Evaluation and Optimization of Influence of Permeability Property and Concentration of Polymethacrylic Polymers on Microspheres of Metformin HCl

Hasan, Ikramul; Paul, Sangita; Akhter, Sharmin; Ayon, Navid J.; Reza, Selim

doi:10.3329/dujps.v12i2.17611

Cited by 5 publications

(15 citation statements)

References 14 publications

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“…15, 16 Particle sizes of the microspheres prepared with Ethocel and HPMC K100M combined was determined by laser diffracting particle size analyzer (Partica ® 5960). The analyzer provided the particle size according to the refractive index of that particle.…”

Section: Particle Size Analysismentioning

confidence: 99%

Preparation and characterization of Gliclazide incorporated Cellulosic Microspheres: studies on drug release, compatibility and micromeritics

Ayon

Hasan

Islam

et al. 2015

Dhaka Univ. J. Pharm. Sci

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Polymeric microspheres of gliclazide were prepared to provide sustained release delivery of gliclazide to aid in continuous therapy with high margin of safety. Gliclazide was microencapsulated with different polymers namely HPMC K100LV, Ethocel (20 cps) and HPMC K100M by emulsion solvent evaporation technique using acetone as internal phase and liquid paraffin as external phase. Seventeen formulations were prepared using different drug loading and polymeric ratio of which nine formulations were prepared by a 3 2 full factorial design. Each formulation was evaluated for flow properties, particle size, surface morphology, drug entrapment efficiency, drug release and compatibility. Yield (%) for every batch of microspheres was measured. Flow properties of the microspheres were examined by determining bulk density, tapped density, Carr's compressibility index, Hausner ratio and angle of repose. Particle size distribution was examined by sieving and particle size analyzer. Surface morphology was determined by scanning electron microscopy (SEM). In-vitro drug release was studied in a paddle type dissolution apparatus (USP Type II Dissolution Apparatus) for a period of 8 hours at 37°C using phosphate buffer ( pH 7.4). FTIR and DSC studies established compatibility of the drug with the polymers. Microspheres prepared with Ethocel (20 cps) and HPMC K100M were free flowing than those prepared only with HPMC K100LV. Entrapment efficiencies were within 75.88-99.69%. Microspheres prepared with Ethocel (20 cps) and HPMC K100M showed more sustained release when compared to microspheres prepared with HPMC K100LV only. Increase in drug loading resulted in increased drug release for the microspheres. Kinetic modeling of in vitro dissolution profiles revealed the drug release mechanism ranging from diffusion controlled to anomalous type. Ethocel and HPMC K100M in a ratio of 1:3 exhibited better sustained release properties than 1:1 and 3:1 ratios. The release rate of gliclazide from microspheres prepared with Ethocel (20 cps) and HPMC K100M was less than the release rate of gliclazide from microspheres prepared with HPMC K100LV, demonstrating Ethocel and HPMC K100M as suitable polymeric blend for preparing the controlled release formulation for gliclazide whereas, HPMC K100LV was found not suitable candidate when used alone as a polymer.

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Section: Particle Size Analysismentioning

confidence: 99%

Preparation and characterization of Gliclazide incorporated Cellulosic Microspheres: studies on drug release, compatibility and micromeritics

Ayon

Hasan

Islam

et al. 2015

Dhaka Univ. J. Pharm. Sci

Self Cite

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“…Subsequently, n-hexane was used to wash the settled microspheres numerous times before being dried naturally at room temperature (approximately 25 °C). 29 …”

Section: Methodsmentioning

confidence: 99%

“…The formulations were attached to aluminum SEM sample stabs, which were then covered with double-sided adhesive tape, sealed, and enveloped with gold (200 Å) using an ion sputtering apparatus for 15 min at a low pressure (0.001 Torr). 29 Using a scanning electron microscope (Zeiss Sigma VP), the platinum-coated materials were imaged at various magnifications to produce photomicrographs at relevant scales (20 µm for microspheres and 5 µm for nanoparticles). Before testing, the microspheres and nanoparticles were dried thoroughly.…”

Section: Methodsmentioning

confidence: 99%

Metformin Hydrochloride Loaded Mucoadhesive Microspheres and Nanoparticles for Anti-Hyperglycemic and Anticancer Effects Using Factorial Experimental Design

Kotha,

Ahmad,

Dewan

et al. 2023

DDDT

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Background Metformin hydrochloride (HCl) microspheres and nanoparticles were formulated to enhance bioavailability and minimize side effects through sustained action and optimized drug-release characteristics. Initially, the same formulation design with different ratios of metformin HCl and Eudragit RSPO was used to formulate four batches of microspheres and nanoparticles using solvent evaporation and nanoprecipitation methods, respectively. Methods The produced formulations were evaluated based on particle size and shape (particle size distribution (PSD), scanning electron microscope (SEM)), incompatibility (differential scanning calorimetry (DSC), Fourier-transform infrared (FTIR)), drug release pattern, permeation behavior, in vivo hypoglycemic effects, and in vitro anticancer potential. Results Compatibility studies concluded that there was minimal interaction between metformin HCl and the polymer, whereas SEM images revealed smoother, more spherical nanoparticles than microspheres. Drug release from the formulations was primarily controlled by the non-Fickian diffusion process, except for A1 and A4 by Fickian, and B3 by Super case II. Korsmeyer-Peppas was the best-fit model for the maximum formulations. The best formulations of microspheres and nanoparticles, based on greater drug release, drug entrapment, and compatibility characteristics, were attributed to the study of drug permeation by non-everted intestinal sacs, in vivo anti-hyperglycemic activity, and in vitro anticancer activity. Conclusion This study suggests that the proposed metformin HCl formulation can dramatically reduce hyperglycemic conditions and may also have anticancer potential.

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“…PEG is partially soluble in the oil phase and thus during the matrix formation the migration of PEG 4000 from the internal phase had led to the formation of pores in the microspheres [17]. Moreover the surface roughness could be due to the slow evaporation of solvent or high permeability of Eudragit RLPO [18]. In Formulation B11 as showed in Fig.…”

Section: Magnification Of B11 Image At X30 Se Magnification Of B11 Immentioning

confidence: 99%

Preparation and Characterization of Methocel K4m, Eudragit Rlpo and Peg 4000 Loaded Carbamazepine Microspheres.

Sultana¹,

ijar²

2018

IJAR

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Evaluation and Optimization of Influence of Permeability Property and Concentration of Polymethacrylic Polymers on Microspheres of Metformin HCl

Cited by 5 publications

References 14 publications

Preparation and characterization of Gliclazide incorporated Cellulosic Microspheres: studies on drug release, compatibility and micromeritics

Preparation and characterization of Gliclazide incorporated Cellulosic Microspheres: studies on drug release, compatibility and micromeritics

Metformin Hydrochloride Loaded Mucoadhesive Microspheres and Nanoparticles for Anti-Hyperglycemic and Anticancer Effects Using Factorial Experimental Design

Preparation and Characterization of Methocel K4m, Eudragit Rlpo and Peg 4000 Loaded Carbamazepine Microspheres.

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