Ethylcellulose Floating Microspheres of Antidiabetic Agent: In Vitro and in Vivo Evaluation

Objective: The purpose of the present investigation was to develop and characterize a novel herbal formulation (polymeric microspheres) of Syzygium cumini seed extract.Methods: The extract-loaded microspheres using biological macromolecule ethyl cellulose (EC) was prepared by o/w emulsion solvent evaporation technique using polyvinyl alcohol (PVA) emulsifier. The effect of various process and formulation variables (stirring speed, evaporation time, drug/polymer ratio and organic/aqueous phase ratio) on the properties of microspheres was evaluated.Results: Micromeritic properties indicated good flow properties, and scanning electron microscopy (SEM) confirmed the spherical nature of the prepared microspheres. The particle size and entrapment efficiency were varied between 34.25 to 176.25 µm and 10.51 to 42% depending upon the variables. All the formulations showed minimal drug release in an acidic environment (pH 1.2) confirming the prevention of drug release in the stomach and enteric nature of the polymer. Sustained drug release has been observed in alkaline dissolution media (pH 7.4) after 12 h of drug release study except for formulation F7 which contains a lower concentration of polymer. The fourier transform infrared spectroscopy (FTIR) analysis indicated the compatibility of the extract with the polymer. The absence of extract-polymer interaction was indicated by the differential scanning calorimetry (DSC) thermogram. x-ray diffraction (XRD) analysis revealed the amorphous nature of the extract in the microspheres which in pure form exhibits a crystalline structure.Conclusion: The findings of this present study suggest that microsphere formulation was a promising carrier for novel delivery of herbal drugs.

Section: Production Yieldmentioning

confidence: 96%

Development and Characterization of Novel Herbal Formulation (Polymeric Microspheres) of Syzygium Cumini Seed Extract

Biswas

Sen²

2018

“…The size of the microspheres also depends on the concentration of polymer solution and stirring speed. The size of the microspheres was increased by increasing the amount of polymers [45,46], but decreases with increasing the stirring speed.…”

Section: Particle Size Of Microspheresmentioning

confidence: 96%

Formulation and Optimization of Mucoadhesive Microspheres of Valsartan by Using Box-Behnken Design

Lal

Garg²,

Gupta³

2019

Objective: The purpose of this study was to formulate and optimize mucoadhesive microspheres of antihypertensive drug (valsartan) within ethyl cellulose as a carrier polymer and carbopol 934P as a mucoadhesive polymer for controlling the release of valsartan. Methods: The emulsion solvent evaporation technique was used for preparation of microspheres of valsartan and the Box-Behnken design was employed with thee independent variables that is amount of ethyl cellulose (X1) and amount of carbopol 934P (X2) and stirring speed (X3) and evaluate four dependent variables such as percentage mucoadhesion, Q1 h, t90% and drug entrapment efficiency. Results: The optimum conditions were found to be X1= 200 mg, X2= 107 mg and X3= 1200rpm. The optimized batch exhibited a high drug entrapment efficiency of 85.63±1.384%, percentage mucoadhesion was 66.76±0.986% and drug release was also sustained for more than 12 h. Conclusion: The analysis of variance showed a significant effect of independent variables. The scaning electron microscopy (SEM) analysis showed that the microspheres were spherical and free-flowing. The microspheres of valsartan were stable after thee month stability study at accelerated condition.

“…RG is a good candidate [10] for the development of a gastroretentive dosage form because of its short duration of action, quick clearance, stability against enzymes, and most of its absorption takes place in the upper GIT (stomach). Repaglinide Gastro-retentive Floating tablet (RG-GRF Tablet) was used to improve the residence duration in the stomach [11] so that we can reduce the dosing frequency of the drug since this medication must be taken for an extended period to improve patient compliance [12,13].…”

Section: Introductionmentioning

confidence: 99%

Optimization, Development and Evaluation of Repaglinide Controlled Release Gastro-Retentive Floating Tablet Using Central Composite Design

PATEL

MASHEER

2023

Objective: The recent study's objective was to optimize and formulate a controlled-release gastro-retentive floating tablet of RG using a central composite design, which provides continuous release of Repaglinide for up to 24 h. Methods: Repaglinide gastro-retentive floating tablet (RG-GRF Tablet) was prepared by direct compression method. The optimization was carried out using a three-factor and three-level Central Composite design. The amount of Eudragit RSPO (A), HPMC K-100M (B) and Sodium bicarbonate (C) were selected as independent variables and the Cumulative % drug release in 1.5 h (DR1.5), Cumulative % drug release in 8 h (DR8), Cumulative % drug release in 24 h (DR24) and Floating lag time (FLT) were used as dependent variables. Results: CCD analysis results shows that predicted and experimental values for optimized formulation were found to be almost similar. Optimized amounts of Eudragit RSPO, HPMC K-100M, and NaHCO3 were 14.351 mg, 44.438 mg, and 10 mg, respectively, with the highest possible desirability value of 0.898. The experimental values at optimized preparation conditions were found to be DR1.5 is 30.68%, DR8 is 64.90%, DR24 is 96.54%, and FLT is 4.41 min. The release data from the optimized formulation were closely matched with the Korsmeyer-Peppas model and in vitro drug release studies indicated that the RG-GRF Tablet continuously releases the drug for 24 h in a controlled manner. Conclusion: Current research concludes that RG-GRF Tablets provide drug release for up to 24 h, and the derived central composite design can be used for forecasting the DR1.5, DR8 and DR24 as well. RG can also be made more bioavailable by extending the gastric residence time.