Preparation and in vivo evaluation of anti-plasmodial properties of artemisinin-loaded PCL–PEG–PCL nanoparticles. (21st October 2018)

• Record Type: Journal Article
• Authors: Ramazani, Ali; Keramati, Mojtaba; Malvandi, Hojat; Danafar, Hossein; Kheiri Manjili, Hamidreza
• Is Part Of: Pharmaceutical development and technology. Volume 23:Number 9(2018)
• Page Start: 911
• Page End: 920
• Publication Date: 2018-10-21
• Subjects: Artemisinin -- Plasmodium berghei -- drug delivery -- micelles -- PCL–PEG–PCL; Drug delivery systems -- Periodicals; Pharmaceutical technology -- Periodicals; Drugs -- Administration -- Research -- Periodicals; Drug Delivery Systems -- Periodicals; Pharmaceutical Preparations -- Periodicals; Technology, Pharmaceutical -- Periodicals; 615
• DOI: 10.1080/10837450.2017.1372781
• Languages: English
• ISSNs: 1083-7450

Abstract

Abstract: Purpose: Artemisinin (ART) has anti-inflammatory, antimicrobial, antioxidant, anti-amyloid, and anti-malarial effects, but its application is limited due to its low water solubility and poor oral bioavailability. In this study, the bioavailability, water solubility, and anti-plasmodial property of ART were improved by PCL–PEG–PCL tri-block copolymers. Methods: The structure of the copolymers was characterized by 1 H NMR, FT-IR, DSC, and GPC techniques. ART was encapsulated within micelles by a single-step nano-precipitation method, leading to the formation of ART-loaded PCL–PEG–PCL micelles. The obtained micelles were characterized by dynamic light scattering (DLS) and atomic force microscopy (AFM). The in vivo anti-plasmodial activity of ART-loaded micelles was measured against Plasmodium berghei infected Swiss albino mice. Results: The results showed that the zeta potential of ART-loaded micelles was about −8.37 mV and the average size was 91.87 nm. ART was encapsulated into PCL–PEG–PCL micelles with a loading capacity of 19.33 ± 0.015% and encapsulation efficacy of 87.21 ± 3.32%. In vivo anti-plasmodial results against P. berghei showed that multiple injections of ART-loaded micelles could prolong the circulation time and increase the therapeutic efficacy of ART. Conclusion: These results suggested that PCL–PEG–PCL micelles would be a potential carrier for ART for the treatment of malaria.