Essential oils (EOs) have been widely used for their antimicrobial and antifungal properties but their instability to light and high volatility can limit the clinical practice [1]. A useful strategy to improve their biopharmaceutical properties is represented by drug delivery systems. Aim of the present study was to formulate, optimize and evaluate vesicles loaded by Artemisia annua essential oil (AEO). The inflorescence of A. annua were collected in November and hydro-distilled in a Clevenger like apparatus. GC-MS analyses of the resulting EO revealed that his main constituents were camphor (22,6 %), artemisia ketone (17,3 %) and 1,8-cineole (15,8 %). Phosphatidylcholine and cholesterol liposomes loaded with 100 µL/mL of EO were optimized for their size, polydispersity index (PDI), ζ-potential and morphology. The recovery, encapsulation efficiency (EE%) and release properties were evaluated both for PBS liposomes both for the one made using RPMI-MOPS medium. On this last type of vesicle were performed the antifungal assay on Candida species [2]. Results showed that the vesicles exhibit spherical shape, average sizes about 250 nm, the ζ potential about -10 mV, the PDI was about 0.21, EE% were around 75% while the recovery were over 90%. The drug release study showed that after 14 hours almost 100% EO was released from the vesicles. Quantitative analysis were carried out using a HPLC1100-DAD. Liposomes were physically and chemically stable over one month period if stored at 4°C. The minimum fungicidal concentrations (MFCs) of AEO and EO-loaded liposomes was performed against 10 fungal strains of Candida. Positive control was made by amphotericin B. The MFC values ranged from 9.8 to 42 μL/mL of EO and from 5 to 10 μL/mL of EO-load in liposomes. Among the Candida species tested, the most susceptible to EO was C. norvegensis (6.25 μL/mL), followed by C. albicans ATCC 10231 and C. krusei ATCC 6258 while the most susceptible specie to EO-loaded liposomes was C. norvegensis (5.00 μL/mL), followed by C. krusei from our collection. Statistic was made by t student test. Significant difference was expressed as p<0.01. The findings suggest that EOloaded liposome proved to be more effective against Candida species than the free essential oil. The findings suggest that these formulations can decrease the volatility of EOs, optimize their biological properties and defeat antifungal infections.
Artemisia annua essential oils liposomes: optimization and in vitro antifungal activity evaluation against Candida species / Laura Risaliti, Gabriella Pini, Rosa Donato, Cristiana Sacco, Roberta Ascrizzi, G. Vanti, M.C. Bergonzi, A.R. Bilia. - ELETTRONICO. - 85:(2019), pp. 1424-1424. (Intervento presentato al convegno XVI Congress of the italian society of fitochemestry jointly with 2nd international Congress on edible, medicinal and aromatic plants (ICEMAP 2019) tenutosi a Alghero nel 19-21 giugno 2019).
Artemisia annua essential oils liposomes: optimization and in vitro antifungal activity evaluation against Candida species.
Laura RisalitiMembro del Collaboration Group
;Gabriella PiniMembro del Collaboration Group
;Rosa DonatoMembro del Collaboration Group
;Cristiana SaccoMembro del Collaboration Group
;G. VantiMembro del Collaboration Group
;M. C. BergonziMembro del Collaboration Group
;A. R. BiliaMembro del Collaboration Group
2019
Abstract
Essential oils (EOs) have been widely used for their antimicrobial and antifungal properties but their instability to light and high volatility can limit the clinical practice [1]. A useful strategy to improve their biopharmaceutical properties is represented by drug delivery systems. Aim of the present study was to formulate, optimize and evaluate vesicles loaded by Artemisia annua essential oil (AEO). The inflorescence of A. annua were collected in November and hydro-distilled in a Clevenger like apparatus. GC-MS analyses of the resulting EO revealed that his main constituents were camphor (22,6 %), artemisia ketone (17,3 %) and 1,8-cineole (15,8 %). Phosphatidylcholine and cholesterol liposomes loaded with 100 µL/mL of EO were optimized for their size, polydispersity index (PDI), ζ-potential and morphology. The recovery, encapsulation efficiency (EE%) and release properties were evaluated both for PBS liposomes both for the one made using RPMI-MOPS medium. On this last type of vesicle were performed the antifungal assay on Candida species [2]. Results showed that the vesicles exhibit spherical shape, average sizes about 250 nm, the ζ potential about -10 mV, the PDI was about 0.21, EE% were around 75% while the recovery were over 90%. The drug release study showed that after 14 hours almost 100% EO was released from the vesicles. Quantitative analysis were carried out using a HPLC1100-DAD. Liposomes were physically and chemically stable over one month period if stored at 4°C. The minimum fungicidal concentrations (MFCs) of AEO and EO-loaded liposomes was performed against 10 fungal strains of Candida. Positive control was made by amphotericin B. The MFC values ranged from 9.8 to 42 μL/mL of EO and from 5 to 10 μL/mL of EO-load in liposomes. Among the Candida species tested, the most susceptible to EO was C. norvegensis (6.25 μL/mL), followed by C. albicans ATCC 10231 and C. krusei ATCC 6258 while the most susceptible specie to EO-loaded liposomes was C. norvegensis (5.00 μL/mL), followed by C. krusei from our collection. Statistic was made by t student test. Significant difference was expressed as p<0.01. The findings suggest that EOloaded liposome proved to be more effective against Candida species than the free essential oil. The findings suggest that these formulations can decrease the volatility of EOs, optimize their biological properties and defeat antifungal infections.
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