Association of PLGA Microspheres to Carrier Pellets by Fluid Bed Coating: A Novel Approach towards Improving the Flowability of Microparticles

Beringhs, André O’Reilly; Fonseca, Aline Benedita dos Santos; Campos, Angela Machado de; Sonaglio, Diva

doi:10.1155/2018/3874348

Cited by 3 publications

(2 citation statements)

References 27 publications

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“…The resultant lipids microspheres were composed of irregular masses, which could not be distinguished as individual microspheres. A similar emulsifier concentration was reported for wax microspheres prepared by melt dispersion method 17 . The temperature of the aqueous phase was maintained at 5 °C higher than the melting point of the lipids in the corresponding formulations.…”

Section: Resultssupporting

confidence: 82%

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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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Section: Resultssupporting

confidence: 82%

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2022

IJPSR

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“…The Hausner's ratio for microspheres was calculated as the ratio of tapped density to bulk density and the value was calculated by using the equation-7 [23],…”

Section: Hausner's Ratiomentioning

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

Bahadur¹,

Chhitij²,

Ghimire³

et al. 2020

J App Pharm Sci

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The objective was to prepare an Enalapril Maleate (EnM)-loaded floating microsphere with minimum particle size, maximum drug loading, and drug entrapment efficiency. Formulations were prepared by varying drug-to-polymer ratio (A), solvent ratio (B), and stirring time (C). The solvent evaporation method was used to prepare the microsphere. "Box-Behnken's design" (3 factors × 3 levels) was utilized for optimization. The independent variables were polymerto-drug ratio (A), solvent ratio (B), and stirring time (C), while particle size (R 1 ), drug loading (R 2 ), and entrapment efficiency (R 3 ) were considered as dependent variables. EnM-loaded alcohol microsphere (Formulation-A) was prepared and optimized. Both Formulation-A and EnM-loaded acetonitrile microspheres (Formulation-B) were subjected to morphological, micrometric, characterization, and in vitro release studies. The particle size, drug loading, and entrapment efficiency of Formulation-A and Formulation-B were 143 ± 27.75 µm, 37.31% ± 5.73%, and 76.89% ± 4.97%, and 158.13 ± 25.1 µm, 40.13% ± 6.12%, and 99.19% ± 1.14%, respectively. The cumulative drug releases of Formulation-A and Formulation-B were 90.52% ± 4.11% and 86.23% ± 3.81%, respectively. Both formulations followed the Higuchi model of drug release. EnM-floating microsphere was effectively prepared and both formulations showed excellent continuous release properties for more than 12 hours.

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Association of PLGA Microspheres to Carrier Pellets by Fluid Bed Coating: A Novel Approach towards Improving the Flowability of Microparticles

Cited by 3 publications

References 27 publications

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

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

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