasion after harmine treatment. Flow cytometry was applied to assess the effect of harmine in inducing cell apoptosis. Furthermore, western blotting assay was used to detect the biomarkers of epithelial-mesenchymal transition and phosphatidylinositol 3 kinase (PI3K) signaling pathway. The tumorigenesis ability was detected by subcutaneous implantation. Harmine dose-dependently suppressed the viability and proliferative capacity of breast cancer cells. Flow cytometry showed that harmine induced apoptosis in MCF-7 and MDA-MB-231 cells. In addition, harmine effectively inhibited the migration and invasion abilities of breast cancer cells. Western blotting indicated harmine significantly promoted E-cadherin and PTEN expression, while suppressed N-cadherin, vimentin, PI3K, p-mTOR, and AKT levels. Interfering the PTEN expression by siRNA partly rescued the activity of PI3K signaling pathway. Moreover, harmine injection also suppressed the tumorigenesis of breast cancer cells. Our results suggested that Hermine could suppress multiple malignant phenotypes and inhibit PI3K signaling, which supports that harmine might be a potential tumor-suppressive natural compound against breast cancer.

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Section: Introductionmentioning

confidence: 99%

Harmine suppresses the malignant phenotypes and PI3K activity in breast cancer

Yao

et al. 2022

Anti-Cancer Drugs

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“…More specifically, the complexation of polymers and CDs offers several advantages, including enhanced encapsulation efficiency and drug loading values than those achieved with pristine drugs [28][29][30][31], improved activity/efficacy [28,30,32,33], superior biocompatibility [32,[34][35][36], greater release profile [20], long-term stability [30,36], improved inhibition efficacy against targeted cells [34], excellent rheological characteristics [34], and alleviated toxic effects [30,33,35]. Similarly, among the advantages that polymer-surfactant systems offer are enhanced bioavailability [37][38][39][40][41], improved drug targeting capability [38,40], ameliorated activity [39,40], long-term stability [40], and superior release profile [40]. Taking into account all the mentioned properties, it is worth examining the combination of biocompatible block copolymers with surfactants and CDs to design and develop complex structures that represent a new class of advanced nose-to-brain drug delivery systems.…”

Section: Introductionmentioning

confidence: 99%

Fabricating Polymer/Surfactant/Cyclodextrin Hybrid Particles for Possible Nose-to-Brain Delivery of Ropinirole Hydrochloride: In Vitro and Ex Vivo Evaluation

Saitani,

Pippa,

Perinelli

et al. 2024

IJMS

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Ropinirole is a non-ergolinic dopamine agonist used to manage Parkinson’s disease and it is characterized by poor oral bioavailability. This study aimed to design and develop advanced drug delivery systems composed of poloxamer 407, a non-ionic surfactant (Tween 80), and cyclodextrins (methyl-β-CD or hydroxy-propyl-β-CD) for possible brain targeting of ropinirole after nasal administration for the treatment of Parkinson’s disease. The hybrid systems were formed by the thin-film hydration method, followed by an extensive physicochemical and morphological characterization. The in vitro cytotoxicity of the systems on HEK293 cell lines was also tested. In vitro release and ex vivo mucosal permeation of ropinirole were assessed using Franz cells at 34 °C and with phosphate buffer solution at pH 5.6 in the donor compartment, simulating the conditions of the nasal cavity. The results indicated that the diffusion-controlled drug release exhibited a progressive increase throughout the experiment, while a proof-of-concept experiment on ex vivo permeation through rabbit nasal mucosa revealed a better performance of the prepared hybrid systems in comparison to ropinirole solution. The encouraging results in drug release and mucosal permeation indicate that these hybrid systems can serve as attractive platforms for effective and targeted nose-to-brain delivery of ropinirole with a possible application in Parkinson’s disease. Further ex vivo and in vivo studies to support the results of the present work are ongoing.

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“…For example, surfactants, denaturants, alcohols, and similar compounds act as salting in agents, while NaCl, KCl, and similar salts act as salting-out agents. 5,23,24,[39][40][41] In general, adding salt to BCPs facilitate the disruption of hydrogen bonds between the copolymer and water molecules, leading to enhanced PPO-PPO hydrophobic interactions. Consequently, the process of micellization occurs earlier and at a lower temperature when salt is present compared to its absence.…”

Section: Introductionmentioning

confidence: 99%