Comparative efficacy of amphotericin B-loaded chitosan nanoparticles and free amphotericin B drug against Leishmania tropica

Abstract Background The preparation of an effective drug delivery formulation is an urgent need to treat cutaneous leishmaniasis (CL). Pentavalent antimonials and Amphotericin B (AmB) are considered to treat leishmaniasis; however, their clinical usage is hampered by poor solubility, high cost, toxi...

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Autores principales: Aamir Sohail, Rahat Ullah Khan, Momin Khan, Mehvish Khokhar, Safat Ullah, Arshad Ali, Hazrat Bilal, Saadullah Khattak, Mirwaise Khan, Baseer Ahmad
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spelling oai:doaj.org-article:f76deb20fe7c444b9b927c5878e5baeb2021-11-08T11:13:12ZComparative efficacy of amphotericin B-loaded chitosan nanoparticles and free amphotericin B drug against Leishmania tropica10.1186/s42269-021-00644-52522-8307https://doaj.org/article/f76deb20fe7c444b9b927c5878e5baeb2021-11-01T00:00:00Zhttps://doi.org/10.1186/s42269-021-00644-5https://doaj.org/toc/2522-8307Abstract Background The preparation of an effective drug delivery formulation is an urgent need to treat cutaneous leishmaniasis (CL). Pentavalent antimonials and Amphotericin B (AmB) are considered to treat leishmaniasis; however, their clinical usage is hampered by poor solubility, high cost, toxicity, and the emergence of drug-resistant Leishmania spp. The drug delivery systems (DDS) could be used as an alternative treatment option for the treatment of CL to circumvent these problems. We tested the antileishmanial efficacies of free AmB and amphotericin B-loaded chitosan nanoparticles (AmB-CNPs) under in vitro conditions. Results Chitosan nanoparticles (CNPs) were synthesized using the ionic gelation method with negatively charged tripolyphosphate (TPP). During the synthesis of CNPs, AmB was incorporated into the nanoparticles (NPs). The NPs were characterized for their size, surface morphology, encapsulation efficacy (EE), drug loading content (DLC), and surface charge using different techniques. Their efficacy was evaluated against promastigotes and axenic amastigotes forms of Leishmania tropica using MTT assay. The synthesized AmB-CNPs displayed a spherical shape with a mean particle size of 118 nm, a positive zeta potential of (+ 6.21 ± 2.02 mV), and an encapsulation efficacy of 88%. Dynamic light scattering technique (DLS) shows that the average size of prepared AmB-CNPs was 95.5 nm. Free AmB presented very low efficacy (only 65% and 67% inhibition of the promastigotes and axenic amastigotes parasite load), whereas AmB-CNPs exhibited 90% and 84% parasite inhibition after 72 h incubation. The AmB-CNPs exhibited significantly higher efficacy than free AmB in terms of reduction in parasite viability. Half-maximal inhibitory concentration (IC50) measured values of the AmB-CNPs were significant lowers than free AmB. Conclusions The present data indicated that AmB-CNPs exhibited vigorous anti-leishmanial activity than free AmB by dose and time-dependent manner. This formulation can be used for local therapy of CL after in vivo efficacy conformational studies.Aamir SohailRahat Ullah KhanMomin KhanMehvish KhokharSafat UllahArshad AliHazrat BilalSaadullah KhattakMirwaise KhanBaseer AhmadSpringerOpenarticleAmphotericin BAntileishmanial activityCutaneous leishmaniasisChitosan nanoparticlesDrug deliveryMTT assayScienceQENBulletin of the National Research Centre, Vol 45, Iss 1, Pp 1-9 (2021)
institution DOAJ
collection DOAJ
language EN
topic Amphotericin B
Antileishmanial activity
Cutaneous leishmaniasis
Chitosan nanoparticles
Drug delivery
MTT assay
Science
Q
spellingShingle Amphotericin B
Antileishmanial activity
Cutaneous leishmaniasis
Chitosan nanoparticles
Drug delivery
MTT assay
Science
Q
Aamir Sohail
Rahat Ullah Khan
Momin Khan
Mehvish Khokhar
Safat Ullah
Arshad Ali
Hazrat Bilal
Saadullah Khattak
Mirwaise Khan
Baseer Ahmad
Comparative efficacy of amphotericin B-loaded chitosan nanoparticles and free amphotericin B drug against Leishmania tropica
description Abstract Background The preparation of an effective drug delivery formulation is an urgent need to treat cutaneous leishmaniasis (CL). Pentavalent antimonials and Amphotericin B (AmB) are considered to treat leishmaniasis; however, their clinical usage is hampered by poor solubility, high cost, toxicity, and the emergence of drug-resistant Leishmania spp. The drug delivery systems (DDS) could be used as an alternative treatment option for the treatment of CL to circumvent these problems. We tested the antileishmanial efficacies of free AmB and amphotericin B-loaded chitosan nanoparticles (AmB-CNPs) under in vitro conditions. Results Chitosan nanoparticles (CNPs) were synthesized using the ionic gelation method with negatively charged tripolyphosphate (TPP). During the synthesis of CNPs, AmB was incorporated into the nanoparticles (NPs). The NPs were characterized for their size, surface morphology, encapsulation efficacy (EE), drug loading content (DLC), and surface charge using different techniques. Their efficacy was evaluated against promastigotes and axenic amastigotes forms of Leishmania tropica using MTT assay. The synthesized AmB-CNPs displayed a spherical shape with a mean particle size of 118 nm, a positive zeta potential of (+ 6.21 ± 2.02 mV), and an encapsulation efficacy of 88%. Dynamic light scattering technique (DLS) shows that the average size of prepared AmB-CNPs was 95.5 nm. Free AmB presented very low efficacy (only 65% and 67% inhibition of the promastigotes and axenic amastigotes parasite load), whereas AmB-CNPs exhibited 90% and 84% parasite inhibition after 72 h incubation. The AmB-CNPs exhibited significantly higher efficacy than free AmB in terms of reduction in parasite viability. Half-maximal inhibitory concentration (IC50) measured values of the AmB-CNPs were significant lowers than free AmB. Conclusions The present data indicated that AmB-CNPs exhibited vigorous anti-leishmanial activity than free AmB by dose and time-dependent manner. This formulation can be used for local therapy of CL after in vivo efficacy conformational studies.
format article
author Aamir Sohail
Rahat Ullah Khan
Momin Khan
Mehvish Khokhar
Safat Ullah
Arshad Ali
Hazrat Bilal
Saadullah Khattak
Mirwaise Khan
Baseer Ahmad
author_facet Aamir Sohail
Rahat Ullah Khan
Momin Khan
Mehvish Khokhar
Safat Ullah
Arshad Ali
Hazrat Bilal
Saadullah Khattak
Mirwaise Khan
Baseer Ahmad
author_sort Aamir Sohail
title Comparative efficacy of amphotericin B-loaded chitosan nanoparticles and free amphotericin B drug against Leishmania tropica
title_short Comparative efficacy of amphotericin B-loaded chitosan nanoparticles and free amphotericin B drug against Leishmania tropica
title_full Comparative efficacy of amphotericin B-loaded chitosan nanoparticles and free amphotericin B drug against Leishmania tropica
title_fullStr Comparative efficacy of amphotericin B-loaded chitosan nanoparticles and free amphotericin B drug against Leishmania tropica
title_full_unstemmed Comparative efficacy of amphotericin B-loaded chitosan nanoparticles and free amphotericin B drug against Leishmania tropica
title_sort comparative efficacy of amphotericin b-loaded chitosan nanoparticles and free amphotericin b drug against leishmania tropica
publisher SpringerOpen
publishDate 2021
url https://doaj.org/article/f76deb20fe7c444b9b927c5878e5baeb
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