GLUCAN PARTICLES AS PROMISING CARRIERS FOR ENHANCING THE BIOAVAILABILITY OF ATORVASTATIN

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22340%2F19%3A43919868" target="_blank" >RIV/60461373:22340/19:43919868 - isvavai.cz</a>

Výsledek na webu

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DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

GLUCAN PARTICLES AS PROMISING CARRIERS FOR ENHANCING THE BIOAVAILABILITY OF ATORVASTATIN

Popis výsledku v původním jazyce

Atorvastatin (ATO) is a member of the statins, a group of drugs used to prevent cardiovascular diseases. Statins inhibit 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA), the enzyme involved in the synthesis of cholesterol; therefore, they are widely used for the treatment of hypercholesterolemia. More recently, statins have been studied for their potential to promote the formation of new bone by increasing the expression of bone morphogenic protein-2 (BMP-2) gene in bone cells, becoming potential candidates in treatment of osteoporosis or bone fractures. However, the delivery of statins is challenging. Atorvastatin, for instance, is poorly soluble in water and undergoes first-past metabolism, leading to low bioavailability. In this work, we propose the use of glucan particles (GPs) as promising carriers for atorvastatin. Glucan particles are obtained from Saccharomyces cerevisiae (baker’s yeast); they are mainly composed of amorphous polysaccharides (&gt;85% β-glucans) and they exhibit immunomodulatory properties. In our previous work, we encapsulated low-water soluble drugs into glucan particles and the resulting composites were completely amorphous and exhibited much faster dissolution kinetics. In addition, due to their immunomodulatory activity, the encapsulated drug can potentially be distributed through the lymphatic system into blood circulation. This approach affords possibility to increase the bioavailability of drug inside organism. The ATO/GPs composites were produced by spray drying method, and characterized by SEM, XRD, flowability, encapsulation efficiency and dissolution kinetics. The cytotoxicity and anti-inflammatory activity were tested in vitro. With an encapsulation efficiency of (96.7 ± 4.5%), the ATP/GPs composites were completely amorphous and did not show any cytotoxicity in vitro. In conclusion, glucan particles are suitable as natural carriers for atorvastatin, and the results obtained evidence their potential to enhance its bioavailability and improve its dissolution in biological environment.

Název v anglickém jazyce

GLUCAN PARTICLES AS PROMISING CARRIERS FOR ENHANCING THE BIOAVAILABILITY OF ATORVASTATIN

Popis výsledku anglicky

Atorvastatin (ATO) is a member of the statins, a group of drugs used to prevent cardiovascular diseases. Statins inhibit 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA), the enzyme involved in the synthesis of cholesterol; therefore, they are widely used for the treatment of hypercholesterolemia. More recently, statins have been studied for their potential to promote the formation of new bone by increasing the expression of bone morphogenic protein-2 (BMP-2) gene in bone cells, becoming potential candidates in treatment of osteoporosis or bone fractures. However, the delivery of statins is challenging. Atorvastatin, for instance, is poorly soluble in water and undergoes first-past metabolism, leading to low bioavailability. In this work, we propose the use of glucan particles (GPs) as promising carriers for atorvastatin. Glucan particles are obtained from Saccharomyces cerevisiae (baker’s yeast); they are mainly composed of amorphous polysaccharides (&gt;85% β-glucans) and they exhibit immunomodulatory properties. In our previous work, we encapsulated low-water soluble drugs into glucan particles and the resulting composites were completely amorphous and exhibited much faster dissolution kinetics. In addition, due to their immunomodulatory activity, the encapsulated drug can potentially be distributed through the lymphatic system into blood circulation. This approach affords possibility to increase the bioavailability of drug inside organism. The ATO/GPs composites were produced by spray drying method, and characterized by SEM, XRD, flowability, encapsulation efficiency and dissolution kinetics. The cytotoxicity and anti-inflammatory activity were tested in vitro. With an encapsulation efficiency of (96.7 ± 4.5%), the ATP/GPs composites were completely amorphous and did not show any cytotoxicity in vitro. In conclusion, glucan particles are suitable as natural carriers for atorvastatin, and the results obtained evidence their potential to enhance its bioavailability and improve its dissolution in biological environment.

Druh

O - Ostatní výsledky

CEP obor

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OECD FORD obor

20401 - Chemical engineering (plants, products)

Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Rok uplatnění

2019

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů