Curcuminoids-loaded lipid nanoparticles: Novel approach towards malaria treatment

Aditya, Nayak P.; Tiyaboonchai, Waree; Patankar, Swati; Madhusudhan, Basavaraj; Souto, Eliana B.

doi:10.1016/j.colsurfb.2010.07.020

Cited by 238 publications

(134 citation statements)

References 46 publications

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“…This drift may be due to layering of liquid lipid on the surface of the solid lipid, which were not accommodated within the core of the NLCs or due to the formation of small emulsions or oil droplets. This corroborates with earlier studies, which have shown similar trend of increasing zeta potential along with increase in liquid lipid concentration (Nayak et al, 2010). In all the formulations, zeta potential was high enough to stabilize the nanoparticles against aggregation (Teng et al, 2013).…”

Section: Resultssupporting

confidence: 92%

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Development of artemether and lumefantrine co-loaded nanostructured lipid carriers: physicochemical characterization and in vivo antimalarial activity

2014

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Context: Artemether and lumefantrine combination therapy is well-accepted for uncomplicated malaria treatment. However, the current available formulation has several pharmacokinetic mismatches such as drug degradation in gastrointestinal tract, erratic absorption, etc. Hence, need of the hour is the injectable formulation, which can overcome the pharmacokinetic mismatch associated with current available formulation in the market. Objective: To fabricate artemether and lumefantrine co-loaded injectable nanostructured lipid carriers (NLCs) formulation. Materials and methods: Artemether and lumefantrine co-loaded NLCs were fabricated using homogenization followed by ultra-sonication method. Fabricated NLCs were evalauated for their physicochemical characteristics, and suitability of the formulation for malaria treatment was evaluated using in vivo animal model (Plasmodium berghei-infected mice). Results, discussion and conclusion: Artemether and lumefantrine co-loaded NLCs had a hydrodynamic diameter of $145 nm with the surface charge of À66 mV. Due to the lipophilic nature of both antimalarial drugs, both single drugs-loaded and co-loaded NLCs have shown high encapsulation efficiency, which is 84% for artemether and 79% for lumefantrine. In vitro drug release study has shown a biphasic drug release pattern, which has shown 63% artemether release and 45% of lumefantrine release over a time period of 30 h. Plasmodium berghei-infected mice treated with artemether and lumefantrine co-loaded NLCs showed better antimalarial activity with respect to parasitemia progression and survivability period.

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Section: Resultssupporting

confidence: 92%

“…Moreover, size and PDI of the formulations remained within the acceptable range for administration of drugs through various injectable routes such as i.p., intravenous, etc., which is generally 5200 nm (Nayak et al, 2010;Aditya et al, 2012). Furthermore, to study the morphology and to confirm the size, TEM was used (Figure 2).…”

Section: Resultsmentioning

confidence: 99%

Development of artemether and lumefantrine co-loaded nanostructured lipid carriers: physicochemical characterization and in vivo antimalarial activity

2014

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“…Trimyristin is also found in Myristica fragrans, which belongs to the Myristicaceae family. Trimyristin is used as a nanoparticle lipid, which is combined with the curcuminoidin malaria treatment [30]. Triglycerides also have roles in malaria treatment as oil-phase transporters of antimalarial, for example, Self-microemulsifying Drug Delivery Systems that alter into a microemulsion after passing through the oral route [31].…”

Section: Resultsmentioning

confidence: 99%

In Silico Screening of Antimalarial From Indonesian Medicinal Plants Database to Plasmepsin Target

Rifai

Hayun

Yanuar

2017

Asian J Pharm Clin Res

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Objective: Malaria is a disease that impacts millions of people annually. Among the enzymes, plasmepsin is the main enzyme in the plasmodium life cycle that degrades hemoglobin during the erythrocytic phase in the food vacuole. Recently, pharmaceutical industries have been trying to develop therapeutic agents that can cure malaria through the discovery of new plasmepsin inhibitor compounds. One of the developing approaches is the in silico method. Methods:The chosen in silico screening method in this experiment is a structure-based screening using GOLD software and the Indonesian medicinal plants database.Results: From ten in silico screening runs, three of the compounds always ranked in the top ten. These three compounds are trimyristin, cyanidin 3,5-di-(6-malonylglucoside), and isoscutellarein 4'-methyl ether 8-(6"-n-butylglucuronide). Another compound that emerged with high frequency is cyanidin 3,5-di-(6-malonylglucoside). Conclusions:Based on the results obtained from this screening, 11 inhibitor candidates are expected to be developed as antimalarial. These compounds are trimyristin; cyanidin 3,5-di-(6-malonylglucoside); isoscutellarein 4'-methyl ether 8-(6"-n-butylglucuronide); cyanidin 3-(6"-malonylglucoside)-5-glucoside; multifloroside; delphinidin 3-(2-rhamnosyl-6-malonylglucoside); delphinidin 3-(6-malonylglucoside)-3',5'-di-(6-p-coumaroylglucoside); cyanidin 3-[6-(6-sinapylglucosyl)-2-xylosylgalactoside; kaempferol 3-glucosyl-(1-3)-rhamnosyl-(1-6)-galactoside; sanggenofuran A; and lycopene with a GOLD score range from 78.4647 to 98.2836. Two of them, Asp34 and Asp214, bind with all residues in the catalytic site of plasmepsin.

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“…SLNs showed a sustained the release of curcumin, as opposed to spontaneous diffusion of free curcumin control, dissolved only in 10 mM Tween 60 . A biphasic release pattern was observed: the sustained release profile showed an initial burst release 20,22 . The release processes of all the systems were analyzed up to 100 h. There was an initial burst release of 20-25 of curcumin within 9-10 h, which was due to the weakly adsorbed curcumin.…”

Section: In Vitro Release Studiesmentioning

confidence: 98%

“…The decrease in DL capacity was also noted with the increasing FA chain length Table S1, supplementary section . Curcumin, being an amphiphilic compound, is expected to be located on the SLN surface to a greater extent than a hydrophobic drug, which would be localized to the core of SLNs 20 . LA and MA, being more fluid than PA and SA, can be more flexible; therefore, the corresponding SLN can accommodate a greater number of drug molecules.…”

Section: Spectroscopic Analysismentioning

confidence: 99%

Effects of Fatty Acids on the Interfacial and Solution Behavior of Mixed Lipidic Aggregates Called Solid Lipid Nanoparticles

et al. 2016

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Curcuminoids-loaded lipid nanoparticles: Novel approach towards malaria treatment

Cited by 238 publications

References 46 publications

Development of artemether and lumefantrine co-loaded nanostructured lipid carriers: physicochemical characterization and in vivo antimalarial activity

Development of artemether and lumefantrine co-loaded nanostructured lipid carriers: physicochemical characterization and in vivo antimalarial activity

In Silico Screening of Antimalarial From Indonesian Medicinal Plants Database to Plasmepsin Target

Effects of Fatty Acids on the Interfacial and Solution Behavior of Mixed Lipidic Aggregates Called Solid Lipid Nanoparticles

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