Spray-Dried Proliposomes: an Innovative Method for Encapsulation of Rosmarinus officinalis L. Polyphenols

This work aims to improve the functionality of Rosmarinus officinalis L. (rosemary) polyphenols by encapsulation in an optimized proliposome formulation. A 2 3 Box-Wilson central composite design (CCD) was employed to determine lone and interaction effects of composition variables on moisture conten...

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Veröffentlicht in:AAPS PharmSciTech 2020-05, Vol.21 (5), p.143-143, Article 143
Hauptverfasser: Bankole, Victor Oloruntoba, Osungunna, Michael Oluwole, Souza, Claudia Regina Fernandes, Salvador, Sergio Luiz, Oliveira, Wanderley Pereira
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container_issue 5
container_start_page 143
container_title AAPS PharmSciTech
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creator Bankole, Victor Oloruntoba
Osungunna, Michael Oluwole
Souza, Claudia Regina Fernandes
Salvador, Sergio Luiz
Oliveira, Wanderley Pereira
description This work aims to improve the functionality of Rosmarinus officinalis L. (rosemary) polyphenols by encapsulation in an optimized proliposome formulation. A 2 3 Box-Wilson central composite design (CCD) was employed to determine lone and interaction effects of composition variables on moisture content ( X p ); water activity ( A w ); concentration and retention of rosemary polyphenols—rosmarinic acid (ROA), carnosol (CAR), and carnosic acid (CNA); and recovery of spray-dried proliposomes (SDP). Processing conditions which generate proliposomes with optimum physicochemical properties were determined by multi-response analysis (desirability approach). Antioxidant and antifungal activities were evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH • ) sequestering and minimum inhibitory concentration (MIC)/minimum fungicidal concentration (MFC) assays, respectively. SDP exhibited high polyphenol retention, ranging from 62.0 to 100.0% w/w, showing dependence on composition variables and polyphenol lipophilicity. SDP recovery ranged from 20.1 to 45.8%, with X p and A w of 1.7 ± 0.14–2.5 ± 0.23% w/w and 0.30 ± 0.004–0.47 ± 0.003, respectively, evidencing product with good chemical and microbiological stability. Optimum liposomal composition was determined, namely, lipid concentration (4.26% w/w), lyophilized extract (LE) concentration (4.48% w/w), and drying aid:(lipid+extract) ratio (7.55% w/w) on wet basis. Relative errors between experimental and predicted values for SDP properties showed concurrence for all responses except CAR retention, being 22% lower. SDP showed high antioxidant activity with IC 50 of 9.2 ± 0.2 μg/mL, superior to results obtained for LE (10.8 μg/mL) and butylated hydroxytoluene (BHT), a synthetic antioxidant (12.5 μg/mL). MIC and MFC against Candida albicans (ATCC1023) were 312.5 μg/mL and 1250 μg/mL, respectively, a moderate antimicrobial activity for phytochemical-based products. SDP is shown as a veritable tool to encapsulate hydrophilic and lipophilic rosemary polyphenols generating a product with optimal physicochemical and biological properties.
doi_str_mv 10.1208/s12249-020-01668-2
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Processing conditions which generate proliposomes with optimum physicochemical properties were determined by multi-response analysis (desirability approach). Antioxidant and antifungal activities were evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH • ) sequestering and minimum inhibitory concentration (MIC)/minimum fungicidal concentration (MFC) assays, respectively. SDP exhibited high polyphenol retention, ranging from 62.0 to 100.0% w/w, showing dependence on composition variables and polyphenol lipophilicity. SDP recovery ranged from 20.1 to 45.8%, with X p and A w of 1.7 ± 0.14–2.5 ± 0.23% w/w and 0.30 ± 0.004–0.47 ± 0.003, respectively, evidencing product with good chemical and microbiological stability. Optimum liposomal composition was determined, namely, lipid concentration (4.26% w/w), lyophilized extract (LE) concentration (4.48% w/w), and drying aid:(lipid+extract) ratio (7.55% w/w) on wet basis. Relative errors between experimental and predicted values for SDP properties showed concurrence for all responses except CAR retention, being 22% lower. SDP showed high antioxidant activity with IC 50 of 9.2 ± 0.2 μg/mL, superior to results obtained for LE (10.8 μg/mL) and butylated hydroxytoluene (BHT), a synthetic antioxidant (12.5 μg/mL). MIC and MFC against Candida albicans (ATCC1023) were 312.5 μg/mL and 1250 μg/mL, respectively, a moderate antimicrobial activity for phytochemical-based products. 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Polyphenols</title><title>AAPS PharmSciTech</title><addtitle>AAPS PharmSciTech</addtitle><addtitle>AAPS PharmSciTech</addtitle><description>This work aims to improve the functionality of Rosmarinus officinalis L. (rosemary) polyphenols by encapsulation in an optimized proliposome formulation. A 2 3 Box-Wilson central composite design (CCD) was employed to determine lone and interaction effects of composition variables on moisture content ( X p ); water activity ( A w ); concentration and retention of rosemary polyphenols—rosmarinic acid (ROA), carnosol (CAR), and carnosic acid (CNA); and recovery of spray-dried proliposomes (SDP). Processing conditions which generate proliposomes with optimum physicochemical properties were determined by multi-response analysis (desirability approach). Antioxidant and antifungal activities were evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH • ) sequestering and minimum inhibitory concentration (MIC)/minimum fungicidal concentration (MFC) assays, respectively. SDP exhibited high polyphenol retention, ranging from 62.0 to 100.0% w/w, showing dependence on composition variables and polyphenol lipophilicity. SDP recovery ranged from 20.1 to 45.8%, with X p and A w of 1.7 ± 0.14–2.5 ± 0.23% w/w and 0.30 ± 0.004–0.47 ± 0.003, respectively, evidencing product with good chemical and microbiological stability. Optimum liposomal composition was determined, namely, lipid concentration (4.26% w/w), lyophilized extract (LE) concentration (4.48% w/w), and drying aid:(lipid+extract) ratio (7.55% w/w) on wet basis. Relative errors between experimental and predicted values for SDP properties showed concurrence for all responses except CAR retention, being 22% lower. SDP showed high antioxidant activity with IC 50 of 9.2 ± 0.2 μg/mL, superior to results obtained for LE (10.8 μg/mL) and butylated hydroxytoluene (BHT), a synthetic antioxidant (12.5 μg/mL). MIC and MFC against Candida albicans (ATCC1023) were 312.5 μg/mL and 1250 μg/mL, respectively, a moderate antimicrobial activity for phytochemical-based products. 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Antioxidant and antifungal activities were evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH • ) sequestering and minimum inhibitory concentration (MIC)/minimum fungicidal concentration (MFC) assays, respectively. SDP exhibited high polyphenol retention, ranging from 62.0 to 100.0% w/w, showing dependence on composition variables and polyphenol lipophilicity. SDP recovery ranged from 20.1 to 45.8%, with X p and A w of 1.7 ± 0.14–2.5 ± 0.23% w/w and 0.30 ± 0.004–0.47 ± 0.003, respectively, evidencing product with good chemical and microbiological stability. Optimum liposomal composition was determined, namely, lipid concentration (4.26% w/w), lyophilized extract (LE) concentration (4.48% w/w), and drying aid:(lipid+extract) ratio (7.55% w/w) on wet basis. Relative errors between experimental and predicted values for SDP properties showed concurrence for all responses except CAR retention, being 22% lower. SDP showed high antioxidant activity with IC 50 of 9.2 ± 0.2 μg/mL, superior to results obtained for LE (10.8 μg/mL) and butylated hydroxytoluene (BHT), a synthetic antioxidant (12.5 μg/mL). MIC and MFC against Candida albicans (ATCC1023) were 312.5 μg/mL and 1250 μg/mL, respectively, a moderate antimicrobial activity for phytochemical-based products. SDP is shown as a veritable tool to encapsulate hydrophilic and lipophilic rosemary polyphenols generating a product with optimal physicochemical and biological properties.</abstract><cop>Cham</cop><pub>Springer International Publishing</pub><pmid>32424702</pmid><doi>10.1208/s12249-020-01668-2</doi><tpages>1</tpages><oa>free_for_read</oa></addata></record>
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subjects Biochemistry
Biomedical and Life Sciences
Biomedicine
Biotechnology
Pharmacology/Toxicology
Pharmacy
Research Article
title Spray-Dried Proliposomes: an Innovative Method for Encapsulation of Rosmarinus officinalis L. Polyphenols
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