دورية أكاديمية
Novel transdermal bioadhesive surfactant-based system for release and solubility improvement of antimalarial drugs artemether-lumefantrine.
| العنوان: | Novel transdermal bioadhesive surfactant-based system for release and solubility improvement of antimalarial drugs artemether-lumefantrine. |
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| المؤلفون: | Volpe-Zanutto F; Graduate School of Bioscience and Technology of Bioactive Products, Biology Institute, University at Campinas, Campinas, Sao Paulo, Brazil.; School of Pharmacy, Queen's University Belfast, Belfast, United Kingdom., Fonseca-Santos B; UNESP- University Estadual Paulista, Faculdade de Ciências Farmacêuticas, UNESP, Araraquara, Sao Paulo, Brazil.; Faculty of Pharmaceutical Science, University at Campinas, Campinas, Sao Paulo, Brazil., McKenna PE; School of Pharmacy, Queen's University Belfast, Belfast, United Kingdom., Paredes AJ; School of Pharmacy, Queen's University Belfast, Belfast, United Kingdom., Dávila JL; Centre for Information Technology 'Renato Archer' (CTI), 3D Printing open lab-Laprint, Campinas, Sao Paulo, Brazil., McCrudden MTC; School of Pharmacy, Queen's University Belfast, Belfast, United Kingdom., Tangerina MMP; Universidade de São Paulo, Departamento de Botânica, Instituto de Biociências, Sao Paulo, Sao Paulo, Brazil., Ceccheto Figueiredo M; Faculdade de Ciências Médicas, Universidade Estadual de Campinas, Campinas, Sao Paulo, Brazil., Vilegas W; UNESP- Univ Estadual Paulista, Instituto de Biociências, São Vicente, Sao Paulo, Brazil., Brisibe A; University of Calabar, Calabar, Nigeria., Akira D'Ávila M; School of Mechanical Engineering, University of Campinas, Campinas, Sao Paulo, Brazil., Donnelly RF; School of Pharmacy, Queen's University Belfast, Belfast, United Kingdom., Chorilli M; UNESP- University Estadual Paulista, Faculdade de Ciências Farmacêuticas, UNESP, Araraquara, Sao Paulo, Brazil., Foglio MA; Faculty of Pharmaceutical Science, University at Campinas, Campinas, Sao Paulo, Brazil. |
| المصدر: | Biomedical materials (Bristol, England) [Biomed Mater] 2021 Oct 04; Vol. 16 (6). Date of Electronic Publication: 2021 Oct 04. |
| نوع المنشور: | Journal Article; Research Support, Non-U.S. Gov't |
| اللغة: | English |
| بيانات الدورية: | Publisher: Institute of Physics Pub Country of Publication: England NLM ID: 101285195 Publication Model: Electronic Cited Medium: Internet ISSN: 1748-605X (Electronic) Linking ISSN: 17486041 NLM ISO Abbreviation: Biomed Mater Subsets: MEDLINE |
| أسماء مطبوعة: | Original Publication: Bristol, UK : Institute of Physics Pub., |
| مواضيع طبية MeSH: | Antimalarials*/administration & dosage , Antimalarials*/chemistry , Antimalarials*/pharmacokinetics , Artemether, Lumefantrine Drug Combination*/administration & dosage , Artemether, Lumefantrine Drug Combination*/chemistry , Artemether, Lumefantrine Drug Combination*/pharmacokinetics, Surface-Active Agents/*chemistry, Administration, Cutaneous ; Animals ; Humans ; Skin/metabolism ; Solubility ; Swine |
| مستخلص: | Artemether (ART) and lumefantrine (LUM) are the gold standard antimalarial drugs used for the treatment of malaria in children and pregnant women. Typically, ART and LUM are delivered orally in the form of a combined tablet, however, the appropriateness of this route of administration for these drugs is questionable due to the poor absorption and therefore bioavailability observed unless administered alongside lipid-rich foods. Transdermal drug delivery in the form of a patch-type system has been identified as a viable alternative to the conventional tablet-based therapy. A novel, surfactant-based ART-LUM formulation (S3AL), developed for transdermal delivery, may eliminate the shortcomings associated with oral delivery; namely poor drug absorption which is caused by the inherently low solubility of ART and LUM. Moreover, by successfully delivering these antimalarials transdermally, first-pass metabolism will be avoided leading to enhanced drug bioavailability in both cases. The S3AL formulation contained ART and LUM at equal concentrations (2.5% w/w of each) as well as Procetyl® AWS (30% w/w), oleic acid (10% w/w), 1-methyl-2-pyrrolidone (10% w/w), and water (45% w/w). The addition of LUM to the formulation changed the system from a striae structure to a dark field structure when visualized by a polarized light microscope. Additionally, this system possessed higher viscosity and superior skin bioadhesion, as evidenced by mechanical characterization, when compared to a similar formulation containing ART alone. S3AL was also proven to be biocompatible to human keratinocyte cells. Finally, in vitro studies demonstrated the propensity of S3AL for successful delivery via the transdermal route, with 2279 ± 295 µg cm -2 of ART and 94 ± 13 µg cm -2 of LUM having permeated across dermatomed porcine skin after 24 h, highlighting its potential as a new candidate for the treatment of malaria. (Creative Commons Attribution license.) |
| فهرسة مساهمة: | Keywords: artemether; lumefantrine; malaria; surfactant-based system; transdermal |
| المشرفين على المادة: | 0 (Antimalarials) 0 (Artemether, Lumefantrine Drug Combination) 0 (Surface-Active Agents) |
| تواريخ الأحداث: | Date Created: 20210920 Date Completed: 20220311 Latest Revision: 20220311 |
| رمز التحديث: | 20221213 |
| DOI: | 10.1088/1748-605X/ac2885 |
| PMID: | 34544052 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1748-605X |
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| DOI: | 10.1088/1748-605X/ac2885 |