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1.
Food Chem ; 446: 138286, 2024 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-38428073

RESUMO

We successfully designed curcumin (Cur)-loaded composite nanoparticles consisting of high-hydrostatic-pressure-treated (HHP-treated) zein and pectin with a pressure of 150 MPa (zein-150 MPa-P-Cur), showing nano-spherical structure with high zeta-potential (-36.72 ± 1.14 mV) and encapsulation efficiency (95.64 ± 1.23 %). We investigated the interaction mechanism of the components in zein-150 MPa-P-Cur using fluorescence spectroscopy, molecular dynamics simulation, Fourier-transform infrared spectrometry and scanning electron microscopy techniques. Compared with zein-P-Cur, the binding sites and binding energy (-53.68 kcal/mol vs. - 44.22 kcal/mol) of HHP-treated zein and Cur were increased. Meanwhile, the interaction force among HHP-treated zein, pectin, and Cur was significantly enhanced, which formed a tighter and more stable particle structure to further improve package performance. Additionally, Cur showed the best chemical stability in zein-150 MPa-P-Cur. And the bioavailability of Cur was increased to 65.53 ± 1.70 %. Collectively, composite nanoparticles based on HHP-treated zein and pectin could be used as a promising Cur delivery system.


Assuntos
Curcumina , Nanopartículas , Zeína , Pectinas/química , Curcumina/química , Zeína/química , Nanopartículas/química , Espectrofotometria Infravermelho , Tamanho da Partícula
2.
ACS Appl Bio Mater ; 7(4): 2175-2185, 2024 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-38478917

RESUMO

Lung cancer and Mycobacterium avium complex infection are lung diseases associated with high incidence and mortality rates. Most conventional anticancer drugs and antibiotics have certain limitations, including high drug resistance rates and adverse effects. Herein, we aimed to synthesize mannose surface-modified solid lipid nanoparticles (SLNs) loaded with curcumin (Man-CUR SLN) for the effective treatment of lung disease. The synthesized Man-CUR SLNs were analyzed using various instrumental techniques for structural and physicochemical characterization. Loading curcumin into SLNs improved the encapsulation efficiency and drug release capacity, as demonstrated by high-performance liquid chromatography analysis. Furthermore, we characterized the anticancer effect of curcumin using the A549 lung cancer cell line. Cells treated with Man-CUR SLN exhibited an increased cellular uptake and cytotoxicity. Moreover, treatment with free CUR could more effectively reduce cancer migration than treatment with Man-CUR SLNs. Similarly, free curcumin elicited a stronger apoptosis-inducing effect than that of Man-CUR SLNs, as demonstrated by reverse transcription-quantitative PCR analysis. Finally, we examined the antibacterial effects of free curcumin and Man-CUR SLNs against Mycobacterium intracellulare (M.i.) and M.i.-infected macrophages, revealing that Man-CUR SLNs exerted the strongest antibacterial effect. Collectively, these findings indicate that mannose-receptor-targeted curcumin delivery using lipid nanoparticles could be effective in treating lung diseases. Accordingly, this drug delivery system can be used to target a variety of cancers and immune cells.


Assuntos
Curcumina , Lipossomos , Neoplasias Pulmonares , Nanopartículas , Humanos , Curcumina/farmacologia , Curcumina/química , Manose , Lipídeos , Neoplasias Pulmonares/tratamento farmacológico
3.
Biomater Adv ; 160: 213830, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38552500

RESUMO

Cancer, namely breast and prostate cancers, is the leading cause of death in many developed countries. Controlled drug delivery systems are key for the development of new cancer treatment strategies, to improve the effectiveness of chemotherapy and tackle off-target effects. In here, we developed a biomaterials-based wireless electrostimulation system with the potential for controlled and on-demand release of anti-cancer drugs. The system is composed of curcumin-loaded poly(3,4-ethylenedioxythiophene) nanoparticles (CUR/PEDOT NPs), encapsulated inside coaxial poly(glycerol sebacate)/poly(caprolactone) (PGS/PCL) electrospun fibers. First, we show that the PGS/PCL nanofibers are biodegradable, which allows the delivery of NPs closer to the tumoral region, and have good mechanical properties, allowing the prolonged storage of the PEDOT NPs before their gradual release. Next, we demonstrate PEDOT/CUR nanoparticles can release CUR on-demand (65 % of release after applying a potential of -1.5 V for 180 s). Finally, a wireless electrostimulation platform using this NP/fiber system was set up to promote in vitro human prostate cancer cell death. We found a decrease of 67 % decrease in cancer cell viability. Overall, our results show the developed NP/fiber system has the potential to effectively deliver CUR in a highly controlled way to breast and prostate cancer in vitro models. We also show the potential of using wireless electrostimulation of drug-loaded NPs for cancer treatment, while using safe voltages for the human body. We believe our work is a stepping stone for the design and development of biomaterial-based future smarter and more effective delivery systems for anti-cancer therapy.


Assuntos
Compostos Bicíclicos Heterocíclicos com Pontes , Glicerol/análogos & derivados , Nanopartículas , Poliésteres , Polímeros , Tecnologia sem Fio , Humanos , Compostos Bicíclicos Heterocíclicos com Pontes/química , Nanopartículas/química , Polímeros/química , Poliésteres/química , Curcumina/administração & dosagem , Curcumina/química , Glicerol/química , Masculino , Neoplasias da Próstata/terapia , Antineoplásicos/administração & dosagem , Decanoatos/química , Nanofibras/química , Sistemas de Liberação de Medicamentos/instrumentação , Sistemas de Liberação de Medicamentos/métodos , Linhagem Celular Tumoral , Estimulação Elétrica/instrumentação , Estimulação Elétrica/métodos
4.
ACS Appl Mater Interfaces ; 16(8): 9749-9767, 2024 Feb 28.
Artigo em Inglês | MEDLINE | ID: mdl-38359334

RESUMO

The treatment of diabetic chronic wounds is still faced with great challenges, mainly due to wound infection, excessive inflammation, and peripheral vascular disease in the wound area. Therefore, it is of great importance to develop a novel multifunctional hydrogel with high efficiency to accelerate diabetic wound healing. Curcumin (Cur), a Chinese herbal, has shown great potential in enhancing the healing of diabetic chronic wounds because of its immunomodulatory and pro-angiogenic properties. However, its low aqueous solubility, poor bioavailability, and chemical instability have limited its clinical applications. To address these current bottlenecks, novel poly(vinyl alcohol) (PVA)-chitosan (CS)/sodium alginate (SA)-Cur (PCSA) hydrogels were prepared for the first time, and they demonstrated all of the above intriguing performances by the Michael addition reaction of CS and Cur. PCSA hydrogels show multiple dynamic bonds, which possess strong mechanical properties (tensile stress: ∼0.980 MPa; toughness: ∼258.45 kJ/m3; and compressive strength: ∼7.38 MPa at strain of 80%). These intriguing performances provided an optimal microenvironment for cell migration and proliferation and also promoted the growth of blood vessels, leading to early angiogenesis. Importantly, the experimental results demonstrated that PCSA hydrogels can effectively transform pro-inflammatory M1 macrophages into anti-inflammatory M2 macrophages without the need for additional ingredients in vitro. Benefiting from these characteristics, a full-thickness diabetic wound in a rat model demonstrated that PCSA hydrogels can effectively accelerate wound healing via ROS-scavenging, downregulation of IL-1ß, and upregulation of CD31 expression, resulting in angiogenesis and collagen deposition. This strategy not only provides a simple and safe Cur-based hydrogel for diabetic wound healing but also highlights the significant potential for the development of high-performance biomaterials for promoting diabetic wound healing using traditional Chinese medicine.


Assuntos
Anti-Infecciosos , Quitosana , Curcumina , Diabetes Mellitus , Ratos , Animais , Hidrogéis/farmacologia , Hidrogéis/química , Curcumina/química , Antioxidantes/farmacologia , Angiogênese , Cicatrização , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Anti-Infecciosos/farmacologia , Quitosana/farmacologia , Antibacterianos/química
5.
J Biomater Sci Polym Ed ; 35(5): 628-656, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38284334

RESUMO

In this study, the pH-responsive API-CMCS-SA (ACS) polymeric nanoparticles (NPs) based on 1-(3-amino-propyl) imidazole (API), stearic acid (SA), and carboxymethyl chitosan (CMCS) were fabricated for the effective transport of curcumin (CUR) in liver cancer. CUR-ACS-NPs with various degrees of substitution (DS) were employed to prepare through ultrasonic dispersion method. The effect of different DS on NPs formation was discussed. The obtained CUR-ACS-NPs (DSSA=12.4%) had high encapsulation rate (more than 85%) and uniform particle size (186.2 ± 1.42 nm). The CUR-ACS-NPs showed better stability than the other groups. Drug release from the CUR-ACS-NPs was pH-dependent, and more than 90% or 65% of CUR was released in 48 h in weakly acid medium (pH 5.0 or 6.0, respectively). Additionally, the CUR-ACS-NPs increased the intracellular accumulation of CUR and demonstrated high anticancer effect on HepG2 cells compared with the other groups. CUR-ACS-NPs prolonged the retention time of the drug, and the area under the curve (AUC) increased significantly in vivo. The in vivo antitumor study further revealed that the CUR-ACS-NPs exhibited the capability of inhibiting tumor growth and lower systemic toxicity. Meanwhile, CUR, CUR-CS-NPs, and CUR-ACS-NPs could be detected in the evaluated organs, including tumor, liver, spleen, lung, heart, and kidney in distribution studies. Among them, CUR-ACS-NPs reached the maximum concentration at the tumor site, indicating the tumor-targeting properties. In short, the results suggested that CUR-ACS-NPs could act a prospective drug transport system for effective delivery of CUR in cancer treatment.


Assuntos
Quitosana , Curcumina , Neoplasias Hepáticas , Nanopartículas , Humanos , Curcumina/química , Quitosana/química , Portadores de Fármacos/química , Nanopartículas/química , Neoplasias Hepáticas/tratamento farmacológico , Concentração de Íons de Hidrogênio , Tamanho da Partícula
6.
Luminescence ; 39(1): e4668, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38286596

RESUMO

Curcumin (Cur) is an acidic polyphenol with some effects on α-glucosidase (α-Glu), but Cur has disadvantages such as being a weak target, lacking passing the blood-brain barrier and having low bioavailability. To enhance the curative effect of Cur, the hybrid composed of ZnO nanoparticles decorated on rGO was used to load Cur (ZnO@rGO-Cur). The use of the multispectral method and enzyme inhibition kinetics analysis certify the inhibitory effect and interaction mechanism of ZnO@rGO-Cur with α-Glu. The static quenching of α-Glu with both Cur and ZnO@rGO-Cur is primarily driven by hydrogen bond and van der Waals interactions. The conformation-changing ability by binding to the neighbouring phenolic hydroxyl group of Cur increased their ability to alter the secondary structure of α-Glu, resulting in the inhibition of enzyme activity. The inhibition constant (Ki, Cur > Kis,ZnO@rGO-Cur ) showed that the inhibition effect of ZnO@rGO-Cur on α-Glu was larger than that of Cur. The CCK-8 experiments proved that ZnO@rGO nanocomposites have good biocompatibility. These results suggest that the therapeutic potential of ZnO@rGO-Cur composite is an emerging nanocarrier platform for drug delivery systems for the potential treatment of diabetes mellitus.


Assuntos
Curcumina , Diabetes Mellitus , Nanopartículas , Óxido de Zinco , Humanos , alfa-Glucosidases/efeitos dos fármacos , Curcumina/farmacologia , Curcumina/química , Sistemas de Liberação de Medicamentos , Óxido de Zinco/farmacologia , Óxido de Zinco/química , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia
7.
Biomed Mater ; 19(2)2024 Jan 25.
Artigo em Inglês | MEDLINE | ID: mdl-38215475

RESUMO

Curcumin (Cur) possesses remarkable pharmacological properties, including cardioprotective, neuroprotective, antimicrobial, and anticancer activities. However, the utilization of Cur in pharmaceuticals faces constraints owing to its inadequate water solubility and limited bioavailability. To overcome these hurdles, there has been notable focus on exploring innovative formulations, with nanobiotechnology emerging as a promising avenue to enhance the therapeutic effectiveness of these complex compounds. We report a novel safe, effective method for improving the incorporation of anticancer curcumin to induce apoptosis by reducing the expression levels of miR20a and miR21. The established method features three aspects that, to our knowledge, have not been formally verified: (1) use of a novel formula to incorporate curcumin, (2) use of all biocompatible biodegradable materials to produce this formula without leaving harmful residues, and (3) an incorporation process at temperatures of approximately 50 °C. The formula was prepared from lecithin (LE), and chitosan (CH) with an eco-friendly emulsifying agent and olive oil as the curcumin solvent. The formula was converted to nanoscale through ultrasonication and probe sonication at a frequency of 20 kHz. Transmission electron microscopy showed that the nano formula was spherical in shape with sizes ranging between 49.7 nm in diameter and negative zeta potentials ranging from 28 to 34 mV. Primers miR20a and miR21 were designed for molecular studies. Nearly complete curcumin with an encapsulation efficiency of 91.1% was established using a straight-line equation. The nano formula incorporated with curcumin was used to prepare formulations that exhibited anticancer activities. The apoptosis pathway in cancer cells was activated by the minimum inhibitory concentration of the nano formula. These findings suggest the potential of this nanoformulation as an effective and selective cancer treatment that does not affect the normal cells.


Assuntos
Neoplasias Colorretais , Curcumina , MicroRNAs , Nanopartículas , Humanos , Curcumina/química , Nanopartículas/química , Portadores de Fármacos/química , Solubilidade , Neoplasias Colorretais/tratamento farmacológico , Tamanho da Partícula
8.
Int J Biol Macromol ; 254(Pt 1): 127758, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38287596

RESUMO

This study has explored the potential of plant-derived oil bodies (OBs)-based oleogels as novel drug delivery systems for in vitro release under simulated physiological conditions. To obtain stable OBs-based oleogels, gum arabic (GA) and chitosan (CH) were coated onto the curcumin-loaded OBs using an electrostatic deposition technique, followed by 2,3,4-trihydroxybenzaldehyde (TB) induced Schiff-base cross-linking. Microstructural analyses indicated successful encapsulation of curcumin into the hydrophobic domain of the OBs through a pH-driven method combined with ultrasound treatment. The curcumin encapsulation efficiency of OBs increased up to 83.65 % and 92.18 % when GA and GA-CH coatings were applied, respectively, compared to uncoated OBs (63.47 %). In addition, GA-CH coatings retained the structural integrity of oleogel droplets with superior oil-holding capacity (99.07 %), while TB addition induced interconnected 3D-network structures with excellent gel strength (≥4.8 × 105 Pa) and thermal stability (≥80 °C). GA-CH coated oleogels appeared to provide the best protection for loaded bioactive against UV irradiation and high temperature-induced degradation during long-term storage. The combination of biopolymer coatings and TB-induced Schiff-base cross-linking synergistically hindered the simulated gastric degradability of oleogels, releasing only 23.35 %, 12.46 % and 7.19 % of curcumin by GA, GA-CH and GA-CH-TB stabilized oleogels, respectively, while also resulting in sustained release effects during intestinal conditions.


Assuntos
Quitosana , Curcumina , Goma Arábica/química , Curcumina/química , Quitosana/química , Preparações de Ação Retardada , Gotículas Lipídicas , Óleos de Plantas , Compostos Orgânicos
9.
J Biomol Struct Dyn ; 42(3): 1145-1156, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-37066617

RESUMO

Two-dimensional (2D) nanomaterials can improve drug delivery by reducing toxicity, increasing bioavailability and boosting efficacy. In this study, the simultaneous use of transition metal carbides and nitrides (MXenes) along with copper (II) benzene-1, 3, 5-tricarboxylate metal-organic framework (Cu - BTC/MOF) as attractive nanocarriers are investigated for loading and delivering curcumin (CUR) and paclitaxel (PTX) drugs to cancer cells. The efficiency of surface termination (bare and oxygen) in the adsorption of PTX and CUR drugs and the co-loading of these two drugs are evaluated. Our results show that the strongest interaction energy belongs to the adsorption of drug CUR on the MXNNO-Cu-BTC adsorbent, while the interaction of PTX drug with the MXNO- Cu-BTC in the MXNO-Cu-BTC/PTX&CUR system is the lowest due to the particular structure of the drug and the adsorbent. Our results show that at the beginning simulation, the interaction energy between the PTX drug and water in PTX/MXN system is -4645.48 kJ/mol, which reduces to -3848.71 kJ/mol after the system reaches equilibrium. Therefore, the inspected adsorbents have a good performance in adsorbing CUR and PTX drugs. The obtained results from this investigation provide valuable information about experimental studies by medical scientists in the future.Communicated by Ramaswamy H. Sarma.


Assuntos
Curcumina , Neoplasias , Nitritos , Elementos de Transição , Paclitaxel/farmacologia , Paclitaxel/química , Curcumina/farmacologia , Curcumina/química , Adsorção , Cobre/química , Água , Neoplasias/tratamento farmacológico
10.
Nanotechnology ; 35(13)2024 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-38096580

RESUMO

Nanoencapsulation, employing safe materials, holds substantial promise for enhancing bioactive compounds' delivery, stability, and bioactivity. In this study, we present an innovative and safe methodology for augmenting the incorporation of the anticancer agent, curcumin, thereby inducing apoptosis by downregulating miR20a and miR21 expression. Our established methodology introduces three pivotal elements that, to our knowledge, have not undergone formal validation: (1) Novel formulation: We introduce a unique formula for curcumin incorporation. (2) Biocompatibility and biodegradability: our formulation exclusively consists of biocompatible and biodegradable constituents, ensuring the absence of detrimental residues or undesirable reactions under varying conditions. (3) Low-temperature incorporation: Curcumin is incorporated into the formulation at temperatures approximating 50 °C. The formulation comprises lecithin (LE), chitosan (CH), an eco-friendly emulsifying agent, and olive oil as the solvent for curcumin. Nanoscale conversion is achieved through ultrasonication and probe sonication (20 kHz). Transmission electron microscopy (TEM) reveals spherical nanoparticles with diameters ranging from 29.33 nm and negative zeta potentials within the -28 to -34 mV range. Molecular studies involve the design of primers for miR20a and miR21. Our findings showcase a remarkable encapsulation efficiency of 91.1% for curcumin, as determined through a linear equation. The curcumin-loaded nanoformulation demonstrates potent anticancer activity, effectively activating the apoptosis pathway in cancer cells at the minimum inhibitory concentration. These results underscore the potential of our nanoformulation as a compelling, cancer-selective treatment strategy, preserving the integrity of normal cells, and thus, warranting further exploration in the field of cancer therapy.


Assuntos
Quitosana , Curcumina , Neoplasias Esofágicas , MicroRNAs , Nanopartículas , Humanos , Curcumina/química , Quitosana/química , Lecitinas , Sobrevivência Celular , Nanopartículas/química , MicroRNAs/genética , MicroRNAs/farmacologia , Portadores de Fármacos/química
11.
Acta Biomater ; 174: 372-385, 2024 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-38072226

RESUMO

Targeted delivery of therapeutic drugs to fibrosis-promoting macrophages (FPMs) holds promise as a challenging yet effective approach for the treatment of idiopathic pulmonary fibrosis (IPF). Here, nanocarriers composed of Mn-curcumin metal-organic frameworks (MOFs) were utilized to deliver the immune inhibitor BLZ-945 to the lungs, with the goal of depleting fibrosis-promoting macrophages (FPMs) from fibrotic lung tissues. FPM targeting was achieved by functionalizing the nanocarrier surface with an M2-like FPM binding peptide (M2pep). As a result, significant therapeutic benefits were observed through the successful depletion of approximately 80 % of the M2-like macrophages (FPMs) in a bleomycin-induced fibrosis mouse model treated with the designed M2-like FPM-targeting nanoparticle (referred to as M2NP-BLZ@Mn-Cur). Importantly, the released Mn2+ and curcumin after the degradation of M2NP-BLZ@Mn-Cur accumulated in the fibrotic lung tissue, which can alleviate inflammation and oxidative stress reactions, thereby further improving IPF therapy. This study presents a novel strategy with promising prospects for molecular-targeted fibrosis therapy. STATEMENT OF SIGNIFICANCE: Metal-organic frameworks (MOFs)- based nanocarriers equipped with both fibrosis-promoting macrophage (FPM)-specific targeting ability and therapeutic drugs are appealing for pulmonary fibrosis treatment. Here, we prepared M2pep (an M2-like FPM binding peptide)-modified and BLZ945 (a small molecule inhibitor of CSF1/CSF-1R axis)-loaded Mn-curcumin MOF nanoparticles (M2NP-BLZ@Mn-Cur) for pulmonary fibrosis therapy. The functionalized M2NP-BLZ@Mn-Cur nanoparticles can be preferentially taken up by FPMs, resulting in their depletion from fibrotic lung tissues. In addition, Mn2+and curcumin released from the nanocarriers have anti-inflammation and immune regulation effects, which further enhance the antifibrotic effect of the nanoparticles.


Assuntos
Curcumina , Fibrose Pulmonar Idiopática , Estruturas Metalorgânicas , Camundongos , Animais , Estruturas Metalorgânicas/farmacologia , Curcumina/farmacologia , Curcumina/uso terapêutico , Curcumina/química , Macrófagos/metabolismo , Fibrose Pulmonar Idiopática/tratamento farmacológico , Fibrose Pulmonar Idiopática/metabolismo , Peptídeos/farmacologia
12.
J Mater Chem B ; 12(4): 952-961, 2024 Jan 24.
Artigo em Inglês | MEDLINE | ID: mdl-37975827

RESUMO

The development of multifunctional nanohybrid systems for combined photo-induced hyperthermia and drug release is a challenging topic in the research of advanced materials for application in the biomedical field. Here, we report the first example of a three-component red-light-responsive nanosystem consisting of graphene oxide, gold nanoparticles and poly-N-isopropylacrylamide (GO-Au-PNM). The GO-Au-PNM nanostructures were characterized by spectroscopic techniques and atomic force microscopy. They exhibited photothermal conversion effects at various wavelengths, lower critical solution temperature (LCST) behaviour, and curcumin (Curc) loading capacity. The formation of GO-Au-PNM/Curc adducts and photothermally controlled drug release, triggered by red-light excitation (680 nm), were demonstrated using spectroscopic techniques. Drug-polymer interaction and drug-release mechanism were well supported by modelling simulation calculations. The cellular uptake of GO-Au-PNM/Curc was imaged by confocal laser scanning microscopy. In vitro experiments revealed the excellent biocompatibility of the GO-Au-PNM that did not affect the viability of human cells.


Assuntos
Curcumina , Grafite , Hipertermia Induzida , Nanopartículas Metálicas , Humanos , Polímeros/química , Ouro , Linhagem Celular Tumoral , Luz Vermelha , Liberação Controlada de Fármacos , Hipertermia Induzida/métodos , Curcumina/química
13.
Int J Biol Macromol ; 254(Pt 2): 127812, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-37923038

RESUMO

In the paper, Nisin was grafted onto native pectin by the 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC·HCl) method. Structure characterisation showed that the carboxyl group of pectin interacted with the amino group of Nisin and formed an amide bond. The highest grafting ratio of the modified pectin was up to 24.89 %. The emulsifying property of modified pectin, significantly improved, and emulsification performance improved with increasing grafting ratio. Emulsifying activity, emulsion stability, Zeta potential, and droplet morphology data demonstrate a notable enhancement in pectin's emulsifying properties due to Nisin's introduction, with the degree of grafting showing a direct correlation with the improvement observed. Pectin-based emulsion is utilized to load curcumin, enhancing its stability and bioavailability. Research findings highlight that the incorporation of Nisin-modified pectin significantly elevates curcumin encapsulation efficiency, while decelerating its release rate. Moreover, the stability of curcumin loaded in the modified pectin under light exposure, alkaline conditions, and long-term storage is also significantly improved. Ultimately, the bioavailability of curcumin escalates from 0.368 to 0.785.


Assuntos
Curcumina , Nisina , Emulsões/química , Curcumina/química , Nisina/química , Pectinas/química , Polímeros/química
14.
Eur J Pharm Biopharm ; 194: 62-73, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38042509

RESUMO

Recently, there has been an accelerating interest in novel biocompatible wound dressings made of nano-sized materials, especially nanofibers. Electrospun nanofibers provide high surface area and mimic the extracellular matrix which enhances biocompatibility. Besides, nanofibrous structures have high active ingredient loading capacity as a result of their high surface-to-volume ratio and porosity. In the present study, curcumin-loaded poly(ω-pentadecalactone-co-δ-valerolactone)/gelatin (PDL-VL/Gel) nanofibrous membranes were fabricated to be used for healing skin wounds. Poly(ω-pentadecalactone-co-δ-valerolactone) copolymer has been enzymatically synthesized in previous studies, thus it improves the originality of the membrane. It was aimed to obtain a synergetic effect and increase the novelty of the work by blending synthetic and natural polymers. Moreover, it was preferred to provide antibacterial activity by the incorporation of a herbal ingredient (curcumin) as a natural alternative to commercial antibiotics. Varied amounts of curcumin (5-25 %, w:v) were electrospun together with PDL-VL/Gel (equal volume ratio) polymer blend (fiber diameters ranged between 554 and 1074 nm) and several characterizations (morphological and molecular structure, wettability characteristics, and thermal behavior) were applied to examine the curcumin incorporation. Afterwards, in vitro curcumin release studies were carried out and mathematical modeling was applied to release data to clarify the transport mechanism. Curcumin release profiles comprised of an initial burst release in the first hour followed by a sustained release through 24 h. Based on the antibacterial activity test results, 15 % curcumin loading ratio was found to be sufficient for the treatment of skin wounds infected by Gram-negative (E. coli) and Gram-positive (S. aureus and B. subtilis) bacteria. Additionally, nanofibrous membranes did not lead to cytotoxicity, and curcumin content further enhanced the viability of fibroblasts. Thus, the presented antibacterial nanofibrous membrane is suggested to be applied for the treatment of wound infections and accelerating the healing process.


Assuntos
Curcumina , Nanofibras , Nanofibras/química , Gelatina/química , Staphylococcus aureus , Curcumina/farmacologia , Curcumina/química , Escherichia coli , Antibacterianos/química
15.
Int J Biol Macromol ; 257(Pt 1): 128603, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38056733

RESUMO

An intelligent and active food packaging film based on chitosan (CS), pectin (P), calcium propionate (CP), and curcumin-ß-cyclodextrin complex (Cur-ß-CD) was prepared. The CS/P/CP/Cur-ß-CD film exhibited improved hydrophobicity (74.78 ± 0.53°), water vapor (4.55 ± 0.16 × 10-11 g·(m·s·Pa)-1), and oxygen (1.50 ± 0.06 × 10-12 g·(m·s·Pa)-1) barrier properties, as well as antioxidant (72.34 ± 3.79 % for DPPH and 86.05 ± 0.14 % for ABTS) and antibacterial (79.41 ± 2.89 % for E. coli and 83.82 ± 3.96 % for S. aureus) activities. The release of CP and Cur could be triggered by pectinase, with their cumulative release reaching 92.62 ± 1.20 % and 42.24 ± 1.15 %, respectively. The CS/P/CP/Cur-ß-CD film showed delayed alterations in surface color, pH value, total volatile bases nitrogen, total viable counts, thiobarbituric acid reactive substance, hardness, and springiness of pork. Additionally, the fluorescence intensity of the film gradually decreased. In conclusion, we have developed a pH-responsive film with pectinase-triggered release function, providing a new concept for the design of multi-signal responsive intelligent food packaging.


Assuntos
Quitosana , Curcumina , Carne de Porco , Propionatos , Carne Vermelha , beta-Ciclodextrinas , Animais , Suínos , Curcumina/farmacologia , Curcumina/química , Pectinas , Poligalacturonase , Carne Vermelha/análise , Quitosana/química , Escherichia coli , Staphylococcus aureus , Fluorescência , Embalagem de Alimentos , beta-Ciclodextrinas/química , Concentração de Íons de Hidrogênio
16.
Int J Biol Macromol ; 255: 128235, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-37981268

RESUMO

Licorice was widely used in food and herbal medicine. In its extract industry, a substantial amount of licorice protein was produced and discarded as waste. Herein, we extracted Licorice Protein Isolate (LPI) and explored its potential as a curcumin nanocarrier. Using a pH-driven method, we fabricated LPI-curcumin nanoparticles with diameters ranging from 129.30 ± 3.21 nm to 75.03 ± 1.19 nm, depending on the LPI/curcumin molar ratio. The formation of LPI-curcumin nanoparticles was primarily driven by hydrophobic interactions, with curcumin entrapped in LPI being in an amorphous form. These nanoparticles significantly enhanced curcumin properties in terms of solubility, photochemical stability, and stability under varying pH, storage, and physiological conditions. Moreover, the loaded curcumin exhibited a 2.58-fold increase in cellular antioxidant activity on RAW 264.7 cells and a 1.86-fold increase in antitumor activity against HepG2 cells compared to its free form. These findings suggested that LPI could potentially serve as a promising novel delivery material.


Assuntos
Curcumina , Glycyrrhiza , Nanopartículas , Curcumina/farmacologia , Curcumina/química , Solubilidade , Antioxidantes/farmacologia , Antioxidantes/química , Nanopartículas/química , Tamanho da Partícula , Portadores de Fármacos/química
17.
Eur J Med Chem ; 265: 116070, 2024 Feb 05.
Artigo em Inglês | MEDLINE | ID: mdl-38134747

RESUMO

Alzheimer's disease (AD) is the most common neurodegenerative disease among the elderly. Contemporary treatments can only relieve symptoms but fail to delay disease progression. Curcumin is a naturally derived compound that has demonstrated significant therapeutic effects in AD treatment. Recently, molecular hybridization has been utilized to combine the pharmacophoric groups present in curcumin with those of other AD drugs, resulting in a series of novel compounds that enhance the therapeutic efficacy through multiple mechanisms. In this review, we firstly provide a concise summary of various pathogenetic hypotheses of AD and the mechanism of action of curcumin in AD, as well as the concept of molecular hybridization. Subsequently, we focus on the recent development of hybrid molecules derived from curcumin, summarizing their structures and pharmacological activities, including cholinesterase inhibitory activity, Aß aggregation inhibitory activity, antioxidant activity, and other activities. The structure-activity relationships were further discussed.


Assuntos
Doença de Alzheimer , Curcumina , Doenças Neurodegenerativas , Humanos , Idoso , Doença de Alzheimer/tratamento farmacológico , Curcumina/farmacologia , Curcumina/uso terapêutico , Curcumina/química , Doenças Neurodegenerativas/tratamento farmacológico , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Relação Estrutura-Atividade , Peptídeos beta-Amiloides
18.
Biomed Pharmacother ; 170: 116034, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38141282

RESUMO

The curry powder spices turmeric (Curcuma longa L.), which contains curcumin (diferuloylmethane), an orange-yellow chemical. Polyphenols are the most commonly used sources of curcumin. It combats oxidative stress and inflammation in diseases, such as hyperlipidemia, metabolic syndrome, arthritis, and depression. Most of these benefits are due to their anti-inflammatory and antioxidant properties. Curcumin consumption leads to decreased bioavailability, resulting in limited absorption, quick metabolism, and quick excretion, which hinders health improvement. Numerous factors can increase its bioavailability. Piperine enhances bioavailability when combined with curcumin in a complex. When combined with other enhancing agents, curcumin has a wide spectrum of health benefits. This review evaluates the therapeutic potential of curcumin with a specific emphasis on its approach based on molecular signaling pathways. This study investigated its influence on the progression of cancer, inflammation, and many health-related mechanisms, such as cell proliferation, apoptosis, and metastasis. Curcumin has a significant potential for the prevention and treatment of various diseases. Curcumin modulates several biochemical pathways and targets involved in cancer growth. Despite its limited tissue accumulation and bioavailability when administered orally, curcumin has proven useful. This review provides an in-depth analysis of curcumin's therapeutic applications, its molecular signaling pathway-based approach, and its potential for precision medicine in cancer and human health.


Assuntos
Curcumina , Neoplasias , Humanos , Curcumina/farmacologia , Curcumina/uso terapêutico , Curcumina/química , Neoplasias/tratamento farmacológico , Anti-Inflamatórios/uso terapêutico , Transdução de Sinais , Inflamação/tratamento farmacológico
19.
Int J Biol Macromol ; 259(Pt 1): 128875, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38154719

RESUMO

The utilization of biocompatible drug delivery systems with extended drug release capabilities is highly advantageous in cancer therapy, as they can mitigate adverse effects. To establish such a biocompatible system with prolonged drug release behavior, researchers developed an innovative drug carrier. In this study, a sustainable approach was employed to synthesize a new zinc-based metal-organic framework (Zn-MOF) through the reaction between synthesized Schiff base ligands and zinc ions. Comprehensive analyses, including FT-IR, XRD, SEM, BET surface area, and TGA techniques, were employed to thoroughly characterize the frameworks. Following comprehensive characterization, curcumin (CUR) was loaded onto the Zn-MOF, resulting in CUR entrapment efficiency and loading capacity of 79.23 % and 26.11 %, respectively. In vitro evaluations of CUR release from CUR@MOF exhibited controlled release patterns, releasing 78.9 % and 50.0 % of CUR at pH 5.0 and pH 7.4, respectively. To mitigate initial burst release, a coating of the biopolymer sodium alginate (SA) was applied to CUR@Zn-MOF. In vitro CUR release tests indicated that SA/CUR@Zn-MOF outperformed pristine CUR@Zn-MOF. The release of CUR conformed to the Korsmeyer-Peppas model, displaying non-Fickian diffusion. Furthermore, an in vitro cytotoxicity study clearly demonstrated the potent anti-tumor activity of the synthesized CUR@Zn-MOF attributed to its controlled release of CUR. This led to the induction of apoptotic effects and cell death across HeLa, HEK293, and SH-SY5Y cell lines. These findings strongly suggest that the developed pH-sensitive carriers hold remarkable potential as targeted vehicles for drug delivery in cancer therapy.


Assuntos
Curcumina , Estruturas Metalorgânicas , Neuroblastoma , Humanos , Curcumina/química , Estruturas Metalorgânicas/química , Preparações de Ação Retardada , Alginatos , Células HEK293 , Espectroscopia de Infravermelho com Transformada de Fourier , Neuroblastoma/tratamento farmacológico , Sistemas de Liberação de Medicamentos , Portadores de Fármacos/química , Zinco , Liberação Controlada de Fármacos
20.
Assay Drug Dev Technol ; 22(1): 18-27, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38150563

RESUMO

This study aimed at enhancing the efficacy of curcumin (CR) by formulating and coating it with chitosan. In silico molecular docking studies revealed that CR exhibited almost similar and low binding energies when compared to artemisinin, indicating high stability at the target site. It can be confirmed that CR is effective in treating and reducing Plasmodium falciparum parasites. Fourier transform infrared studies confirmed that there was a shift and disappearance of some drug peaks in the formulation which revealed complexation with phospholipids. The F2EXT3-developed formulation exhibited greater solubility (24.31 ± 3.47 µg/mL) when compared to pure CR (7.99 ± 1.95 µg/mL). Proton nuclear magnetic resonance studies confirmed the formation of Curcumin-phospholipid hydrogen bonding in F2EXT3. The in vitro drug release studies revealed that the developed formulation F2EXT3 exhibited better drug release at 71.98% at 48 h; this might be due to the effective entrapment efficiency of the drug inside the phospholipid, presence of polyethylene glycol 4000 and chitosan further assisted in sustained release of the drug. Scanning electron microscopy studies revealed that optimized F2EXT3 CR nanophytosomes were nearly spherical with narrow size distribution and smooth surface. The zeta potential of the F2EXT3 showed -3.5 mV. Stability studies revealed that the formulation remained stable even after 6 months. It was observed from the hemin assay that CR and F2EXT3 exhibited (50 µg/mL curcumin) exhibited IC50 values of 47 ± 2.45 and 22 ± 1.58 µM, respectively. Further in vivo antimalarial activity on resistant and sensitive strains needs to be performed to evaluate the efficacy of the developed formulation.


Assuntos
Quitosana , Curcumina , Malária , Humanos , Curcumina/farmacologia , Curcumina/química , Quitosana/química , Portadores de Fármacos/química , Simulação de Acoplamento Molecular , Fosfolipídeos
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