Dry state microcrystals stabilized by an HPMC film to improve the bioavailability of andrographolide

Hu, Xi; Liu, Xiaolin; Yu, Daoyong; Di, Donghua; Yin, Tian; Zhang, Shu; Tang, Xing

doi:10.1016/j.ijpharm.2015.07.057

Cited by 27 publications

(21 citation statements)

References 35 publications

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“…Of note, ANDRO and ANDRO-related compounds have been tested in humans in short-term clinical trials in patients with rheumatoid arthritis 39 and inflammatory bowel disease with no relevant safety issues 40 . Some potential limitations for the clinical use of ANDRO are related to its high insolubility, poor bioavailability, and short plasma half-life although efforts are being made to improve these shortcomings through modifying the molecule 41 or complexing it with bigger compounds such as polyethyleneglycol 42 .…”

Section: Discussionmentioning

confidence: 99%

Andrographolide Ameliorates Inflammation and Fibrogenesis and Attenuates Inflammasome Activation in Experimental Non-Alcoholic Steatohepatitis

Cabrera

Wree

Povero

et al. 2017

Sci Rep

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Therapy for nonalcoholic steatohepatitis (NASH) is limited. Andrographolide (ANDRO), a botanical compound, has a potent anti-inflammatory activity due to its ability to inhibit NF-κB. ANDRO has been also shown to inhibit the NLRP3 inflammasome, a relevant pathway in NASH. Our aim was to evaluate the effects of ANDRO in NASH and its influence on inflammasome activation in this setting. Thus, mice were fed a choline-deficient-amino-acid–defined (CDAA) diet with/without concomitant ANDRO administration (1 mg/kg, 3-times/week). Also, we assessed serum levels of alanine-aminotransferase (ALT), liver histology, hepatic triglyceride content (HTC) and hepatic expression of pro-inflammatory, pro-fibrotic and inflammasome genes. Inflammasome activation was also evaluated in fat-laden HepG2 cells. Our results showed that ANDRO administration decreased HTC and attenuated hepatic inflammation and fibrosis in CDAA-fed mice. ANDRO treatment determined a strong reduction in hepatic macrophage infiltration and reduced hepatic mRNA levels of both pro-inflammatory and pro-fibrotic genes. In addition, mice treated with ANDRO showed reduced expression of inflammasome genes. Finally, ANDRO inhibited LPS-induced interleukin-1β expression through NF-κB inhibition in fat-laden HepG2 cells and inflammasome disassembly. In conclusion, ANDRO administration reduces inflammation and fibrosis in experimental NASH. Inflammasome modulation by a NF-κB-dependent mechanism may be involved in the therapeutic effects of ANDRO.

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Section: Discussionmentioning

confidence: 99%

Andrographolide Ameliorates Inflammation and Fibrogenesis and Attenuates Inflammasome Activation in Experimental Non-Alcoholic Steatohepatitis

Cabrera

Wree

Povero

et al. 2017

Sci Rep

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“…Andrographolide (AG), a diterpenoid lactone, is isolated from the Chinese herb Andrographis paniculata. It has been proved to have many pharmacological actions, such as analgesic, antipyretic, anti-inflammatory, antiviral, and anticancer [15][16][17][18]. e potential use of AG has attracted great attention in recent years.…”

Section: Introductionmentioning

confidence: 99%

Preparation and Characterization of PEG4000 Palmitate/PEG8000 Palmitate-Solid Dispersion Containing the Poorly Water-Soluble Drug Andrographolide

Zeng

Zhao

et al. 2020

Advances in Polymer Technology

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Solid dispersion (SD) is the effective approach to improve the dissolution rate and bioavailability of class II drugs with low water solubility and high tissue permeability in the Biopharmaceutics Classification System. is study investigated the effects of polyethylene glycol (PEG) molecular weight in carrier material PEG palmitate on the properties of andrographolide (AG)-SD. We prepared SDs containing the poorly water-soluble drug AG by the freeze-drying method. e SDs were manufactured from two different polymers, PEG4000 palmitate and PEG8000 palmitate. e physicochemical properties of the AG-SDs were characterized by Fourier transform infrared spectroscopy, thermogravimetric analysis, differential scanning calorimetry, powder X-ray diffraction, scanning electron microscopy, dissolution testing, and so on. We found that AG-PEG4000 palmitate-SD and AG-PEG8000 palmitate-SD were similar in the surface morphology, specific surface area, and pore volume. Compared with the AG-PEG4000 palmitate-SD, the intermolecular interaction between PEG8000 palmitate and AG was stronger, and the thermal stability of AG-PEG8000 palmitate-SD was better. In the meanwhile, the AG relative crystallinity was lower and the AG dissolution rate was faster in AG-PEG8000 palmitate-SD. e results demonstrate that the increasing PEG molecular weight in the PEG palmitate can improve the compatibility between the poorly water-soluble drug and carrier material, which is beneficial to improve the SD thermal stability and increases the dissolution rate of poorly water-soluble drug in the SD.

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“…Comparing with the oral administration of pure ADG, we found that the mean C max and AUC values of ADG for ADG‐Soluplus solid dispersion were approximately increased 1.96‐ to 2.53‐fold, confirming the superiority of Soluplus as ADG solid dispersion carrier owing to the strong binding affinity between ADG and Soluplus. Compared to other ADG solid dispersions, the ADG‐Soluplus solid dispersion 1:7 had significant high oral bioavailability . Other solid dispersion, including ADG‐PEG 6000, ADG‐PVP VA64, and ADG‐F68, showed little effect on AGD absorption.…”

Section: Resultsmentioning

confidence: 94%

“…However, its high lipophilicity (log P = 2.63), low aqueous solubility (74 μg mL −1 ), and poor stability seriously limit its application . ADG can be normally made into tablet, capsule, and dropping pill, whereas its oral bioavailability is low due to its low solubility (74 μg mL −1 ) . In order to tackle this problem, soluble salt and superfine grinding have been used.…”

Section: Introductionmentioning

confidence: 99%

Andrographolide solid dispersions formulated by Soluplus to enhance interface wetting, dissolution, and absorption

Song¹,

Wang

Lu³

et al. 2019

J of Applied Polymer Sci

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Andrographolide (ADG) had profound functions as drug health‐care product. To improve ADG application in medical care, solid dispersion technique was introduced. Initially, several polymers were chosen to prepare ADG solid dispersion using hot‐melt extrusion. Working mechanisms of ADG solid dispersion, which include molecular docking and wetting property, were studied. The strongest molecular binding energy of ADG with Soluplus contributed to carrier‐controlled mechanism, leading to its highest drug dissolution. Soluplus as solid dispersion excipient could significantly improve drug absorption. In addition, ADG solid dispersions formulated by Soluplus were prepared and studied, and the ratios of drug to polymer were 1:5, 1:7, 1:9, and 1:12, respectively. It demonstrated that hydrogen bond interactions were formed between ADG and Soluplus based on infrared (IR) spectroscopy analysis. The characteristic peaks of crystal state of ADG at 11.97°, 14.95°, 15.86°, and 9.78° disappeared in ADG solid dispersion, demonstrating that excipient was efficient in transforming drug crystal state to amorphous phase by interacting with ADG. ADG‐Soluplus solid dispersion of 1:7 turned out to be the best with maximum cumulative release amount of more than 80%, whereas other ADG solid dispersions were in the range of 60–70%. The cumulative release amount of pure ADG was below 20%. Comparing with the oral administration of pure ADG, we found that the mean Cmax and AUC values of ADG for ADG‐Soluplus solid dispersion were approximately increased 1.96‐ to 2.53‐fold. © 2019 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2020, 137, 48354.

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Dry state microcrystals stabilized by an HPMC film to improve the bioavailability of andrographolide

Cited by 27 publications

References 35 publications

Andrographolide Ameliorates Inflammation and Fibrogenesis and Attenuates Inflammasome Activation in Experimental Non-Alcoholic Steatohepatitis

Andrographolide Ameliorates Inflammation and Fibrogenesis and Attenuates Inflammasome Activation in Experimental Non-Alcoholic Steatohepatitis

Preparation and Characterization of PEG4000 Palmitate/PEG8000 Palmitate-Solid Dispersion Containing the Poorly Water-Soluble Drug Andrographolide

Andrographolide solid dispersions formulated by Soluplus to enhance interface wetting, dissolution, and absorption

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