In vitro and in vivo studies of pharmacokinetics and antitumor efficacy of D07001-F4, an oral gemcitabine formulation

2012 ◽  
Vol 71 (2) ◽  
pp. 379-388 ◽  
Author(s):  
Wei-Hua Hao ◽  
Jong-Jing Wang ◽  
Shu-Ping Hsueh ◽  
Pei-Jing Hsu ◽  
Li-Chien Chang ◽  
...  
Keyword(s):  
Antitumor Efficacy ◽  
In Vivo Studies

scholarly journals Nano-encapsulated tryptanthrin derivative for combined anticancer therapy via inhibiting indoleamine 2,3-dioxygenase and inducing immunogenic cell death

Nanomedicine ◽  
2019 ◽  
Vol 14 (18) ◽  
pp. 2423-2440 ◽  
Author(s):  
Canyu Yang ◽  
Bing He ◽  
Qiang Zheng ◽  
Dakuan Wang ◽  
Mengmeng Qin ◽  
...  
Keyword(s):  
Cell Death ◽  
Single Agent ◽  
Tumor Burden ◽  
Antitumor Efficacy ◽  
In Vivo Studies ◽  
Immunogenic Cell Death ◽  
Indoleamine 2,3 Dioxygenase ◽  
Tumor Tissues

Aim: We developed a polycaprolactone-based nanoparticle (NP) to encapsulate tryptanthrin derivative CY-1-4 and evaluated its antitumor efficacy. Materials & methods: CY-1-4 NPs were prepared and evaluated for their cytotoxicity and associated mechanisms, indoleamine 2,3-dioxygenase (IDO)-inhibitory ability, immunogenic cell death (ICD)-inducing ability and antitumor efficacy. Results: CY-1-4 NPs were 123 nm in size. In vitro experiments indicated that they could both induce ICD and inhibit IDO. In vivo studies indicated that a medium dose reduced 58% of the tumor burden in a B16-F10-bearing mouse model, decreased IDO expression in tumor tissues and regulated lymphocytes subsets in spleen and tumors. Conclusion: CY-1-4 is a potential antitumor candidate that could act as a single agent with combined functions of IDO inhibition and ICD induction.

scholarly journals Biocompatible Nanoparticles as a Platform for Enhancing Antitumor Efficacy of Cisplatin–Tetradrine Combination

2021 ◽  
Vol 16 (1) ◽  
Author(s):  
Fangcen Liu ◽  
Xinyue Wang ◽  
Qin Liu ◽  
Huan Zhang ◽  
Li Xie ◽  
...  
Keyword(s):  
Side Effects ◽  
Double Emulsion ◽  
Antitumor Efficacy ◽  
In Vivo Studies ◽  
Pet Ct ◽  
Pharmacokinetic Properties ◽  
Metabolic Activities ◽  
Fdg Pet Ct

AbstractCombination therapy has been a standard strategy in the clinical tumor treatment. We have demonstrated that combination of Tetradrine (Tet) and Cisplatin (CDDP) presented a marked synergistic anticancer activity, but inevitable side effects limit their therapeutic concentration. Considering the different physicochemical and pharmacokinetic properties of the two drugs, we loaded them into a nanovehicle together by the improved double emulsion method. The nanoparticles (NPs) were prepared from the mixture of poly(ethyleneglycol)–polycaprolactone (PEG–PCL) and polycarprolactone (HO-PCL), so CDDP and Tet can be located into the NPs simultaneously, resulting in low interfering effect and high stability. Images from fluorescence microscope revealed the cellular uptake of both hydrophilic and hydrophobic agents delivered by the NPs. In vitro studies on different tumor cell lines and tumor tissue revealed increased tumor inhibition and apoptosis rates. As to the in vivo studies, superior antitumor efficacy and reduced side effects were observed in the NPs group. Furthermore, 18FDG-PET/CT imaging demonstrated that NPs reduced metabolic activities of tumors more prominently. Our results suggest that PEG–PCL block copolymeric NPs could be a promising carrier for combined chemotherapy with solid efficacy and minor side effects.

scholarly journals Sonodynamic and sono-photodynamic therapy in oncology

2019 ◽  
Vol 8 (2) ◽  
pp. 31-46
Author(s):  
D. A. Tzerkovsky ◽  
E. L. Protopovich ◽  
D. S. Stupak
Keyword(s):  
Photodynamic Therapy ◽  
Aminolevulinic Acid ◽  
Pulse Frequency ◽  
Antitumor Efficacy ◽  
In Vivo Studies ◽  
Malignant Neoplasms ◽  
Serious Adverse Events ◽  
Treatment Methods

In the present publication, authors have analyzed the results of using sonodynamic and sono-photodynamic therapy with photosensitizing agents of various classes (hematoporphyrin, 5-aminolevulinic acid, chlorin derivatives, etc.) in experimental oncology. In a number of in vitro and in vivo studies, the high antitumor efficacy of the above treatment methods has been proven. Ultrasonic treatment with a pulse frequency of 1–3 MHz and an intensity of 0.7 to 5 W/cm2 , independently and in combination with photo-irradiation of experimental tumors, can significantly improve the cytotoxic properties of photosensitizers. This became the basisfor testing the methodsin patients with malignant neoplasms of various localizations. Scientists fromSouth-East Asia presented the preliminary results of the use of sonodynamic and sono-photodynamic therapy with photosensitizers in the treatment of malignant pathology of the mammary gland, stomach, esophagus, prostate, lung and brain. Analysis of the obtained data indicates the absence of serious adverse events and an increase in the antitumor efficacy of treatment, which included these treatment methods with chlorin-type photosensitizers. 

scholarly journals Biocompatible Nanoparticles as a Platform for Enhancing Antitumor Efficacy of Cisplatin-Tetradrine Combination

2021 ◽  
Author(s):  
Fangcen Liu ◽  
Xinyue Wang ◽  
Qin Liu ◽  
Huan Zhang ◽  
Li Xie ◽  
...  
Keyword(s):  
Side Effects ◽  
Double Emulsion ◽  
Antitumor Efficacy ◽  
In Vivo Studies ◽  
Pet Ct ◽  
Pharmacokinetic Properties ◽  
Metabolic Activities ◽  
Fdg Pet Ct

Abstract Combination therapy has been a standard strategy in the clinical tumor treatment. We have demonstrated that combination of Tetradrine (Tet) and Cisplatin (CDDP) presented a marked synergistic anticancer activity, but inevitable side effects limit their therapeutic concentration. Considering the different physicochemical and pharmacokinetic properties of the two drugs, we loaded them into a nanovehicle together by the improved double emulsion method. The nanoparticles (NPs) were prepared from the mixture of poly(ethyleneglycol)-polycaprolactone (PEG-PCL) and polycarprolactone (HO-PCL), so CDDP and Tet can be located into the NPs simultaneously, resulting in low interfering effect and high stability. Images from fluorescence microscope revealed the cellular uptake of both hydrophilic and hydrophobic agents delivered by the NPs. In vitro studies on different tumor cell lines and tumor tissue revealed increased tumor inhibition and apoptosis rates. As to the in vivo studies, superior antitumor efficacy and reduced side effects were observed in the NPs group. Furthermore, 18 FDG-PET/CT imaging demonstrated that NPs reduced metabolic activities of tumors more prominently. Our results suggest that PEG-PCL block copolymeric NPs could be a promising carrier for combined chemotherapy with solid efficacy and minor side effects.

Doxorubicin-loaded micelles of amphiphilic diblock copolymer with pendant dendron improve antitumor efficacy: In vitro and in vivo studies

2017 ◽  
Vol 534 (1-2) ◽  
pp. 136-143 ◽  
Author(s):  
Siew Hui Voon ◽  
Chin Siang Kue ◽  
Toyoko Imae ◽  
Wen Shang Saw ◽  
Hong Boon Lee ◽  
...  
Keyword(s):  
Diblock Copolymer ◽  
Antitumor Efficacy ◽  
In Vivo Studies ◽  
Amphiphilic Diblock Copolymer

In vitro and in vivo studies of new cationic Zn(II)‐benzonaphthoporphyrazines as photosensitizers for PDT

2001 ◽  
Vol 5 (8) ◽  
pp. 645-651
Author(s):  
M. Peeva ◽  
M. Shopova ◽  
U. Michelsen ◽  
D. Wöhrle ◽  
G. Petrov ◽  
...  
Keyword(s):  
In Vivo Studies

Effect of caffeine on theophyliine on cerebral blood flow response to brain activation: In vitro and in vivo studies

2005 ◽  
Vol 25 (1_suppl) ◽  
pp. S198-S198
Author(s):  
Joseph R Meno ◽  
Thien-son K Nguyen ◽  
Elise M Jensen ◽  
G Alexander West ◽  
Leonid Groysman ◽  
...  
Keyword(s):  
Blood Flow ◽  
Cerebral Blood Flow ◽  
Brain Activation ◽  
In Vivo Studies ◽  
Blood Flow Response ◽  
Flow Response

Effects of Unfractionated and Low Molecular Weight Heparins on Platelet Thromboxane Biosynthesis “In Vivo”

1994 ◽  
Vol 72 (06) ◽  
pp. 942-946 ◽  
Author(s):  
Raffaele Landolfi ◽  
Erica De Candia ◽  
Bianca Rocca ◽  
Giovanni Ciabattoni ◽  
Armando Antinori ◽  
...  
Keyword(s):  
Molecular Weight ◽  
Unfractionated Heparin ◽  
Low Molecular Weight Heparin ◽  
Primary Source ◽  
In Vivo Studies ◽  
Low Molecular Weight ◽  
Heparin Administration ◽  
To Receive

SummarySeveral “in vitro” and “in vivo” studies indicate that heparin administration may affect platelet function. In this study we investigated the effects of prophylactic heparin on thromboxane (Tx)A2 biosynthesis “in vivo”, as assessed by the urinary excretion of major enzymatic metabolites 11-dehydro-TxB2 and 2,3-dinor-TxB2. Twenty-four patients who were candidates for cholecystectomy because of uncomplicated lithiasis were randomly assigned to receive placebo, unfractionated heparin, low molecular weight heparin or unfractionaed heparin plus 100 mg aspirin. Measurements of daily excretion of Tx metabolites were performed before and during the treatment. In the groups assigned to placebo and to low molecular weight heparin there was no statistically significant modification of Tx metabolite excretion while patients receiving unfractionated heparin had a significant increase of both metabolites (11-dehydro-TxB2: 3844 ± 1388 vs 2092 ±777, p <0.05; 2,3-dinor-TxB2: 2737 ± 808 vs 1535 ± 771 pg/mg creatinine, p <0.05). In patients randomized to receive low-dose aspirin plus unfractionated heparin the excretion of the two metabolites was largely suppressed thus suggesting that platelets are the primary source of enhanced thromboxane biosynthesis associated with heparin administration. These data indicate that unfractionated heparin causes platelet activation “in vivo” and suggest that the use of low molecular weight heparin may avoid this complication.

Effectiveness of the integration of quercetin, turmeric, and N-acetylcysteine in reducing inflammation and pain associated with endometriosis. In-vitro and in-vivo studies

2020 ◽  
Vol 72 (5) ◽  
Author(s):  
Mario Fadin ◽  
Maria C. Nicoletti ◽  
Marzia Pellizzato ◽  
Manuela Accardi ◽  
Maria G. Baietti ◽  
...  
Keyword(s):  
In Vivo Studies
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