In Situ Incorporation of Praziquantel in Polymer Microparticles through Suspension Polymerization for Treatment of Schistosomiasis. Issue 1 (27th December 2018)

• Record Type: Journal Article
• Authors: Paiva, Thamiris; Vieira, Lorena; Melo, Príamo; Nele, Márcio; Pinto, José Carlos
• Is Part Of: Macromolecular reaction engineering. Volume 13:Issue 1(2019)
• Page Start: n/a
• Page End: n/a
• Publication Date: 2018-12-27
• Subjects: poly(methyl methacrylate) -- praziquantel -- smart polymers -- suspension polymerization; Polymers -- Periodicals; Polymerization -- Periodicals; Reaction mechanisms (Chemistry) -- Periodicals; Electronic journals; 547.705
• DOI: 10.1002/mren.201800064
• Languages: English
• ISSNs: 1862-832X

Abstract

Abstract: Schistosomiasis is one of the major public health problems worldwide. Even though this is a common illness among preschool children in poor countries, treatment is carried out mainly through the administration of praziquantel tablets, which has some disadvantages, such as the strong bitter taste. As an alternative to overcome this problem, the development of new encapsulated praziquantel formulations is demanded. For this reason, suspension polymerizations are carried out for the in situ encapsulation of praziquantel into polymer microparticles, using methyl methacrylate (MMA) and cationic compounds (diethylaminoethyl methacrylate, DEAEMA, and dimethylaminoethyl methacrylate, DMAEMA) as comonomers. This technique allows for the preparation of polymer microparticles with high encapsulation efficiencies (>90%) with characteristic sizes ranging from 0.5 to 1500 µm. Drug release profiles show that praziquantel is released from poly(methyl methacrylate) microparticles slowly due to the existence of strong diffusional resistance. On the other hand, the addition of cationic comonomers renders polymer particles sensitive to pH variations, allowing for faster release of praziquantel in acidic environments, as found in the stomach. Abstract : A new poly(methyl methacrylate)‐based suspension formulation intended for oral administration of praziquantel is developed. The main novelty regards the use of smart copolymer microparticles produced through suspension polymerization as vehicles for the controlled release of praziquantel in the body, which does not exhibit the characteristic bitter taste of the drug.