Optimization of the process variables of tilianin-loaded composite phospholipid liposomes based on response surface-central composite design and pharmacokinetic study

Zeng, Cheng; Wen, Jiangqi; Tan, Meie; Yang, Xiaoyi; He, Chenghui; Huang, Wei; Xing, Jianguo

doi:10.1016/j.ejps.2016.02.007

Cited by 29 publications

(10 citation statements)

References 23 publications

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“…Modern pharmacological studies have illustrated that the active ingredients in D. moldavica displayed the ability to prevent or treat neurodegenerative disorders and inflammatory disorders (García-Díaz et al, 2016;Liu et al, 2018), and suppressed the growth and proliferation of various types of cancer cells (Sato et al, 2015;Chakrabarti and Ray, 2016). Tilianin is the major effective component of the total flavonoid extract from D. moldavica (Zeng et al, 2016). Tilianin has been reported to have neuroprotective and cardioprotective effects in the treatment of cardiovascular and cerebrovascular diseases (Zeng et al, 2018;Jiang et al, 2019).…”

Section: Introductionmentioning

confidence: 99%

Tilianin Extracted From Dracocephalum moldavica L. Induces Intrinsic Apoptosis and Drives Inflammatory Microenvironment Response on Pharyngeal Squamous Carcinoma Cells via Regulating TLR4 Signaling Pathways

et al. 2020

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Tilianin Regulates Tumor Immunosuppressive Microenvironment these results showed that tilianin treatment increased cytotoxicity as well as the apoptotic population of FaDu cells in a dose-dependent manner. Furthermore, tilianin treatment decreased the level of anti-apoptotic markers Bcl-2 and Bcl-xL, increased the level of apoptotic factors Bad and Bax, and stimulated cytochrome c release, caspase-3 and poly ADP ribose polymerase (PARP) activation in FaDu cells. Furthermore, our findings indicated that tilianin treatment activated TLR4/p38/JNK/NF-κB signaling pathways and increased the release of inflammatory cytokines. This promoted the maturation of DCs to enhance immune system function in the tumor microenvironment. Moreover, the effects of tilianin on immune system function were abolished by TLR4 siRNA and p65 siRNA. In conclusion, these findings suggested that tilianin may be of immunotherapeutic value for inhibiting human pharyngeal squamous cell carcinoma.

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Section: Introductionmentioning

confidence: 99%

Tilianin Extracted From Dracocephalum moldavica L. Induces Intrinsic Apoptosis and Drives Inflammatory Microenvironment Response on Pharyngeal Squamous Carcinoma Cells via Regulating TLR4 Signaling Pathways

et al. 2020

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“…Commonly known as XinJiang in China, DML contains a potent antioxidant flavonoid component, tilianin (acacetin 7-glucoside, molecular formula: C 22 H 22 O 10 , molecular weight: 446.4, Fig 1A ), which is used to prevent and treat hypertension and heart failure [ 12 , 18 ]. Specifically, tilianin isolated from this medicinal herb has been shown to prevent MIRI in rats [ 19 , 20 ] by conferring cardioprotection [ 21 ].…”

Section: Introductionmentioning

confidence: 99%

Cardioprotection of tilianin ameliorates myocardial ischemia-reperfusion injury: Role of the apoptotic signaling pathway

et al. 2018

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Our previous research demonstrated that tilianin protects the myocardium in a myocardial ischemia reperfusion injury (MIRI) rat model and has prominent pharmacological potential as a cardiovascular drug. Our study aimed to investigate the molecular signaling implicated in the improvement of myocardial survival induced by tilianin, a flavonoid antioxidant. Tilianin (2.5, 5, and 10 mg/kg/d) or saline was orally administered to rats for 14 days. On the 15th day, ischemia was induced by ligating the left anterior descending artery for 45 min, followed by 4 h of reperfusion. The levels of MIRI-induced serum myocardial enzymes and cardiomyocyte apoptosis as well as infarct size were examined to assess the cardioprotective effects. Cardiac tissues were collected for western blot analyses to determine the protein expression of anti-apoptotic signaling molecules. In MIRI-treated rats, our results revealed that pre-administration of high dose-tilianin the reduced release of LDH, MDA, and CK-MB and increased the plasma SOD level, and significantly attenuated the infarct size. Western blot analysis showed that a remarkable rise in expression of Bcl-2 and XIAP, and decline in expression of Bax, Smac/Diablo, HtrA2/Omi, cleaved caspase-3, caspase-7 and caspase-9 was observed in the myocardium. The apoptosis index of cardiomyocytes further supports the cardioprotective effect of tilianin. Additionally, compared with the MIRI model group, pretreatment with high dose-tilianin group upregulated phosphorylated Akt and PI3K. In contrast, using the PI3K inhibitor LY294002 to block Akt activation effectively inhibited the protective effects of tilianin against MIRI. Tilianin pretreatment was beneficial for activating the PI3K/Akt signaling pathway and inhibiting myocardial apoptosis.

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“…Response surface methodology (RSM) is a combination of mathematical and statistical techniques that is useful for modeling and analysis. RSM analyzes response surface contours to identify optimal process parameters and uses multiple quadratic regression equations to determine the fit between factors and response functions [ 24 , 25 ]. Given its many advantages, RSM has been widely used to optimize and model liposome preparation conditions.…”

Section: Introductionmentioning

confidence: 99%

Optimization of Conditions for Cyanidin-3-OGlucoside (C3G) Nanoliposome Production by Response Surface Methodology and Cellular Uptake Studies in Caco-2 Cells

et al. 2017

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We aimed to optimize the formulation of C3G nanoliposomes using response surface methodology. Additionally, we evaluated the stability, particle change, and encapsulation efficiency (EE) of C3G nanoliposomes under different temperatures and storage durations, as well as in simulated gastrointestinal juice (SGF) and simulated intestinal fluid. The morphology of C3G nanoliposomes was observed by transmission electron microscope. The ability of C3G nanoliposomes to affect cancer cell morphology and inhibit cancer cell proliferation was studied with Caco-2 cells. Reverse-phase evaporation method is a simple and efficient method for liposome preparation. The optimal preparation conditions for this method were as follows: C3G concentration of 0.17 mg/mL, phosphatidylcholine/cholesterol ratio of 2.87, and rotary evaporation temperature of 41.41 °C. At optimal conditions, the particle size and EE of the C3G nanoliposomes were 165.78 ± 4.3 nm and 70.43% ± 1.95%, respectively. The C3G nanoliposomes showed an acceptable stability in SGF at 37 °C for 4 h, but were unstable under extended storage durations and high temperatures. Moreover, our results showed that different concentrations of C3G nanoliposomes affected the morphology and inhibited the proliferation of Caco-2 cells.

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Optimization of the process variables of tilianin-loaded composite phospholipid liposomes based on response surface-central composite design and pharmacokinetic study

Cited by 29 publications

References 23 publications

Tilianin Extracted From Dracocephalum moldavica L. Induces Intrinsic Apoptosis and Drives Inflammatory Microenvironment Response on Pharyngeal Squamous Carcinoma Cells via Regulating TLR4 Signaling Pathways

Tilianin Extracted From Dracocephalum moldavica L. Induces Intrinsic Apoptosis and Drives Inflammatory Microenvironment Response on Pharyngeal Squamous Carcinoma Cells via Regulating TLR4 Signaling Pathways

Cardioprotection of tilianin ameliorates myocardial ischemia-reperfusion injury: Role of the apoptotic signaling pathway

Optimization of Conditions for Cyanidin-3-OGlucoside (C3G) Nanoliposome Production by Response Surface Methodology and Cellular Uptake Studies in Caco-2 Cells

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