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Journal ArticleDOI

Andrographolide nanoparticles in leishmaniasis: characterization and in vitro evaluations.

09 Dec 2010-International Journal of Nanomedicine (Dove Press)-Vol. 5, Iss: 1, pp 1113-1121
TL;DR: Antileishmanial activity was found to be significant for the nanoparticle preparation with 4% PVA in about one-fourth of the dosage of the pure compound AG (IC50 160 μM), which have significant potential to target the infested macrophage cells and prove valuable in chemotherapy of neglected tropical diseases such as leishmaniasis.
Abstract: Andrographolide (AG) is a diterpenoid lactone isolated from the leaves of Andrographis paniculata. AG is a potent and low-toxicity antileishmanial agent. Chemotherapy applications of AG are, however, seriously constrained because of poor bioavailability, short plasma half-life, and inappropriate tissue localization. Nanoparticulation of AG was therefore envisaged as a possible solution. AG nanoparticles (AGnp) loaded in 50:50 poly(DL-lactide-co-glycolic acid) were prepared for delivery into the monocyte-macrophage cells infested with the amastigote form of leishmanial parasite for evaluation in the chemotherapy of leishmaniasis. Particle characteristics of AGnp were optimized by proportionate application of a stabilizer, polyvinyl alcohol (PVA). Physicochemical characterization of AGnp by photon correlation spectroscopy exhibited an average particle size of 173 nm and zeta potential of -34.8 mV. Atomic force microscopy visualization revealed spherical nanoparticles with a smooth surface. Antileishmanial activity was found to be significant for the nanoparticle preparation with 4% PVA (IC₅₀) 34 μM) in about one-fourth of the dosage of the pure compound AG (IC₅₀) 160 μM). AGnp therefore have significant potential to target the infested macrophage cells and prove valuable in chemotherapy of neglected tropical diseases such as leishmaniasis.
Citations
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Journal ArticleDOI
Daode Hu1, Changchun Lin1, Liang Liu1, Sining Li1, Yaping Zhao1 
TL;DR: In this paper, a solution enhanced dispersion by supercritical fluids (SEDS) was applied for the production of lutein/zein nanoparticles and the effects of the process variables on the morphology, drug loading, entrapment efficiency, and mean particle size of the nanoparticles were investigated.

165 citations

Journal ArticleDOI
TL;DR: The present article covers antiviral properties of andrographolide in variety of viral infections, with the hope of developing of a new highly potent antiviral drug with multiple effects.
Abstract: Andrographolide, a diterpenoid, is known for its anti-inflammatory effects. It can be isolated from various plants of the genus Andrographis, commonly known as 'creat'. This purified compound has been tested for its anti-inflammatory effects in various stressful conditions, such as ischemia, pyrogenesis, arthritis, hepatic or neural toxicity, carcinoma, and oxidative stress, Apart from its anti-inflammatory effects, andrographolide also exhibits immunomodulatory effects by effectively enhancing cytotoxic T cells, natural killer (NK) cells, phagocytosis, and antibody-dependent cell-mediated cytotoxicity (ADCC). All these properties of andrographolide form the foundation for the use of this miraculous compound to restrain virus replication and virus-induced pathogenesis. The present article covers antiviral properties of andrographolide in variety of viral infections, with the hope of developing of a new highly potent antiviral drug with multiple effects.

120 citations

Journal ArticleDOI
TL;DR: New quercetin conjugated gold nanoparticles (QAunp) were successfully evaluated for the first time against leishmanial macrophage infections.

104 citations

Journal ArticleDOI
TL;DR: Some of the recent advances in the nanotechnological research regarding the treatment of leishmaniasis are presented and further efforts will still be necessary for this therapy to have greater clinical applicability in humans.
Abstract: Leishmaniasis, a vector-borne disease caused by obligate intramacrophage protozoa, threatens 350 million people in 98 countries around the world. There are already 12 million infected people worldwide and two million new cases occur annually. Leishmaniasis has three main clinical presentations: cutaneous (CL), mucosal (ML), and visceral (VL). It is considered an opportunistic, infectious disease and the HIV-leishmaniasis correlation is well known. Antimonial compounds are used as first-line treatment drugs, but their toxicity, which can be extremely high, leads to a number of undesirable side effects and resultant failure of the patients to adhere to treatment. There is also a reported increase in Leishmania sp. resistance to these drugs. Nanotechnology has emerged as an attractive alternative because of its improved bioavailability and lower toxicity, and other characteristics that help to relieve the burden of this disease. In this review we will present some of the recent advances in the nanotechnological research regarding the treatment of leishmaniasis. The preclinical results regarding the approaches for a biomedical treatment of the disease have been encouraging, but further efforts will still be necessary for this therapy to have greater clinical applicability in humans.

94 citations

Journal ArticleDOI
TL;DR: The mechanisms of classical drug resistance and potential drug targets in Leishmania infection are described and the current drug-delivery systems and future perspectives towards Leishmaniasis treatment are covered.
Abstract: Leishmaniasis is a complex of diseases with numerous clinical manifestations for instance harshness from skin lesions to severe disfigurement and chronic systemic infection in the liver and spleen. So far, the most classical leishmaniasis therapy, despite its documented toxicities, remains pentavalent antimonial compounds. The available therapeutic modalities for leishmaniasis are overwhelmed with resistance to leishmaniasis therapy. Mechanisms of classical drug resistance are often related with the lower drug uptake, increased efflux, the faster drug metabolism, drug target modifications and over-expression of drug transporters. The high prevalence of leishmaniasis and the appearance of resistance to classical drugs reveal the demand to develop and explore novel, less toxic, low cost and more promising therapeutic modalities. The review describes the mechanisms of classical drug resistance and potential drug targets in Leishmania infection. Moreover, current drug-delivery systems and future perspectives towards Leishmaniasis treatment are also covered.

75 citations

References
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TL;DR: In this article, the authors present a survey of research work in physics, physical sciences, and physical chemistry, focusing on physics, chemistry, physics, and biology. But they do not discuss their work in this paper.
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TL;DR: It is highly feasible for nanoparticles of biodegradable polymers to be applied to promote oral chemotherapy by using Caco-2 cells, showing that surface modification of PLGA nanoparticles with vitamin E TPGS notably improved the cellular uptake.

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"Andrographolide nanoparticles in le..." refers background in this paper

  • ...Nanoparticle cellular uptake is markedly dependent on size and surface charge.(30) Nanoparticles in a size range below 200 nm are associated with increased phagocytosis and can easily localize in macrophages predominantly infested with leishmanial parasite....

    [...]

Journal ArticleDOI
TL;DR: Important findings of the past decade on the encapsulation and release profiles of macromolecular therapeutics from PLGA and PLGA-based nano/microparticles are discussed critically in relation to nature and type of bioactive molecule, carrier polymer and experimental variables that influence the delivery of macrochemical therapeutics.

999 citations