The overall goal of this paper was to develop poly(lactic-co-glycolic acid) nanoparticles (PLGA-NPs) of curcumin (CUR), named CUR-PLGA-NPs, and to study the effect and mechanisms enhancing the oral bioavailability of CUR. CUR-PLGA-NPs were prepared according to a solid-in-oil-in-water (s/o/w) solvent evaporation method and exhibited a smooth and spherical shape with diameters of about 200 nm. Characterization of CUR-PLGA-NPs showed CUR was successfully encapsulated on the PLGA polymer. The entrapment efficiency and loading rate of CUR were 91.96 and 5.75%, respectively. CUR-PLGA-NPs showed about 640-fold in water solubility relative to that of n-CUR. A sustained CUR release to a total of approximately 77% was discovered from CUR-PLGA-NPs in artificial intestinal juice, but only about 48% in artificial gastric juice. After oral administration of CUR-PLGA-NPs, the relative bioavailability was 5.6-fold and had a longer half-life compared with that of native curcumin. The results showed that the effect in imp...
Last. Tung-Hu Tsai(PRC: China Medical University (PRC))H-Index: 64
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Abstract This study has optimised the poly lactic-co-glycolic acid (PLGA) nano-formulation of curcumin to prolong its retention time in the body and improve bioavailability. High-pressure emulsification–solvent-evaporation was designed to obtain curcumin-loaded PLGA nanoparticles (C-NPs) prepared with 2% of PVA containing 20% sucrose as aqueous phase and dichloromethane as oil phase. The size and entrapment efficiency of C-NPs was 158 ± 10 nm and 46.6 ± 13.5%, respectively. The stable storage ti...
#1Ran Mo(CPU: China Pharmaceutical University)H-Index: 27
#2Xiang Jin(CPU: China Pharmaceutical University)H-Index: 5
Last. Qineng Ping(CPU: China Pharmaceutical University)H-Index: 45
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Abstract The overall objective of the present investigation was to demonstrate the effect of N-octyl-O-sulfate chitosan (NOSC) micelles on enhancing the oral absorption of paclitaxel (PTX) in vivo and in vitro , and identify the mechanism of this action of NOSC. In vivo , the oral bioavailability of PTX loaded in NOSC micelles (PTX-M) was 6-fold improved in comparison with that of an orally dosed Taxol ® . In the Caco-2 uptake studies, NOSC micelles brought about a significantly higher amount of...
Polymer-drug conjugates have gained much attention largely to circumvent lower drug solubility and to enhance drug stability. Curcumin is widely known for its medicinal properties including its anticancer efficacy. One of the serious drawbacks of curcumin is its poor water solubility which leads to reduced bioavailability. With a view to address these issues, we synthesized hyaluronic acid–curcumin (HA–Cur) conjugate. The drug conjugate was characterized using FT-IR, NMR, Dynamic light scatterin...
Curcumin is a polyphenol that is commonly used for its perceived health benefits. However, the absorption efficacy of curcumin is too low to exhibit beneficial effects. We have successfully developed a highly absorptive curcumin dispersed with colloidal nano-particles, and named it THERACURMIN. The absorption efficacy of THERACURMIN was investigated and compared with that of curcumin powder. The area under the blood concentration–time curve (AUC) after the oral administration of THERACURMIN was ...
Last. Robert O. Ryan(Children's Hospital Oakland Research Institute)H-Index: 62
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Abstract Nanodisks (NDs) are nanoscale, disk-shaped phospholipid bilayers whose edge is stabilized by apolipoproteins. In the present study, NDs were formulated with the bioactive polyphenol curcumin at a 6:1 phospholipid-to-curcumin molar ratio. Atomic force microscopy revealed that curcumin-NDs are particles with diameters From the Clinical Editor Nanodisks (NDs), disk-shaped phospholipid bilayers stabilized by apolipoproteins, are shown entrap curcumin and improve its delivery to HepG2 and ma...
This work aimed to compare methods for the formation of complexes of bixin and curcumin with β-cyclodextrin (β-CD) and to evaluate the stability of the complexes formed by these methods and their food applications. The stoichiometric relationship between curcumin and β-CD was 1:2 and that between bixin and β-CD was 1:1. Curcumin-β-CD and bixin-β-CD complexes formed by kneading, coprecipitation, and simple mixing were evaluated by differential scanning calorimetry (DSC), thermogravimetry analysis...
Last. Shile Huang(LSU Health Sciences Center New Orleans)H-Index: 56
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Curcumin (diferuloylmethane), an orange-yellow component of turmeric or curry powder, is a polyphenol natural product isolated from the rhizome of the plant Curcuma longa. For centuries, curcumin has been used in some medicinal preparation or used as a food-coloring agent. In recent years, extensive in vitro and in vivo studies suggested curcumin has anticancer, antiviral, antiarthritic, anti-amyloid, antioxidant, and anti-inflammatory properties. The underlying mechanisms of these effects are d...
Last. Indu Pal Kaur(Panjab University, Chandigarh)H-Index: 40
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Scope: Curcumin, a molecule with pluripharmacological properties, was loaded into solid lipid nanoparticles (SLNs) with a view to improve its oral bioavailability (BA). Methods and results: Curcumin-loaded solid lipid nanoparticles (C-SLNs) with an average particle size of 134.6 nm and a total drug content of 92.33±1.63% was produced using a microemulsification technique. The particles were spherical in shape, with high drug entrapment of 81.92±2.91% at 10% drug loading. The in vitro release was...
Curcumin is a highly potent, nontoxic, bioactive agent found in turmeric and has been known for centuries as a household remedy to many ailments. The only disadvantage that it suffers is of low aqueous solubility and poor bioavailability. The aim of the present study was to develop a method for the preparation of nanoparticles of curcumin with a view to improve its aqueous-phase solubility and examine the effect on its antimicrobial properties. Nanoparticles of curcumin (nanocurcumin) were prepa...
Abstract Curcumin a poly-phenolic compound possesses diverse pharmacologic activities; however, its development as a drug has been severely impeded by extremely poor oral bioavailability. Poor aqueous solubility and extensive metabolism have been implicated for this but the role of membrane permeability has not been investigated. In the present study, permeability of curcumin was assessed using the Caco-2 cell line. Curcumin was poorly permeable with a P app (A → B) value of 2.93 ± 0.94 × 10 −6 ...
#1Qian Li(HBUT: Hubei University of Technology)H-Index: 10
#2Jinglan Shi(HBUT: Hubei University of Technology)H-Index: 2
Last. Xiaoqiang Chen(HBUT: Hubei University of Technology)H-Index: 10
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Abstract null null With increasing consumer demand for label-friendly products, there is a push towards the identification and utilization of effective natural emulsifiers from botanical sources. In this study, we investigated the effect of controlled thermal treatments on the physicochemical and functional properties of tea polysaccharide conjugates (TPCs). Thermal treatment of the TPCs at 110 °C for 3 days (TPC-3d) markedly improved their emulsifying activity without negatively impacting their...
Abstract null null Propolis is a resinous material produced by bees (Apis mellifera) from different botanical sources. It has a wide variety of biological activities attributed to its chemical constituents, which are mainly phenolic acids and polyphenols such as flavonoids. These components usually have low water solubility and poor bioavailability. Polymeric, lipid and inorganic nanocarriers had been mainly used as drug delivery systems to overcome the physiological limitations of propolis chem...
Purpose 4-Hydroxyisophthalic acid (4-HIA) is a bioactive compound present in the roots of Decalepis hamiltonii, which has attracted considerable attention in attenuating oxidative stress-related neurodegenerative diseases. However, its efficacy is limited because of its low solubility and bioavailability. Therefore, the present study aimed to encapsulate 4-HIA using biocompatible copolymer polylactide-co-glycolide (PLGA) and evaluate its antioxidant and neuroprotective potential. Methods The nan...
Last. Pasarapa Towiwat(Chula: Chulalongkorn University)H-Index: 8
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Chronic pain is a persistent and unremitting condition that has immense effects on patients’ quality of life. Studies have shown that neuroinflammation is associated with the induction and progression of chronic pain. The activation of microglia and astrocytes is the major hallmark of spinal neuroinflammation leading to neuronal excitability in the projection neurons. Excessive activation of microglia and astrocytes is one of the major contributing factors to the exacerbation of pain. However, t...
#1Giulia Vanti(UniFI: University of Florence)H-Index: 5
Natural products are major molecules for drug discovery due to their structural diversity and their interaction with various biological targets, yet their clinical application is limited by poor water solubility or low lipophilicity, inappropriate molecular size, low dissolution rate and permeation, instability, high metabolic rate and rapid clearance. These issues can be solved by nanomedicine, by improving bioavailability and therapeutic efficacy. Here we review nanocarriers made of polymer or...
Last. Stefano Dusi(University of Verona)H-Index: 26
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Oxyresveratrol, a polyphenol extracted from the plant Artocarpus lakoocha Roxb, has been reported to be an antioxidant and an oxygen-free radical scavenger. We investigated whether oxyresveratrol affects the generation of superoxide anion (O2−) by human monocytes, which are powerful reactive oxygen species (ROS) producers. We found that oxyresveratrol inhibited the O2− production induced upon stimulation of monocytes with β-glucan, a well known fungal immune cell activator. We then investigated ...
Abstract Herein, we report a novel type of NPs by loading paeonol (Pae) into PLGA NPs, to enhance drug stability and oral bioavailability. The paeonol (Pae)-loaded polylactic-co-Gly-colic acid (PLGA) nanoparticles (Pae-PLGA-NPs) were prepared by nanoprecipitation method. The resultant NPs were in spherical shape with an average particle size around 237.7 ± 4.92 nm, and the PDI and zeta potential were 0.110 ± 0.01 and -25.33 ± 1.37 mV, respectively. The encapsulation efficiency (EE) and drug load...
Thymoquinone (TQ), the active constituent of Nigella sativa, possesses several benefits in traditional and modern medicines. This study examined the effect of a single dose of Nano-TQ on chronic lung injury induced by repetitive intratracheal installation of lipopolysaccharide (LPS). Rats received LPS twice weekly for 8 weeks via intratracheal installation and a single dose of TQ-PLGA NPs on the day after the last dose of LPS. Six rats from each group were sacrificed after 8 and 10 weeks, and sa...
