Semisynthetic Derivative of Artemisia annua-Loaded Transdermal Bioadhesive for the Treatment of Uncomplicated Malaria Caused by Plasmodium falciparum in Children

Author(s):Show less -

Zanutto, Fabiana Volpe ^{[1, 2, 3]} ; McAlister, Emma ^[2] ; Pereira Tangerina, Marcelo Marucci ^[4] ; Fonseca-Santos, Bruno ^[5] ; Costa Salles, Tais Helena ^[6] ; Oliveira Souza, Ilza Maria ^[1] ; Brisibe, Andi ^[7] ; Vilegas, Wagner ^[8] ; Chorilli, Marlus ^[5] ; d'Avila, Marcos Akira ^[6] ; Donnelly, Ryan F. ^[2] ; Foglio, Mary Ann ^[9]

Affiliation

^[1] Ctr Pluridisciplinar Pesquisas Quim Biol & Agr, Paulinia, SP - Brazil

^[2] Queens Univ Belfast, Sch Pharm, Belfast, Antrim - North Ireland

^[3] Univ Estadual Campinas, Inst Biol, Grad Sch Biosci & Technol Bioact Prod, Campinas, SP - Brazil

^[4] Univ Sao Paulo, Inst Biociencias, Dept Bot, Sao Paulo - Brazil

^[5] UNESP Univ Estadual Paulista, Fac Ciencias Farmaceut, Araraquara, SP - Brazil

^[6] Univ Estadual Campinas, Sch Mech Engn, Campinas, SP - Brazil

^[7] Univ Calabar, Calabar - Nigeria

^[8] UNESP Univ Estadual Paulista, Inst Biociencias, Sao Vicente, S Glam - Wales

^[9] Univ Estadual Campinas, Fac Pharmaceut Sci, Campinas, SP - Brazil

• Document type: Journal article
• Source: Journal of Pharmaceutical Sciences; v. 108, n. 3, p. 1177-1188, MAR 2019.
• Web of Science Citations: 2

Abstract

According to the most recent World Health Organization statistics, malaria infected approximately 219 million people in 2017, with an estimate of 435,000 deaths (World Health Organization, 2018). Communities isolated from cities are the most deprived of access to the necessary hospital facilities. Herein we report the development of a transdermal bioadhesive containing artemether (ART), an alternative, potentially lifesaving, treatment regimen for malaria in low-resource settings. Bioadhesives were prepared from an aqueous blend of hydroxyethylcellulose (4.5% w/w), ART, propoxylated-ethoxylated-cetyl-alcohol, polysorbate 80, propyleneglycol, glycerine, mineral oil, and oleic acid. In this study, the average pore size of bioadhesive 5.5b was 52.6 +/- 15.31 mm. Differential scanning calorimetry and thermogravimetric analyses confirm the thermal stability of ART bioadhesives at room temperature. Tensile tests indicated good mechanical properties for bioadhesive 5.5b, when compared to 5.5a, where 5.5b showed elastic modulus 0.19 MPa, elongation at break 204%, tensile stress 0.31 MPa, tensile strength at break 0.23 MPa. Bioadhesion assays suggested that formulations containing surfactants had higher detachment forces. Permeation studies demonstrated that the best outcome was achieved with a bioadhesive containing 25 mg ART (5.5b) that after 24 h released 6971 +/- 125 mu g, which represents approximately 28% of drug permeation. Data reported presents a promising candidate for a new antimalarial transdermal formulation. (c) 2019 American Pharmacists Association (R). Published by Elsevier Inc. All rights reserved. (AU)

• FAPESP's process: 16/18384-8 - Development of patches containing the association of artemether-lumefantrine for the treatment of malaria caused by Plasmodium falciparum
• Grantee: Fabiana Volpe Zanutto
• Support Opportunities: Scholarships abroad - Research Internship - Doctorate
• FAPESP's process: 14/16008-3 - Development of patches containing the association of artemether - lumefantrine for the treatment of malaria caused by Plasmodium falciparum
• Grantee: Fabiana Volpe Zanutto
• Support Opportunities: Scholarships in Brazil - Doctorate