Enhancement of in vivo hypoglycemic effect of gliclazide by developing self-microemulsifying pellet dosage form

Patel, Hetal; Pandey, Niharika; Patel, Bhoomi; Ranch, Ketan M.; Bodiwala, Kunjan B.; Vyas, Bhavin

doi:10.1186/s43094-020-00034-0

Cited by 9 publications

(6 citation statements)

References 46 publications

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“…Furthermore, the optimized batch remained stable throughout the study period, suggesting that steric contributions from nonionic surfactants may promote stability in such systems. Our results are more promising than those reported by Patel et al, (17) . When the surface charge (Zeta potential) on oil globules is positively charged, emulsions become electrostatically attracted to the mucosal cell surface, resulting in increased drug bioavailability.…”

Section: Globule Size Zeta Potential Pi and Drug Contentsupporting

confidence: 73%

“…The study conducted by Patel et al also showed the highest solubility of Gliclazide in Capmul MCM C8 so used as oil for the development of SNEDDS. According to them, drug solubility is higher in medium-chain triglycerides (MCT) than in long-chain triglycerides (LCT) because MCT has a higher ester content per gram (17) . Our results are also consistent with already published research work.…”

Section: Saturation Solubility Studiesmentioning

confidence: 99%

“…In the present study, the globule size of the emulsion was found to be within the acceptable range for optimized formulation (C2) i.e., <100 nm (Figure 1 B) which might be helpful for the permeation of the drug delivery system through various biological membranes. Furthermore, the nonionic surfactant used in this study can also enhance the penetration of the EZE through epithelial lining by enhancing solubility and dissolution of the https://www.indjst.org/ drug as well as by reducing the interfacial tension between the two phases (17) . The results of globule size, zeta potential, and PI are presented in Table 3.…”

Section: Globule Size Zeta Potential Pi and Drug Contentmentioning

confidence: 99%

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Solubility Enhancement of Poorly Soluble Drug Ezetimibe by Developing Self Nano Emulsifying Drug Delivery System

Doke¹,

Khutle²,

Sharma³

et al. 2022

IJST

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Objectives: To enhance solubility, dissolution, and permeability of poorly water-soluble drug Ezetimibe (EZE) using a self-nano emulsifying drug delivery system (SNEDDS). Methods: Initially, the solubility of the EZE was determined in various oils and buffers. Surfactants and co-surfactants were screened based on the solubility of the drug in oil as per the emulsification efficacy test. Liquid SNEDDS was developed and characterized. Solid SNEDDS was developed and characterized using optimized liquid SNEDDS followed by the development of EZE-loaded Tablet SNEDDS. Finding: Liquid SNEDDS (L-SNEDDS) was formulated using Capmul MCM C8 EP, Cremophore RH 40, and Labrafil M 2125 CS as oil, surfactant, and co-surfactant respectively. Optimized L-SNEDDS formulation was found to be efficient with an average %T of 99.5%, drug content of 98.43%, flask inversion 0 numbers, and the average particle size of 36.7 nm, zeta potential of -57.5 mV, Polydispersibility index in of 0.119. Also, the in vitro release profile of drug from L-SNEDDS encapsulated in hard gelatin capsules was evaluated in different dissolution media viz. simulated gastric fluid and simulated intestinal fluid. For the drug, more than 95% cumulative release was observed within 30 min exclusive of the pH of the medium. The L-SNEDDS were adsorbed on a solid support and then mixed with tablet blends and compressed into tablets. Further, no adverse changes in globule size, shape, the zeta potential of SNEDDS, and dissolution profile were apparent on conversion to solid powder form and tablet form. Novelty: The developed liquid SNEDDS form of EZE showed enhanced solubility, dissolution, and permeability in comparison to pure drugs. Conversion of L-SNEDDS to P-SNEDDS would be a novel approach to overcome the limitations associated https://www.indjst.org/ 1504

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Section: Globule Size Zeta Potential Pi and Drug Contentsupporting

confidence: 73%

Section: Saturation Solubility Studiesmentioning

confidence: 99%

Section: Globule Size Zeta Potential Pi and Drug Contentmentioning

confidence: 99%

See 1 more Smart Citation

Solubility Enhancement of Poorly Soluble Drug Ezetimibe by Developing Self Nano Emulsifying Drug Delivery System

Doke¹,

Khutle²,

Sharma³

et al. 2022

IJST

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“…Several formulation techniques have been adapted to improve the bioavailability and therapeutic effectiveness of gliclazide such as the preparation of solid dispersion [ 8 , 9 ], inclusion complex with β-cyclodextrin [ 10 ], nanocrystals [ 11 ], liquid–solid systems [ 12 ], solid lipid nanoparticles [ 13 ], and self-micro-emulsifying delivery system [ 14 ]. The previously mentioned approaches rely on increasing the solubility of gliclazide as a mechanism for bioavailability improvement.…”

Section: Introductionmentioning

confidence: 99%

Bioavailability and Antidiabetic Activity of Gliclazide-Loaded Cubosomal Nanoparticles

et al. 2021

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In this study, gliclazide-loaded cubosomal particles were prepared for improving the oral bioavailability and antidiabetic activity of gliclazide. Four formulations of gliclazide-loaded cubosomal nanoparticles dispersions were prepared by the emulsification method using four different concentrations of glyceryl monooleate (GMO) and poloxamer 407 (P407) as the stabilizer. The prepared formulations were in vitro and in vivo evaluated. In vitro, the prepared gliclazide-loaded cubosomal dispersions exhibited disaggregated regular poly-angular particles with a nanometer-sized particle range from 220.60 ± 1.39 to 234.00 ± 2.90 nm and entrapped 73.84 ± 3.03 to 88.81 ± 0.94 of gliclazide. In vitro gliclazide release from cubosomal nanoparticles revealed an initially higher drug release during the first 2 h in acidic pH medium; subsequently, a comparatively higher drug release in alkaline medium relative to gliclazide suspension was observed. An in vivo absorption study in rats revealed a two-fold increase in the bioavailability of gliclazide cubosomal formulation relative to plain gliclazide suspension. Moreover, the study of in vivo hypoglycemic activity indicated that a higher percentage reduction in glucose level was observed after the administration of gliclazide cubosomal nanoparticles to rats. In conclusion, gliclazide-loaded cubosomal nanoparticles could be a promising delivery system for improving the oral absorption and antidiabetic activity of gliclazide.

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“…Theses formulations were developed as promising controlled delivery systems and loaded with Capmul ® MCM C8 for the potential enhancement of release and bioavailability of poorly water soluble drug. Patel et al have employed Capmul ® MCM C8 as a bioavailability enhancer in pellets designed for improved oral drug delivery of gliclazide [29]. The prepared formulations were loaded with 5% w/w of the antihypertensive agent, felodipine, as a model drug.…”

Section: Preparation Of Polymeric Films With Different Concentrationsmentioning

confidence: 99%

Drug Release Control and Enhancement Using Carriers With Different Concentrations of Capmul® MCM C8

Bayan

2021

Int J App Pharm

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Objective: The main aim of this study was to design a drug carrier capable to control and enhance the release of poorly water soluble drugs. Methods: Three polymeric formulations, based on poly (2-hydroxyethyl methacrylate) and loaded with different Capmul® MCM C8 concentrations (0, 10 and 20 % w/w), were prepared. Felodipine, which is a poorly soluble substance, was selected as a model drug. The effect of Capmul® MCM C8 on swelling behavior and in vitro release profile of the prepared polymer was investigated in PBS. Results: The swelling profiles of allformulationswere statistically similar, which indicated the non-significant effect of added Capmul® MCM C8 on polymer's swelling behavior. All formulations showed a delayed drug release. Formulation-F3, which is loaded with 20% w/wCapmul® MCM C8 displayed a significant higher release compared to the other formulations. Conclusion: Capmul® MCM products, which are widely used in food industries, can be used to improve the oral delivery of poorly soluble substances. The optimized formulation exhibited the ability to control and enhance the release of the model drug.

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Enhancement of in vivo hypoglycemic effect of gliclazide by developing self-microemulsifying pellet dosage form

Cited by 9 publications

References 46 publications

Solubility Enhancement of Poorly Soluble Drug Ezetimibe by Developing Self Nano Emulsifying Drug Delivery System

Solubility Enhancement of Poorly Soluble Drug Ezetimibe by Developing Self Nano Emulsifying Drug Delivery System

Bioavailability and Antidiabetic Activity of Gliclazide-Loaded Cubosomal Nanoparticles

Drug Release Control and Enhancement Using Carriers With Different Concentrations of Capmul® MCM C8

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