Preliminary studies on drug delivery of polymeric primaquine microparticles using the liver high uptake effect based on size of particles to improve malaria treatment.

Autor: da Silva de Barros AO; Brazilian Nuclear Energy Commission, Nuclear Engineering Institute, Laboratory of Novel Radiopharmaceuticals and Nano-radiopharmacy, Rio de Janeiro 21941906, Brazil., Portilho FL; Brazilian Nuclear Energy Commission, Nuclear Engineering Institute, Laboratory of Novel Radiopharmaceuticals and Nano-radiopharmacy, Rio de Janeiro 21941906, Brazil., Dos Santos Matos AP; Federal University of Rio de Janeiro, School of Pharmacy, Rio de Janeiro 21941901, Brazil., Ricci-Junior E; Federal University of Rio de Janeiro, School of Pharmacy, Rio de Janeiro 21941901, Brazil., Alencar LMR; Federal University of Maranhão, Laboratory of Biophysics and Nanosystems, São Luis do Maranhão 65080805, Brazil., Dos Santos CC; Federal University of Maranhão, Laboratory of Biophysics and Nanosystems, São Luis do Maranhão 65080805, Brazil., Paumgartten FJR; National School of Public Health, Oswaldo Cruz Foundation (FIOCRUZ), Rio de Janeiro 21041361, Brazil., Iram SH; Department of Chemistry and Biochemistry, College of Natural Sciences, South Dakota State University, Brookings, SD 57007, USA., Mazier D; Sorbonne Université, INSERM, CNRS, INSERM U1135, Centre d'Immunologie et des Maladies Infectieuses, CIMI-Paris, Paris 75005, France., Franetich JF; Sorbonne Université, INSERM, CNRS, INSERM U1135, Centre d'Immunologie et des Maladies Infectieuses, CIMI-Paris, Paris 75005, France., Alexis F; School of Biological Sciences and Engineering, Yachay Tech University, Urcuquí 100119, Ecuador., Santos-Oliveira R; Brazilian Nuclear Energy Commission, Nuclear Engineering Institute, Laboratory of Novel Radiopharmaceuticals and Nano-radiopharmacy, Rio de Janeiro 21941906, Brazil; Zona Oeste State University, Laboratory of Nanoradiopharmaceuticals and Radiopharmacy, Rio de Janeiro 23070200, Brazil. Electronic address: roliveira@ien.gov.br.
Jazyk: angličtina
Zdroj: Materials science & engineering. C, Materials for biological applications [Mater Sci Eng C Mater Biol Appl] 2021 Sep; Vol. 128, pp. 112275. Date of Electronic Publication: 2021 Jun 25.
DOI: 10.1016/j.msec.2021.112275
Abstrakt: Malaria is the most common parasitic disease around the world, especially in tropical and sub-tropical regions. This parasitic disease can have a rapid and severe evolution. It is transmitted by female anopheline mosquitoes. There is no reliable vaccine or diagnostic test against malaria; instead, Artesunate is used for the treatment of severe malaria and Artemisinin is used for uncomplicated falciparum malaria. However, these treatments are not efficient against severe malaria and improvements are needed. Primaquine (PQ) is one of the most widely used antimalarial drugs. It is the only available drug to date for combating the relapsing form of malaria. Nevertheless, it has severe side effects. Particle drug-delivery systems present the ability to enhance the therapeutic properties of drugs and decrease their side effects. Here, we report the development of Polymeric Primaquine Microparticles (PPM) labeled with 99mTc for therapeutic strategy against malaria infection. The amount of primaquine encapsulated into the PPM was 79.54%. PPM presented a mean size of 929.47 ± 37.72 nm, with a PDI of 0.228 ± 0.05 showing a homogeneous size for the microparticles and a monodispersive behavior. Furthermore, the biodistribution test showed that primaquine microparticles have a high liver accumulation. In vivo experiments using mice show that the PPM treatments resulted in partial efficacy and protection against the development of the parasite compared to free Primaquine. These results suggest that microparticles drug delivery systems of primaquine could be a possible approach for malaria prevention and treatment.
(Copyright © 2021 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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