Delivery Of Curcumin Research Articles

Preparation and Characterization of Novel Oleogels Using Jasmine Floral Wax and Wheat Germ Oil for Oral Delivery of Curcumin.

Oleogels (OGs) have gained a lot of interest as a delivery system for a variety of pharmaceuticals. The current study explains the development of jasmine floral wax (JFW) and wheat germ oil (WGO)-based OGs for oral drug (curcumin) delivery application. The OGs were made by dissolving JFW in WGO at 70 °C and cooling it to room temperature (25 °C). The critical gelation concentration of JFW that induces the gelation of WGO was found to be 10% (w/w). The OGs were characterized using various techniques such as Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), microscopic analysis, and mechanical test. XRD data indicated that JFW influences the crystallinity of the OGs. Among the prepared OGs, OG 17.5 showed higher crystallization in the series. Optical microscopic studies demonstrated the formation of fiber structures due to the entanglement of crystals whereas, polarized light micrographs suggested the formation of spherulites or clustered crystallite structures. The mechanical properties of the OGs increased linearly with the increase in the JFW concentration. Curcumin-loaded OGs were examined for their controlled release applications. In summary, the developed OGs were found to have the necessary features for modulating the oral delivery of curcumin.

Evaluation of quaternization effect on chitosan-HAP composite for bone tissue engineering application

This study attempts to improve the aqueous solubility of chitosan and utilizes it in the fabrication of composites with hydroxyapatite (HAP). The composites were evaluated as a curcumin delivery vehicle for bone regeneration. The chitosan was modified by quaternization, with a quaternization degree of 5 % for low quaternized chitosan (LQC) and 11 % for high quaternized chitosan (HQC). The modified chitosan, at alkaline pH 11, facilitated in situ HAP growth and formed LQC-HAP and HQC-HAP composites. The quaternization weakens intermolecular hydrogen bonds, facilitates interaction with the apatite precursor ions and promotes the growth of HAP. The modification significantly improved drug encapsulation (2.6 fold) but at the cost of a slight decrease in mechanical strength and increase in drug release. The in vitro studies with human osteoblast-like MG-63 cells established that the curcumin-loaded composites, LQC-HAP-C and HQC-HAP-C are biocompatible, encourage proliferation and promote a 2-fold increase in calcium mineralization over drug-free composites. The study exemplifies the reciprocity between quaternization degree and drug load/release properties and also illustrates that the magnitude of the latter reflects bioactivity. Thus, the quaternized chitosan-based HAP composite with tailorable bio-physicochemical properties becomes an interesting drug delivery system in bone regeneration.

Structural transitions in mixed Phosphatidylcholine/Pluronic micellar systems and their in vitro therapeutic evaluation for poorly water-soluble drug

The self-assemblies of phosphatidylcholine (PC) liposomes and Pluronic polymers with varying compositions have been studied. The micellar transition formed in the mixed PC and Pluronics (F127, P123, and mixed F127/P123) systems was investigated through dynamic light scattering (DLS), small-angle neutron scattering (SANS), rheology, and transmission electron microscopy (TEM) measurements.Results indicated that the PC appeared to be perfectly large bilayer vesicles. With an increasing concentration of Pluronics, the PC vesicle is also transformed intospherical micelles. The transitions from large lamellar vesicles to spherical micelles have been found with all the mixed systems, in which mixed F127/P123 performed better. The mixed PC/Pluronic micellar systems (PCFP) are being investigated for the problems associated with curcumin delivery, such as poor solubility and stability. The solubilization of curcumin in the PCFP systems has been examined and found to be better. The curcumin-loaded PCFP micellar system was synthesized through the thin-film method and evaluated in-vitro. Nuclear magnetic resonance(NMR) analysis indicated location of curcumin has found in the core of the PCFP micelles. The curcumin-loaded PCFP showed a slower and more sustained drug release under physiological conditions. The resistance to the oxidation of curcumin-loaded PCFP micelles is considerably higher than that of pure curcumin. Results also revealed that the curcumin-loaded PCFP effectively inhibits the cell proliferation of human breast adenocarcinoma cells (MCF-7) and induces cell death. This study suggests that the curcumin-loaded mixed PC/Pluronic micellar system enhances the bioavailability of curcumin.

Folic Acid-Conjugated Iron Oxide Magnetic Nanoparticles Based on Bovine Serum Albumin (BSA) for Targeted Delivery of Curcumin to Suppress Liver Cancer Cells

Folic Acid-Conjugated Iron Oxide Magnetic Nanoparticles Based on Bovine Serum Albumin (BSA) for Targeted Delivery of Curcumin to Suppress Liver Cancer Cells

Encapsulation of curcumin in gliadin-pectin in a core–shell nanostructure for efficient delivery of curcumin to cancer cells in vitro

Encapsulation of curcumin in gliadin-pectin in a core–shell nanostructure for efficient delivery of curcumin to cancer cells in vitro

Formation mechanism of binary complex based on β-lactoglobulin and propylene glycol alginate with different molecular weights: Structural characterization and delivery of curcumin.

The complexation of protein and polysaccharide has shown considerable potential for the encapsulation of functional food components. In this work, propylene glycol alginate (PGA) molecules with different molecular weights (100, 500, and 2,000 kDa) were prepared through H2O2 oxidation, which were further combined with β-lactoglobulin nanoparticles (β-lgNPs) to form PGA-β-lgNPs complexes for the delivery of curcumin (Cur). Results showed that the depolymerization of PGA molecule was resulted from the breakage of glycosidic bonds in the main chain, and the depolymerization rate of PGA molecule depended on the reaction time, temperature, solution pH and H2O2 concentration. As the increasing molecular weight of PGA, the particle size, zeta-potential and turbidity of the complexes were obviously increased. The formation of PGA/β-lgNPs complexes was mainly driven by non-covalent interaction, including electrostatic gravitational interaction, hydrogen bonding and hydrophobic effect. Interestingly, the difference in the molecular weight of PGA also led to significantly differences in the micro-morphology of the complexes, as PGA with a high molecular weight (2,000 kDa) generated the formation of a “fruit-tree” shaped structure, whereas PGA with relatively low molecular weight (100 and 500 kDa) led to spherical particles with a “core-shell” structure. In addition, the incorporation of PGA molecules into β-lgNPs dispersion also contributed to the improvement in the encapsulation efficiency of Cur as well as physicochemical stability of β-lgNPs, and PGA with a higher molecular weight was confirmed with a better effect. Findings in the current work may help to further understand the effect of molecular weight of polysaccharide on the physical and structural properties as well as effectiveness as delivery systems of polysaccharide-protein complexes, providing for the possibility for the design and development of more efficient carriers for bioactive compounds in food system.

Lasered Graphene Microheaters Modified with Phase-Change Composites: New Approach to Smart Patch Drug Delivery.

The combination of paraffin wax and O,O′-bis(2-aminopropyl) polypropylene glycol–block–polyethylene glycol–block–polypropylene glycol was used as a phase-change material (PCM) for the controlled delivery of curcumin. The PCM was combined with a graphene-based heater derived from the laser scribing of polyimide film. This assembly provides a new approach to a smart patch through which release can be electronically controlled, allowing repetitive dosing. Rather than relying on passive diffusion, delivery is induced and terminated through the controlled heating of the PCM with transfer only occurring when the PCM transitions from solid to liquid. The material properties of the device and release characteristics of the strategy under repetitive dosing are critically assessed. The delivery yield of curcumin was found to be 3.5 µg (4.5 µg/cm2) per 3 min thermal cycle.

Skin-targeted delivery of extracellular vesicle-encapsulated curcumin using dissolvable microneedle arrays

Therapeutic benefits of curcumin for inflammatory diseases have been demonstrated. However, curcumin's potential as a clinical therapeutic has been hindered due to its low solubility and stability in vivo. We hypothesized that a hybrid curcumin carrier that incorporates albumin-binding and extracellular vesicle (EV) encapsulation could effectively address the current challenges of curcumin delivery. We further postulated that using dissolvable microneedle arrays (dMNAs) for local delivery of curcumin-albumin-EVs (CA-EVs) could effectively control skin inflammation in vivo. Mild sonication was used to encapsulate curcumin and albumin into EVs, and the resulting CA-EVs were integrated into tip-loaded dMNAs. In vitro and in vivo studies were performed to assess the stability, cellular uptake, and anti-inflammatory bioactivity of dMNA-delivered CA-EVs. Curcumin in CA-EVs exhibited at least five-fold higher stability in vitro than naïve curcumin or curcumin-EVs without albumin. Incorporating CA-EVs into dMNAs did not alter their cellular uptake or anti-inflammatory bioactivity. The dMNA embedded CA-EVs retained their bioactivity when stored at room temperature for at least 12 months. In rat and mice models, dMNA delivered CA-EVs suppressed and significantly reduced lipopolysaccharide and Imiquimod-triggered inflammation. We conclude that dMNA delivery of CA-EVs has the potential to become an effective local-delivery strategy for inflammatory skin diseases. Statement of significanceWe introduce and evaluate a skin-targeted delivery system for curcumin that synergistically combines albumin association, extracellular-vesicle encapsulation, and dissolvable microneedle arrays (dMNAs) . In vitro, curcumin-albumin encapsulated extracellular vesicles (CA-EVs) inhibit and reverse the LPS-triggered expression of inflammatory transcription factor NF-κB. The integration of CA-EVs into dMNAs does not affect them physically or functionally. Importantly, dMNAs extend EV storage stability for at least 12 months at room temperature with minimal loss in their bioactivity. We demonstrate that dMNA delivered CA-EVs effectively block and reverse skin inflammation in vivo in mouse and rat models.

Nano-in-micro alginate/chitosan hydrogel via electrospray technology for orally curcumin delivery to effectively alleviate ulcerative colitis

Although nano-systems can promote the cellular internalization, polymeric nanoparticles (NPs) are easily to be destroyed or eliminated in the gastrointestinal tract, which leads to premature drug release or insufficient colonic accumulation. A novel oral nano-in-micro system for the efficient colonic delivery of curcumin (Cur) was developed in this study, in which the hyaluronic acid (HA)/zein complex NPs loading Cur were embedded in alginate/chitosan hydrogel microparticles (Cur@NMPs) with the electrospray technology. The Cur@NMPs showed uniform-sized sphere with an average size of 218.36 ± 10 μm, encapsulating Cur@HA/zein NPs with the average size of 148.64 ± 3.21 nm. Cur in NMPs showed the sustained drug-release profiles in simulated gastric fluid, whereas it showed the rapid release in simulated colonic fluid. Mediated by the HA-CD44 receptor recognition, Cur@HA/zein NPs had the increased cellular uptake efficiency in macrophages. Furthermore, NMPs had the significant colon-retention and bio-adhesiveness capacity in colon tissues. As expected, the oral administration of Cur@NMPs significantly mitigated colitis symptoms in DSS-induced UC mice by inhibiting TLR4/NF-κB pathway. The above results can provide a useful drug delivery strategy for Cur in the treatment of UC by retaining the advantages of nano- and micro-scaled carriers.

Development of eucalyptol enriched nano vesicles for better transdermal delivery of curcumin: Preparation, characterisation and ex vivo skin analysis

Development of eucalyptol enriched nano vesicles for better transdermal delivery of curcumin: Preparation, characterisation and ex vivo skin analysis

Intracellular K+-Responsive Block Copolymer Micelles for Targeted Drug Delivery of Curcumin.

Curcumin (CUR) is a natural bioactive compound that has attracted attention as a “golden molecule” due to its therapeutic properties against several types of tumors. Nonetheless, the antitumor application of CUR is hampered due to its extremely low aqueous solubility and chemical instability. Herein, a novel type of CUR-loaded polymeric micelles with intracellular K+-responsive controlled-release properties is designed and developed. The polymeric micelles are self-assembled by poly (N-isopropylacrylamide-co-acryloylamidobenzo-15-crown-5-co-N, N-dimethylacrylamide)-b-DSPE (PNDB-b-DSPE) block copolymers, and CUR. CUR is successfully loaded into the micelles with a CUR loading content of 6.26 wt%. The proposed CUR-PNDB-DSPE polymeric micelles exhibit a significant CUR release in simulated intracellular fluid due to the formation of 2 : 1 ‘‘sandwich’’ host–guest complexes of 15-crown-5 and K+, which lead to the hydrophilic outer shell of micelles to collapse and the drug to rapidly migrate out of the micelles. In vitro, the B16F10 cell experiment indicates that CUR-PNDB-DSPE micelles exhibit a high cellular uptake and excellent intracellular drug release in response to the intracellular K+ concentration. Moreover, CUR-PNDB-DSPE micelles show high cytotoxicity to B16F10 cells compared to free CUR and CUR-PEG-DSPE micelles. The polymeric micelles with intracellular K+-responsive controlled release properties proposed in this study provide a new strategy for designing novel targeted drug delivery systems for CUR delivery for cancer treatment.

BTN-PEG-PCL nanoparticles for targeted delivery of curcumin: In vitro and in Ovo assessment

The major challenge of curcumin (CUR) therapy is the low bioavailability in the tumor cells, which could be solved by targeting and manipulating nanoparticles (NPs) in the drug delivery systems (DDS) through enhancement of CUR uptake. In our study, ligand-targeted micelle NPs including BTN-poly ethylene glycol-polycaprolactone(PCL) (BTNcment-PEG-PCL) and mono methoxy poly (ethylene glycol)-poly (caprolactone) (mPEG-PCL) diblock co-polymers series were synthesized by way of a single-step nano-precipitation method and characterized by H NMR, FT-IR, DSC, DLS, TEM, and GPC techniques. Following CUR-loading on the NP series, cytotoxicity and cellular uptake of CUR-BTN-PEG-PCL and CUR-mPEG-PCL on human breast adenocarcinoma (MCF-7), Human embryonic kidney (HEK293), and human umbilical vein endothelial (HUVEC) cell lines were evaluated by MTT assay and microscope fluorescence, respectively. Then, in vitro studies of targeted and untargeted NPs for the cell cycle and apoptosis assessment using flow cytometry have shown that CUR in CUR-BTN-PEG-PCL as a novel and targeted nanocarrier increases the cell population of Sub G1 and apoptosis. Moreover, in Ovo chick chorioallantoic membrane (CAM) assay demonstrated that CUR-BTN-PEG-PCL has notably decreased tumor cell proliferation and angiogenesis due to enhanced CUR bioavailability for the site-specific tumor. In conclusion, BTN-PEG–PCL NPs as a novel and efficiently targeted nanocarrier predominantly improved CUR potential for cancer therapy.

Oral Bioavailability of Curcumin Enhanced Using Different Surfactant for Preparing Proniosomal Gel

Purpose: The aim of the present study was to enhance the oral bioavailability of curcumin using different surfactant and vehicle for preparing proniosomal gel. Methods: Curcumin comes under BCS Class IV which is having low solubility and low permeability and poor bioavailability. Buccal drug delivery can bypass such problems and leads to increase in bioavailability. Proniosomes offer excellent potential for improved drug delivery through versatile routes, by overcome the permeation barriers. Trial batches of proniosomal gel are prepared by coacervation phase separation method using different concentration of surfactant (Span 20, Span 40, Span 60, and Span 80) with cholesterol, soyalecithin, and vehicles such as 0.1% glycerol solution or pH 6.8. The formulated systems were characterized to find out the effects of surfactant on vesicle size, % entrapment efficiency, and % drug release and permeation at 6 h. Stability studies for proniosomal gel were carried out for 4 weeks. Results and Conclusion: It suggested that formulation (F2) containing Span 20 and phosphate buffer pH 6.8 has high entrapment efficiency, drug release, and permeation as compare to the other formulations and it can enhance the delivery of curcumin through oral route and can improve the bioavailability of drug.

Preparation of carrageenan/ chitosan-based (N,N,N-trimeth(yl chitosan chloride) silver nanocomposites as pH sensitive carrier for effective controlled curcumin delivery in cancer cells

PurposeThis work aims to formulate a novel pH-sensitive biocompatible metallic nanocomposite as a carrier for hydrophobic drugs with efficient loading and controlled drug release. The proposed carrier consists of a polyelectrolyte complex of chitosan-based, N,N,N-trimethyl chitosan chloride (TMC), and carrageenan (CAR) biopolymers with different silver nanoparticles (AgNPs) molar ratios forming CAR/TMC-Ag nanocomposites that investigated to be used as a carrier for controlled gastro-intestinal tract (GIT) release of curcumin (CUR) as a model of lipophilic drugs. MethodsThe structure of nanocomposites was scrutinized via FTIR, TEM, SEM, XRD and EDX, whereas the potential cytotoxicity and antimicrobial efficacy of loaded nanocomposite with 3% AgNPs (NC-3% Ag) were probed, as well. ResultsSuccessful loading and release of CUR were detected from the prepared nanocomposites without change in its functionality with a higher releasing profile in pH 7.4 (simulated intestinal fluid) than pH 1.2 (simulated gastric fluid). In vitro release study of CUR loaded NC-3% Ag showed the favored sustained drug release reaching 98.9% ± 0.9 within 24 h in pH 7.4, following Korsmeyer−Peppas model. Additionally, successful release from loaded CAR/TMC nanocomposite with 3% AgNPs (NC-3% Ag), revealed high cytotoxic effect with apoptotic induction against human colon cancerous cells (Caco-2) through G2/M cell cycle arrest and antibacterial potency against different bacterial strains. Moreover, cell viability results of NC-3% Ag against human normal cells exhibited good biocompatibility. ConclusionAccordingly, we suggested NC-3% Ag as a promising controlled drug delivery vehicle for hydrophobic drugs with preferred intestinal targeting effectiveness.

Co-delivery of methotrexate and curcumin with mPEG-PCL polymeric nanoparticles and evaluation of toxicity effect on MCF7 breast cancer cell line

Therapeutic strategies used to treat cancer are focused on cytotoxic drugs as the main form of chemotherapy. Recently nanocarrier-based chemotherapy has been widely used to treat cancer. Drugs covalently attached to a polymer chain, known as prodrugs, can significantly enhance drug incorporation efficiency. This study aimed to synthesis a biodegradable mPEG-PCL copolymers for effective and targeted drug delivery of the anticancer compounds curcumin and methotrexate and to investigate their physicochemical properties and effects on breast cancer cells.In this study, mPEG-PCL copolymer was synthesized by polymerization of ὲ-Caprolactone dehydrated monomer in the presence of dry methoxy polyethylene glycol as the initiator and Sn(Oct)2 as catalyst. The mPEG-PCL copolymers were synthesized and their structure was evaluated using Fourier Transform Infrared Spectroscopy (FTIR). Then, methotrexate was conjugated to a copolymer. The methotrexate conjugated mPEG–PCL(MTX–mPEG-PCL) was self-assembled into micelles in the presence of curcumin by nano-precipitation method and the drug loading was assessed. Finally, the cytotoxicity of methotrexate, curcumin and conjugated nanoparticles with methotrexate and curcumin were investigated through 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay on Michigan Cancer Foundation-7 (MCF-7) cancer cell lines. The size of mPEG-PCL-MTX and mPEG-PCL-MTX-CUR nanoparticles were evaluated by zeta sizer with an average size of 51.89 ± 0.46 nm (PDI = 0.127), and 88.21 ± 0.31 nm (PDI = 0.344), respectively. The zeta potential of nanoparticles was −4.22 mV. FTIR studies showed methotrexate was conjugated to the copolymer. The amount of drug released in nanoparticles at pH = 5.5 was higher than pH = 7.4. By increasing the drug concentration in the drug-carrying nanosystem, cell survival was further reduced. Among the treatment groups, mPEG-PCL-MTX-CUR group demonstrated the greatest impact, while, the MTX group showed the least impact on cancer cell mortality. These findings suggest that micelles conjugated with MTX and loading CUR appear to be promising systems for achieving Enhanced Permeability and Retention (EPR) effect, and pH sensitivity, which could improve the release and accumulation of drugs at tumor sites.

PH-Responsive Hydrogel Beads Based on Alginate, κ-Carrageenan and Poloxamer for Enhanced Curcumin, Natural Bioactive Compound, Encapsulation and Controlled Release Efficiency.

Polyphenolic compounds are used for treating various diseases due to their antioxidant and anticancer properties. However, utilization of hydrophobic compounds is limited due to their low bioavailability. In order to achieve a greater application of hydrophobic bioactive compounds, hydrogel beads based on biopolymers can be used as carriers for their enhanced incorporation and controlled delivery. In this study, beads based on the biopolymers-κ-carrageenan, sodium alginate and poloxamer 407 were prepared for encapsulation of curcumin. The prepared beads were characterized using IR, SEM, TGA and DSC. The curcumin encapsulation efficiency in the developed beads was 95.74 ± 2.24%. The release kinetics of the curcumin was monitored in systems that simulate the oral delivery (pH 1.2 and 7.4) of curcumin. The drug release profiles of the prepared beads with curcumin indicated that the curcumin release was significantly increased compared with the dissolution of curcumin itself. The cumulative release of curcumin from the beads was achieved within 24 h, with a final release rate of 12.07% (gastric fluid) as well as 81.93% (intestinal fluid). Both the in vitro and in vivo studies showed that new hydrogel beads based on carbohydrates and poloxamer improved curcumin’s bioavailability, and they can be used as powerful carriers for the oral delivery of different hydrophobic nutraceuticals.

PH/ROS dual-responsive nanoparticles with curcumin entrapment to promote antitumor efficiency in triple negative breast cancer

Triple negative breast cancer (TNBC) remains a serious carcinoma threatening women's life. Natural compounds such as curcumin (CUR) have shown promising potential in TNBC therapy without conventional toxicity like chemotherapeutics. To improve the therapeutic efficiency, a pH/redox nanocarrier (CUR@PCPP NPs) was developed for tumor specific delivery of CUR. CUR@PCPP NPs showed good size distribution, encapsulation efficiency and stability under physiological conditions. Detachment of polyethylene glycol (PEG) facilitated cellular uptake of CUR@PCPP NPs after exposure to extracellular tumor pH. Subsequently CUR was released due to the intracellular redox environment. Thereafter, released CUR could efficiently induce apoptosis and cycle arrest, and inhibit TNBC cells. We further verified the biodistribution and antitumor effects in vivo and the results showed that CUR@PCPP NPs demonstrated high tumor specific accumulation and effectively suppressed tumor growth without noticeable toxicity.

Curcumin-loaded zein/pectin nanoparticles: Caco-2 cellular uptake and the effects on cell cycle arrest and apoptosis of human hepatoma cells (HepG2)

Curcumin is a natural plant component with enormous in vitro anticancer effects. However, the bioavailability of curcumin is limited due to its poor solubility in water. Our previous studies showed that zein pectin core/shell nanoparticle-encapsulated curcumin (En-CUR) improved the solubility and bioaccessibility of curcumin. In this study, the transportation mechanism of En-CUR into Caco-2 cells and the inhibitory effects of En-CUR on HepG2 cell proliferation were investigated. The results showed that the uptake of En-CUR by Caco-2 cells required energy consumption. Caveolae-mediated endocytosis, clathrin-dependent endocytosis, and macropinocytosis were involved in the uptake of En-CUR by Caco-2 cells. The apoptosis rate of HepG2 cells after En-CUR treatment was 31.2%, which was approximately two-fold higher than that of the CUR-treated cells treated with curcumin at a concentration of 10 μg/mL, and the early apoptosis rate of En-CUR-treated cells was 2.7–3.3 times higher than that of CUR-treated cells. En-CUR-treated HepG2 cells exhibited more significant cell cycle arrest at cell cycle checkpoints S and G2/M than CUR-treated cells. En-CUR also decreased mitochondrial membrane potential. Western blot analysis revealed that En-CUR increased Bax protein expression, activated caspase-3 and caspase-9, and increased cytochrome c and p53 protein levels in HepG2 cells. Our results suggested that zein-pectin core/shell nanoparticles were desirable curcumin delivery systems and exhibited superior cancer cell antiproliferative effects.

Dual Nanostructured Lipid Carriers/Hydrogel System for Delivery of Curcumin for Topical Skin Applications.

This work focuses on the development and evaluation of a dual nanostructured lipid carrier (NLC)/Carbopol®-based hydrogel system as a potential transporter for the topical delivery of curcumin to the skin. Two populations of different sized negatively charged NLCs (P1, 70–90 nm and P2, 300–350 nm) were prepared and characterized by means of dynamic light scattering. NLCs presented an ovoid platelet shape confirmed by transmission electron microscopy techniques. Curcumin NLC entrapment efficiency and release profiles were assessed by HPLC (high pressure liquid chromatography) and spectrophotometric methods. Preservation and enhancement of curcumin (CUR) antioxidant activity in NLCs (up to 7-fold) was established and cell viability assays on fibroblasts and keratinocytes indicated that CUR-NLCs are non-cytotoxic for concentrations up to 10 μM and exhibited a moderate anti-migration/proliferation effect (20% gap reduction). CUR-NLCs were then embedded in a Carbopol®-based hydrogel without disturbing the mechanical properties of the gel. Penetration studies on Franz diffusion cells over 24 h in CUR-NLCs and CUR-NLCs/gels demonstrated an accumulation of CUR in Strat-M® membranes of 22% and 5%, respectively. All presented data support the use of this new dual CUR-NLC/hydrogel system as a promising candidate for adjuvant treatment in topical dermal applications.

Efficient Delivery of Curcumin by Alginate Oligosaccharide Coated Aminated Mesoporous Silica Nanoparticles and In Vitro Anticancer Activity against Colon Cancer Cells.

We designed and synthesized aminated mesoporous silica (MSN-NH2), and functionally grafted alginate oligosaccharides (AOS) on its surface to get MSN-NH2-AOS nanoparticles as a delivery vehicle for the fat-soluble model drug curcumin (Cur). Dynamic light scattering, thermogravimetric analysis, and X-ray photoelectron spectroscopy were used to characterize the structure and performance of MSN-NH2-AOS. The nano-MSN-NH2-AOS preparation process was optimized, and the drug loading and encapsulation efficiencies of nano-MSN-NH2-AOS were investigated. The encapsulation efficiency of the MSN-NH2-Cur-AOS nanoparticles was up to 91.24 ± 1.23%. The pH-sensitive AOS coating made the total release rate of Cur only 28.9 ± 1.6% under neutral conditions and 67.5 ± 1% under acidic conditions. According to the results of in vitro anti-tumor studies conducted by MTT and cellular uptake assays, the MSN-NH2-Cur-AOS nanoparticles were more easily absorbed by colon cancer cells than free Cur, achieving a high tumor cell targeting efficiency. Moreover, when the concentration of Cur reached 50 μg/mL, MSN-NH2-Cur-AOS nanoparticles showed strong cytotoxicity against tumor cells, indicating that MSN-NH2-AOS might be a promising tool as a novel fat-soluble anticancer drug carrier.