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Carvacrol encapsulated nanocarrier/ nanoemulsion abrogates angiogenesis by downregulating COX-2, VEGF and CD31 in vitro and in vivo in a lung adenocarcinoma model

Carvacrol encapsulated nanocarrier/ nanoemulsion abrogates angiogenesis by downregulating COX-2, VEGF and CD31 in vitro and in vivo in a lung adenocarcinoma model
Khan, lImranBhardwaj, MonikaShukla, ShrutiLee, HoominOh, Mi-WahBajpai, Vivek K.Huh, Yun SukKang, Sun Chul
Issue Date
Colloids and Surfaces B: Biointerfaces, 181, 612-622
Article Type
Author Keyword
A549; Angiogenesis; Carvacrol encapsulated nanoemulsion; In silico; In vivo
Binding energy; Binding sites; Biological organs; Cells; Cytology; Emulsification; Emulsions; Medical applications; A549; Angiogenesis; In-silico; In-vivo; Nanoemulsion; Targeted drug delivery; carvacrol; cyclooxygenase 2; matrix metalloproteinase; medium chain triacylglycerol; mitogen activated protein kinase; mitogen activated protein kinase p38; nanocarrier; oil; phosphatidylcholine; platelet endothelial cell adhesion molecule 1; polysorbate; vasculotropin; water; A-549 cell line; angiogenesis; animal cell; animal experiment; animal model; animal tissue; antiangiogenic activity; antiangiogenic therapy; Article; binding site; computer model; controlled study; down regulation; drug delivery system; drug efficacy; drug formulation; emulsion; enzyme activation; human; human cell; hydrodynamics; IC50; in vitro study; in vivo study; lung adenocarcinoma; male; mouse; nanoemulsion; nanoencapsulation; nonhuman; priority journal; protein expression; transmission electron microscopy; ultrasound assisted extraction
Nanoemulsion-based synthesis has been introduced to enhance the bioavailability of natural compounds at target sites for their various biomedical applications. In this study, we synthesized carvacrol nanoemulsion (CN) an oil-in-water (O/W) as a nano-emulsion vehicle system by using ultrasonication emulsification for anti-angiogenesis therapy formulated by combining MCT, lecithin, and polysorbate 80 at the O/W interface called carvacrol encapsulated nanoemulsion (CEN). The diameter of CEN determined by TEM analysis was 105.32 nm. The hydrodynamic droplet size was 101.0 nm with a -39.38-mV zeta potential. The stability of the synthesized CEN was approved till 100 days without any change in diameter size distribution and encapsulation efficiency. We evaluated the role of CEN on angiogenesis in lung adenocarcinoma A549 cells both in vitro and in vivo and observed that it reduced the growth and MMP levels of A549 cells in a dose-dependent manner. Exposure to CEN decreased the activation of MAPK p38 as well as ERK. Moreover, we found that CEN reduced the expression of VEGF and CD31 in A549 cells both in vitro and in vivo. Our in-silico study also indicated the binding of carvacrol to COX-2 and VEGF at the active and allosteric sites of CD31 with low binding energy. Overall, CEN induced anti-angiogenic effects in A549 cells in vitro, in silico, and in vivo, thereby establishing its potential as targeted drug delivery vehicle against angiogenesis. © 2019 Elsevier B.V.
Elsevier BV
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