onoketonic Curcuminoid-Lidocaine Co-Deliver Using Thermosensitive Organogels: From Drug Synthesis to Epidermis Structural Studie

Autor(es):Mostrar menos -

Vigato, Aryane A. ^[1] ; Machado, Ian P. ^[2] ; del Valle, Matheus ^[3] ; da Ana, Patricia A. ^[3] ; Sepulveda, Anderson F. ^[1] ; Yokaichiya, Fabiano ^[4] ; Franco, Margareth K. K. D. ^[5] ; Loiola, Messias C. ^[1] ; Tofoli, Giovana R. ^[6] ; Cereda, Cintia Maria S. ^[6] ; de Sairre, Mirela I. ^[1] ; de Araujo, Daniele R. ^[1]

Afiliação do(s) autor(es)

^[1] Fed Univ ABC, Human & Nat Sci Ctr, BR-09210580 Sao Paulo, SP - Brazil

^[2] Univ Sao Paulo, Inst Chem, Dept Fundamental Chem, BR-05508000 Sao Paulo, SP - Brazil

^[3] Fed Univ ABC, Ctr Engn Modeling & Appl Social Sci, BR-09606045 Sao Bernardo, SP - Brazil

^[4] Helmholtz Zentrum Berlin Mat, Dept Quantum Phenomena Novel Mat, D-14109 Berlin - Germany

^[5] Nucl & Energy Res Inst, BR-01000000 Sao Paulo, SP - Brazil

^[6] Sao Leopoldo Mandic Res Unit, BR-13000000 Campinas, SP - Brazil

• Tipo de documento: Artigo Científico
• Fonte: HARMACEUTIC; v. 14, n. 2 FEB 2022.
• Citações Web of Science: 0

Resumo

Organogels (ORGs) are remarkable matrices due to their versatile chemical composition and straightforward preparation. This study proposes the development of ORGs as dual drug-carrier systems, considering the application of synthetic monoketonic curcuminoid (m-CUR) and lidocaine (LDC) to treat topical inflammatory lesions. The monoketone curcuminoid (m-CUR) was synthesized by using an innovative method via a NbCl5-acid catalysis. ORGs were prepared by associating an aqueous phase composed of Pluronic F127 and LDC hydrochloride with an organic phase comprising isopropyl myristate (IPM), soy lecithin (LEC), and the synthesized m-CUR. Physicochemical characterization was performed to evaluate the influence of the organic phase on the ORGs supramolecular organization, permeation profiles, cytotoxicity, and epidermis structural characteristics. The physico-chemical properties of the ORGs were shown to be strongly dependent on the oil phase constitution. Results revealed that the incorporation of LEC and m-CUR shifted the sol-gel transition temperature, and that the addition of LDC enhanced the rheological G `/G `' ratio to higher values compared to original ORGs. Consequently, highly structured gels lead to gradual and controlled LDC permeation profiles from the ORG formulations. Porcine ear skin epidermis was treated with ORGs and evaluated by infrared spectroscopy (FTIR), where the stratum corneum lipids were shown to transition from a hexagonal to a liquid crystal phase. Quantitative optical coherence tomography (OCT) analysis revealed that LEC and m-CUR additives modify skin structuring. Data from this study pointed ORGs as promising formulations for skin-delivery. (AU)

• Processo FAPESP: 19/20303-4 - Organogéis termosensíveis como estratégias para o tratamento de processos inflamatórios: da estrutura supramolecular à avaliação farmacológica
• Beneficiário: Daniele Ribeiro de Araujo
• Modalidade de apoio: Auxílio à Pesquisa - Regular
• Processo FAPESP: 16/18045-9 - Estudo da reação multicomponente de Hantzsch para a síntese de novos inibidores da dipeptidil peptidase 4 (DPP-4) para o tratamento de Diabetes tipo II
• Beneficiário: Mirela Inês de Sairre
• Modalidade de apoio: Auxílio à Pesquisa - Regular
• Processo FAPESP: 19/14773-8 - Organogéis lecitina-poloxamer como carreadores de fármacos para aplicação tópica: desenvolvimento, perfil de permeação e avaliação estrutural do estrato córneo
• Beneficiário: Aryane Alves Vigato
• Modalidade de apoio: Bolsas no Brasil - Doutorado Direto