Cur Release Research Articles

Curcumin-loaded zein nanoparticles: A quality by design approach for enhanced drug delivery and cytotoxicity against cancer cells

Zein, a maize protein, has been explored for constructing potential biomaterial due to its hydrophobic nature, self-assembly capability, and biocompatibility. In its nanoparticulate form, zein is a promising material for drug delivery applications, particularly in cancer treatment. Despite the importance of colloidal stability for effective drug delivery, systematic studies investigating the effect of various surface modifying agents (MAs) on the zein nanoparticles (ZNPs)-based formulations are limited. This study employs quality-by-design (QbD) approach to optimize curcumin-loaded ZNPs, enhancing colloidal stability, size, and drug-encapsulation efficiency using different MAs for potential cancer therapy. Gum arabic (GA) emerged as the optimal stabilizer, with GA-stabilized curcumin-loaded ZNPs (GA-Cur-ZNPs) achieving a particle size of 184.8 ± 2.85 nm, zeta potential of −23.4 ± 0.56 mV and 87.1 ±1.55 % drug encapsulation efficiency, along with excellent colloidal stability over two months. The optimal formulation also demonstrated sustained release of Cur over 72 h. GA-Cur-ZNPs demonstrated lower IC50 values and higher anti-proliferative effects on three different cancer cell lines compared to the free drug, while also exhibiting superior intracellular uptake. With negligible toxicity to human dermal fibroblast cells, the optimized Cur-GA-ZNPs show promise for safe and effective killing of cancer cells.

Release kinetics and protective effect of novel curcumin-based nanoliposome modified with pectin, whey protein isolates and hyaluronic acid against oxidative stress

In the present study, a novel nanoliposome loaded with Curcumin (Cur) (NNLs-Cur) was established to overcome the gastrointestinal digestive barrier and enhance mitochondrial targeting capacity, exerting the antioxidant capacity of Cur. Noteworthy, NNLs-Cur was modified by pectin, whey protein isolates and hyaluronic acid. The results showed that the structure of traditional nanoliposomes loaded with Cur (NLs-Cur) was destroyed during digestion. However, NNLs-Cur maintained intact structural morphology, and the release of Cur in the stomach and intestines was consistent with zero-order and first-order kinetic models, respectively. Interestingly, the survival rate of HL-7702 cells after being damaged by H2O2 was 40.53 %, while the survival rate after treated with NNLs-Cur reached 99.87 %. Besides, the fluorescence localization indicated Cur in NNLs-Cur could escape lysosomal and achieve mitochondria targeting. Compared with NLs-Cur, the damaged cells treated with NNLs-Cur increased activities of catalase (CAT), glutathione peroxide (GSH-Px) and superoxide dismutase (SOD) from 16.16 ± 0.52, 16.92 ± 2.28 and 30.10 ± 0.93 U/mgprot to 19.09 ± 0.52, 20.41 ± 1.79 and 33.81 ± 0.29 U/mgprot, respectively. Malondialdehyde (MDA) content and reactive oxygen species (ROS) level of the oxidative damaged cells were reduced, mitochondrial membrane potential was restored, and cell apoptosis was reduced. This study provides theoretical guidance for realizing the industrial application of efficient targeted delivery Cur.

Novel amphiphilic rhamnogalacturonnan I‐based nanomicelles for targeted delivery of curcumin to hepatocellular carcinoma cells

AbstractCurcumin (Cur) is a bioactive nutraceutical with great potential in biological, nutritional, and medical applications. However, these applications are limited by various factors such as insufficient ingestion, low aqueous solubility, and relatively high toxicity to normal cells. To tackle these obstacles, we synthesized a novel Cur‐modified‐rhamnogalacturonan (RG‐C) nano‐micelle carrier to target‐deliver Cur to hepatocellular carcinoma HepG2 cells via specific recognition of RG‐I by the overexpressed surface galactin‐3 receptor. Fourier transfer infrared, UV–vis, and 1H NMR analyses confirmed the conjugation between RG and Cur RG‐C loaded with Cur (RG‐CC) was formed via self‐assembly in an aqueous solution with a drug loading efficiency of 12.2%. RG‐CC micelle was ellipsoidal or cubic with a size ranging between 100 and 200 nm by scanning electron microscopy observation. Cur release from RG‐CC exhibited a controlled and pH‐dependent manner with 50% at pH 5.0 in contrast to 5% at pH 7.4 after 24 h exposure. RG‐CC possessed more potent anti‐proliferative activity against HepG2 cells than normal embryonic kidney 293T cells. Compared to free Cur, both the anti‐proliferative effect and uptake of RG‐CC were significantly higher in HepG2 cells as revealed from laser confocal microscopy and flow cytometry analyses. RG‐CC was a promising anticancer candidate and deserves further preclinical and clinical investigations.

Development of dual drug loaded-hydrogel scaffold combining microfluidics and coaxial 3D-printing for intravitreal implantation

Treating diabetic retinopathy (DR) effectively is challenging, aiming for high efficacy with minimal discomfort. While intravitreal injection is the current standard, it has several disadvantages. Implantable systems offer an alternative, less invasive, with long-lasting effects drug delivery system (DDS). The current study aims to develop a soft, minimally invasive, biodegradable, and bioadhesive material-based hydrogel scaffold to prevent common issues with implants. A grid-shaped scaffold was created using coaxial 3D printing (3DP) to extrude two bioinks in a single filament. The scaffold comprises an inner core of curcumin-loaded liposomes (CUR-LPs) that prepared by microfluidics (MFs) embedded in a hydrogel of hydroxyethyl cellulose (HEC), and an outer layer of hyaluronic acid-chitosan matrix with free resveratrol (RSV), delivering two Sirt1 agonists synergistically activating Sirt1 downregulated in DR. Optimized liposomes, prepared via MFs, exhibit suitable properties for retinal delivery in terms of size (<200 nm), polydispersity index (PDI) (<0.3), neutral zeta potential (ZP), encapsulation efficiency (∼97 %), and stability up to 4 weeks. Mechanical studies confirm scaffold elasticity for easy implantation. The release profiles show sustained release of both molecules, with different patterns related to different localization of the molecules. RSV released initially after 30 min with a total release more than 90 % at 336 h. CUR release starts after 24 h with only 4.78 % of CUR released before and gradually released thanks to its internal localization in the scaffold. Liposomes and hydrogels can generate dual drug-loaded 3D structures with sustained release. Microscopic analysis confirms optimal distribution of liposomes within the hydrogel scaffold. The latter resulted compatible in vitro with human retinal microvascular endothelial cells up to 72 h of exposition. The hydrogel scaffold, composed of hyaluronic acid and chitosan, shows promise for prolonged treatment and minimally invasive surgery.

Biocompatible PAMAM-PLGA-PCL Nanocarrier for Efficient Curcumin Delivery to Lung Cancer Cells: In Vitro Studies.

Lung cancer, as the leading cause of death among other types of cancer, has a high rate of incidence throughout the world. Although conventional modalities, like chemotherapy, have been applied for the inhibition of this cancer, they have not led to the suppression of lung cancer owing to their deficiencies. Thus, we developed a novel polylactic-co-glycolic acid (PLGA)-polyamidoamine G4 (PAMAM G4)-polycaprolactone (PCL) nanocarrier for efficient delivery of curcumin (Cur) to A549 lung cancer cells. The synthesized nanocarrier was characterized by applying analytical techniques, FT-IR, DLS, TEM, and TGA. Successful synthesis, nano-size diameter (40-80 nm), near neutral surface charge (8.0 mV), and high drug entrapment (11.5 %) were measured for the nanocarrier. Controlled (about 5 folds within first 2 h) and pH-sensitive (2-3 folds faster within first hours) Cur release observed for PLGA-PAMAM-PCL-Cur. Cell viability test (MTT assay) indicated the high capability of nanocarrier in suppression of A549 cancer cells (21 % viability after 24 h of treatment with 200 nM) while did not result in toxicity on MSC normal cells. The IC50 observed for 50 nM at 24 h of post-treatment in A549 cells. The qRT-PCR technique indicated inducing the expression of apoptotic genes (Caspase9 and Bax) by 6-8 folds and suppressing anti-apoptotic gene (Bcl2) by 7 folds. ROS considerably increased in cancer cells as well. This nanocarrier would be a promising drug delivery system against lung cancer.

Bioconjugated clicked chitosan/alginate nanocarriers with trastuzumab: Unlocking curcumin's potential in targeting breast cancer

Curcumin (Cur) has shown potential anticancer effects against various cancers, including colorectal and breast cancers. The aim of this study was to develop nanocarriers (NCs) bioconjugated with trastuzumab (Tras) using click reactions. Chitosan-maleimide (CHI-Mal) and thiolated alginate (SH-ALG) were synthesized to prepare CS-Mal/SH-ALG NCs, which were then conjugated with Tras as a receptor-targeting ligand via click chemistry. The characteristics of the NCs, including Cur loading and release profiles, were examined. Biocompatibility, anticancer effects, targetability, and cell death analysis were conducted on HER2-positive breast cancer cell line (SK-BR-3). The developed NCs exhibited a nano-scaled size, relatively spherical shape, and positive surface charge. The 7-day release of Cur from the Cur-loaded CHI-Mal/SH-ALG NCs (Cur-NCs) was significantly higher in the cancer environment (pH 5.5; 98%) compared to body fluid (pH 7.4; 57%). Tras-conjugated Cur-NCs (Tras-Cur-NCs) demonstrated superior anticancer effects, receptor-targeting efficiency, and cellular uptake compared to free Cur and non-targeted Cur-NCs. Additionally, Tras-Cur-NCs enhanced apoptotic cell death, indicating a non-inflammatory cell death with strong anticancer effect against HER2-positive SK-BR-3 cells. The spontaneous click reaction successfully formed pH-responsive Tras-conjugated NCs for targeted Cur delivery to HER2-positive breast cancer cells.

Development and characterization of polyvinyl alcohol/chitosan crosslinked malic acid composite films with curcumin encapsulated in β-cyclodextrin for food packaging application

Considering that fruits are vulnerable to damage and waste during stockpiling, transport and marketing. Given this, an innovative curcumin inclusion compound (Cur@β-CD) was devised in this study to introduce oil-soluble curcumin (Cur) into water-soluble polyvinyl alcohol (PVA) materials, thereby fabricating food packaging films endowed with excellent properties. DPPH test manifested that the oxidation resistance for PCOMC-Cur@β-CD film was 95 % above PVA material. It was ascribed to the fact that the Cur@β-CD elevated the water solubility of Cur while the increase of water solubility heightened the antioxidant effect for Cur in the film. Additionally, the chitosan (CS) was crosslinked with malic acid (MA), which elevated the barrier property of the film, reduced the amount of oxygen transmission and further retarded the oxidation reaction of the fruits for packaging. The antibacterial test demonstrated that the antibacterial rates of PCOMC-Cur@β-CD film against E. coli and S. aureus reached 92 % and 95 %, respectively, which was attributed to the slow release of Cur when Cur@β-CD was dissolved in PVA material and the Schiff base reaction between Cur and amino groups on CS. These findings indicate that the PCOMC-Cur@β-CD film developed in this work can provide certain insights into the field of food packaging.

Core-shell structured nanomembrane with sequential immune and vascular isolation effects followed by chondrogenic induction to promote stable stem cell-based subcutaneous cartilage regeneration in large animals

Bone marrow stem cell (BMSC)-regenerated cartilage (BRC) shows promising prospects for clinically repairing cartilage defects. However, when subcutaneously implanted into immunocompetent large animals, BRC is prone to ossification due to vascular invasion and inflammatory infiltration, compromising its chondrogenic stability. To address this challenge, we developed a core–shell structured KGN/Gel@Cur/PLCL nanomembrane using coaxial electrospinning technology to enhance the chondrogenic stability of BRC in subcutaneous niche. The shell layer comprises curcumin (Cur), known for its potent immunomodulatory and anti-angiogenic effects, and poly(L-lactide-co-caprolactone) (PLCL). The core layer comprises Kartogenin (KGN), a recognized chondrogenic inducer, and gelatin (Gel). This nanomembrane encapsulated BRCs induced from goat BMSCs in vitro and was subcutaneously implanted into autologous goats. The nanomembrane’s physical barrier and Cur release from the shell layer prevented vascular invasion and inflammatory infiltration. Additionally, KGN release from the core layer maintained the BRC’s chondrogenic phenotype and promoted cartilage maturation. These combined mechanisms significantly inhibited BRC ossification and preserved its chondrogenic stability. chondrogenic phenotype and promoted cartilage maturation. These combined mechanisms significantly inhibited BRC ossification and maintained its chondrogenic stability. Overall, this study highlights the effectiveness of the core–shell structured KGN/Gel@Cur/PLCL nanomembrane in providing sequential immune and vascular isolation, followed with chondrogenic induction, to prevent BRC ossification and preserve the chondrogenic stability of subcutaneously implanted BRC in large animal. This is crucial for the clinical translation of stem cell therapy into subcutaneous cartilage repair.

In Vitro and In Vivo Evaluation of Electrospun PVA Nanofiber Containing ZnO/Curcumin for Wound Healing Application.

The development of biocompatible wound dressings containing therapeutic agents to accelerate wound healing is an interesting field of study in biomedical sciences. Polyvinyl alcohol (PVA) nanofibers were loaded with zinc oxide nanoparticles (ZnO NPs) and curcumin (Cur) through electrospinning. Thedressings were characterized by SEM and XRD and FTIR. The antioxidant, antibacterial, and cytotoxic activities Cur/ZnO/PVA nanodressing were evaluated using DPPH radical scavenging assay, disc diffusion method, and MTT assay, respectively. Cur/ZnO/PVA nanodressing showed sustained Cur release about 19.7% and 61.1% after 8h and 168h, respectively. Cur/ZnO NPs/PVA mixture had higher antioxidant potential than PVA, ZnO NPs, and Cur. The dressing showed a good antibacterial effect. The in vivo wound healing effect of different types of prepared dressings, includingPVA, Cur/PVA,Cur/ZnO/PVA, and ZnO/PVAnanofibers, was also investigated. PVA dressing containing Cur/ZnO NPs resulted in the highestincrease of wound contraction in rats. The assembly of Cur and ZnO NPs on PVA nanofibers could propose as an effective delivery method toimprovethe wound healing process. The investigated wound dressing could be commercialized and used on a large scale after proper further studies, including clinical trials.

Chondroitin sulfate-tocopherol succinate modified exosomes for targeted drug delivery to CD44-positive cancer cells

Exosomes (Exos), natural nanovesicles released by various cell types, show potential as an effective drug delivery platform due to their intrinsic role as transporters of biomolecules between different cells. However, Exos functionalization with targeting ligands is a critical step to enhance their targeting capability, which could be challenging. In this study, Exos were modified to specifically bind to CD44-positive cells by anchoring chondroitin sulfate (CS) to their surface. Exo modification was facilitated with CS conjugation with alpha-tocopherol succinate (TOS) as an anchorage. The modified Exos were utilized for delivering curcumin (Cur) to pancreatic cancer (PC) cells. In vitro Cur release studies revealed that Exos play a crucial role in maintaining Cur within themselves, demonstrating their potential as effective carriers for drug delivery to targeted locations. Notably, Cur loaded into the modified Exos exhibited enhanced cytotoxicity compared to unmodified Exo-Cur. Meanwhile, Exo-Cur-TOS-CS induced apoptosis more effectively in AsPC-1 cells than unmodified Exos (70.2 % versus 56.9 %). It is worth mentioning that with CD44-mediated cancer-specific targeting, Exo-CS enabled increased intracellular accumulation in AsPC-1 cells, showing promise as a targeted platform for cancer therapy. These results confirm that Exo modification has a positive impact on enhancing the therapeutic efficacy and cytotoxicity of drugs.

Targeted nanoparticles triggered by plaque microenvironment for atherosclerosis treatment through cascade effects of reactive oxygen species scavenging and anti-inflammation

Inflammatory factors and reactive oxygen species (ROS) are risk factors for atherosclerosis. Many existing therapies use ROS-sensitive delivery systems to alleviate atherosclerosis, which achieved certain efficacy, but cannot eliminate excessive ROS. Moreover, the potential biological safety concerns of carrier materials through chemical synthesis cannot be ignored. Herein, an amphiphilic low molecular weight heparin- lipoic acid conjugate (LMWH-LA) was used as a ROS-sensitive carrier material, which consisted of injectable drug molecules used clinically, avoiding unknown side effects. LMWH-LA and curcumin (Cur) self-assembled to form LLC nanoparticles (LLC NPs) with LMWH as shell and LA/Cur as core, in which LMWH could target P-selectin on plaque endothelial cells and competitively block the migration of monocytes to endothelial cells to inhibit the origin of ROS and inflammatory factors, and LA could be oxidized to trigger hydrophilic-hydrophobic transformation and accelerate the release of Cur. Cur released within plaques further exerted anti-inflammatory and antioxidant effects, thereby suppressing ROS and inflammatory factors. We used ultrasound imaging, pathology and serum analysis to evaluate the therapeutic effect of nanoparticles on atherosclerotic plaques in apoe−/− mice, and the results showed that LLC showed significant anti-atherosclerotic effects. Our finding provided a promising therapeutic nanomedicine for the treatment of atherosclerosis.

Gelatin-nanocellulose stabilized emulsion-filled hydrogel beads loaded with curcumin: Preparation, encapsulation and release behavior

In this study, the curcumin was firstly encapsulated in gelatin (GLT) and/or cellulose nanocrystals (CNC) stabilized emulsions, then further mixed with sodium alginate (SA) to form emulsion-filled hydrogel beads loaded with curcumin (Cur). The Cur-loaded emulsions showed a droplet size of 20.3–24.4 μm with a uniform distribution. Introducing CNC and/or SA increased the viscosity of emulsions accompanied by viscoelastic transition, while the modulus was reduced due to destruction of GLT gel. Cur was doubly immobilized in the hydrogel beads with >90 % of encapsulation efficiency. The results of simulated gastrointestinal tract experiments revealed that the beads possessed a good pH sensitivity and controlled release behavior to prolong the retention of Cur in the gastrointestinal tract. After 6 h of UV irradiation, the Cur-loaded emulsion-filled hydrogel beads showed a higher antioxidant activity than that of pure Cur, effectively delaying the photodegradation of Cur. In addition, the beads had better stability in aqueous and acidic environments, which was favorable for prolonging the release of Cur. These results suggest that the emulsion-filled hydrogel beads have great potential for the delivery of lipophilic bioactive molecules.

New Chitosan-Based Co-Delivery Nanosystem for Diabetes Mellitus Therapy.

Type 2 diabetes mellitus (T2DM) is one of the most common metabolic disorders, with a major involvement of oxidative stress in its onset and progression. Pioglitazone (Pio) is an antidiabetic drug that mainly works by reducing insulin resistance, while curcumin (Cur) is a powerful antioxidant with an important hypoglycemic effect. Both drugs are associated with several drawbacks, such as reduced bioavailability and a short half-life time (Pio), as well as instability and poor water solubility (Cur), which limit their therapeutic use. In order to overcome these disadvantages, new co-delivery (Pio and Cur) chitosan-based nanoparticles (CS-Pio-Cur NPs) were developed and compared with simple NPs (CS-Pio/CS-Cur NPs). The NPs were characterized using dynamic light scattering (DLS), transmission electron microscopy (TEM), X-ray diffraction (XRD), and Fourier-transform infrared spectroscopy (FTIR). In addition, the entrapment efficiency (EE) and loading capacity (LC), as well as the release profile, of the APIs (Pio and Cur) from the CS-APIs NPs in simulated fluids (SGF, SIF, and SCF) were also assessed. All the CS-APIs NPs presented a small particle size (PS) (211.6-337.4 nm), a proper polydispersity index (PI) (0.104 and 0.289), and a positive zeta potential (ZP) (21.83 mV-32.64 mV). Based on the TEM results, an amorphous state could be attributed to the CA-APIs NPs, and the TEM analysis showed a spherical shape with a nanometric size for the CS-Pio-Cur NPs. The FT-IR spectroscopy supported the successful loading of the APIs into the CS matrix and proved some interactions between the APIs and CS. The CS-Pio-Cur NPs presented increased or similar EE (85.76% ± 4.89 for Cur; 92.16% ± 3.79 for Pio) and LC% (23.40% ± 1.62 for Cur; 10.14% ± 0.98 for Pio) values in comparison with simple NPs, CS-Cur NPs (EE = 82.46% ± 1.74; LC = 22.31% ± 0.94), and CS-Pio NPs (EE = 93.67% ± 0.89; LC = 11.24% ± 0.17), respectively. Finally, based on the release profile results, it can be appreciated that the developed co-delivery nanosystem, CS-Pio-Cur NPs, assures a controlled and prolonged release of Pio and Cur from the polymer matrix along the GI tract.

Extracellular matrix coated three-dimensional-printed polycaprolactone scaffolds containing curcumin for cartilage tissue engineering applications

Extracellular matrix (ECM) is widely used for clinical purposes in tissue engineering (TE). Since ECM does not have favorable mechanical properties, its use has been limited. Therefore, it is helpful to use synthetic polymers such as polycaprolactone (PCL) to improve the mechanical properties of ECM-based scaffolds. PCL scaffolds were prepared via the three-dimensional (3D) printing method. Cartilaginous ECM was obtained from bovine femur, and then it was decellularized and solubilized. PCL scaffolds were functionalized using 1,6-hexanediamine; consequently, the scaffolds were coated with solubilized decellularized ECM (SDECM) using two types of crosslinkers; namely, N-(3-dimethylaminopropyl)-N-ethylcarbodiimide hydrochloride/N-hydroxysuccinimide (EDC/NHS) and genipin. Genipin-crosslinked SDECM-coated (PCL/ECM-Gen) scaffolds and EDC/NHS-crosslinked SDECM-coated (PCL/ECM-EN) scaffolds were characterized by different tests. Following loading the curcumin (Cur) on the scaffolds, the Cur release rate was investigated. Finally, human chondrocyte cells were cultured on the scaffolds to explore cell viability, cell attachment, and histological studies. Following functionalization via amine groups, 5% SDECM was used to coat the scaffolds, and this increased the wettability and cell viability of the PCL. Genipin crosslinked and coated the SDECM more efficiently compared to the EDC/NHS and led to lower porosity, water absorption capacity, degradation rate, higher cell proliferation, and cell attachment. Genipin-crosslinked Cur-loaded (PCL/ECM-Gen + Cur) scaffolds showed higher cell viability but lower antibacterial activity compared to EDC/NHS-crosslinked Cur-loaded (PCL/ECM-EN + Cur) scaffolds, which may indicate EDC/NHS-induced cytotoxicity. This study elucidates the value of PCL/ECM-Gen + Cur scaffolds as highly biocompatible scaffolds that can be considered a promising tool for cartilage TE applications.

Time-programmed release of curcumin and Zn2+ from multi-layered RSF coating modified PET graft for improvement of graft-host integration

Artificial graft serves as the primary grafts used in the clinical management of sports-related injuries. Until now, optimizing its graft-host integration remains a great challenge due to the excessive inflammatory response during the inflammatory phase, coupled with an absence of tissue-inductive capacity during the regeneration phase. Here, a multi-layered regenerated silk fibroin (RSF) coating loaded with curcumin (Cur) and Zn2+ on the surface of the PET grafts (Cur@Zn2+@PET) was designed and fabricated for providing time-matched regulation specifically tailored to address issues arising at both inflammatory and regeneration phases, respectively. The release of Cur and Zn2+ from the Cur@Zn2+@PET followed a time-programmed pattern in vitro. Specifically, cellular assays revealed that Cur@Zn2+@PET initially released Cur during the inflammatory phase, thereby markedly inhibit the expression of inflammatory cytokines TNF-a and IL-1β. Meanwhile, a significant release of Zn2+ was major part during the regeneration phase, serving to induce the osteogenic differentiation of rBMSC. Furthermore, rat model of anterior cruciate ligament reconstruction (ACLR) showed that through time-programmed drug release, Cur@Zn2+@PET could suppress the formation of fibrous interface (FI) caused by inflammatory response, combined with significant new bone (NB) formation during regeneration phase. Consequently, the implementation of the Cur@Zn2+@PET characterized by its time-programmed release patterns hold considerable promise for improving graft-host integration for sports-related injuries.

PH-responsive Aminated mesoporous silica microspheres modified with soybean hull polysaccharides for curcumin encapsulation and controlled release

Mesoporous silica microspheres (MSMs) possess poor biocompatibility. This study focuses on integrating MSMs with polymers to obtain hybrid materials with superior performance compared to the individual components and responsive release in specific environments. The synthesized MSMs were aminated, and subsequently, soybean hull polysaccharide (SHPs) was modified onto MSMs-NH2 to produce MSMs-NH2@SHPs nanoparticles. The encapsulation rate, loading rate of curcumin (Cur), and in vitro release behavior were investigated. Results indicated that the encapsulation efficiency of Cur by MSMs-NH2@SHPs nanoparticles reached 75.58%, 6.95 times that of MSMs-NH2 with a load capacity of 35.12%. It is noteworthy that these nanoparticles exhibit pH-responsive release capacity in vitro. The cumulative release rate of the three nanoparticles at pH 5.0 was higher than that at pH 7.4. MSMs-NH2@SHPs had a cumulative release rate of 56.55% at pH 7.4, increasing to 76.21% at pH 5.0. In vitro experiments have shown that MSMs-based nanoparticles have high delivery efficiency and can achieve pH-sensitive drug release, with a high release rate in a slightly acidic acid, highlighting the potential for controlled release of Cur.

Chitosan based niosomal hydrogel with polyethylene glycol and halloysite nanotubes for curcumin delivery

The use of curcumin (Cur) as an anticancer drug is restricted due to its poor solubility and bioavailability. In this study, a pH-sensitive niosomal hydrogel composed of halloysite nanotubes (HNTs), polyethylene glycol (PEG), and chitosan (Cs) was developed for Cur delivery. Fourier transform infrared (FT-IR) spectroscopy and X-ray diffraction (XRD) analyses confirmed the successful synthesis of the nanocomposite and provided insights into the interactions between its components and its crystalline structure. Zeta potential analysis corroborated its colloidal stability, and scanning electron microscopy (SEM) images revealed its spherical shape and size in the range of 514–554 nm. The homogeneous size distribution was corroborated by dynamic light scattering (DLS) experiments. Cs/PEG/HNTs nanocarrier showed high Cur loading and encapsulation efficiencies (44.2 % and 84.0 %, respectively), as well as a smart, pH-sensitive release mechanism over a 96-hour period, highlighting its potential for sustained and targeted drug delivery. Cur release data were well-fitted to the Korsmeyer-Peppas and Zero-Order models at pH 5.4 and 7.4, respectively. The reduced survival of U-87 MG human brain tumor cells in the presence of Cs/PEG/HNTs@Cur samples compared to Cs, Cs/PEG, Cs/PEG/HNTs, and free Cur corroborates the hydrogel anti-cancer properties. The percentage of late apoptotic cells in Cs/PEG/HNTs@Cur was higher than in Cs/PEG/HNTs and free Cur, which is attributed to the sustained and smart release of Cur from Cs/PEG/HNTs@Cur. The biocompatibility, stability, biodegradability, ability to effectively encapsulate Cur and regulate its release to specifically target tumors makes the designed hydrogel a highly versatile and promising nanocarrier for Cur-based cancer therapies.

Preparation and application of curcumin loaded with citric acid crosslinked chitosan-gelatin hydrogels

While oral administration offers safety benefits, its therapeutic efficacy is hindered by various physiological factors within the body. In this study, a novel approach was explored using a matrix consisting of 2 % chitosan and 2 % gelatin, with citric acid (CA) serving as a green cross-linking agent (ranging from 0.4 % to 1.0 %), and curcumin (Cur) as the model drug to formulate hydrogel carriers. The results showed that a 0.4 % CA concentration, the hydrogel (CGA0.4) reached swelling equilibrium in deionized water within 40 min, exhibiting a maximum swelling index was 539 g/g. The addition of Cur to the CGA hydrogel (CGACur) notably enhanced release efficiency, particularly in simulated intestinal fluid, where Cur release rates exceeded 40 % within 100 min compared to below 8 % in other solutions. Among these hydrogels, CGA0.4Cur exhibited the fastest degradation rate in the combined solution, reaching >90 % degradation after 7 days. Additionally, Cur and CA demonstrated positive effects on the tensile strength, antioxidant activity and antibacterial activity of hydrogels. Compare to the bioaccessibility of CGC (27 %), those of CGACur had increased to over 34 %. These findings offer provide theoretical support for CA-crosslinked chitosan/gelatin gels in delivering hydrophobic bioactive molecules and their application in intestinal drug delivery system.

DESIGN OF JACKFRUIT GUM-BASED GENIPIN CROSSLINKED NANOPARTICLES FOR SUSTAINED RELEASE OF CURCUMIN: OPTIMIZATION AND IN VITRO CHARACTERIZATION

The present work aims to design jackfruit gum-based curcumin-loaded nanoparticles (CUR-NPs) for improved drug entrapment and modified release of CUR using ionotropic gelation. Briefly, the optimization of CUR-NPs was confirmed using a 32 response surface methodology. The diffractogram and thermogram of CUR-NPs confirmed reduction of crystallinity of CUR (optimized batch: F5) due to jackfruit gum and genipin cross-linked polymeric network. The particle size and zeta potential analysis confirmed formation of nanosized and stable CUR-NPs, respectively. Also, the nanoparticles demonstrated 83.99 ± 1.23% entrapment efficiency, whereas they showed 98.36 ± 0.96% of CUR release within 12 h at pH 7.4. The CUR-NPs exhibited good mucoadhesive properties due to the presence of jackfruit gum. Finally, the MTT assay showed a decrease in colorectal cancer cell viability due to tailored CUR release from CUR-NPs. In conclusion, jackfruit gum-genipin-based CUR-NPs offered high entrapment efficiency, tailored releases of CUR, good mucoadhesive property and improved anticancer activity.

Construction, characterization and bioactivity evaluation of curcumin nanocrystals with extremely high solubility and dispersion prepared by ultrasound-assisted method

Curcumin (Cur) as a natural pigment and biological component, can be widely used in food and beverages. However, the water insolubility of Cur significantly limits its applications. In this study, we prepared a series of nanocrystals via ultrasound-assisted method to improve the solubility and availability of Cur. The results showed artemisia sphaerocephala krasch polysaccharide (ASKP), gum arabic (GA) and wheat protein (WP) were outstanding stabilizers for nanocryatals except traditional agent, poloxamer 188 (F68). The obtained curcumin nanocrystals (Cur-NC) displayed a rod-shaped, crystal- and nanosized structure, and extremely high loading capacity (more over 80 %, w/w). Compared with raw powder, Cur-NC greatly improved the water solubility and dispersibility, and the slow and complete release of Cur of Cur-NC also endowed them excellent antioxidant capacities even at 10 μg/mL. Importantly, as functional factor additive in beverages (e.g. water and emulsion), Cur-NC could increase the content of Cur to at least 600 μg/mL and retain a good stability. Overall, we provided an effective improvement method for the liposoluble active molecules (e.g. Cur) based on the nanocrystals, which not only tremendously enhanced its water solubility, but also strengthened its bioactivity. Notably, our findings broadened the application of water-insoluble compounds.