Optimization of preparation method by W/O/W emulsion for entrapping metformin hydrochloride into poly (lactic acid) microparticles using Box-Behnken design

Bouriche, Sihem; Rezgui, Farouk; Álvarez, Antonio Merchán; González-Rodrı́guez, Marı́a Luisa

doi:10.1016/j.jddst.2019.03.011

Cited by 21 publications

(22 citation statements)

References 43 publications

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“…As shown in Figure 2B, in all range of stirring speed, the larger the wall material dose, the higher the EE. As shown in Figure 2C, at a low emulsifier dosage, the response EE showed a tendency of first increasing and then decreasing with the growth of wall material dosage (Bouriche et al, 2019). This is mainly due to the lack of emulsifiers, which led to the failure of stabilizing the O/W emulsion, in turn, reducing the polymerization of isocyanate at the interface and resulting in inhibition of microcapsule formation.…”

Section: Data Analyses and Validation Of The Applied Model On The Encmentioning

confidence: 94%

“…Response surface methodology (RSM) is a set of mathematical and statistical techniques that are commonly used to design experiments, build models, evaluate influencing factors, and find the best conditions for expected response factors (Aslan and Cebeci, 2007;Almeida et al, 2019;Yousefi et al, 2019). Box-Behnken design (BBD) is a type of response surface design that does not include embedded factor or partial factor, which can provide conclusions and detailed information through the interaction of a small number of experiments and operating parameters on all responses (Ferreira et al, 2007;Prakash Maran et al, 2013;Bouriche et al, 2019). BBD as applied in response surface methodology (RSM), constitutes an important design tool for the optimization of different processes.…”

Section: Introductionmentioning

confidence: 99%

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Pretilachlor Releasable Polyurea Microcapsules Suspension Optimization and Its Paddy Field Weeding Investigation

et al. 2020

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In this study, pretilachlor was encapsulated into polyurea microcapsules prepared by water-initiated polymerization of polyaryl polymethylene isocyanate and eventually made into pretilachlor microcapsules suspension (PMS). We used response surface methodology (RSM) combined with the Box-Behnken design (BBD) model to optimize the formulation of PMS. The encapsulation efficiency (EE) of PMS was investigated with respect to three independent variables including wall material dosage (X 1), emulsifier dosage (X 2), and polymerization stirring speed (X 3). The results showed that the regression equation model had a satisfactory accuracy in predicting the EE of PMS. To achieve an optimal condition for PMS preparation, the dose of wall material was set to 5%, the dose of emulsifier was set to 3.5% and the polymerization stirring speed was set to 200 rpm. The EE of PMS was up to 95.68% under the optimized condition, and the spherical shape with smooth surface morphology was observed. PMS was also proven to have delayed release capability and in vivo herbicidal activity against barnyard grass [Echinochloa crusgalli (L.) Beauv.] with an LC 50 value of 274 mg/L. Furthermore, PMS had efficient weed management compared to commercially available 30% pretilachlor emulsifier (PE), showing a promising potential application for weeding paddy fields.

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Section: Data Analyses and Validation Of The Applied Model On The Encmentioning

confidence: 94%

Section: Introductionmentioning

confidence: 99%

Pretilachlor Releasable Polyurea Microcapsules Suspension Optimization and Its Paddy Field Weeding Investigation

et al. 2020

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“…In a previous study, we showed the successful preparation of poly (lactic acid) microparticles loaded metformin using the double emulsion (w/o/w) solvent evaporation method. In this method, the effect of microencapsulation parameters such as the amount of metformin, pH of the external aqueous phase, PVA concentration and the stirring rate on the encapsulation e ciency, microparticles size and zeta potential were evaluated and optimized using response surface methodology by Box-Behnken Design [14]. In the present study after microparticles characterization, the potential of poly (lactic acid) microparticles loaded metformin to sustain the in vivo release carried out on rabbits under standard fed conditions.…”

Section: Discussionmentioning

confidence: 99%

“…Metformin HCl loaded PLA microparticles were prepared by the W/O/W solvent evaporation method described previously [14]. Brie y, 1 mL of aqueous internal phase was emulsi ed for 5 min in 10 mL of methylene chloride (containing 200 mg of PLA) with an ultrasound bath (Branson 5510, BioBlock Scienti c, Spain) at 135 W output.…”

Section: Preparation Of Metformin Hcl-microparticlesmentioning

confidence: 99%

“…The literature does not indicate studies involving microparticles containing metformin, using PLA as polymer. Recently, an optimisation of metformin encapsulation/formulation in PLA microparticlesin terms of encapsulation e ciency was investigated by using response surface design [14]. However, in vivo bioavailability of the prepared microparticles was not done.…”

Section: Introductionmentioning

confidence: 99%

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Potential of Sustained Release Microparticles of Metformin in Veterinary Medicine: An in Vivo Pharmacokinetic Study of Metformin Microparticles as Oral Sustained Release Formulation in Rabbits.

Bouriche¹,

Alonso-García²,

Cárceles-Rodríguez³

et al. 2020

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Background: Metformin hydrochloride a biguanide derivative has been widely used in the treatment of type 2 diabetes in humans. In veterinary medicine, metformin has been increasing his potential in different species as equids for insulin dysregulation, dogs and cats with diabetes. It is a highly soluble hydrophilic drug, shows incomplete absorption from the gastrointestinal tract and the absolute bioavailability is 40-60 % with a short biological half-life of 1.5-1.6 h in humans. In this study, to improve its efficacy a sustained-release microparticles of metformin was developed by loading within poly lactic acid (PLA) polymer followed by an in vivo pharmacokinetics study in rabbits. Results: Pharmacokinetic study in rabbits showed the sustained-release characteristic from the prepared microparticles with delayed time to reach maximum concentrations Tmax, decreased Cmax, increased Mean Residence Time (MRT) and half-life compared to the pure drug solution. Physicochemical characterization suggested that PLA and metformin hydrochloride interacted within the microparticles via hydrogen bonds and that the drug was transformed to an amorphous state. Conclusions: The The pharmacokinetics parameters resulted in delayed Tmax, increased MRT and t1/2, decreased Cmax of metformin from microparticles that show promise for prolonged/sustained release of metformin after oral administration in different animal species affected by insulin disorders. PLA microparticles provided sustained release of the drug, and these systems can be useful as drug carriers for hydrophilic drugs in long term disease treatment such as diabetes.

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Injectable sustained‐release poly(lactic‐co‐glycolic acid) (PLGA) microspheres of exenatide prepared by supercritical fluid extraction of emulsion process based on a design of experiment approach

Park

Kim

et al. 2023

Bioengineering & Transla Med

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This study aimed to develop an improved sustained‐release (SR) PLGA microsphere of exenatide using supercritical fluid extraction of emulsions (SFEE). As a translational research, we investigated the effect of various process parameters on the fabrication of exenatide‐loaded PLGA microspheres by SFEE (ELPM_SFEE) using the Box–Behnken design (BBD), a design of experiment approach. Further, ELPM obtained under optimized conditions and satisfying all the response criteria were compared with PLGA microspheres prepared using the conventional solvent evaporation (ELPM_SE) method through various solid‐state characterizations and in vitro and in vivo evaluations. The four process parameters selected as independent variables were pressure (X1), temperature (X2), stirring rate (X3), and flow ratio (X4). The effects of these independent variables on five responses, namely the particle size, its distribution (SPAN value), encapsulation efficiency (EE), initial drug burst release (IBR), and residual organic solvent, were evaluated using BBD. Based on the experimental results, a desirable range of combinations of various variables in the SFEE process was determined by graphical optimization. Solid‐state characterization and in vitro evaluation revealed that ELPM_SFEE improved properties, including a smaller particle size and SPAN value, higher EE, lower IBR, and lower residual solvent. Furthermore, the pharmacokinetic and pharmacodynamic study results indicated better in vivo efficacy with desirable SR properties, including a reduction in blood glucose levels, weight gain, and food intake, for ELPM_SFEE than those generated using SE. Therefore, the potential drawback of conventional technologies such as the SE for the preparation of injectable SR PLGA microspheres could be improved by optimizing the SFEE process.

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Optimization of preparation method by W/O/W emulsion for entrapping metformin hydrochloride into poly (lactic acid) microparticles using Box-Behnken design

Cited by 21 publications

References 43 publications

Pretilachlor Releasable Polyurea Microcapsules Suspension Optimization and Its Paddy Field Weeding Investigation

Pretilachlor Releasable Polyurea Microcapsules Suspension Optimization and Its Paddy Field Weeding Investigation

Potential of Sustained Release Microparticles of Metformin in Veterinary Medicine: An in Vivo Pharmacokinetic Study of Metformin Microparticles as Oral Sustained Release Formulation in Rabbits.

Injectable sustained‐release poly(lactic‐co‐glycolic acid) (PLGA) microspheres of exenatide prepared by supercritical fluid extraction of emulsion process based on a design of experiment approach

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