Formulation and optimization of Enalapril Maleate-loaded floating microsphere using Box–Behnken design: in vitro study

Bahadur, Kumal Vijay; Chhitij, Thapa; Ghimire, Prakash; Chaudhari, Pradyumna; Jitendra, Yadhav

doi:10.7324/japs.2020.10811

Cited by 4 publications

(4 citation statements)

References 26 publications

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“…After 3 mo of storage, the percent drug content, percent entrapment efficiency, and percent drug release, percent mucoadhesion, and particle size (µm) of the chosen formulation (F18) were determined. The studies revealed that there no noticable change in drug content, entrapment efficiency, mucoadhesion, drug release and particle size after storage for 3 mo at 4±1 °C, 25±2 °C; 60±5% RH and 37±2 °C; 65±5% RH as reported by Bahadur K. V. et al, 2020 [12]. It was also revealed that formulation F18 stored at 4±1 °C showed maximum drug content of (65.32 %) followed by the storage at 25±2 °C; 60±5% RH and 37±2 °C; 65±5% RH conditions.…”

Section: In Vivo Pharmacodynamic Studysupporting

confidence: 52%

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Quality by Design-Driven Formulation Development and Optimization of Enalapril Maleate Loaded Mucoadhesive Microspheres: In Vitro and in Vivo Characterization

Komati

Rao²,

Swain³

et al. 2023

Int J App Pharm

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Objective: The study is to formulate the enalapril maleate-loaded mucoadhesive microspheres with varied compositions of selected polymers for developing the oral controlled release formulations prepared by ionic gelation method and optimization through central composite design. Methods: Systematic optimization of microspheres was accomplished by the central composite design and characterized for particle size, entrapment efficiency, in vitro drug release and ex vivo mucoadhesion strength, which indicated that microspheres were a consequence to be spherical and free-flowing in nature. The microspheres exhibited high drug entrapment efficiency and in vitro drug release in a sustained manner, which was considered to be dependent on the concentration of rate-controlling polymers. The microspheres are showed 389.2 to 850 µm particle size and 22.36 to 85.22 % encapsulation efficiency. In vitro studies indicated optimized formulation showed 89.26% drug release after 12h and reduced blood pressure effectively. Results: The pharmacokinetic parameters were evaluated with Cmax of 75.39 µg/ml, tmax of 8h, and AUC of 53.55 µg/hr/ml, elimination rate constant of 0.0392 and t1/2 of 10h. The stability studies were conducted for 3 mo under various conditions and identified no significant deviations in selected key quality attributes. Conclusion: The formulated mucoadhesive microspheres of enalapril maleate tend to reduce the blood pressure in the animal model, with the novel drug delivery approach in the efficient management of hypertension.

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Section: In Vivo Pharmacodynamic Studysupporting

confidence: 52%

“…Twenty different runs have been undertaken, and the responses for each run were documented. The composition with the optimal outcomes was chosen for future research [12].…”

Section: Optimization Of Formulation By Central Composite Designmentioning

confidence: 99%

Quality by Design-Driven Formulation Development and Optimization of Enalapril Maleate Loaded Mucoadhesive Microspheres: In Vitro and in Vivo Characterization

Komati

Rao²,

Swain³

et al. 2023

Int J App Pharm

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“…The kinetic study was performed to determine the mechanism of drug release from oating microspheres. The drug release data were plotted into the different kinetic models, such as zero order, rst order, higuchi and korsemeyer-peppas kinetics [29,31].…”

Section: Lag Timementioning

confidence: 99%

Floating microspheres of Miglitol as gastro retentive drug delivery system: 32 full factorial design and in vitro evaluation

Cheran

Bolmal

Patil

et al. 2021

Preprint

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Background: The goal of this study was to develop a gastro retentive floating drug delivery system that would improve site specific activity, patient compliance and therapeutic efficacy.Methodology: Floating microspheres of Miglitol were formulated by double emulsion method using ethyl cellulose and eudragit E100 different weight ratio and PVA as an emulsifier. It has been prepared with respect quantity of polymer concentration and stirring speed to evaluate for % buoyancy, drug entrapment efficiency, particle size drug release rate. Result: The percent of buoyancy, drug entrapment efficiency, particle size, and percentage yield were increased with increase the polymer mixture concentration. Among all formulation batches, F6 showed acceptable results drug entrapment efficiency (86.57%) and buoyancy (94.25%). F10 formulation was prepared to check the predicted and actual factors and compared with optimized formulation F6. The drug release was increased as the polymer concentration was decrease. The kinetic model zero order had the highest regression coefficient value, it was described as a sustained release dosage form. According to ICH guideline accelerated stability studies of F6 and F10 formulations were conducted for 90 days. After 90 days buoyancy and in vitro drug release was performed and the results were F6 and F10 buoyancy was found to be 88.21%, 87.22% and in vitro drug release was found to be 62.87%, 63.51%. Conclusion: The present study, showed compatibility of drug with polymers by FTIR in formulation. Floating microsphere of Miglitol was prepared by double emulsion technique. The F6 Miglitol floating microsphere was optimized formulation demonstrated with excellent drug entrapment performance (86.57%), good floating behaviour (94.25%), and the largest particle size (670µm). The present study concludes that floating based gastro retentive delivery system of Miglitol microspheres has a safe and effective drug delivery system with increased therapeutic efficacy and a longer duration of action.

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“…Microsphere drug delivery systems have been formulated by various techniques, including phase separation or precipitation, emulsion/solvent evaporation, and spraying, melt congeal /dispersion technique 7 . The principle of lipid microsphere preparation offers a simple and practical approach to achieve increased gastric residence time for the dosage form and controlled drug release 8 .…”

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confidence: 99%

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2022

IJPSR

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Microspheres drug delivery system have improved patient compliance, decreased toxicity, and increased efficacy. This work aimed to design a controlled-release drug-delivery system for lipid microspheres of Verapamil hydrochloride that would retain the drug in the stomach and continuously release the drug in a controlled manner up to a predetermined time. Lipid microspheres were prepared by using a melt solidification method. Microspheres with spherical shapes and narrow size distribution were formed. In the present investigation, two lipids were used in various concentrations; Ceresine wax & Bees Wax. In-vitro performance was evaluated, such as particle size analysis, drug entrapment efficiency, compatibility study, Preformulation study, flow properties, in-vitro drug release studies, stability studies, etc. The drug in microspheres was found to be stable and compatible with waxes, as confirmed by DSC and FTIR methods. The mixing ratio of lipids with drug affected the size, size distribution, Yield, drug content, and drug release of microspheres. Results showed that the solid, discrete, reproducible free-flowing microspheres were obtained. In most cases, good in vitro microsphere behavior was observed, and a broad variety of drug release patterns could be achieved by variation of the drug-lipid ratio. The release kinetics followed different transport mechanisms. The surface morphology of microspheres was characterized by scanning electron microscopy (SEM). The release of the drug was controlled for more than 12h. INTRODUCTION:The need to design new drug delivery systems will reduce or eliminate the variable plasma concentration. Controlled-release drug delivery systems are developed to address many of the difficulties associated with traditional methods of administration 1 . The real issue in developing oral controlled release dosage forms is to prolong the residence time of the dosage form in the stomach or upper gastrointestinal tract until the drug is completely released 2 .

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Formulation and optimization of Enalapril Maleate-loaded floating microsphere using Box–Behnken design: in vitro study

Cited by 4 publications

References 26 publications

Quality by Design-Driven Formulation Development and Optimization of Enalapril Maleate Loaded Mucoadhesive Microspheres: In Vitro and in Vivo Characterization

Quality by Design-Driven Formulation Development and Optimization of Enalapril Maleate Loaded Mucoadhesive Microspheres: In Vitro and in Vivo Characterization

Floating microspheres of Miglitol as gastro retentive drug delivery system: 32 full factorial design and in vitro evaluation

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