PLGA nanoparticles loaded with Gallic acid- a constituent of Leea indica against Acanthamoeba triangularis

Abstract

Acanthamoeba, a genus that contains at least 24 species of free-living protozoa, is ubiquitous in nature. Successful treatment of Acanthamoeba infections is always very difficult and not always effective. More effective drugs must be developed, and medicinal plants may have a pivotal part in the future of drug discovery. Our research focused on investigating the in vitro anti-acanthamoebic potential of Leea indica and its constituent gallic acid in different concentrations. Water and butanol fractions exhibited significant amoebicidal activity against trophozoites and cysts. Gallic acid (100 µg/mL) revealed 83% inhibition of trophozoites and 69% inhibition of cysts. The butanol fraction induced apoptosis in trophozoites, which was observed using tunnel assay. The cytotoxicity of the fractions and gallic acid was investigated against MRC-5 and no adverse effects were observed. Gallic acid was successfully loaded within poly (D,L-lactide-co-glycolide) (PLGA) nanoparticles with 82.86% encapsulation efficiency, while gallic acid showed 98.24% in vitro release at 48 hours. Moreover, the gallic acid encapsulated in the PLGA nanoparticles exhibited 90% inhibition against trophozoites. In addition, gallic acid encapsulated nanoparticles showed reduced cytotoxicity towards MRC-5 compared to gallic acid, which evidenced that natural product nanoencapsulation in polymeric nanoparticles could play an important role in the delivery of natural products. Leea indica (Burm. f.) Merr. (Family-Leeaceae), commonly known as kur jiwa, arengi or achila gaeh, is widespread in tropical and subtropical regions, for example, Malaysia, China, Thailand, India and Bangladesh 1. Several known chemical compounds have been isolated from the leaves of Leea indica, which includes phthalic acid, ursolic acid, gallic acid, β-sitosterol, palmitic acid, farnesol, lupeol and 1-eicosanol. Apart from that, Srinivasan et al. identified other compounds such as lycopersen, heptadecane, isooctyl phthalate, butyl-2-phthalate, butyl-2-ethylhexyl phthalate, din -butyl phthalate, butyl gallate, triterpenes and sterol from the methanol extract 2. Among these isolated compounds, din -butyl phthalate exhibited antibacterial and antifungal properties 3 , while butyl gallate was an antioxidant 4. Interestingly, gallic acid is the one that has been reported to have several biological activities, mainly antioxidant, anti-tyrosinase, antimicrobial, anti-inflammatory, anticancer and neuro-protective activities 5. Gallic acid was isolated from several medicinal plants, including the butanol fraction of Crassula ovata (Mill.) Druce leaves by Tombozara et al. 6. More recently, through LC-MS/MS, some phytochemicals have been

Potential anti-Acanthamoeba and anti-adhesion activities of Annona muricata and Combretum trifoliatum extracts and their synergistic effects in combination with chlorhexidine against Acanthamoeba triangularis trophozoites and cysts

“…To support this, nanoparticle synthesis using plant extracts or plant-derive compounds has been reported as one option to enhance the efficiency of these compounds against the pathogens. Recently, there has been a report on the synthesis of nanoparticles using gallic acid, a component of Leea indica loaded in poly-D, L-lactide-co-glycolide nanoparticles inhibited the growth of trophozoites and cysts of A. triangularis (Mahboob et al, 2020). In light of our promising results, future study is strongly recommended to investigate the mechanism of the pure compounds in terms of nano-synthesis, metabolomics or docking simulation that will further enhance the discovery on the drug target of Acanthamoeba infection.…”

Gentiopicroside PLGA Nanospheres: Fabrication, in vitro Characterization, Antimicrobial Action, and in vivo Effect for Enhancing Wound Healing in Diabetic Rats

“…Free GPS remained in the supernatant after centrifugation step during preparation of PLGA-NSs has been estimated using UV-visible spectrophotometry (Evolution 300 spectrophotometer, Thermo Scientific, UK) at a detection wavelength of 230 nm. 20 The percent of GPS entrapment has been calculated as follows: 21 …”

Synthesis of M-Ag3PO4, (M = Se, Ag, Ta) Nanoparticles and Their Antibacterial and Cytotoxicity Study

“…They are widely used in the diagnosis and treatment of diseases [ 6 , 7 ]. Due to their small size, several drugs can be delivered by using nanoparticles [ 8 , 9 , 10 , 11 , 12 , 13 , 14 ]. Different nanoparticles have been used as drug enhancers to improve the stability, efficacy, treatment, and safety of anti-cancer drugs [ 15 , 16 , 17 , 18 ].…”