Poly(D,L-lactic-co-glycolic acid)-based artesunate nanoparticles: formulation, antimalarial and toxicity assessments

Dauda, Kabiru; Busari, Zulaikha; Morenikeji, Olajumoke A.; Afolayan, Funmilayo I. D.; Oyeyemi, Oyetunde T.; Meena, Jairam; Sahu, D. R.; Panda, Amulya K.

doi:10.1631/jzus.b1600389

Cited by 16 publications

(18 citation statements)

References 27 publications

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“…This is slightly higher compared to recent studies done using polymer-based artesunate nanoparticles by Dauda et al [8], who obtained an EE of 38.4 ± 10.1%. This could be related to the preparation conditions.…”

Section: Discussioncontrasting

confidence: 62%

“…Amongst these derivatives, artesunate is the most therapeutically versatile drug used in mild to severe malaria [6]. It has the greatest antimalarial activity compared to other artemisinins [7] and has also been extensively documented for its strong cytotoxicity against cancerous cells [8]. Despite its wide therapeutic use, artesunate exhibits variable pharmacokinetics which subsequently compromises its optimal therapeutic efficacy.…”

Section: Introductionmentioning

confidence: 99%

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Intestinal Permeability of Artesunate-Loaded Solid Lipid Nanoparticles Using the Everted Gut Method

Masiiwa

Gadaga

2018

Journal of Drug Delivery

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Background Artesunate is one of the most potent, rapidly acting and therapeutically versatile antimalarial drugs. Its efficacy is hampered by poor aqueous solubility and stability resulting in low oral bioavailability. Recent efforts to nanoformulate artesunate have shown great potential of improving its dissolution profile and bioavailability. However, no study has yet been done to investigate the intestinal permeability of these nanoformulations, which is a critical determinant of systemic absorption. Objective of the Study The main aim of the study was to determine the intestinal permeability of artesunate-loaded solid lipid nanoparticles (SLN). Method The microemulsion dilution technique was used to fabricate artesunate-loaded solid lipid nanoparticles. In vitro drug release studies were performed at pH 1.2 and 6.8 using the dialysis membrane method. The everted gut sac method was used to assess the intestinal permeability of the prepared nanoparticles. Results The average particle size was 1109 nm and the polydispersity index (PDI) was 0.082. The zeta potential was found to be −20.7 mV. The encapsulation efficiency of the solid lipid nanoparticles obtained was 51.7%. At both pH 1.2 and 6.8, pure artesunate was rapidly released within the first 30 mins while the SLN showed a biphasic release pattern with an initial burst release during the first hour followed by a prolonged release over time. The rate of drug release increased with increasing pH. The apparent permeability (Papp) of SLN was found to be greater (0.169 mg/cm2) as compared to that of pure artesunate (0.117 mg/cm2) at the end of the experiment. Conclusion The results obtained in this study showed that the microemulsion dilution technique can be used to formulate artesunate solid lipid nanoparticles. The formulation exhibited a sustained drug release profile. The intestinal permeability of artesunate could be enhanced by the nanoformulation.

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Section: Discussioncontrasting

confidence: 62%

Section: Introductionmentioning

confidence: 99%

Intestinal Permeability of Artesunate-Loaded Solid Lipid Nanoparticles Using the Everted Gut Method

Masiiwa

Gadaga

2018

Journal of Drug Delivery

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“…Clear zeta cell was used for zeta potential analysis. Drug encapsulation efficiency was determined by a modified method described by Dauda et al [ 13 ].…”

Section: Methodsmentioning

confidence: 99%

“…Nanotechnology has gained increasing interest in biomedicine with the utmost aim of effective delivery of bioactive agents. Particularly it has been widely applied to combat parasitic agents [ 12 , 13 ]. While attention is often drawn towards Schistosoma parasites [ 14 , 15 ], little is known about the application of nanomedicine against the snail intermediate hosts of the parasites.…”

Section: Introductionmentioning

confidence: 99%

Molluscicidal activities of curcumin-nisin polylactic acid nanoparticle on Biomphalaria pfeifferi

2017

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BackgroundSnail intermediate host control is a widely canvassed strategy for schistosomiasis control in endemic countries. While there have been increasing studies on the search for potent molluscicides in the past years, the use of nanoparticulate agents as molluscicides is yet to gain wide attention. The aim of this study was to assess the molluscicidal potential of curcumin-nisin poly lactic acid (PLA) entrapped nanoparticle (CurNisNp) against Biomphalaria pfeifferi, a snail intermediate host for Schistosoma mansoni.Methodology/Principal findingsCurNisNp formulated by double emulsion method was tested against the young adults, < 1 week, 1-2-week old juveniles, 1 day (blastula) and 7 day-old (hippo-stage) egg masses of B. pfeifferi. Mortality in the different stages was determined after 96-h of exposure at varying concentrations (350, 175, 87.5, 43.75 and 21.88 ppm). The sub-lethal effects of CurNisNp on the hatchability of the 7-day-old egg masses and egg laying capacity of the young adult snails were determined. The CurNisNp diameter, polydispersity index (PDI), zeta potential and drug entrapment efficiency were 284.0 ± 17.9 nm, 0.166 ± 0.03, -16.6 ± 2.45 mV and 35.0% respectively. The < 1 week old juveniles and the 1-day-old egg stage (blastula) of B. pfeifferi with LC50 277.9 ppm and 4279.5 ppm were the most susceptible and resistant stages to the drug respectively. CurNisNp was also observed to cause significant reductions (P<0.05) in egg hatchability and egg laying capacity with strong negative correlation between egg laying capacity and concentration (r = -0.928; P<0.05).Conclusion/SignificanceThis study showed that CurNisNp has molluscicidal activities on different developmental stages of B. pfeifferi. It is therefore recommended that the formulation be more optimised to give a nanoparticle with a narrow range monodispersed PDI for better drug distribution and eventual greater molluscicidal activities.

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“…8,9 Consequently, several strategies have been proposed to enhance the bioavailability and efficacy of drugs. The use of colloidal carriers such as nanocapsules as delivery vehicles has been effective at improving the efficacy of drugs, including antimalarials; [10][11][12] one strategy for targeting drugs to infected erythrocytes is the use of intravenously administered nanocarriers. 13,14 Our research group has developed nanocapsules as antimalarial drug delivery systems.…”

Section: Introductionmentioning

confidence: 99%

<p>Effects of Surface Characteristics of Polymeric Nanocapsules on the Pharmacokinetics and Efficacy of Antimalarial Quinine</p>

Michels¹,

Maciel²,

Nakama³

et al. 2019

IJN

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Introduction: The surface charge of nanoparticles, such as nanospheres (NS) and nanocapsules (NC), has been studied with the purpose of improving the in vivo performance of drugs. The aim of this study was to develop, characterize, and evaluate the in vitro antimalarial efficacy of NCP80 and NSP80 (polysorbate coated) or NCEUD and NSEUD (prepared with Eudragit RS 100) loading quinine (QN). Methods: Formulations were prepared by the nanoprecipitation method, followed by wide physicochemical characterization. Antimalarial activity in Plasmodium berghei-infected mice and populational pharmacokinetics (PopPK) in rats were evaluated. Results: The formulations showed a nanometric range (between 138 ± 3.8 to 201 ± 23.0 nm), zeta potential (mV) of −33.1 ± 0.7 (NCP80), −30.5 ± 1 (UNCP80), −25.5 ± 1 (NSP80), −20 ± 0.3 (UNSP80), 4.61 ± 1 (NCEUD), 14.1 ± 0.9 (UNCEUD), 2.86 ± 0.3 (NSEUD) and 2.84 ± 0.6 (UNSEUD), content close to 100%, and good QN protection against UVA light. There was a twofold increase in the penetration of QN into infected erythrocytes with NC compared to that with NS. There was a significant increase in t 1/2 for all NC evaluated compared to that of Free-QN, due to changes in Vdss. PopPK analysis showed that NCP80 acted as a covariate to Q (intercompartmental clearance) and V2 (volume of distribution in the peripheral compartment). For NCEUD, V1 and Q were modified after QN nanoencapsulation. Regarding in vivo efficacy, NCEUD increased the survival of mice unlike Free-QN. Conclusion: Cationic nanocapsules modified the pharmacology of QN, presenting a potential alternative for malaria treatment.

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Poly(D,L-lactic-co-glycolic acid)-based artesunate nanoparticles: formulation, antimalarial and toxicity assessments

Abstract: A simple treatment of PLGA-entrapped artesunate nanoparticles with dual advantages of low toxicity and better antiplasmodial efficacy has been developed.

Cited by 16 publications

References 27 publications

Intestinal Permeability of Artesunate-Loaded Solid Lipid Nanoparticles Using the Everted Gut Method

Intestinal Permeability of Artesunate-Loaded Solid Lipid Nanoparticles Using the Everted Gut Method

Molluscicidal activities of curcumin-nisin polylactic acid nanoparticle on Biomphalaria pfeifferi

<p>Effects of Surface Characteristics of Polymeric Nanocapsules on the Pharmacokinetics and Efficacy of Antimalarial Quinine</p>

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