Absorption Of Curcumin Research Articles

Trends in advanced oral drug delivery system for curcumin: A systematic review.

Although curcumin is globally recognized for its health benefits, its clinical application has been restricted by its poor aqueous solubility and stability. To overcome these limitations, nanocarrier-based drug delivery systems (NDS) are one of the most effective approaches being extensively explored over the last few decades to improve curcumin's physicochemical and pharmacological effects. Various NDS could provide productive platforms for addressing the formulation challenge of curcumin, but evidence of such systems has not been summarized. This study aimed to systematically review current evidence of lipid and polymer-based NDS for an oral delivery of curcumin focusing on in vivo models and clinical studies. Among the 48 included studies, 3 studies were randomized controlled clinical trials, while 45 studies were animal models. To date, only five curcumin NDS have been studied in healthy volunteers: γ-cyclodextrin, phytosome, liposome, microemulsion and solid dispersion, while most curcumin NDS have been studied in animal models. Most included studies found that NDS could increase oral bioavailability of curcumin as compared to free curcumin. In conclusion, this systematic review showed evidence of the positive effect of NDS for enhancement of oral bioavailability of curcumin. EXECUTIVE SUMMARY: Curcumin is globally recognized for its health benefits, but its clinical application has been limited by its poor aqueous solubility and stability, which causes poor absorption in the gastrointestinal tract (GI tract) via oral administration. Nanocarrier-based drug delivery systems (NDS) are considered as a productive platform to solve the formulation challenge of curcumin, but evidence of such systems has not been summarized. This study aimed to systematically review current evidence of lipid and polymer-based NDS for an oral delivery of curcumin focusing on in vivo models and clinical studies. Overall, most studies found that all studied NDS could increase the absorption of curcumin as compared to free curcumin. Curcumin was rapidly absorbed and exhibited a long residence time after oral administration of curcumin NDS. In summary, this systematic review showed positive impacts of NDS for enhancement of oral absorption of curcumin.

Observation of curcumin-loaded hydroxypropyl methylcellulose (HPMC) oleogels under in vitro lipid digestion and in situ intestinal absorption in rats

Curcumin-loaded nanostructured lipid carriers (Cur-NLCs)-based hydroxypropyl methylcellulose (HPMC) oleogels (Cur-NLCs-HPMC-OGs) were fabricated using a cryogel template. The effect of the HPMC viscosity grade on the oleogel characteristics and in situ intestinal absorption were examined. Highly stable Cur-NLCs were prepared with a mean particle size of 314 nm and polydispersity index of 0.275. Cur-NLCs affected the creamy texture of self-standing Cur-NLCs-HPMC-OGs. The Cur-NLCs were tightly packed as oil droplets in the network of HPMC. However, a high viscosity of HPMC-4000 led to a greater ability to entrap and prevent droplet coalescence compared to a low viscosity of HPMC-400. NLCs promoted the release of free fatty acids during in vitro lipid digestion, whereas HPMC-4000 maintained the strength and durability of oleogels against mechanical and enzymatic breakdown. The in situ loop results revealed higher curcumin absorption by Cur-NLCs-HPMC-OGs than by Cur-HPMC-OGs. HMPC-4000 showed slightly higher curcumin absorption compared to HPMC-400.

Pharmacological considerations for treating neuroinflammation with curcumin in Alzheimer's disease.

Prof. Dr. Peter Riederer, the former Head of the Neurochemistry Department of the Psychiatry and Psychotherapy Clinic at the University of Würzburg (Germany), has been one of the pioneers of research into oxidative stress in Parkinson's and Alzheimer's disease (AD). This review will outline how his scientific contribution to the field has opened a new direction for AD treatment beyond "plaques and tangles". In the 1990s, Prof. Riederer was one of the first scientists who proposed oxidative stress and neuroinflammation as one of the major contributors to Alzheimer's disease, despite the overwhelming support for the "amyloid-only" hypothesis at the time, which postulated that the sole and only cause of AD is β-amyloid. His group also highlighted the role of advanced glycation end products, sugar and dicarbonyl-derived protein modifications, which crosslink proteins into insoluble aggregates and potent pro-inflammatory activators of microglia. For the treatment of chronic neuroinflammation, he and his group suggested that the most appropriate drug class would be cytokine-suppressive anti-inflammatory drugs (CSAIDs) which have a broader anti-inflammatory action range than conventional non-steroidal anti-inflammatory drugs. One of the most potent CSAIDs is curcumin, but it suffers from a variety of pharmacokinetic disadvantages including low bioavailability, which might have tainted many human clinical trials. Although a variety of oral formulations with increased bioavailability have been developed, curcumin's absorption after oral delivery is too low to reach therapeutic concentrations in the micromolar range in the systemic circulation and the brain. This review will conclude with evidence that rectally applied suppositories might be the best alternatives to oral medications, as this route will be able to evade first-pass metabolism in the liver and achieve high concentrations of curcumin in plasma and tissues, including the brain.

Curcumin: Biological Activities and Modern Pharmaceutical Forms.

Curcumin (1,7-bis-(4-hydroxy-3-methoxyphenyl)-hepta-1,6-diene-3,5-dione) is a natural lipophilic polyphenol that exhibits significant pharmacological effects in vitro and in vivo through various mechanisms of action. Numerous studies have identified and characterised the pharmacokinetic, pharmacodynamic, and clinical properties of curcumin. Curcumin has an anti-inflammatory, antioxidative, antinociceptive, antiparasitic, antimalarial effect, and it is used as a wound-healing agent. However, poor curcumin absorption in the small intestine, fast metabolism, and fast systemic elimination cause poor bioavailability of curcumin in human beings. In order to overcome these problems, a number of curcumin formulations have been developed. The aim of this paper is to provide an overview of recent research in biological and pharmaceutical aspects of curcumin, methods of sample preparation for its isolation (Soxhlet extraction, ultrasound extraction, pressurised fluid extraction, microwave extraction, enzyme-assisted aided extraction), analytical methods (FTIR, NIR, FT-Raman, UV-VIS, NMR, XRD, DSC, TLC, HPLC, HPTLC, LC-MS, UPLC/Q-TOF-MS) for identification and quantification of curcumin in different matrices, and different techniques for developing formulations. The optimal sample preparation and use of an appropriate analytical method will significantly improve the evaluation of formulations and the biological activity of curcumin.

Study on the stability and oral bioavailability of curcumin loaded (-)-epigallocatechin-3-gallate/poly(N-vinylpyrrolidone) nanoparticles based on hydrogen bonding-driven self-assembly

The biological activity and absorption of curcumin (Cur) is limited in application due to its low water solubility, poorstabilityand rapid metabolism. In this work, Cur loaded (-)-epigallocatechin-3-gallate (EGCG)/poly(N-vinylpyrrolidone) (PVP) nanoparticles (CEP-NPs) was successfully fabricated via self-assembly driven by hydrogen bonding, providing with desirable Cur-loading efficiency, high stability, strong antioxidant capacity, and pH-triggered intestinal targeted release properties. Molecular dynamics simulations further indicated the Cur was coated with EGCG and PVP in CEP-NPs and high acid prolonged release property was attribute to low ionization degree of EGCG. Besides, the enhanced intestinal absorption of Cur was related to inhibition of Cur metabolism by EGCG, enhancement of cellular uptake and higher Caco-2 monolayer permeation. Pharmacokinetic study showed that the oral bioavailability presented nearly 12-fold increment. Therefore, this study provides a new horizon for improving the Cur utilization in food and pharmaceutical fields.

Development and Evaluation of Tannic Acid-Coated Nanosuspension for Enhancing Oral Bioavailability of Curcumin.

Curcumin (CUR) has been used in the treatment of various diseases such as cough, fever, skin disease, and infection because of various biological benefits such as anti-inflammatory, antiviral, antibacterial, and antitumor activity. However, CUR is a BCS class 4 group and has a limitation of low bioavailability due to low solubility and permeability. Therefore, the purpose of this study is to prepare a nanosuspension (NSP) loaded with CUR (CUR-NSP) using a statistical design approach to improve the oral bioavailability of CUR, and then to develop CUR-NSP coated with tannic acid to increase the mucoadhesion in the GI tract. Firstly, the optimized CUR-NSP, composed of sodium dodecyl sulfate (SDS) and polyvinylpyrrolidone/vinyl acetate (PVP/VA), was modified with tannic acid (TA). The particle size and polydispersity index of the formulation measured by laser scattering analyzer were 127.7 ± 1.3 nm and 0.227 ± 0.010, respectively. In addition, the precipitation in distilled water (DW) was 1.52 ± 0.58%. Using a differential scanning calorimeter and X-ray diffraction analysis, the stable amorphous form of CUR was confirmed in the formulation, and it was confirmed that CUR-NSP formulation was coated with TA through a Fourier transform-infrared spectroscopy. In the mucoadhesion assay using the turbidity, it was confirmed that TA-CUR-NSP had higher affinity for mucus than CUR-NSP under all pH conditions. This means that the absorption of CUR can be improved by increasing the retention time in the GI tract of the formulation. In addition, the drug release profile showed more than 80% release, and in the cellular uptake study, the absorption of the formulation (TA-CUR-NSP) containing TA acting as an inhibitor of P-gp was increased by 1.6-fold. In the evaluation of antioxidant activity, the SOD activity of TA-CUR-NSP was remarkably high due to TA, which improves cellular uptake and has antioxidant activity. In the pharmacokinetic evaluation, the maximum drug plasma concentration of the TA-coated NSP formulation was 7.2-fold higher than that of the pure drug. In all experiments, it was confirmed that the TA-CUR-NSP is a promising approach to overcome the low oral bioavailability of CUR.

Comparative pharmacokinetics of Theracurmin, a highly bioavailable curcumin, in healthy adult subjects.

Objective: Theracurmin is a submicron dispersed formulation of curcumin, which was developed to increase the bioavailability of curcumin. This study aimed to compare the pharmacokinetics of curcumin administered as two Theracurmin powder products and unformulated curcumin powder. Materials and methods: This randomized, three-treatment, six-sequence, and three-period crossover study enrolled 24 healthy subjects. Blood sampling was done until 12 hours after the administration of Theracurmin and curcumin powder to assess pharmacokinetics using a non-compartmental method. The plasma concentration of curcumin was determined using high-performance liquid chromatography coupled with tandem mass spectrometry. Results: The median time to reach the maximum concentration was 1.5 – 3 hours for Theracurmin and 8 hours for curcumin powder. The two Theracurmin products showed systemic exposure profiles that were comparable to each other. The exposure ratio of Theracurmin to curcumin powder was 18.4 – 20.5 for the maximum plasma concentration and 35.9 – 42.6 for the area under the concentration-time curve from dosing to the last measurable time. Conclusion: In conclusion, this study showed similar systemic exposure between the two Theracurmin products. The absorption of curcumin after the administration of Theracurmin was significantly enhanced compared with curcumin powder.

Chitosan-Curcumin Coating Characterization on Cobalt-Chrome Surface by 100 kHz Ultrasonic Spray Method

Curcumin possesses anticoagulant, anti-proliferative, and anti-inflammatory properties and is applicable to prevent in-stent restenosis. This research investigated curcumin coating with biodegradable chitosan polymer as a drug carrier universally made on Co-Cr L605 surface by the ultrasonic spray method. Three curcumin doses were implemented: low dose (150 μg of curcumin per sample), medium dose (300 μg of curcumin per sample), and high dose (480 μg of curcumin per sample). The metal surface morphologies before and after coating were examined by using a stylus profilometer and a scanning electron microscope (SEM). The result showed that coating films were formed fine and uniform with an average roughness level below 0.2 μm. The coating film structure characterization by Fourier-transform infrared (FTIR) spectroscopy showed that curcumin absorption spectra still occurred in the chitosan-curcumin coating, although chitosan strong absorption spectra were dominant.

Hydrogel Films Based on Chitosan and Oxidized Carboxymethylcellulose Optimized for the Controlled Release of Curcumin with Applications in Treating Dermatological Conditions.

Cross-linked chitosan (CS) films with aldehyde groups obtained by oxidation of carboxymethyl cellulose (CMC) with NaIO4 were prepared using different molar ratios between the CHO groups from oxidized carboxymethyl cellulose (CMCOx) and NH2 groups from CS (from 0.25:1 to 2:1). Fourier-transform infrared (FTIR) and nuclear magnetic resonance (NMR) spectroscopy demonstrated the aldehyde groups’ presence in the CMCOx. The maximum oxidation degree was 22.9%. In the hydrogel, the amino groups’ conversion index value increased when the -CHO/-NH2 molar ratio, cross-linking temperature, and time increased, while the swelling degree values decreased. The hydrogel films were characterized by scanning electron microscopy (SEM) and FTIR analysis. The curcumin encapsulation efficiency decreases from 56.74% to 16.88% when the cross-linking degree increases. The immobilized curcumin release efficiency (REf%) and skin membrane permeability were evaluated in vitro in two different pH solutions using a Franz diffusion cell, and it was found to decrease when the molar ratio -CH=O/NH2 increases. The curcumin REf% in the receptor compartment was higher at pH = 7.4 (18%- for the sample with a molar ratio of 0.25:1) than at pH = 5.5 (16.5%). The curcumin absorption in the skin membrane at pH = 5.5 (47%) was more intense than at pH = 7.4 (8.6%). The curcumin-loaded films’ antioxidant activity was improved due to the CS presence.

Anti-ulcer Effect of Gastroretentive Drug Delivery System of Alginate Beads Containing Turmeric Extract Solid Dispersion

BACKGROUND: Treatment of gastric ulcer using turmeric extract is less effective because curcumin has low solubility and degraded in alkaline intestinal pH. Therefore, it is necessary to convert turmeric extract into turmeric solid dispersion to increase the dissolution of curcumin and the preparation is made in gastroretentive drug delivery system to improve the absorption of curcumin in the stomach.
 AIM: The aim of the study was to determine the anti-ulcer effect of gastroretentive drug delivery system of alginate beads containing turmeric extract solid dispersion compared to alginate beads containing turmeric extract (without solid dispersion) and negative control.
 METHODS: Turmeric powder was macerated with 96% ethanol for 8 days. The macerate was evaporated with a rotary evaporator at 50°C to obtain a concentrated extract. Turmeric extract solid dispersion was prepared by the solvent method using polyvinylpyrrolidone as a carrier. The turmeric extract solid dispersion was encapsulated with alginate gel by gelation method. The antiulcer test was performed on rats with gastric ulcer that induced by 0.6 N HCl solution. The ulcer healing was observed macroscopically and microscopically (histopathology).
 RESULTS: The results of observation on the treatment of rats gastric ulcer that induced by 0.6 N HCl showed the gastroretentive drug delivery system of alginate beads containing turmeric extract solid dispersion effective in healing the gastric ulcer compared to negative control. The effectiveness was statistically significantly different (p < 0.05). Alginate beads containing turmeric solid dispersion were slightly more effective than alginate beads containing turmeric extract, but the effectiveness was not statistically significant (p > 0.05).
 CONCLUSION: Alginate beads containing turmeric extract solid dispersion were effective in treatment of gastric ulcer in rats.

Facile microwave-assisted synthesis of Ti3C2 MXene quantum dots for ratiometric fluorescence detection of hypochlorite.

Adual-channel "naked-eye" colorimetric and ratio fluorescent probe has been developedbased on titanium carbide quantum dots for the detection of curcumin and hypochlorite (ClO-). The fluorescence emission of Ti3C2 MXene quantum dots (Ti3C2 MQDs) is in the range 350-600nm, and the maximum emission peak is at 430nm that overlaps with the UV absorption of curcumin at 430nm to a large extent. This facilitates the fluorescence resonance energy transfer (FRET) between Ti3C2 MQDs and curcumin. When ClO- is added, the phenolic and methoxy groups of curcumin are oxidized to quinones, resulting in the restoration of the fluorescence of Ti3C2 MQD. In addition, the probe designed makes it easier to distinguish colors with the naked eye to detect curcumin and ClO-. The linear detection range of curcumin was 0.05-10μM, and the detection limit was 20nM. The linear detection ranges of ClO- are 25-150μM and 150-275μM, and the detection limit is 5μM. This study is the first report on the determination of curcumin and ClO- based on Ti3C2 MQDs by dual-channel "naked-eye" colorimetric and ratio fluorescence method.

Studies on Biotinylated Liposomes as Potential Carries for Enhancing Oral Absorption of Curcumin

Studies on Biotinylated Liposomes as Potential Carries for Enhancing Oral Absorption of Curcumin

Solid dispersion improves release of curcumin from nanoparticles: Potential benefit for intestinal absorption

Curcumin-loaded nanocarriers clustered into hollow porous microspheres composed of arabic gum (AG) and xanthan gum (XG) form a solid dispersion, so-called nanoencapsulated curcumin (NEC), were investigated. In vitro study shows little or no release of curcumin from NEC into a buffer at pH 1.2, whereas a release rate of 1.4 %/h was obtained from that at pH 6.8 after 6 h, indicating intestinal absorption. In vivo evaluation in hamsters presented a peak plasma curcumin level of 400 ng/mL at 24 h after oral administration indicated an extended release of curcumin. Mucoadhesive NEC was rarely observed in stomach tissues but mostly in intestine after 72 h consumption, resulting in curcumin was detectable in plasma up to 3 days. NEC was not cytotoxic to normal fibroblasts but cytotoxic to cholangiocarcinoma cell line, suggesting anti-cholangiocarcinoma potentials. Under normal storage conditions for 3 years, up to 97 % of curcumin could be found in NEC, suggesting long-term stability. Therefore, NEC, a solid dispersion of curcumin-loaded nanocarriers in AG/XG gums, prolonged release with mucoadhesion providing enhanced intestinal absorption of curcumin and indicating cholangiocarcinoma potentials.

Interaction between curcumin and a peptide and their protective effects against hepatic steatosis in mice

Curcumin is antioxidative, liver protective and it has lipid regulatory effects. However, its in vivo efficiency is limited because of the low absorption rate and bioavailability. LVYP (Leu-Val-Tyr-Pro) is a tetrapeptide isolated, purified and identified from Corbicula fluminea with strong antioxidant activity. The interaction mechanisms between curcumin and LVYP were investigated using UV–vis absorption and fluorescence spectra. The results showed that the interaction between curcumin and LVYP was hydrophobic. When the temperature was increased from 25 to 37 °C, ΔG decreased and the number of ligand molecules increased, the interaction was quenched statically explained the formation of some compounds. On the other hand, dynamic quenching occurred when the temperature reached 60 °C, ΔG increased and the number of ligand molecules decreased, which indicated that temperature affected the interaction between curcumin and LVYP. This study also showed that LVYP could promote intestinal absorption of curcumin, predominantly in the ileum, which was explored using a non-everted intestinal sac model. In vivo experiments showed that the liver's protective effect with the combined administration of LVYP and curcumin was better than the curcumin alone, and LVYP could promote the hepatoprotective function of curcumin. It was hypothesized that the interaction of LVYP and curcumin enhanced the intestinal absorption rate of curcumin, thereby increasing its liver protection effect.

The combination of bromelain and curcumin as an immune-boosting nutraceutical in the prevention of severe COVID-19

The coronavirus disease 2019 (COVID-19) pandemic is still ongoing, while no treatment has been proven effective. COVID-19 pathophysiology involves the activation of three main pathways: the inflammatory, the coagulation and the bradykinin cascades. Here, we highlight for the first time the joint potential therapeutic role of bromelain and curcumin, two well-known nutraceuticals, in the prevention of severe COVID-19. Bromelain (a cysteine protease isolated from the pineapple stem) and curcumin (a natural phenol found in turmeric) exert important immunomodulatory actions interfering in the crucial steps of COVID-19 pathophysiology. Their anti-inflammatory properties include inhibition of transcription factors and subsequent downregulation of proinflammatory mediators. They also present fibrinolytic and anticoagulant properties. Additionally, bromelain inhibits cyclooxygenase and modulates prostaglandins and thromboxane, affecting both inflammation and coagulation, and also hydrolyzes bradykinin. Interestingly, curcumin has been shown in silico studies to prevent entry of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) into cells as well as viral replication, while a recent experimental study has demonstrated that bromelain may also inhibit viral entry into cells. Notably, bromelain substantially increases the absorption of curcumin after oral administration. To the best of our knowledge, this is the first report highlighting the significance of bromelain and, most importantly, the potential preventive value of the synergistic effects of bromelain and curcumin against severe COVID-19.

Potential enhancement of host immunity and anti-tumor efficacy of nanoscale curcumin and resveratrol in colorectal cancers by modulated electro- hyperthermia

BackgroundModulated electro-hyperthermia (mEHT) is a form of hyperthermia used in cancer treatment. mEHT has demonstrated the ability to activate host immunity by inducing the release of heat shock proteins, triggering apoptosis, and destroying the integrity of cell membranes to enhance cellular uptake of chemo-drugs in tumor cells. Both curcumin and resveratrol are phytochemicals that function as effective antioxidants, immune activators, and potential inhibitors of tumor development. However, poor bioavailability is a major obstacle for use in clinical cancer treatment.MethodsThis purpose of this study was to investigate whether mEHT can increase anti-cancer efficacy of nanosized curcumin and resveratrol in in vitro and in vivo models. The in vitro study included cell proliferation assay, cell cycle, and apoptosis analysis. Serum concentration was analyzed for the absorption of curcumin and resveratrol in SD rat model. The in vivo CT26/BALB/c animal tumor model was used for validating the safety, tumor growth curve, and immune cell infiltration within tumor tissues after combined mEHT/curcumin/resveratrol treatment.ResultsThe results indicate co-treatment of mEHT with nano-curcumin and resveratrol significantly induced cell cycle arrest and apoptosis of CT26 cells. The serum concentrations of curcumin and resveratrol were significantly elevated when mEHT was applied. The combination also inhibited the growth of CT26 colon cancer by inducing apoptosis and HSP70 expression of tumor cells while recruiting CD3+ T-cells and F4/80+ macrophages.ConclusionsThe results of this study have suggested that this natural, non-toxic compound can be an effective anti-tumor strategy for clinical cancer therapy. mEHT can enable cellular uptake of potential anti-tumor materials and create a favorable tumor microenvironment for an immunological chain reaction that improves the success of combined treatments of curcumin and resveratrol.

The influence of oil composition on the transformation, bioaccessibility, and intestinal absorption of curcumin in nanostructured lipid carriers.

In this study, the influences of liquid medium-chain triglyceride (MCT) and solid glyceryl tristearate (GTS) contents in the lipid matrix of nanostructured lipid carriers (NLCs) on their delivering capacities with respect to curcumin (Cur) were investigated by using a simulated gastrointestinal tract and Caco-2 monolayer models. The transformation of the encapsulated Cur decreased on increasing the MCT content in the lipid matrix of NLCs because it facilitated their lipolysis and promoted the exposure of Cur to a harsher exterior environment. Cur bioaccessibility was positively correlated with the level of micellized stearic acid resulting from GTS hydrolysis, which might be attributed to the fact that it could afford large hydrophobic domains to accommodate Cur. This value initially increased with an increase in the MCT content, reaching a maximum at 20% (w/w) and decreasing thereafter. The intestinal absorption of micellar Cur ranged from 26.06% to 38.76%, and a majority of the transported molecules were its reductive and conjugative metabolites. Overall, NLC containing 20% MCT in the lipid matrix afforded the highest Cur bioavailability, followed by that containing 10, 0, 40, 60, and 100% MCT. This work provides useful insights into the rational design of NLCs to optimize the bioavailability of the loaded agent.

Curcumin loaded Chitosan Nanoparticle for Accelerating the Post Extraction Wound Healing in Diabetes Mellitus Patient: A Review

Diabetes mellitus (DM) is a metabolic disease that has manifestations of hyperglycemia caused by an impaired insulin secretion in the body. The prevalence of type-II DM is a disease that affects around 382 million people worldwide with an increase in the number of sufferers reaching to 451 million in 2017. DM patients have a longer period of post-extraction wound healing than normal patient. Although there are many drugs to accelerate the wound healing for DM patients, there are still side effects. Therefore, a low side effect drug is needed to accelerate the post-extraction wound healing. The administration of curcumin with the effective chitosan nanoparticles is proposed because it can accelerate wound healing with low side effects and is obtained from natural ingredients. This review was aimed to summarize the potential of curcumin loaded chitosan nanoparticle for post-extraction wound healing in patients with type-II DM. Curcumin plays an important role at each stage of wound healing. In the inflammatory stage, the antioxidant effects of curcumin help controlling the inflammatory response by reducing the levels of Reactive Oxygen Species (ROS). In patients with DM type-II, the inflammatory response occurs uncontrollably due to the increased production of ROS, consequently, the tissue remodeling is inhibited. Furthermore, the administration of curcumin prevents the inhibition of tissue remodeling process. Curcumin loaded chitosan nanoparticle is more effective because it increases the bioavailability and accelerates the absorption of curcumin. Finally, Curcumin loaded chitosan nanoparticle has potential to accelerate the post-extraction wound healing in DM patients.

Nanocurcumin: preparation, characterization and cytotoxic effects towards human laryngeal cancer cells.

The aim of the present study was to prepare curcumin nanoparticles (nanocurcumin) by a sol-oil method to improve curcumin absorption and bioavailability, and to investigate the therapeutic effects of the prepared nanoparticles on the inhibition mechanisms towards human Hep-2 cancer cells. The nanoparticles were characterized by Fourier transform infrared spectroscopy, transmission electron microscopy, X-ray diffraction, and zeta potential analysis. The prepared curcumin nanoparticles possessed a narrow particle size distribution with an average diameter of 28 nm. The inhibition effects on the growth of human Hep-2 cells were investigated using neutral red uptake and lactate dehydrogenase assays. The results indicated that the nanocurcumin has a selective effect in inhibiting Hep-2 cell growth in a dose- and time-dependent mode with the most effective IC50 value (17 ± 0.31 μg ml−1) obtained after 48 h of incubation without any cytotoxic effects on normal cells. This IC50 value of nanocurcumin revealed a significant increase of early and late apoptotic cells with an intense comet nucleus of Hep-2 cells as a marker of DNA damage. Flow cytometry analysis of the progression of apoptosis in nanocurcumin Hep-2 treated cells showed that arresting in the cell cycle in the G2/M phase with increasing apoptotic cells in the sub-G1 phase. At the same time, real-time PCR analysis indicated that the treatment of Hep-2 cells with nanocurcumin resulted in upregulation of P53, Bax, and Caspase-3, whereas there was downregulation of Bcl-XL. These findings gave insights into understanding that the inhibition mechanisms of nanocurcumin on the proliferation of Hep-2 cancer cells was through the G2/M cell cycle arrest and the induction of apoptosis was dependent on Caspase-3 and p53 activation. However, in vivo studies with an animal model are essential to validate these results.

Gastric environment-stable oral nanocarriers for in situ colorectal cancer therapy

Colorectal cancer (CRC) is a prevalent and fatal cancer. Oral administration provided the potential for in situ treatment of the colorectal cancer. However, drugs couldn't be well-absorbed mainly due to its degradation in the gastric area and poor intestinal permeability. In this study, we synthesized deoxycholic acid and hydroxybutyl decorated chitosan nanoparticles (DAHBC NPs) as oral curcumin (CUR) delivery system for colorectal cancer treatment. DAHBC with lower critical solution temperature (LCST) below 37 °C (27–33 °C) was obtained. DAHBC NPs were correspondingly stable in simulated gastric conditions (pH 1.2, 37 °C), due to the offset of size change between pH-responsive expansion and thermo-responsive shrinkage. In simulated intestinal tract (pH 7.0–7.4, 37 °C), DAHBC NPs exhibited burst release of CUR owing to the onefold effect of thermo-responsive shrinkage. DAHBC27 NPs showed the minimum CUR leakage (~10%) in simulated gastric conditions, because a furthest temperature-sensitive shrinkage caused by the lowest LCST offset the expansion in acid environment. DAHBC27 NPs induced ~10-fold increased (P < 0.05) CUR absorption by paracellular transport pathway, compared to the free CUR. Thus, DAHBC NPs stabilized in the gastric environment may be a promising oral drugs delivery system for effective in situ colorectal cancer therapy.