In vitro and in vivo evaluation of enzymatic and antioxidant activity, cytotoxicity and genotoxicity of curcumin-loaded solid dispersions

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.

Download Full-text

In vitro and in vivo evaluation of antioxidant activity of Petasites japonicus Maxim. flower buds extracts

Bioscience Biotechnology and Biochemistry ◽

10.1080/09168451.2019.1691913 ◽

2019 ◽

Vol 84 (3) ◽

pp. 621-632 ◽

Cited By ~ 2

Author(s):

Miki Hiemori-Kondo ◽

Mika Nii

Keyword(s):

Antioxidant Activity ◽

Flower Buds ◽

In Vivo Evaluation ◽

Petasites Japonicus

Download Full-text

PREPARATION AND IN VIVO EVALUATION OF CANDESARTAN CILEXETIL SOLID DISPERSIONS

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2021.v14i8.42037 ◽

2021 ◽

pp. 129-133

Author(s):

UPPULURU ASHOK KUMAR ◽

GANDE SURESH

Keyword(s):

Candesartan Cilexetil ◽

Solid Dispersions ◽

Selective Laser Sintering ◽

In Vitro Release ◽

In Vivo Studies ◽

In Vivo Evaluation ◽

Enhanced Solubility ◽

Pure Drug

Objective: The present study aims at development of solid dispersions (SD) of candesartan cilexetil for enhanced solubility and bioavailability. Methods: About 18 SD formulations of candesartan cilexetil were prepared by solvent evaporation technique and evaluated. The in vitro release studies were conducted and the best formulation chosen was further characterized for Fourier transform infrared spectroscopy, Scanning electron microscope, X-ray, and stability. The in vivo evaluation study conducted in rats. Results: The formulation SD16 containing drug and Soluplus in 1:3 ratio along with 2% selective laser sintering was chosen optimal based on drug content (99.08%), and drug release (99.7%). In vivo studies conducted on SD16 showed that mean time to peak concentration (Tmax) was 2.0±0.05 and 4±0.2 h for the optimized and pure drug, respectively, while mean maximum drug concentration (Cmax) was 570.63±2.65 ng/mL and was significant as compared to the candesartan pure drug 175.146±0.07 ng/mL. Area under curve AUC0-∞ infinity for candesartan SD16 was higher (4860.61±1.05 ng.h/ml) than pure drug suspension 1480±1.72 ng.h/ml. Conclusion: Hence, the developed SD formulations enhanced the bioavailability of drug by 3 folds.

Download Full-text

In Vitro and In Vivo Evaluation of Amorphous Solid Dispersions Generated by Different Bench-Scale Processes, Using Griseofulvin as a Model Compound

The AAPS Journal ◽

10.1208/s12248-013-9469-3 ◽

2013 ◽

Vol 15 (2) ◽

pp. 608-617 ◽

Cited By ~ 20

Author(s):

Po-Chang Chiang ◽

Yong Cui ◽

Yingqing Ran ◽

Joe Lubach ◽

Kang-Jye Chou ◽

...

Keyword(s):

Model Compound ◽

Solid Dispersions ◽

Amorphous Solid ◽

Amorphous Solid Dispersions ◽

In Vivo Evaluation ◽

Bench Scale

Download Full-text

Cellulose derivatives as effective recrystallization inhibitor for ternary ritonavir solid dispersions: In vitro-in vivo evaluation

Carbohydrate Polymers ◽

10.1016/j.carbpol.2021.118562 ◽

2021 ◽

Vol 273 ◽

pp. 118562

Author(s):

Qingran Guan ◽

Qisan Ma ◽

Yanna Zhao ◽

Xinxin Jiang ◽

Huaizhen Zhang ◽

...

Keyword(s):

Solid Dispersions ◽

Cellulose Derivatives ◽

In Vivo Evaluation

Download Full-text

Formulation, In Vitro and In Vivo Evaluation of Gefitinib Solid Dispersions Prepared Using Different Techniques

Processes ◽

10.3390/pr9071210 ◽

2021 ◽

Vol 9 (7) ◽

pp. 1210

Author(s):

Sultan Alshehri ◽

Abdullah Alanazi ◽

Ehab M. Elzayat ◽

Mohammad A. Altamimi ◽

Syed S. Imam ◽

...

Keyword(s):

Oral Absorption ◽

Solid Dispersions ◽

Water Soluble ◽

In Vitro Dissolution ◽

Pharmacokinetic Parameters ◽

Pharmacokinetic Studies ◽

In Vivo Evaluation ◽

Significant Release

Gefitinib (Gef) is a poorly water-soluble antitumor drug, which shows poor absorption/bioavailability after oral administration. Therefore, this study was carried out to develop Gef solid dispersions (SDs) using different carriers and different techniques in order to enhance its dissolution and oral absorption/bioavailability. Various SD formulations of Gef were established using fusion and microwave methods utilizing Soluplus, Kollidone VA64, and polyethylene glycol 4000 (PEG 4000) as the carriers. Developed SDs of Gef were characterized physicochemically and evaluated for in vitro dissolution and in vivo pharmacokinetic studies. The physicochemical evaluation revealed the formation of Gef SDs using fusion and microwave methods. In vitro dissolution studies indicated significant release of Gef from all SDs compared to the pure Gef. Optimized SD of Gef (S2-MW) presented significant release of Gef (82.10%) compared with pure Gef (21.23%). The optimized Gef SD (S2) was subjected to in vivo pharmacokinetic evaluation in comparison with pure Gef in rats. The results indicated significant enhancement in various pharmacokinetic parameters of Gef from an optimized SD S2 compared to the pure Gef. In addition, Gef-SD S2 resulted in remarkable improvement in bioavailability compared to the pure Gef. Overall, this study suggested that the prepared Gef-SD by microwave method showed marked enhancement in dissolution and bioavailability.

Download Full-text

Modification of In Vitro and In Vivo Antioxidant Activity by Consumption of Cooked Chickpea in a Colon Cancer Model

Nutrients ◽

10.3390/nu12092572 ◽

2020 ◽

Vol 12 (9) ◽

pp. 2572 ◽

Cited By ~ 2

Author(s):

María S. Cid-Gallegos ◽

Xariss M. Sánchez-Chino ◽

Isela Álvarez-González ◽

Eduardo Madrigal-Bujaidar ◽

Verónica R. Vásquez-Garzón ◽

...

Keyword(s):

Colon Cancer ◽

Antioxidant Activity ◽

Nutritional Composition ◽

Standard Diet ◽

In Vivo Evaluation ◽

Phytochemical Compounds ◽

Nutritional Compounds ◽

In Vitro Antioxidant Activity

Chickpea has been classified as a nutraceutical food due to its phytochemical compounds, showing antioxidant, anti-inflammatory, and anticancer activity. To investigate this, we evaluated the effect of cooking on the nutritional and non-nutritional composition and the in vitro and in vivo antioxidant activity of chickpea seed. The latter was determined by the variation in the concentration of nitric oxide (NO), oxidized carbonyl groups (CO), malondialdehyde (MDA), and the expression of 4-hydroxy-2-nonenal (4-HNE) in the colon of male BALB/c mice fed with a standard diet with 10 and 20% cooked chickpea (CC). We induced colon cancer in mice by administering azoxymethane/dextran sulfate sodium (AOM/DSS); for the evaluation, these were sacrificed 1, 7, and 14 weeks after the induction. Results show that cooking does not significantly modify (p < 0.05) nutritional compounds; however, it decreases the concentration of non-nutritional ones and, consequently, in vitro antioxidant activity. The in vivo evaluation showed that animals administered with AOM/DSS presented higher concentrations of NO, CO, MDA, and 4-HNE than those in animals without AOM/DSS administration. However, in the three evaluated times, these markers were significantly reduced (p < 0.05) with CC consumption. The best effect on the oxidation markers was with the 20% CC diet, demonstrating the antioxidant potential of CC.

Download Full-text

PHYTOCHEMICAL EVALUATION AND ANTIOXIDANT SCREENING STUDIES OF OCIMUM TENUIFLORUM LINN SEEDS

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2017.v10s4.21341 ◽

2017 ◽

Vol 10 (16) ◽

pp. 76 ◽

Cited By ~ 1

Author(s):

Jyotsana Sharma ◽

Navneet Khurana ◽

Neha Sharma ◽

Rakesh Garg

Keyword(s):

Antioxidant Activity ◽

In Vivo Evaluation ◽

Pathological Conditions ◽

Dpph Method ◽

Physicochemical Evaluation ◽

Ocimum Tenuiflorum ◽

Cell Inhibition ◽

In Vitro Antioxidant Activity

Objective: In the existing study, Ocimum tenuiflorum was assessed for its antioxidant activity. This activity was assessed using the 2,2-diphenyl-1- picrylhydrazyl (DPPH) method. The drug was identified and standardized on the basis of organoleptic, negligible characters and its quantitative physicochemical standards.Methods: Preliminary phytochemical screening was also carried out to examine out the presence of various phytoconstituents. It revealed the presence of alkaloids, phytosterols, resin, flavonoids, tannins, diterpenes, and protein in the seed extract. DPPH method was done used for evaluating the antioxidant activity.Results: It has been observed that different concentrations (100, 200, 300, 400, and 500 μg/mL) used had shown 82.1%, 83.4%, 86.6%, 89.1%, and 93.2% of cell inhibition, respectively.Conclusion: Thus, the present study on pharmacognostic standardization, physicochemical evaluation and in vitro antioxidant activity of O. tenuiflorum seed would be useful to supplement information in regard to its in vivo evaluation for different pathological conditions.

Download Full-text