Preparation, Characterization and Evaluation of Targeting Potential of Amphotericin B-Loaded Engineered PLGA Nanoparticles

Nahar, Manoj; Jain, Narendra Kumar

doi:10.1007/s11095-009-9973-4

Cited by 95 publications

(47 citation statements)

References 29 publications

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“…[5][6][7] In addition, the stability, tissue permeability, degradation rate, and toxicity of NPs themselves are also concerns in this field. [8][9][10] The recently developed diblock copolymer D-α-tocopheryl polyethylene glycol 1000 succinate-b-poly(ε-caprolactone-ran-glycolide) (TPGS-b-(PCL-ran-PGA) [hereafter, referred to as PLGA-TPGS]) has received special attention as a promising antimicrobial agent, due to its good biocompatibility and biodegradability. 7 Therefore, the synthesis of uniform PLGA-TPGS copolymer NPs (PLGA-TPGS NPs) with specific requirements in terms of size, shape, and physical and chemical properties is of great interest in the development of new drugs.…”

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confidence: 99%

“…7 Therefore, the synthesis of uniform PLGA-TPGS copolymer NPs (PLGA-TPGS NPs) with specific requirements in terms of size, shape, and physical and chemical properties is of great interest in the development of new drugs. 8,9 A variety of studies [8][9][10] have shown they have good biocompatibility and biodegradability and excellent targeted drug delivery, but the antifungal effects of AMB-loaded PLGA-TPGS NPs (AMBNPs) are mostly unknown. In this study, AMB-NPs were synthesized, and their antifungal effects on the Candida spp.…”

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confidence: 99%

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Enhanced antifungal effects of amphotericin B-TPGS-b-(PCL-ran-PGA) nanoparticles in vitro and in vivo

Tang¹,

Zhu²,

Sun³

et al. 2014

IJN

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Background Amphotericin B (AMB) is a polyene antibiotic with broad spectrum antifungal activity, but its clinical toxicities and poor solubility limit the wide application of AMB in clinical practice. Recently, new drug-loaded nanoparticles (NPs) – diblock copolymer D-α-tocopheryl polyethylene glycol 1000 succinate-b-poly(ε-caprolactone-ran-glycolide) (PLGA-TPGS) – have received special attention for their reduced toxicity, and increased effectiveness of drug has also been reported. This study aimed to develop AMB-loaded PLGA-TPGS nanoparticles (AMB-NPs) and evaluate their antifungal effects in vitro and in vivo. Methods AMB-NPs were prepared with a modified nanoprecipitation method and then characterized in terms of physical characteristics, in vitro drug release, stability, drug-encapsulation efficiency, and toxicity. Finally, the antifungal activity of AMB-NPs was investigated in vitro and in vivo. Results AMB-NPs were stable and spherical, with an average size of around 110 nm; the entrapment efficacy was closed to 85%, and their release exhibited a typically biphasic pattern. The actual minimum inhibitory concentration of AMB-NPs against Candida albicans was significantly lower than that of free AMB, and AMB-NPs were less toxic on blood cells. In vivo experiments indicated that AMB-NPs achieved significantly better and prolonged antifungal effects when compared with free AMB. Conclusion The AMB-PLGA-TPGS NP system significantly improves the AMB bioavailability by improving its antifungal activities and reducing its toxicity, and thus, these NPs may become a good drug carrier for antifungal treatment.

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confidence: 99%

Enhanced antifungal effects of amphotericin B-TPGS-b-(PCL-ran-PGA) nanoparticles in vitro and in vivo

Tang¹,

Zhu²,

Sun³

et al. 2014

IJN

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“…Recently, polylactide NPs containing basic acid were more effective than microemulsions in an in vivo hamster model of VL [16]. Other example includes AmBloaded in poly (ε-caprolactone) NPs [17] or in mannose-anchored, PLGA NPs for the efficient delivery of AmB to macrophages [18].…”

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confidence: 99%

Preparation and Characterization of Andrographolide Nanoparticles for Visceral Leishmaniasis Chemotherapy: In Vitro and in Vivo Evaluations

Ghosh

Mondal

Bera

2016

Int J Pharm Pharm Sci

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Objective: To overcome low physiological solubility, poor bioavailability, the short plasma half-life of andrographolide (AG), a delivery system based on poly (D, L-lactide-co-glycolide) (PLGA) nanoparticles (NPs) were developed to increase the efficiency of AG against visceral leishmaniasis (VL).Methods: Andrographolide-PLGA nanoparticles (AGnp) were prepared with Pgp efflux inhibitor vitamin E TPGS (D-α-tocopheryl polyethylene glycol 1000 succinate) by emulsion solvent evaporation method and characterized. Antileishmanial activity was evaluated using in vitro and in vivo VL infection model. Results:The particle size of AGnp was found to be171.4±11.5 nm with an encapsulation efficiency of 81%. The AGnp reduced AG cellular toxicity, retained it's in vitro antileishmanial activity and lead to a reduction (99.9%) of parasite burden in the Leishmania donovani infected spleen and liver. AGnp was more active in infected mice liver at low dose than in spleen. Therapeutic indexes (TI) were 6.9-fold greater in AG and 68-fold in AGnp compared to amphotericin B (AmB) when evaluated in L. donovani infected spleen. Conclusion:Incorporation of AG in PLGA nanoparticles, provided controlled and improved in vivo performance against VL

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“…102 With regard to the active targeting approach, mannosebearing PLGA nano/microparticles have been designed to further improve macrophage targeting of antileishmanial agents. Mannose-grafted PLGA nanoparticles, with and without a PEG spacer, are reported to target AmpB; 103 the presence of PEG spacer resulted in a more efficient inhibition of parasites in comparison to both the one without spacer and the free drug. Furthermore, both drug-polymer interaction and drug miscibility in the polymer affect the drug content of polymer nanoparticles.…”

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confidence: 99%

“…However, in the engineered version of polymer nanoparticles, in which mannose was directly linked to PLGA (M-PNPs) or to the edge of PEG (M-PEG-PNPs), an increased entrapment efficiency was observed, probably due to the higher drug-polymer miscibility, permitting the enhanced drug incorporation. 103 The significant rise in drug content in M-PNPs and M-PEG-PNPs might be due to the stronger drug-polymer interaction (between the hydroxyl group of mannose and PEG and the amine group of AmpB) and to the high miscibility in the case of amphiphilic AmpB. Another study suggested that the acidic end-group of PLGA is responsible for drug incorporation and that increased chain length may increase the drug-polymer interactions, leading to improved drug incorporation efficiency.…”

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Nanostructured delivery systems with improved leishmanicidal activity: a critical review

Bruni¹,

Stella²,

Giraudo³

et al. 2017

IJN

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Leishmaniasis is a vector-borne zoonotic disease caused by protozoan parasites of the genus Leishmania , which are responsible for numerous clinical manifestations, such as cutaneous, visceral, and mucocutaneous leishmaniasis, depending on the site of infection for particular species. These complexities threaten 350 million people in 98 countries worldwide. Amastigotes living within macrophage phagolysosomes are the principal target of antileishmanial treatment, but these are not an easy target as drugs must overcome major structural barriers. Furthermore, limitations on current therapy are related to efficacy, toxicity, and cost, as well as the length of treatment, which can increase parasitic resistance. Nanotechnology has emerged as an attractive alternative as conventional drugs delivered by nanosized carriers have improved bioavailability and reduced toxicity, together with other characteristics that help to relieve the burden of this disease. The significance of using colloidal carriers loaded with active agents derives from the physiological uptake route of intravenous administered nanosystems (the phagocyte system). Nanosystems are thus able to promote a high drug concentration in intracellular mononuclear phagocyte system (MPS)-infected cells. Moreover, the versatility of nanometric drug delivery systems for the deliberate transport of a range of molecules plays a pivotal role in the design of therapeutic strategies against leishmaniasis. This review discusses studies on nanocarriers that have greatly contributed to improving the efficacy of antileishmaniasis drugs, presenting a critical review and some suggestions for improving drug delivery.

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Preparation, Characterization and Evaluation of Targeting Potential of Amphotericin B-Loaded Engineered PLGA Nanoparticles

Abstract: The results suggest that engineering of nanoparticles could lead to development of efficient carrier for macrophage targeting.

Cited by 95 publications

References 29 publications

Enhanced antifungal effects of amphotericin B-TPGS-b-(PCL-ran-PGA) nanoparticles in vitro and in vivo

Enhanced antifungal effects of amphotericin B-TPGS-b-(PCL-ran-PGA) nanoparticles in vitro and in vivo

Preparation and Characterization of Andrographolide Nanoparticles for Visceral Leishmaniasis Chemotherapy: In Vitro and in Vivo Evaluations

Nanostructured delivery systems with improved leishmanicidal activity: a critical review

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