scholarly journals In vitro and in vivo anticancer effect of pH-responsive paclitaxel-loaded niosomes

2021 ◽  
Vol 32 (12) ◽  
Author(s):  
Mahmood Barani ◽  
Mohammad Reza Hajinezhad ◽  
Saman Sargazi ◽  
Abbas Rahdar ◽  
Sheida Shahraki ◽  
...  
Keyword(s):  
Cell Lines ◽  
Biochemical Parameters ◽  
Morphological Changes ◽  
Liver Lipid ◽  
In Vitro Release ◽  
Serum Biochemical Parameters ◽  
Ph Responsive ◽  
Serum Biochemical

AbstractIn this study, paclitaxel (PTX)-loaded pH-responsive niosomes modified with ergosterol were developed. This new formulation was characterized in terms of size, morphology, encapsulation efficiency (EE), and in vitro release at pH 5.2 and 7.4. The in vitro efficacy of free PTX and niosome/PTX was assessed using MCF7, Hela, and HUVEC cell lines. In order to evaluate the in vivo efficacy of niosomal PTX in rats as compared to free PTX, the animals were intraperitoneally administered with 2.5 mg/kg and 5 mg/kg niosomal PTX for two weeks. Results showed that the pH-responsive niosomes had a nanometric size, spherical morphology, 77% EE, and pH-responsive release in pH 5.2 and 7.4. Compared with free PTX, we found markedly lower IC50s when cancer cells were treated for 48 h with niosomal PTX, which also showed high efficacy against human cancers derived from cervix and breast tumors. Moreover, niosomal PTX induced evident morphological changes in these cell lines. In vivo administration of free PTX at the dose of 2.5 mg/kg significantly increased serum biochemical parameters and liver lipid peroxidation in rats compared to the control rats. The situation was different when niosomal PTX was administered to the rats: the 5 mg/kg dosage of niosomal PTX significantly increased serum biochemical parameters, but the group treated with the 2.5 mg/kg dose of niosomal PTX showed fewer toxic effects than the group treated with free PTX at the same dosage. Overall, our results provide proof of concept for encapsulating PTX in niosomal formulation to enhance its therapeutic efficacy.

scholarly journals Simulation, In Vitro, and In Vivo Cytotoxicity Assessments of Methotrexate-loaded pH-Responsive Nanocarriers

Polymers ◽  
2021 ◽  
Vol 13 (18) ◽  
pp. 3153
Author(s):  
Mahmood Barani ◽  
Mohammad Reza Hajinezhad ◽  
Saman Sargazi ◽  
Mahira Zeeshan ◽  
Abbas Rahdar ◽  
...  
Keyword(s):  
Serum Creatinine ◽  
Morphological Changes ◽  
Intraperitoneal Administration ◽  
Strong Hydrogen Bond ◽  
Ph Responsive ◽  
Mcf7 Cells ◽  
Serum Blood Urea Nitrogen ◽  
Span 60

In this study, pH-responsive niosomal methotrexate (MTX) modified with ergosterol was prepared for potential anticancer application. The prepared formulation had a size of 176.7 ± 3.4 nm, zeta potential of −31.5 ± 2.6 mV, EE% of 76.9 ± 2.5%, and a pH-responsive behavior in two different pHs (5.4 and 7.4). In-silico evaluations showed that MTX intended to make a strong hydrogen bond with Span 60 compartments involving N2 and O4 atoms in glutamic acid and N7 atom in pteridine ring moieties, respectively. The cytotoxic effects of free and pH-MTX/Nio were assessed against MCF7 and HUVECs. Compared with free MTX, we found significantly lower IC50s when MCF7 cells were treated with niosomal MTX (84.03 vs. 9.464 µg/mL after 48 h, respectively). Moreover, lower cell killing activity was observed for this formulation in normal cells. The pH-MTX/Nio exhibited a set of morphological changes in MCF7 cells observed during cell death. In-vivo results demonstrated that intraperitoneal administration of free MTX (2 mg/kg) after six weeks caused a significant increase in serum blood urea nitrogen (BUN), serum creatinine, and serum malondialdehyde (MDA) levels of rats compared to the normal control rats. Treatment with 2 and 4 mg/kg doses of pH-MTX/Nio significantly increased serum BUN, serum creatinine, and serum lipid peroxidation. Still, the safety profile of such formulations in healthy cells/tissues should be further investigated.

Efficacy of biotechnologically derived product in counteracting ill effects of aflatoxins in broiler chicken

2016 ◽  
Author(s):  
C. Basavanta Kumar ◽  
B. S.V. Reddy ◽  
R. G. Gloridoss ◽  
T. M. Prabhu ◽  
D. S. Wodeyar ◽  
...  
Keyword(s):  
Biochemical Parameters ◽  
Broiler Chicken ◽  
Basal Diet ◽  
Cellular Level ◽  
Performance Parameters ◽  
Adsorption Study ◽  
Sodium Calcium ◽  
Serum Biochemical

A preliminary in-vitro aflatoxin adsorption study was conducted, and it was found that, the degradability of aflatoxin (AF) by the biotechnologically derived product (BTP) was similar to that of hydrated sodium calcium allumino-sillicate (HSCAS) and mannan ologosachharide (MOS). Further, an in-vivo trial was undertaken to assess BTP over HSCAS in broiler chicken fed diet containing aflatoxin (AF) with experimental design: T1-basal diet; T2-250 ppb of AF; T3-AF 250 ppb with HSCAS at 1 kg/ton; T4 and T5-AF 250 ppb with BTP 200 g/ton and 400 g/ton, respectively. During 42 days, trial revealed non-significant differences in performance parameters, dressing percentage, relative organ weights and serum biochemical parameters among treatments. Whereas, serum profile of ALT (P<0.01) and AST (P<0.05) was significantly increased with addition of AF (T2) indicating limitation of toxicity only to cellular level at liver. Addition of BTP was found to normalize the increased ALT and AST levels.

scholarly journals Fra-1 Induces Morphological Transformation and Increases In Vitro Invasiveness and Motility of Epithelioid Adenocarcinoma Cells

1998 ◽  
Vol 18 (12) ◽  
pp. 7095-7105 ◽  
Author(s):  
Olga Kustikova ◽  
Dmitrii Kramerov ◽  
Mariam Grigorian ◽  
Vladimir Berezin ◽  
Elisabeth Bock ◽  
...  
Keyword(s):  
Tumor Progression ◽  
Cell Lines ◽  
Transcriptional Activation ◽  
Morphological Changes ◽  
Critical Role ◽  
Morphological Transformation ◽  
Morphological Alterations ◽  
Nuclear Extracts

ABSTRACT Two cell lines originating from a common ancestral tumor, CSML0 and CSML100, were used as a model to study AP-1 transcription factors at different steps of tumor progression. CSML0 cells have an epithelial morphology; they express epithelial but not mesenchymal markers and are invasive neither in vitro nor in vivo. CSML100 possesses all characteristics of a highly progressive carcinoma. These cells do not form tight contacts, are highly invasive in vitro, and are metastatic in vivo. AP-1 activity was considerably higher in CSML100 cells than in CSML0 cells. There was a common predominant Jun component, namely, JunD, detected in both cell lines. We found that the enhanced level of AP-1 in CSML100 cells was due to high expression of Fra-1 and Fra-2 proteins, which were undetectable in CSML0 nuclear extracts. Analysis of the transcription of different AP-1 members in various cell lines derived from tumors of epithelial origin revealed a correlation of fra-1 expression with mesenchymal characteristics of carcinoma cells. Moreover, we show here for the first time that the expression of exogenous Fra-1 in epithelioid cells results in morphological changes that resemble fibroblastoid conversion. Cells acquire an elongated shape and become more motile and invasive in vitro. Morphological alterations were accompanied by transcriptional activation of certain genes whose expression is often induced at late stages of tumor progression. These data suggest a critical role of the Fra-1 protein in the development of epithelial tumors.

Reliability of a Single β-Thromboglobulin Measurement in a Diabetic Population : Importance of PGE1 in Anticoagulant Mixture

1987 ◽  
Vol 57 (02) ◽  
pp. 201-204 ◽  
Author(s):  
P Y Scarabin ◽  
L Strain ◽  
C A Ludlam ◽  
J Jones ◽  
E M Kohner
Keyword(s):  
In Vitro Release ◽  
Mean Value ◽  
Reliable Estimate ◽  
Diabetic Patients ◽  
Single Measurement ◽  
Diabetic Population ◽  
The Difference ◽  
Vitro Release

SummaryDuring the collection of samples for plasma β-thromboglobulin (β-TG) determination, it is well established that artificially high values can be observed due to in-vitro release. To estimate the reliability of a single β-TG measurement, blood samples were collected simultaneously from both arms on two separate occasions in 56 diabetic patients selected for a clinical trial. From each arm, blood was taken into two tubes containing an anticoagulant mixture with (tube A) and without (tube B) PGE!. The overall mean value of B-TG in tube B was 1.14 times higher than in tube A (p <0.01). The markedly large between-arms variation accounted for the most part of within-subject variation in both tubes and was significantly greater in tube B than in tube A. Based on the difference between B-TG values from both arms, the number of subjects with artifically high B-TG values was significantly higher in tube B than in tube A on each occasion (overall rate: 28% and 14% respectively). Estimate of between-occasions variation showed that B-TG levels were relatively stable for each subject between two occasions in each tube. It is concluded that the use of PGEi decreases falsely high B-TG levels, but a single measurement of B-TG does not provide a reliable estimate of the true B-TG value in vivo.

Serum biochemical parameters in piglets after the application of essential oils

Planta Medica ◽  
2007 ◽  
Vol 73 (09) ◽  
Author(s):  
J Poracova ◽  
I Salamon ◽  
B Taylorova ◽  
M Zahatnanska ◽  
I Sutiakova
Keyword(s):  
Essential Oils ◽  
Biochemical Parameters ◽  
Serum Biochemical Parameters ◽  
Serum Biochemical

Evaluating The Potential Toxic Effect of Aflatoxin and Ochratoxin on Serum Biochemical Parameters in Coloured (Raja Ii) Broilers

2012 ◽  
Vol 3 (8) ◽  
pp. 215-217
Author(s):  
Dr Jayashree Pattar ◽  
◽  
Dr Shridhar,N.B Dr Shridhar,N.B ◽  
Dr Jagadeesh .S Sanganal ◽  
Dr M.L Satyanarayana Dr M.L Satyanarayana ◽  
...  
Keyword(s):  
Toxic Effect ◽  
Biochemical Parameters ◽  
Serum Biochemical Parameters ◽  
Serum Biochemical

Fenofibrate Solid Dispersion for Improving Oral Bioavailability: Preparation, and Characterization and in vivo Evaluation

2020 ◽  
Vol 13 (5) ◽  
pp. 5102-5109
Author(s):  
Venu Madhav K ◽  
Somnath De ◽  
Chandra Shekar Bonagiri ◽  
Sridhar Babu Gummadi
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation

Fenofibrate (FN) is used in the treatment of hypercholesterolemia. It shows poor dissolution and poor oral bioavailability after oral administration due to high liphophilicity and low aqueous solubility. Hence, solid dispersions (SDs) of FN (FN-SDs) were develop that might enhance the dissolution and subsequently oral bioavailability. FN-SDs were prepared by solvent casting method using different carriers (PEG 4000, PEG 6000, β cyclodextrin and HP β cyclodextrin) in different proportions (0.25%, 0.5%, 0.75% and 1% w/v). FN-SDs were evaluated solubility, assay and in vitro release studies for the optimization of SD formulation. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) analysis was performed for crystalline and morphology analysis, respectively. Further, optimized FN-SD formulation evaluated for pharmacokinetic performance in Wistar rats, in vivo in comparison with FN suspension.  From the results, FN-SD3 and FN-SD6 have showed 102.9 ±1.3% and 105.5±3.1% drug release, respectively in 2 h. DSC and PXRD studies revealed that conversion of crystalline to amorphous nature of FN from FT-SD formulation. SEM studies revealed the change in the orientation of FN when incorporated in SDs. The oral bioavailability FN-SD3 and FN-SD6 formulations exhibited 2.5-folds and 3.1-folds improvement when compared to FN suspension as control. Overall, SD of FN could be considered as an alternative dosage form for the enhancement of oral delivery of poorly water-soluble FN.

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