The prediction of the optimum compositions of a parenteral nanoemulsion system loaded with a low water solubility drug for the treatment of schizophrenia by artificial neural networks

Samiun, Wan Sarah; Basri, Mahiran; Masoumi, Hamid Reza Fard; Khairudin, Nurshafira

doi:10.1039/c5ra26243g

Cited by 4 publications

(4 citation statements)

References 41 publications

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“…A drug’s solubility in oils is the driving force in the selection of the NEs’ components [ 33 ]. For parenteral application, oil cores are usually composed of soybean oil, sunflower seed oil, olive oil, palm kernel oil esters, medium-chain triglycerides or fish oil [ 21 , 34 , 35 , 36 , 37 , 38 , 39 ]. It is advised to combine oils high in long-chain triglycerides, such as soybean or sunflower oil, which may improve drug penetration across the BBB due to linoleic acid content, with oils high in medium-chain triglycerides, having a higher solvent capacity and lower viscosity [ 39 , 40 ].…”

Section: Formulation-related Considerationsmentioning

confidence: 99%

“…Several techniques could be used to prepare lipid nanoparticles, including high-pressure homogenization (HPH) [ 25 , 34 , 36 , 38 , 40 , 44 ], thin film hydration followed by the sonication or filtration of liposomes [ 28 , 29 , 30 , 54 ], a combination of homogenization and sonication [ 46 , 47 ] or solvent-emulsification and evaporation techniques [ 45 ]. The physical and chemical complexity of the laboratory-scale prepared formulations is one of the facets that affect the scale-up of lipid nanoparticles, leading to difficulties in ensuring good stability during the shelf life [ 25 ].…”

Section: Formulation-related Considerationsmentioning

confidence: 99%

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Parenteral Lipid-Based Nanoparticles for CNS Disorders: Integrating Various Facets of Preclinical Evaluation towards More Effective Clinical Translation

et al. 2023

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Contemporary trends in combinatorial chemistry and the design of pharmaceuticals targeting brain disorders have favored the development of drug candidates with increased lipophilicity and poorer water solubility, with the expected improvement in delivery across the blood–brain barrier (BBB). The growing availability of innovative excipients/ligands allowing improved brain targeting and controlled drug release makes the lipid nanocarriers a reasonable choice to overcome the factors impeding drug delivery through the BBB. However, a wide variety of methods, study designs and experimental conditions utilized in the literature hinder their systematic comparison, and thus slows the advances in brain-targeting by lipid-based nanoparticles. This review provides an overview of the methods most commonly utilized during the preclinical testing of liposomes, nanoemulsions, solid lipid nanoparticles and nanostructured lipid carriers intended for the treatment of various CNS disorders via the parenteral route. In order to fully elucidate the structure, stability, safety profiles, biodistribution, metabolism, pharmacokinetics and immunological effects of such lipid-based nanoparticles, a transdisciplinary approach to preclinical characterization is mandatory, covering a comprehensive set of physical, chemical, in vitro and in vivo biological testing.

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Section: Formulation-related Considerationsmentioning

confidence: 99%

Section: Formulation-related Considerationsmentioning

confidence: 99%

Parenteral Lipid-Based Nanoparticles for CNS Disorders: Integrating Various Facets of Preclinical Evaluation towards More Effective Clinical Translation

et al. 2023

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“…The oil mixture was dropped wisely into the aqueous phase containing 2.25 w/w% of glycerol and 91.75 w/w% of deionized water. 25,26 The mixture was then stirred by using overhead stirrer (IKA ® RW 20 Digital, Nara, Japan). High energy emulsification methods, which are high shear homogenizer (Kinematica AG, Luzern, Switzerland) and high pressure homogenizer (Emulsiflex, Canada) were used to prepare the samples.…”

Section: Preparation Of Nanoemulsion Containing Aripiprazolementioning

confidence: 99%

“…[22][23][24] From previous work, nanoemulsions containing aripiprazole were successfully developed utilizing high pressure homogenizer with a homogenization pressure of 1000 bar for 14 cycles by optimizing the compositions of formulation nanoemulsion. 25,26 In this work, RSM was utilized to identify the optimum processing parameters of encapsulation nanoemulsion containing aripiprazole by using the same optimum formulation from previous work. The influences of four independent variables, including overhead stirring time, shear time, shear rate, and the cycle of high-pressure homogenizer were studied on a response variable, namely droplet size by using CCRD.…”

Section: Introductionmentioning

confidence: 99%

<p>Optimization of Processing Parameters of Nanoemulsion Containing Aripiprazole Using Response Surface Methodology</p>

Samiun

Ashari

Salim

et al. 2020

IJN

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Background: Aripiprazole, which is a quinolinone derivative, has been widely used to treat schizophrenia, major depressive disorder, and bipolar disorder. Purpose: A Central Composite Rotatable Design (CCRD) of Response Surface Methodology (RSM) was used purposely to optimize process parameters conditions for formulating nanoemulsion containing aripiprazole using high emulsification methods. Methods: This design is used to investigate the influences of four independent variables (overhead stirring time (A), shear rate (B), shear time (C), and the cycle of high-pressure homogenizer (D)) on the response variable namely, a droplet size (Y) of nanoemulsion containing aripiprazole. Results: The optimum conditions suggested by the predicted model were: 120 min of overhead stirring time, 15 min of high shear homogenizer time, 4400 rpm of high shear homogenizer rate and 11 cycles of high-pressure homogenizer, giving a desirable droplet size of nanoemulsion containing aripiprazole of 64.52 nm for experimental value and 62.59 nm for predicted value. The analysis of variance (ANOVA) showed the quadratic polynomial fitted the experimental values with F-value (9.53), a low p-value (0.0003) and a nonsignificant lack of-fit. It proved that the models were adequate to predict the relevance response. The optimized formulation with a viscosity value of 3.72 mPa.s and pH value of 7.4 showed good osmolality value (297 mOsm/kg) and remained stable for three months in three different temperatures (4°C, 25°C, and 45°C). Conclusion: This proven that response surface methodology is an efficient tool to produce desirable droplet size of nanoemulsion containing aripiprazole for parenteral delivery application.

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Experimental and simulative studies on the implications of natural and green surfactant for extracting flavonoids

Cui

Liu

et al. 2020

Journal of Cleaner Production

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The prediction of the optimum compositions of a parenteral nanoemulsion system loaded with a low water solubility drug for the treatment of schizophrenia by artificial neural networks

Abstract: Aripiprazole was encapsulated in a palm kernel oil esters nanoemulsion for the purpose of brain deliveryviaintravenous administration.

Cited by 4 publications

References 41 publications

Parenteral Lipid-Based Nanoparticles for CNS Disorders: Integrating Various Facets of Preclinical Evaluation towards More Effective Clinical Translation

Parenteral Lipid-Based Nanoparticles for CNS Disorders: Integrating Various Facets of Preclinical Evaluation towards More Effective Clinical Translation

<p>Optimization of Processing Parameters of Nanoemulsion Containing Aripiprazole Using Response Surface Methodology</p>

Experimental and simulative studies on the implications of natural and green surfactant for extracting flavonoids

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