Pure Andrographolide Research Articles

Physical Characterization, Solubility test, and Dissolution test of the Solid Dispersion System of the Andrographolide-chitosan system for effective treatment against colon cancer

This work aimed to examine how varying concentrations of chitosan affect the physiochemical characteristics, and investigate the solubility and dissolving properties of the solid dispersion system including chitosan and andrographolide. A solid-state dispersion system including andrographolide and chitosan was synthesized using various drug-to-polymer ratios. The obtained data were examined for their morphology, physiological state, medication content, test for solubility, and rate of dissolution. The morphology of the system consists of a solid dispersion of andrographolide and chitosan was found to be spherical based on SEM analysis. The solid dispersion systems had infrared spectra with an absorption profile that closely approximated that of the active ingredient. The differences between DTA and XRD analysis indicated a decrease in both the point of melting and the strength of the crystal. The research found a 1.75-fold rise in the soluble state of the system consisting of solid dispersion of andrographolide and chitosan compared to the solubility of the andrographolide component. Furthermore, the chitosan-andrographolide solid dispersion system exhibited a dissolution rate that was 1.6 times higher compared to that of the pure andrographolide molecule. Increasing the amount of chitosan in the system consisting of a solid dispersion of chitosan-andrographolide resulted in a decrease in the degree of crystallinity as well as the andrographolide melting point. This has a beneficial impact on improving the solubility and dissolving rate of andrographolide. The optimized formulation shows a dose-dependent toxicity against HT29 cell lines.

Effect of Andrographis paniculata extract and Andrographolide on the pharmacokinetics of Aceclofenac and Celecoxib in rats

BackgroundIn India, for the treatment of cold, fever and inflammation, people consume herbal remedies containing Andrographis paniculata Nees (APE) as main ingredient, along with NSAIDs. So the purpose of this study is to investigate the effect of APE and pure andrographolide (AN) on the pharmacokinetic of with aceclofenac (ACF) and celecoxib (CXB) after oral co-administration in wistar rats. After co-administration of APE (equivalent to 20 mg/kg of AN) and AN (20 mg/kg) with ACF (5 mg/kg) and CXB (5 mg/kg) in rats, orally, drug concentrations in plasma were determined using HPLC method. Non-compartment model was used to calculate pharmacokinetic parameters like Cmax, Tmax, t1/2, MRT, Vd, CL, and AUC.ResultsCo-administration of ACF and CXB with APE and pure AN altered the systemic exposure level of each compound in vivo. The Cmax, Tmax, MRT of CXB were increased whereas Vd and Cl of CXB were decreased significantly after co-administration of CXB with APE. Whereas co-administration of CXB with AN significantly decreased Vd, CL, and MRT of CXB. The concentration of ACF was increased significantly in co-administered groups with pure AN and APE. The AUC0-∞, AUMC0-∞, MRT, Vd and t1/2 of ACF were also significantly decreased in co-administered groups, hence CL of ACF was increased significantly.ConclusionThis study concludes that APE and pure AN have effect on pharmacokinetic of CXB and ACF in rat. Not only patients but medical practitioners using Andrographis paniculata should have awareness regarding probable herb–drug interactions with ACF and CXB.

"Effect of the Solvent Polarity and Temperature in the Isolation of Pure Andrographolide from Andrographis paniculata"

"Effect of the Solvent Polarity and Temperature in the Isolation of Pure Andrographolide from Andrographis paniculata"

"Effect of the Solvent Polarity and Temperature in the Isolation of Pure Andrographolide from Andrographis paniculata"

"Effect of the Solvent Polarity and Temperature in the Isolation of Pure Andrographolide from Andrographis paniculata"

Isolation and Identification of Andrographolide Compounds from the Leaves of Sambiloto Plant (Andrographis paniculata Ness)

Sambiloto plant (Andrographis paniculata Ness) is a plant that has been used as medicine from generation to generation. Bioactive compounds in Sambiloto have pharmacological effects such as immunostimulants (increase immunity), antibiotic diuretics (facilitate urine), antipyretics, anti-inflammatory (anti-inflammatory), hepatoprotective, hypotensive, hypoglycemic, antibacterial, anti-inflammatory, respiratory tract, and heart and lung meridians - lungs. The bioactive compound in Sambiloto which is mostly found in the leaves is Andrographolide. In this study, the isolation of Andrographolide from the leaves of the sambiloto plant (Andrographis paniculata Ness) was carried out using purification and crystallization methods aimed at obtaining pure Andrographolide isolates more efficiently and identifying the results of Andrographolide isolates. The results showed that the isolates obtained using the purification and crystallization methods obtained a yield of 0.47%. In the qualitative test of Andrographolide isolates using eluent and acetate: n-hexane (3: 2), the Rf value was 0.38. The results obtained from Andrographolide isolates using infrared spectroscopy (FT-IR) were identical to the literature on Andrographolide. The absorption peaks at the wavenumbers obtained includes 3400,41 cm-1, 1979,68 cm-1, 1959,46 cm-1, 2928,22 cm-1, 1727,56 cm-1, 1646,98 cm-1, and 907,53 cm-1.

Induction of root endosymbiosis as a highly sustainable and efficient strategy for overproduction of the medicinally important diterpenoid lactone-andrographolide in Andrographis paniculata (Burm. F.) Wall. ex Nees

Andrographis paniculata [(Burm. f.) Wall. ex Nees, family Acanthaceae], is an important medicinal plant used in Indian and Chinese traditional systems of medicines. The therapeutic activity of A. paniculata is due to the presence of andrographolide, a diterpenoid lactone with potent pharmacological activities. Andrographolide and its various semi synthetic derivatives are of high therapeutic potential and therefore of high demand. Due to the complex structure of andrographolide, chemical synthesis has not been effective till date and thus the pharmaceutical industry depends on A. paniculata for extraction of pure andrographolide. The content of andrographolide in A. paniculata is low (14.28 ± 1.62 mg/g DW) and thus biotechnological interventions are essential for enhanced production of andrographolide. The potential mutualistic role of endosymbiosis in enhancing the yield of andrographolide in in vitro cultures of A. paniculata was studied and the salient findings obtained are reported. It was consistently observed that colonization of roots of A. paniculata seedlings by the mutualistic endosymbiotic fungus Piriformospora indica resulted in significant enhancement of andrographolide (58.2 ± 6.5 mg/g DW) in comparison to control plants (19.5 ± 2.3 mg/g DW), along with a correlated increase in plant biomass. Fractions derived from P. indica such as cell wall and culture exudate were also employed to study their effect on andrographolide and biomass yield. It was observed that these fractions successfully improved the growth rate of the plant along with elevated andrographolide production, with maximum andrographolide content (55.8 ± 3.2 mg/g DW) observed in cell wall fraction treated seedlings. Under all the treatment conditions the transcriptional regulation of andrographolide biosynthetic pathway genes were analysed using RT-qPCR and correlated with andrographolide content. Andographolide biosynthesis pathway genes- GGPS, HMGS and DXR showed a significantly high transcript level expression and correlation with andrographolide accumulation over a period of 35 days in case of all the treatments studied. The potential protective role of P. indica colonization under host abiotic stress was demonstrated in A. paniculata seedlings exposed to abiotic stress conditions induced by poly ethylene glycol. Piriformospora indica colonized plants under drought stress exhibited normal morphology, high antioxidant enzyme content, low malondialdehyde accumulation and high proline content when compared with the control plants. The observations prove that P. indica and P. indica derived fractions can be used as an ideal bio stimulator to enhance the biomass (2.344 fold) and andrographolide content (3.91 fold) in A. paniculata. The findings also showed that as A. paniculata is significantly affected by drought stress, P. indica can also be used as a helpful eco-friendly tool to confer drought stress tolerance, thereby improving biomass and andrographolide yield. Moreover, the biostimulants present in the fungal cell wall fractions and culture exudates can be purified and characterized for exploring their further functional roles in order to develop products of commercial value.

Herb-drug interaction of Andrographis paniculata (Nees) extract and andrographolide on pharmacokinetic and pharmacodynamic of naproxen in rats

Ethnopharmacological relevanceAndrographis paniculata Nees (Acanthacae) have broad range of pharmacological effects such as hepatoprotective, antifertility, antimalarial, antidiabetic, suppression of various cancer cells and anti-inflammatory properties and is widely used medicinal plant in the traditional Unani and Ayurvedic medicinal systems. Andrographolide (AN) is one of the active constituent of the A. paniculata Nees extract (APE). They have been found in many traditional herbal formulations in India and proven to be effective as anti-inflammatory drug. Aim of the studyTo evaluate the pharmacokinetic and pharmacodynamic (anti arthritic) herb-drug interactions of A. paniculata Nees extract (APE) and pure andrographolide (AN) with naproxen (NP) after oral co-administration in wistar rats. Materials and methodsAfter oral co-administration of APE (200mg/Kg) and AN (60mg/kg) with NP (7.5mg/kg) in rats, drug concentrations in plasma were determined using HPLC method. The main pharmacokinetic parameters of Cmax, tmax, t1/2, MRT, Vd, CL, and AUC were calculated by non-compartment model. Change in paw volume, mechanical nociceptive threshold, mechanical hyperalgesia, histopathology and hematological parameters were evaluated to study antiarthritic activity. ResultsCo-administration of NP with APE and pure AN decreased systemic exposure level of NP in vivo. The Cmax, tmax, AUC0−t of NP was decreased. In pharmacodynamic study, NP (10mg/kg) alone and NP+AN (10+60mg/kg) groups exhibited significant synergistic anti-arthritic activity as compared to groups NP+APE, APE and AN alone. ConclusionThe results obtained from this study suggested that NP, APE and pure AN existed pharmacokinetic herb–drug interactions in rat which is correlated with anti-arthritic study. The knowledge regarding possible herb–drug interaction of NP might be helpful for physicians as well as patients using AP. So further studies should be done to understand the effect of other herbal ingredients of APE on NP as well as to predict the herb–drug interaction in humans.

Pharmacokinetic and Pharmacodynamic Interaction of Andrographolide and Standardized Extract of Andrographis paniculata (Nees) with Nabumetone in Wistar Rats.

The aim of the study was to investigate the herb-drug interaction of Andrographis paniculata Nees (Acanthaceae) and Andrographolide (AN) with nabumetone (NAB) in wistar rats. Pharmacokinetic and pharmacodynamic interactions were studied after co-administration of APE and AN with NAB in Wistar rats. In pharmacokinetic studies, significant decrease in Cmax, AUC0-t and AUC0-∞ of 6-MNA after co-administration with pure AN and APE has been observed. Tmax of 6-MNA has been increased to 2 h from 1.5 h in AN + NAB treated group. Changes in mean residential time, clearance and volume of distribution of 6-MNA in APE + NAB treated group and AN + NAB treated group indicated interference of other components of APE other than AN. In pharmacodynamic study, significant decrease in antiarthritic activity of NAB on concomitant administration with APE and AN has been observed. The study concludes that NAB exhibits pharmacokinetic and pharmacodynamic interactions with APE and AN in rats thus alarms the concomitant use of herbal preparations containing APE and AN with NAB. Further study is needed to understand the mechanism and predict the herb-drug interaction in humans. Copyright © 2016 John Wiley & Sons, Ltd.

Beneficial effects of an Andrographis paniculata extract and andrographolide on cognitive functions in streptozotocin-induced diabetic rats

Context Andrographolide containing Andrographis paniculata (Burm. F.) Wall. Ex Nees (Acanthaceae) extracts is often used for treatments of diabetes and other inflammatory disorders commonly accompanying cognitive and other psychiatric disorders.Objective To compare the efficacies of a standardised A. paniculata extract (AP) and pure andrographolide on cognitive functions, oxidative stress and cholinergic function in diabetic rats.Materials and methods Streptozotocin-induced diabetic Charles Foster albino rats treated orally with a hydro-methanolic A. paniculata leaf extract (50, 100 and 200 mg/kg/day), or with pure andrographolide (15, 30 and 60 mg/kg/day) for 10 consecutive days, were subjected to Morris water maze test. After the test, acetylcholinesterase, superoxide dismutase (SOD), and catalase (CAT) activities and lipid peroxidation (LPO) in brain tissues were assessed.Results Acetylcholinesterase activity in pre-frontal cortex and hippocampus of diabetic rats was 2.1 and 2.6 times higher compared to nondiabetic rats. LPO was 1.6 times higher and decreased SOD (56.3%) and CAT (44.9%) activities in pre-frontal cortex of diabetic rats compared to nondiabetic rats. AP or andrographolide treatments dose dependently attenuated cognitive deficits, reduced acetylcholinesterase activity, oxidative stress, improved diabetic hyperglycemia and insulin deficiency. All observed effects of AP were quantitatively almost equal to those expected from its analytically quantified andrographolide content.Discussion and conclusion Reported observations are the very first ones suggesting beneficial effects of andrographolide against diabetes associated cognitive deficits, increased acetylcholinesterase activity and deteriorated antioxidative status. Efforts to exploit A. paniculata extracts enriched in andrographolide as preventive measures against such disorders can be warranted.

Pharmacokinetic and pharmacodynamic herb–drug interaction of Andrographis paniculata (Nees) extract and andrographolide with etoricoxib after oral administration in rats

Ethnopharmacological relevanceAndrographis paniculata Nees (Acanthacae) is commonly used medicinal plant in the traditional. Unani and Ayurvedic medicinal systems. It has broad range of pharmacological effects such as hepatoprotective, antioxidant, antivenom, antifertility, inhibition of replication of the HIV virus, antimalarial, antifungal, antibacterial, antidiabetic, suppression of various cancer cells and anti-inflammatory properties. Andrographolide (AN) is one of the active constituent of the A. paniculata Nees extract (APE). They have been found in many traditional herbal formulations in India and proven to be effective as anti-inflammatory drug Aim of the studyTo evaluate the pharmacokinetic and pharmacodynamic (anti-arthritic) herb–drug interactions of A. paniculata Nees extract (APE) and pure andrographolide (AN) with etoricoxib (ETO) after oral co-administration in wistar rats. Materials and methodsAfter oral co-administration of APE (200mg/Kg) and AN (60mg/kg) with ETO (10mg/kg) in rats, drug concentrations in plasma were determined using HPLC method. The main pharmacokinetic parameters of Cmax, tmax, t1/2, MRT, Vd, CL, and AUC were calculated by non-compartment model. Change in paw volume, mechanical nociceptive threshold, mechanical hyperalgesia, histopathology and hematological parameters were evaluated to study antiarthritic activity. ResultsCo-administration of ETO with APE and pure AN decreased systemic exposure level of each compound in vivo. The Cmax, AUC, t1/2 of ETO was decreased whereas Vd and CL of ETO was increased significantly after co-administration of ETO with pure AN and APE. In pharmacodynamic study, ETO alone and ETO+APE (10+200mg/kg) groups exhibited significant synergistic anti-arthritic activity as compared to groups ETO+AN, APE and AN alone. ConclusionThe results obtained from this study suggested that ETO, APE and pure AN existed pharmacokinetic herb–drug interactions in rat which is correlated with anti-arthritic study. Physicians and patients using A. paniculata should have the knowledge about its possible herb–drug interaction with ETO.

An in vitro study of anti-inflammatory activity of standardised Andrographis paniculata extracts and pure andrographolide.

BackgroundThe anti-inflammatory activity of Andrographis paniculata (Acanthaceae), a traditional medicine widely used in Asia, is commonly attributed to andrographolide, its main secondary metabolite. Commercial A. paniculata extracts are standardised to andrographolide content. We undertook the present study to investigate 1) how selective enrichment of andrographolide in commercial A. paniculata extracts affects the variability of non-standardised phytochemical components and 2) if variability in the non-standardised components of the extract affects the pharmacological activity of andrographolide itself.MethodsWe characterized 12 commercial, standardised (≥30% andrographolide) batches of A. paniculata extracts from India by HPLC profiling. We determined the antioxidant capacity of the extracts using 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging, oxygen radical antioxidant capacity (ORAC) and a Folin-Ciocalteu (FC) antioxidant assays. Their anti-inflammatory activity was assessed by assaying their inhibitory effect on the release of tumor necrosis factor alpha (TNF-α) in the human monocytic cell line THP-1.ResultsThe andrographolide content in the samples was close to the claimed value (32.2 ± 2.1%, range 27.5 to 35.9%). Twenty-one non-standardised constituents exhibited more than 2-fold variation in HPLC peak intensities in the tested batches. The chlorogenic acid content of the batches varied more than 30-fold. The DPPH free radical scavenging activity varied ~3-fold, the ORAC and FC antioxidant capacity varied ~1.5 fold among batches. In contrast, the TNF-α inhibitory activity of the extracts exhibited little variation and comparison with pure andrographolide indicated that it was mostly due to their andrographolide content.ConclusionsStandardised A. paniculata extracts contained the claimed amount of andrographolide but exhibited considerable phytochemical background variation. DPPH radical scavenging activity of the extracts was mostly due to the flavonoid/phenlycarboxylic acid compounds in the extracts. The inhibitory effect of andrographolide on the release of TNF-α was little affected by the quantitative variation of the non-standardised constituents.

Adaptogenic potential of andrographolide: An active principle of the king of bitters (Andrographis paniculata)

Andrographolide is a major bioactive secondary plant metabolite isolated Andrographis paniculata (Burm. F.) Wall. Ex. Nees. (穿心蓮 chuān xīn lián), a well-known traditionally used medicinal herb. The aim of the study was to pharmacologically evaluate the beneficial effect of andrographolide on stress-induced thermoregulatory and other physiological responses in mice. A stress-induced hyperthermia test was conducted in mice. The test agents were orally administered once daily for 11 consecutive days, and treatment effects on body weight changes, basal rectal temperature, and foot-shock-triggered hyperthermic responses were quantified on Day 1, Day 5, Day 7, and Day 10 of the experiments. Pentobarbital-induced hypnosis was quantified on the 11th day of treatment. Observations made during a pilot dose finding experiment revealed that, like A. paniculata extracts, pure andrographolide also possess adaptogenic properties. Observed dose-dependent efficacies of 3 mg/kg/d, 10 mg/kg/d, and 30 mg/kg/d andrographolide in the pilot experiment were reconfirmed by conducting two further analogous experiments using separate groups of either male or female mice. In these confirmatory experiments, efficacies of andrographolide were compared with that of 5 mg/kg/d oral doses of the standard anxiolytic diazepam. Significantly reduced body weights and elevated core temperatures of the three vehicle-treated control groups observed on the 5th day and subsequent observational days were completely absent even in the groups treated with the lowest andrographolide dose (3 mg/kg/d) or diazepam (5 mg/kg/d). Benzodiazepine-like potentiation of pentobarbital hypnosis was observed in andrographolide-treated animals. These observations reveal that andrographolide is functionally a diazepam-like desensitizer of biological mechanisms, and processes involved in stress trigger thermoregulatory and other physiological responses.

Andrographolides and traditionally used Andrographis paniculata as potential adaptogens: Implications for therapeutic innovation

Andrographis paniculata (Burm. F.) Wall. Ex Nees (Family: Anthaceae) is a traditionally known Ayurvedic medicinal plant. Several well-controlled clinical trials conducted during recent years have consistently reconfirmed that Andrographis paniculata extracts are effective in suppressing cardinal symptoms of diverse inflammatory and infectious diseases. Despite extensive efforts though, many questions concerning bioactive constituents of such extracts and their modes of actions still remain unanswered. Amongst diverse diterpene lactones isolated to date from such extracts, andrographolide is often considered to be the major, representative, or bioactive secondary metabolite of the plant. Therefore, it has attracted considerable attention of several drug discovery laboratories as a lead molecule potentially useful for identifying structurally and functionally novel drug. Critical analysis of available preclinical and clinical information on Andrographis paniculata extracts and pure andrographolide strongly suggest that they are pharmacologically polyvalent and that they possess adaptogenic properties. Aim of this communication is to summarize and critically analyze such data, and to point out some possibilities for more rationally exploiting their adaptogenic properties for discovering novel therapeutic leads, or for obtaining pharmacologically better standardized phyto-pharmaceuticals.

Protective effects of Andrographis paniculata extract and pure andrographolide against chronic stress-triggered pathologies in rats.

This study was designed to experimentally verify the possibility that Andrographis paniculata could be another medicinal herb potentially useful for prevention of diverse spectrums of pathologies commonly associated with chronic unavoidable environmental stress, and whether andrographolide could as well be its quantitatively major bioactive secondary metabolite. Preventive effects of 21 daily oral 50, 100 and 200mg/kg doses of a therapeutically used extract of the plant (AP) and 30 and 60mg/kg/day of pure andrographolide were compared in rats subjected to 1-h daily unavoidable foot-shocks. A pharmaceutically well-standardized Withania somnifera (WS) root extract was used as a reference herbal anti-stress agent in all experiments. Effects of the treatments on stress-induced alterations in body weight, gastric ulcer, adrenal and spleen weights, and depressive state and sexual behavior in male rats were quantified. Other parameters quantified were plasma cortisol levels, and expressions of the cytokines TNF-α, IL-10 and IL-1β in blood and brain. All observed stress-induced pathological changes were less pronounced or completely prevented by both AP and pure andrographolide. Even the lowest tested doses of AP (50mg/kg/day) or of andrographolide (30mg/kg/day) suppressed almost maximally the blood IL-1β and IL-10 as well as brain TNF-α and IL-10 expressions induced by chronic stress. Qualitatively, the observed activity profiles of both of them were similar to those of WS dose tested. These results reveal that both AP and andrographolide are pharmacologically polyvalent anti-stress agents, and that biological processes regulating corticosterone and cytokine homeostasis are involved in their modes of actions.

Andrographolide: Solving Chemical Instability and Poor Solubility by Means of Cocrystals

The bioactive agent andrographolide was screened with pharmaceutically acceptable coformers to discover a novel solid form that will solve the chemical instability and poor solubility problems of this herbal medicine. Liquid-assisted grinding of andrographolide with GRAS (generally regarded as safe) coformers in a fixed stoichiometry resulted in cocrystals with vanillin (1:1), vanillic acid (1:1), salicylic acid (1:1), resorcinol (1:1), and guaiacol (1:1). All the crystalline products were characterized by thermal, spectroscopic, and diffraction methods. Interestingly, even though the cocrystals are isostructural, their physicochemical properties are quite different. The andrographolide-salicylic acid cocrystal completely inhibited the chemical transformation of andrographolide to its inactive sulfate metabolite, and moreover, the cocrystal exhibited a dissolution rate that was three times faster and a drug release that was two times higher than pure andrographolide.

Improved bioavailability of orally administered andrographolide from pH-sensitive nanoparticles

Andrographolide, a major bioactive phytoconstituent derived from Androgaphis paniculata that is safe and beneficial in several ailments, was formulated into pH-sensitive nanoparticle suspension with a view of improving its oral bioavailability. The andrographolide-loaded pH-sensitive nanoparticles were prepared by nanoprecipitation technique using Eudragit® EPO (cationic poly methacrylate copolymer). The 3(2) factorial design was used to optimize the amount of polymer and stabilizer (Pluronic® F-68). The optimized batch obtained using 0.45% w/v of Eudragit® EPO and 0.6% w/v of Pluronic® F-68 showed high-encapsulation efficiency of 93.8±0.67% with particle size of 255±9 nm and zeta potential of 29.3±3.4 mV. The bioavailability of andrographolide from optimized nanoparticles and pure andrographolide was assessed in male Wistar albino rats at a dose of 10 mg/kg. As compared to the pure andrographolide, almost 2.2 and 3.2-fold increase in AUC0-∞, Cmax and 121.53% increase in relative bioavailability were observed for andrographolide from pH-sensitive nanoparticles (P<0.05). Shorter Tmax by about fourfold difference were observed with 2.2-fold decrease in Cl/F. The improved dissolution rate owing to its reduced particle size, increased surface area and reduced diffusion layer thickness may have contributed to oral bioavailability. The results clearly indicate the potential of pH-sensitive nanoparticles for oral delivery of low-bioavailability phytoconstituents such as andrographolide.

Andrographolide nanoparticles in leishmaniasis: characterization and in vitro evaluations

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.