New, Biocompatible, Chitosan-Gelled Microemulsions Based on Essential Oils and Sucrose Esters as Nanocarriers for Topical Delivery of Fluconazole
Biocompatible gel microemulsions containing natural origin excipients are promising nanocarrier systems for the safe and effective topical application of hydrophobic drugs, including antifungals. Recently, to improve fluconazole skin permeation, tolerability and therapeutic efficacy, we developed to...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-12-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/14/1/75 |
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| author | Lavinia Vlaia Ioana Olariu Ana Maria Muţ Georgeta Coneac Vicenţiu Vlaia Dan Florin Anghel Monica Elisabeta Maxim Gabriela Stângă Amadeus Dobrescu Maria Suciu Zoltan Szabadai Dumitru Lupuleasa |
| author_facet | Lavinia Vlaia Ioana Olariu Ana Maria Muţ Georgeta Coneac Vicenţiu Vlaia Dan Florin Anghel Monica Elisabeta Maxim Gabriela Stângă Amadeus Dobrescu Maria Suciu Zoltan Szabadai Dumitru Lupuleasa |
| author_sort | Lavinia Vlaia |
| collection | DOAJ |
| description | Biocompatible gel microemulsions containing natural origin excipients are promising nanocarrier systems for the safe and effective topical application of hydrophobic drugs, including antifungals. Recently, to improve fluconazole skin permeation, tolerability and therapeutic efficacy, we developed topical biocompatible microemulsions based on cinnamon, oregano or clove essential oil (CIN, ORG or CLV) as the oil phase and sucrose laurate (D1216) or sucrose palmitate (D1616) as surfactants, excipients also possessing intrinsic antifungal activity. To follow up this research, this study aimed to improve the adhesiveness of respective fluconazole microemulsions using chitosan (a biopolymer with intrinsic antifungal activity) as gellator and to evaluate the formulation variables’ effect (composition and concentration of essential oil, sucrose ester structure) on the gel microemulsions’ (MEGELs) properties. All MEGELs were evaluated for drug content, pH, rheological behavior, viscosity, spreadability, in vitro drug release and skin permeation and antifungal activity. The results showed that formulation variables determined distinctive changes in the MEGELs’ properties, which were nevertheless in accordance with official requirements for semisolid preparations. The highest flux and release rate values and large diameters of the fungal growth inhibition zone were produced by formulations MEGEL-FZ-D1616-CIN 10%, MEGEL-FZ-D1216-CIN 10% and MEGEL-FZ-D1616-ORG 10%. In conclusion, these MEGELs were demonstrated to be effective platforms for fluconazole topical delivery. |
| first_indexed | 2024-03-10T00:42:47Z |
| format | Article |
| id | doaj.art-0680182b21034d30b4775670b2bc0a6e |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T00:42:47Z |
| publishDate | 2021-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-0680182b21034d30b4775670b2bc0a6e2023-11-23T15:03:27ZengMDPI AGPharmaceutics1999-49232021-12-011417510.3390/pharmaceutics14010075New, Biocompatible, Chitosan-Gelled Microemulsions Based on Essential Oils and Sucrose Esters as Nanocarriers for Topical Delivery of FluconazoleLavinia Vlaia0Ioana Olariu1Ana Maria Muţ2Georgeta Coneac3Vicenţiu Vlaia4Dan Florin Anghel5Monica Elisabeta Maxim6Gabriela Stângă7Amadeus Dobrescu8Maria Suciu9Zoltan Szabadai10Dumitru Lupuleasa11Department II—Pharmaceutical Technology, Formulation and Technology of Drugs Research Center, “Victor Babeș” University of Medicine and Pharmacy, 300041 Timișoara, RomaniaDepartment II—Pharmaceutical Technology, Formulation and Technology of Drugs Research Center, “Victor Babeș” University of Medicine and Pharmacy, 300041 Timișoara, RomaniaDepartment II—Pharmaceutical Technology, Formulation and Technology of Drugs Research Center, “Victor Babeș” University of Medicine and Pharmacy, 300041 Timișoara, RomaniaDepartment II—Pharmaceutical Technology, Formulation and Technology of Drugs Research Center, “Victor Babeș” University of Medicine and Pharmacy, 300041 Timișoara, RomaniaDepartment I—Organic Chemistry, Formulation and Technology of Drugs Research Center, “Victor Babeș” University of Medicine and Pharmacy, 300041 Timișoara, Romania“Ilie Murgulescu” Institute of Physical Chemistry of the Romanian Academy, Laboratory of Colloid Chemistry, 060021 Bucharest, Romania“Ilie Murgulescu” Institute of Physical Chemistry of the Romanian Academy, Laboratory of Colloid Chemistry, 060021 Bucharest, Romania“Ilie Murgulescu” Institute of Physical Chemistry of the Romanian Academy, Laboratory of Colloid Chemistry, 060021 Bucharest, RomaniaDepartment X Surgery 2–Surgery 2, “Victor Babeș” University of Medicine and Pharmacy, 300041 Timișoara, RomaniaDepartment II—Pharmacology and Pharmacotherapy, “Victor Babeș” University of Medicine and Pharmacy, 300041 Timișoara, RomaniaNational Institute for Research and Development in Electrochemistry and Condensed Matter, 300569 Timişoara, RomaniaDepartment of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 020956 Bucharest, RomaniaBiocompatible gel microemulsions containing natural origin excipients are promising nanocarrier systems for the safe and effective topical application of hydrophobic drugs, including antifungals. Recently, to improve fluconazole skin permeation, tolerability and therapeutic efficacy, we developed topical biocompatible microemulsions based on cinnamon, oregano or clove essential oil (CIN, ORG or CLV) as the oil phase and sucrose laurate (D1216) or sucrose palmitate (D1616) as surfactants, excipients also possessing intrinsic antifungal activity. To follow up this research, this study aimed to improve the adhesiveness of respective fluconazole microemulsions using chitosan (a biopolymer with intrinsic antifungal activity) as gellator and to evaluate the formulation variables’ effect (composition and concentration of essential oil, sucrose ester structure) on the gel microemulsions’ (MEGELs) properties. All MEGELs were evaluated for drug content, pH, rheological behavior, viscosity, spreadability, in vitro drug release and skin permeation and antifungal activity. The results showed that formulation variables determined distinctive changes in the MEGELs’ properties, which were nevertheless in accordance with official requirements for semisolid preparations. The highest flux and release rate values and large diameters of the fungal growth inhibition zone were produced by formulations MEGEL-FZ-D1616-CIN 10%, MEGEL-FZ-D1216-CIN 10% and MEGEL-FZ-D1616-ORG 10%. In conclusion, these MEGELs were demonstrated to be effective platforms for fluconazole topical delivery.https://www.mdpi.com/1999-4923/14/1/75biocompatible sucrose esteressential oilchitosanmicroemulsionantifungalfluconazole |
| spellingShingle | Lavinia Vlaia Ioana Olariu Ana Maria Muţ Georgeta Coneac Vicenţiu Vlaia Dan Florin Anghel Monica Elisabeta Maxim Gabriela Stângă Amadeus Dobrescu Maria Suciu Zoltan Szabadai Dumitru Lupuleasa New, Biocompatible, Chitosan-Gelled Microemulsions Based on Essential Oils and Sucrose Esters as Nanocarriers for Topical Delivery of Fluconazole Pharmaceutics biocompatible sucrose ester essential oil chitosan microemulsion antifungal fluconazole |
| title | New, Biocompatible, Chitosan-Gelled Microemulsions Based on Essential Oils and Sucrose Esters as Nanocarriers for Topical Delivery of Fluconazole |
| title_full | New, Biocompatible, Chitosan-Gelled Microemulsions Based on Essential Oils and Sucrose Esters as Nanocarriers for Topical Delivery of Fluconazole |
| title_fullStr | New, Biocompatible, Chitosan-Gelled Microemulsions Based on Essential Oils and Sucrose Esters as Nanocarriers for Topical Delivery of Fluconazole |
| title_full_unstemmed | New, Biocompatible, Chitosan-Gelled Microemulsions Based on Essential Oils and Sucrose Esters as Nanocarriers for Topical Delivery of Fluconazole |
| title_short | New, Biocompatible, Chitosan-Gelled Microemulsions Based on Essential Oils and Sucrose Esters as Nanocarriers for Topical Delivery of Fluconazole |
| title_sort | new biocompatible chitosan gelled microemulsions based on essential oils and sucrose esters as nanocarriers for topical delivery of fluconazole |
| topic | biocompatible sucrose ester essential oil chitosan microemulsion antifungal fluconazole |
| url | https://www.mdpi.com/1999-4923/14/1/75 |
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