Development of a Solid Formulation Containing a Microemulsion of a Novel Artemisia Extract with Nematocidal Activity for Oral Administration

Perez-Roman, Ines; Kiekens, Filip; Córdoba-Díaz, Damián; García-Rodríguez, Juan José; Córdoba-Díaz, Manuel

doi:10.3390/pharmaceutics12090873

Cited by 9 publications

(3 citation statements)

References 54 publications

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“…Since, in formulation development, the responses of interest are a function of the composition of the mixture, With D-optimal mixture design, the interactions of the mixture's composition could be modeled, graphically or mathematically, to reveal regions of desirable formulation compositions that meet the product's quality criteria. Our findings that the D-optimal mixture approach provides a model that adequately predicted the optimal design space are similar to those reported in other studies [37][38][39]58].…”

Section: Plos Onesupporting

confidence: 90%

D-optimal mixture design optimized solid formulation containing fruits extracts of Momordica charantia and Abelmoschus esculentus

Peter

Sesaazi

2022

PLoS ONE

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Fruit extracts of Momordica charantia L. (Cucurbitaceae) and Abelmoschus esculentus (L.) Moench (Malvaceae) have shown promising antidiabetic activities in clinical trials. However, they remain underutilized due to insufficient standardization and lack of formulation containing their mixture. This study’s overall purpose was to develop and optimize a capsule dosage form containing dried fruit extracts of M. charantia and A. esculentus. The design of the experiment involved two steps; first, response surface methodology (RSM) with a five-level two-factor central composite rotatable design (CCRD) was employed to determine the optimal dose of a mixture of extracts for adequate glycemic control. The extract of M. charantia and A. esculentus were the independent variables while fasting plasma glucose (FPG) was the dependent factor. In the second step, a D-optimal mixture design was applied to study the interaction effect of the optimal dose and selected excipients on granules flowability and capsules’ disintegration time. Moreover, a second-order quadratic model determined the interrelationship of excipients and the desired capsules’ quality attributes. The validity of the predicted models was confirmed. The findings indicated that a combined dose of 175 A. esculentus and 281 M. charantia (mg/kg) significantly reduced the FPG level compared to vehicle at day 14 (mean difference -2.7 ± 0.21, p < 0.001). This dose was used to make a 600 mg capsule (DM083) with 76% drug loading. The DM083 had 40.4 ± 0.62 mg GAE/gDW total polyphenols, 12 peaks HPLC fingerprint, and 26.6 ± 4.75 min average disintegration time. Together, these findings showed that a mixture of M. charantia and A. esculentus fruit extracts could be formulated in a stable capsule dosage form with acceptable quality standards. Further biological studies such as toxicity assays and long-term efficacy studies of the developed capsules could be carried out before large-scale commercial production.

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Section: Plos Onesupporting

confidence: 90%

D-optimal mixture design optimized solid formulation containing fruits extracts of Momordica charantia and Abelmoschus esculentus

Peter

Sesaazi

2022

PLoS ONE

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“…The scCO 2 extract was first dissolved in heptane, and then silicon dioxide (SiO 2 , Syloid ® XDP3050, Grace GmbH, Worms, Germany) was added [63][64][65]. The solvent mixture was subjected to complete evaporation under rotation and vacuum using a rotary evaporator (Hei-VAP Core HL G3B XL, Heidolph Instruments, Schwabach, Germany).…”

Section: The Extraction and Formulation Of H Perforatummentioning

confidence: 99%

Apolar Extracts of St. John’s Wort Alleviate the Effects of β-Amyloid Toxicity in Early Alzheimer’s Disease

El Menuawy,

Brüning,

Eiriz

et al. 2024

IJMS

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Hypericum perforatum (St. John’s wort) has been described to be beneficial for the treatment of Alzheimer’s disease (AD). Different extractions have demonstrated efficiency in mice and humans, esp. extracts with a low hypericin and hyperforin content to reduce side effects such as phototoxicity. In order to systematically elucidate the therapeutic effects of H. perforatum extracts with different polarities, APP-transgenic mice were treated with a total ethanol extract (TE), a polar extract obtained from TE, and an apolar supercritical CO2 (scCO2) extract. The scCO2 extract was formulated with silicon dioxide (SiO2) for better oral application. APP-transgenic mice were treated with several extracts (total, polar, apolar) at different concentrations. We established an early treatment paradigm from the age of 40 days until the age of 80 days, starting before the onset of cerebral β-amyloid (Aβ) deposition at 45 days of age. Their effects on intracerebral soluble and insoluble Aβ were analyzed using biochemical analyses. Our study confirms that the scCO2H. perforatum formulation shows better biological activity against Aβ-related pathological effects than the TE or polar extracts. Clinically, the treatment resulted in a dose-dependent improvement in food intake with augmentation of the body weight, and, biochemically, it resulted in a significant reduction in both soluble and insoluble Aβ (−27% and −25%, respectively). We therefore recommend apolar H. perforatum extracts for the early oral treatment of patients with mild cognitive impairment or early AD.

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“…Interpretation of the effects might become difficult if more than three mixture components are present, so it can be helpful to virtually consider similar excipients as a single mixture component. In this sense, lipid-based nanocarrier excipients can be formulated as the components of a pseudo-ternary mixture of water, lipids and surfactants-cosurfactants [ 147 , 148 ]. If some upper and/or lower boundaries are known for one or more of the components, constrained mixture designs allow to explore only a subset of the design space [ 149 ].…”

Section: Optimising the Outcomes: Statistical Design Of Experiments (Doe)mentioning

confidence: 99%

Lipid-Based Nanocarriers for Ophthalmic Administration: Towards Experimental Design Implementation

González-Fernández

Bianchera

Gasco³

et al. 2021

Pharmaceutics

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Nanotherapeutics based on biocompatible lipid matrices allow for enhanced solubility of poorly soluble compounds in the treatment of ophthalmic diseases, overcoming the anatomical and physiological barriers present in the eye, which, despite the ease of access, remains strongly protected. Micro-/nanoemulsions, solid lipid nanoparticles (SLN) or nanostructured lipid carriers (NLC) combine liquid and/or solid lipids with surfactants, improving drug stability and ocular bioavailability. Current research and development approaches based on try-and-error methodologies are unable to easily fine-tune nanoparticle populations in order to overcome the numerous constraints of ocular administration routes, which is believed to hamper easy approval from regulatory agencies for these systems. The predictable quality and specifications of the product can be achieved through quality-by-design (QbD) implementation in both research and industrial environments, in contrast to the current quality-by-testing (QbT) framework. Mathematical modelling of the expected final nanoparticle characteristics by variation of operator-controllable variables of the process can be achieved through adequate statistical design-of-experiments (DoE) application. This multivariate approach allows for optimisation of drug delivery platforms, reducing research costs and time, while maximising the understanding of the production process. This review aims to highlight the latest efforts in implementing the design of experiments to produce optimised lipid-based nanocarriers intended for ophthalmic administration. A useful background and an overview of the different possible approaches are presented, serving as a starting point to introduce the design of experiments in current nanoparticle research.

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Development of a Solid Formulation Containing a Microemulsion of a Novel Artemisia Extract with Nematocidal Activity for Oral Administration

Cited by 9 publications

References 54 publications

D-optimal mixture design optimized solid formulation containing fruits extracts of Momordica charantia and Abelmoschus esculentus

D-optimal mixture design optimized solid formulation containing fruits extracts of Momordica charantia and Abelmoschus esculentus

Apolar Extracts of St. John’s Wort Alleviate the Effects of β-Amyloid Toxicity in Early Alzheimer’s Disease

Lipid-Based Nanocarriers for Ophthalmic Administration: Towards Experimental Design Implementation

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