Antileishmanial Activity of Amphotericin B-loaded-PLGA Nanoparticles: An Overview

Novel chitosan-coated nanoparticles with a high payload of amphotericin B (AmB) and doxorubicin (Dox) were formulated employing a nanoprecipitation technique and evaluated for antileishmanial activity against Leishmania donovani.

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Surface-Engineered Dendrimeric Nanoconjugates for Macrophage-Targeted Delivery of Amphotericin B: Formulation Development andIn VitroandIn VivoEvaluation

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.04213-14 ◽

2015 ◽

Vol 59 (5) ◽

pp. 2479-2487 ◽

Cited By ~ 40

Author(s):

Keerti Jain ◽

Ashwni Kumar Verma ◽

Prabhat Ranjan Mishra ◽

Narendra Kumar Jain

Keyword(s):

Drug Release ◽

Amphotericin B ◽

Human Erythrocytes ◽

Antileishmanial Activity ◽

Cell Uptake ◽

Antiparasitic Activity ◽

Content Type ◽

Drug Localization

ABSTRACTThe present study aimed to develop an optimized dendrimeric delivery system for amphotericin B (AmB). Fifth-generation (5.0G) poly(propylene imine) (PPI) dendrimers were synthesized, conjugated with mannose, and characterized by use of various analytical techniques, including Fourier transform infrared spectroscopy (FTIR),1H nuclear magnetic resonance (1H-NMR) spectroscopic analysis, and atomic force microscopy (AFM). Mannose-conjugated 5.0G PPI (MPPI) dendrimers were loaded with AmB and evaluated for drug loading efficiency,in vitrodrug release profile, stability, hemolytic toxicity to human erythrocytes, cytotoxicity to and cell uptake by J774A.1 macrophage cells, antiparasitic activity against intracellularLeishmania donovaniamastigotes,in vivopharmacokinetic and biodistribution profiles, drug localization index, toxicity, and antileishmanial activity. AFM showed the nanometric size of the MPPI dendrimers, with a nearly globular architecture. The conjugate showed a good entrapment efficiency for AmB, along with pH-sensitive drug release. Highly significant reductions in toxicity toward human erythrocytes and macrophage cells, without compromising the antiparasitic activity of AmB, were observed. The dendrimeric formulation of AmB showed a significant enhancement of the parasiticidal activity of AmB toward intramacrophagicL. donovaniamastigotes. In thein vitrocell uptake studies, the formulation showed selectivity toward macrophages, with significant intracellular uptake. Further pharmacokinetic and organ distribution studies elucidated the controlled delivery behavior of the formulation. The drug localization index was found to increase significantly in macrophage-rich organs.In vivostudies showed a biocompatible behavior of MPPIA, with negligible toxicity even at higher doses, and promising antileishmanial activity. From the results, we concluded that surface-engineered dendrimers may serve as optimized delivery vehicles for AmB with enhanced activity and low or negligible toxicity.

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Antileishmanial activity, pharmacokinetics and tissue distribution studies of mannose-grafted amphotericin B lipid nanospheres

Journal of Drug Targeting ◽

10.1080/10611860802528833 ◽

2009 ◽

Vol 17 (2) ◽

pp. 140-147 ◽

Cited By ~ 22

Author(s):

Prabhakar Reddy Veerareddy ◽

Venkateswarlu Vobalaboina ◽

Nahid Ali

Keyword(s):

Tissue Distribution ◽

Amphotericin B ◽

Antileishmanial Activity ◽

Distribution Studies

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Th-1 biased immunomodulation and synergistic antileishmanial activity of stable cationic lipid–polymer hybrid nanoparticle: Biodistribution and toxicity assessment of encapsulated amphotericin B

European Journal of Pharmaceutics and Biopharmaceutics ◽

10.1016/j.ejpb.2014.11.019 ◽

2015 ◽

Vol 89 ◽

pp. 62-73 ◽

Cited By ~ 25

Author(s):

Shalini Asthana ◽

Anil K. Jaiswal ◽

Pramod K. Gupta ◽

Anuradha Dube ◽

Manish K. Chourasia

Keyword(s):

Amphotericin B ◽

Cationic Lipid ◽

Toxicity Assessment ◽

Antileishmanial Activity ◽

Polymer Hybrid ◽

Hybrid Nanoparticle ◽

Th 1

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Antileishmanial Potential of Propolis Essential Oil and Its Synergistic Combination With Amphotericin B

Natural Product Communications ◽

10.1177/1934578x19899566 ◽

2020 ◽

Vol 15 (1) ◽

pp. 1934578X1989956 ◽

Cited By ~ 1

Author(s):

Ayari Jihene ◽

Essid Rym ◽

Karoui Jabri Ines ◽

Hammami Majdi ◽

Tabbene Olfa ◽

...

Keyword(s):

Gas Chromatography ◽

Essential Oil ◽

Amphotericin B ◽

Leishmania Major ◽

Antileishmanial Activity ◽

Mass Spectrometry Analysis ◽

Gas Chromatography Mass Spectrometry ◽

Spectrometry Analysis ◽

Low Cytotoxicity ◽

Promising Source

The antileishmanial activity of Tunisian propolis essential oil (EO) and its combination with amphotericin B was investigated against 2 local clinical strains of Leishmania: Leishmania major and Leishmania infantum. The cytotoxic potential of this EO was evaluated against macrophage Raw264.7. Combination of propolis EO and amphotericin B was investigated using the checkerboard method. The propolis sample was collected from the region of Beni Khalled, a Tunisian city located west of Cape Bon (Nabeul). Its location is particular since it is near to sea with a steppe climate and the predominance of citrus trees. The EO was obtained by Clevenger-type apparatus. Its chemical composition was identified using gas chromatography with flame ionization detector and gas chromatography-mass spectrometry analysis. Our results demonstrate that Tunisian propolis EO exhibit good antileishmanial activity against L. major and L. infantum promastigotes (IC50 = 5.29 ± 0.31 and 3.67 ± 0.52 µg/mL, respectively) and amastigotes (IC50 = 7.38 ± 0.45 and 4.96 ± 0.24 µg/mL, respectively). Moreover, it reduced significantly the parasite proliferation on a dose-dependent response (95%) with low cytotoxicity (selectivity index = 16.18 and 23.33, respectively). Its combination with amphotericin B showed a synergistic potential (fractional inhibitory concentration = 0.37). Interestingly, the data suggest that propolis EO was involved in macrophage activation by hyperproduction of NO. A total of 51 compounds were identified in the propolis EO. The major compound identified was α-pinene (36.7% ± 2.36%) followed by α-cedrol (6.7% ± 0.10%), totarol (6.6% ± 0.09%), and dehydroabietane (5.2% ± 0.10%). Our findings suggest that Tunisian propolis might constitute a promising source for antileishmanial molecules.

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Antileishmanial activity of nano-amphotericin B deoxycholate

Journal of Antimicrobial Chemotherapy ◽

10.1093/jac/dkn189 ◽

2008 ◽

Vol 62 (2) ◽

pp. 376-380 ◽

Cited By ~ 52

Author(s):

K. D. Manandhar ◽

T. P. Yadav ◽

V. K. Prajapati ◽

S. Kumar ◽

M. Rai ◽

...

Keyword(s):

Amphotericin B ◽

Antileishmanial Activity ◽

Amphotericin B Deoxycholate

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Amphotericin B-loaded mannose modified poly(d,l-lactide-co-glycolide) polymeric nanoparticles for the treatment of visceral leishmaniasis: in vitro and in vivo approaches

RSC Advances ◽

10.1039/c7ra04951j ◽

2017 ◽

Vol 7 (47) ◽

pp. 29575-29590 ◽

Cited By ~ 6

Author(s):

Santanu Ghosh ◽

Suman Das ◽

Asit Kumar De ◽

Nabanita Kar ◽

Tanmoy Bera

Keyword(s):

Visceral Leishmaniasis ◽

Amphotericin B ◽

Polymeric Nanoparticles ◽

Plga Nanoparticles

Amphotericin B-loaded mannose modified PLGA nanoparticles are more efficacious in the treatment of visceral leishmaniasis in bothin vitroandin vivomodels than unmodified nanoformulations.

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