Glibenclamide Mini-tablets with an Enhanced Pharmacokinetic and Pharmacodynamic Performance

Tawfeek, Hesham M.; Roberts, Matthew; Hamd, Mohamed A. El; Abdellatif, Ahmed A. H.; Younis, Mahmoud A.

doi:10.1208/s12249-018-1108-y

Cited by 19 publications

(7 citation statements)

References 32 publications

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“…The encapsulation of pheo-a with EC was used to enhance the solubility and spreadability of the final product, and hence to decrease its side effects on the stomach due to ethyl cellulose requires a pH above 7 for release. Furthermore, this ethyl cellulose polymer is cheap, safe, and available [21,22].…”

Section: Introductionmentioning

confidence: 99%

Formulation of Ethyl Cellulose Microparticles Incorporated Pheophytin A Isolated from Suaeda vermiculata for Antioxidant and Cytotoxic Activities

et al. 2019

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Background: This study is designed to discover a method for delivering an efficient potent pheophytin a (pheo-a) into more absorbed and small polymeric ethyl cellulose (EC) microparticles. Methods: Silica gel and Sephadex LH-20 columns were used to isolate pheo-a from the chloroform extract of the edible plant, Suaeda vermiculata. Pheo-a was incorporated into EC microparticles using emulsion-solvent techniques. The antioxidant activity of pheo-a microparticles was confirmed by the level of superoxide radical (SOD), nitric oxide (NO), and reducing power (RP) methods. Meanwhile, the cytotoxic effect of the product was investigated on MCF-7 cells using MTT assay. Results: Pheo-a was isolated from S. vermiculata in a 12% concentration of the total chloroform extract. The structures were confirmed by NMR and IR spectroscopic analysis. The formulated microparticles were uniform, completely dispersed in the aqueous media, compatible as ingredients, and had a mean diameter of 139 ± 1.56 µm as measured by a particle size analyzer. Pheo-a demonstrated a valuable antioxidant activity when compared with ascorbic acid. The IC50 values of pheo-a microparticles were 200.5 and 137.7 µg/mL for SOD, and NO respectively. The reducing power of pheo-a microparticles was more potent than ascorbic acid and had a 4.2 µg/mL for IC50 value. Pheo-a microparticles did not show notable cytotoxicity on the MCF-7 cell line (IC50 = 35.9 µg/mL) compared with doxorubicin (IC50 = 3.2 µg/mL). Conclusions: the results showed that water-soluble pheo-a microparticles were prepared with a valuable antioxidant activity in a wide range of concentrations with a noteworthy cytotoxic effect.

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Section: Introductionmentioning

confidence: 99%

Formulation of Ethyl Cellulose Microparticles Incorporated Pheophytin A Isolated from Suaeda vermiculata for Antioxidant and Cytotoxic Activities

et al. 2019

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“…Glibenclamide is an oral drug classified as sulfonylurea, used as an antidiabetic drug (15,20,21). In patients with hyperglycemia, this drug works by stimulating insulin production from pancreatic beta cells (22).…”

Section: Discussionmentioning

confidence: 99%

Antidiabetic of Hylocereus polyrhizus peel ethanolic extract on alloxan induced diabetic mice

Solikhah

Rani

Septiani

et al. 2022

IJVS

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Diabetes is a disease characterized by high blood glucose due to the abnormal response of the cells in the body on produced insulin or insulin resistance. Indeed, the treatment for diabetes mellitus lasts for a lifetime and causes various side effects, such as headache, hypoglycemia, vomiting, and gastrointestinal symptoms. Interestingly, Dragon fruit has potent antidiabetic activity and without side effects. Thirty Wistar mice were included in the study. Alloxan with a dose of 150 mg/kg was injected intraperitoneally to all groups except the standard control group. Mice with blood glucose levels higher than 200 mg/dL were considered diabetic and employed throughout the study. Mice were divided into five groups: standard control group without alloxan, diabetic control group with alloxan, treatment group of 100 mg/kg and 300mg/kg H. polyrhizus peel extract, and positive control group with 600 µg/kg glibenclamide. All treatments were given orally. Blood glucose level was checked on day 1, 7, and 14 on all groups using Accu-check instant glucometer. This study revealed that administration of alloxan to the diabetic control group significantly increased blood glucose level compared to the normal control group on day-1, 7, and 14 (P < 0.05). In addition, administration of H. polyrhizus peel extract and glibenclamide effectively decreases blood glucose levels, especially on day-7 and 14 compared to the control group (P<0.05).

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“…One millilitre of this solution was diluted with the phosphate buffer to 25 mL in a volumetric flask. The ETO content of the solution was then analysed spectrophotometrically at 317 nm using a UV/Vis spectrophotometer (Ultraviolet double beam Spectrophotometer 1601, Shimadzu, Japan) against a blank solution that was prepared in the same manner using empty microparticles [9,15,16].…”

Section: Determination Of Eto Drug Content In the Ethylcellulose Microparticlesmentioning

confidence: 99%

Freeze-Drying Ethylcellulose Microparticles Loaded with Etoposide for In Vitro Fast Dissolution and In Vitro Cytotoxicity against Cancer Cell Types, MCF-7 and Caco-2

et al. 2021

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The aim of this study was to improve the solubility of etoposide–ethylcellulose (ET–ETO) microparticles using the freeze-drying technique. Ethylcellulose (EC) microparticles loaded with etoposide (ETO) were prepared with different drug–polymer molar ratios of 1:1, 1:3, 1:6, and 1:20 by the solvent evaporation method. The size of the prepared microparticles was 0.088 µm. The results showed that the amount of ETO encapsulated into the microparticles was 387.3, 365.0, 350.0, and 250 µg/50 mg microparticles for microparticles with drug–polymer ratios of 1:1, 1:3, 1:6, and 1:20, respectively. The FT-IR spectra showed no chemical interaction between ETO and the polymer in the solid state. The results obtained from the dissolution experiment showed that the freeze-dried microparticles were stable in 0.1 N HCl (gastric pH) for 2 h. At pH 7.4, the ETO release was 60 to 70% within the first 15 min and approximately 100% within 30 min. Results from the application of different dissolution models showed that the equations that best fit the dissolution data for the ET–ETO microparticles at pH 7.4 were the Higuchi and Peppas model equations. The in vitro cytotoxicity assay of free ETO and freeze-dried microspheres prepared in this study with a drug–polymer ratio of 1:1 was performed in two mammalian cancer cell lines, MCF-7 (for bone cancer of the mammary organ) and Caco-2 (for mammalian epithelial colorectal adenocarcinoma). The results showed that the half-maximal inhibitory concentrations (IC50 values) for ETO and freeze-dried ET–ETO microparticles were 18.6 µM and 27.1 µM, respectively. In conclusion, freeze-dried ET–ETO is a promising formulation for developing a fast-dissolving form of ETO with a significant antiproliferative activity against the tested cell lines used in this study. It is a promising formulation for local duodenal area targeting.

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Glibenclamide Mini-tablets with an Enhanced Pharmacokinetic and Pharmacodynamic Performance

Cited by 19 publications

References 32 publications

Formulation of Ethyl Cellulose Microparticles Incorporated Pheophytin A Isolated from Suaeda vermiculata for Antioxidant and Cytotoxic Activities

Formulation of Ethyl Cellulose Microparticles Incorporated Pheophytin A Isolated from Suaeda vermiculata for Antioxidant and Cytotoxic Activities

Antidiabetic of Hylocereus polyrhizus peel ethanolic extract on alloxan induced diabetic mice

Freeze-Drying Ethylcellulose Microparticles Loaded with Etoposide for In Vitro Fast Dissolution and In Vitro Cytotoxicity against Cancer Cell Types, MCF-7 and Caco-2

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