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1.
Although curcumin is considered to have various therapeutic effects, its use as a functional food or supplement is restricted owing to its low water solubility and bioavailability. To increase the solubility of curcumin in water, the use of polyvinylpyrrolidone (PVP) and vinylpyrrolidone-vinyl acetate copolymers with a pyrrolidone skeleton was noted to be promising. In particular, the bi-component formulations of curcumin/PVP prepared through spray drying exhibited an amorphous state in powder X-ray diffraction observations and temporally increased the apparent solubility of curcumin to over 5000 times that of untreated curcumin; nevertheless, after 24 h, the solubility decreased owing to the unstable supersaturated state of curcumin. The addition of α-cyclodextrin (α-CyD) in the bi-component curcumin/PVP formulation helped maintain the supersaturated state of curcumin, whereas the addition of β- and γ-CyD led to the collapse of the supersaturated state. The addition of α-CyD can likely help inhibit the nucleation and crystal growth of curcumin, through the interaction among the solubilized units of curcumin/PVP and α-CyD.  相似文献   

2.
Curcumin is a natural product possessing therapeutic properties but the low water solubility of this compound limits its use. We have successfully incorporated curcumin into a bilayer of dodecanoic acid attached to magnetite nanoparticles in an effort to maximize solubility and delivery efficiency. Curcumin/magnetite nanoparticles were characterized using diffused reflectance infra-red fourier transform spectroscopy (DRIFTS) and X-ray powder diffraction (XRD). Moreover curcumin associated magnetite nanoparticles inhibited in vitro melanoma cell growth. An inhibitory concentration (IC50) of 66.0 +/- 3.0 microM (48 +/- 2.2 microg-iron/mL) was observed for the curcumin/magnetite nanoparticles. Fluorescent microscopy revealed that curcumin associated magnetite nanoparticles were internalized by the melanoma cells and remained in the cytoplasm. The curcumin/magnetic nanoparticles synthesized in this study possess magnetic and water solubility properties making this a novel curcumin formulation with therapeutic potential.  相似文献   

3.
Objective: To develop clay facial mask containing turmeric extract solid dispersion (TESD) for enhancing curcumin water solubility and permeability and to determine suitable clay based facial mask.

Methods: The TESD were prepared by solvent and melting solvent method with various TE to polyvinylpyrrolidone (PVP) K30 mass ratios. The physicochemical properties, water solubility, and permeability were examined. The effects of clay types on physical stability of TESD, water adsorption, and curcumin adsorption capacity were evaluated.

Results: The TESD prepared by solvent method with a TE to PVP K30 mass ratio of 1:2 showed physically stable, dry powders, when mixed with clay. When TESD was dissolved in water, the obtained TESD micelles showed spherical shape with mean size of ~100?nm resulting in a substantial enhancement of curcumin water solubility,?~5?mg/ml. Bentonite (Bent) and mica (M) showed the highest water adsorption capacity. The TESD’s color was altered when mixed with Bent, titanium dioxide (TiO2) and zinc oxide (ZnO) indicating curcumin instability. Talcum (Talc) showed the greatest curcumin adsorption followed by M and kaolin (K), respectively. Consequently, in vitro permeation studies of the TESD mixed with Talc showed lowest curcumin permeation, while TESD mixed with M or K showed similar permeation profile as free TESD solutions. The developed TESD-based clay facial mask showed lower curcumin permeation as compared to those formulations with Tween 80.

Conclusion: The water solubility and permeability of curcumin in clay based facial mask could be improved using solid dispersion technique and suitable clay base composed of K, M, and Talc.  相似文献   

4.
The surface modification of single-walled carbon nanotubes (SWCNTs) can enhance their solubility and stability in water and biological systems. The present study demonstrated the application of the functionalized SWCNTs (f-SWCNTs) as drug-delivery vehicles. In this study, f-SWCNTs were functionalized with one of four different chemical groups for the delivery of curcumin to splenic lymphocytes. Since free curcumin can modulate the proliferation of splenic lymphocytes, we compared the abilities of different f-SWCNTs for the delivery of water-insoluble curcumin to inhibit cell proliferation, which were stimulated with concanavalin A (Con A) and lipopolysaccharide (LPS). The results showed that curcumin can be loaded onto the f-SWCNTs surface through π?π stacking with a loading capacity of 235–327 mg/g (curcumin/f-SWCNTs). The f-SWCNTs-curcumin complexes display considerable cell proliferation inhibition efficacy when compared with free curcumin diluted in dimethyl sulfoxide (DMSO). Furthermore, curcumin loaded onto SWCNTs functionalized with poly(ethylene glycol) (SW-PEG) showed good dispersion and stability in water, confirming the excellent biocompatibility of SW-PEG as a drug carrier.  相似文献   

5.
Curcumin has been associated with the treatment of various diseases in traditional medicine, among them cancer. The major problems that prevent its approval as therapeutic agent are its low water solubility and its relatively low in vivo bioavailability. Liposomes are considered as effective drug carriers because of their ability to solubilize hydrophobic compounds and to alter their pharmacokinetic properties. The purpose of this study was the development of lyophilised liposomal curcumin fully characterized in terms of its physical properties [(zeta-potential, size, size distribution and Polydispercity index (PI)], and to evaluate its in vitro cytotoxic against colorectal cancer cell lines in a short-term and in a long-term (clonogenic) assay. Curcumin was incorporated in egg-phosphatidylcholine (EPC) liposomes at a drug to lipid molar ratio 1:14 achieving high incorporation efficiency close to 85%. The liposomal curcumin was lyophilized preserving thus its stability. The reconstitution of the formulation resulted in the original liposomal suspension. The release in FBS showed a plateau near 14% at 96 hours of incubation. The in vitro studies against colorectal cancer cell lines have shown that liposomes improve the activity of curcumin especially in the long-term assay and the liposomal formulation found to be more potent against HCT116 and HCT15, cell lines which express the MDR phenotype. EPC liposomal curcumin in a molar ratio of curcumin/EPC 1:14 has shown improved cytotoxic activity versus free curcumin against colorectal cancer cell lines. In vivo studies based on the recent findings are in progress in our laboratory.  相似文献   

6.
In this study, the authors developed pectin‐stabilised selenium nanoparticles (pectin‐SeNPs) for curcumin (Cur) encapsulation and evaluated their physicochemical properties and biological activities. Results showed that pectin‐SeNPs and Cur‐loaded pectin‐SeNPs (pectin‐SeNPs@Cur) exhibited monodisperse and homogeneous spherical structures in aqueous solutions with mean particle sizes of ∼61 and ∼119 nm, respectively. Cur was successfully encapsulated into pectin‐SeNPs through hydrogen bonding interactions with an encapsulation efficiency of ∼60.6%, a loading content of ∼7.4%, and a pH‐dependent and controlled drug release in vitro. After encapsulation was completed, pectin‐SeNPs@Cur showed enhanced water solubility (∼500‐fold), dispersibility, and storage stability compared with those of free Cur. Moreover, pectin‐SeNPs@Cur possessed significant free radical scavenging ability and antioxidant capacity in vitro, which were stronger than those of pectin‐SeNPs. Antitumour activity assay in vitro demonstrated that pectin‐SeNPs@Cur could inhibit the growth of HepG2 cells in a concentration‐dependent manner, and the nanocarrier pectin‐SeNPs exhibited a low cytotoxic activity against HepG2 cells. Therefore, the results suggested that pectin‐SeNPs could function as effective nanovectors for the enhancement of the water solubility, stability, and in vitro bioactivities of hydrophobic Cur.Inspec keywords: hydrogen bonds, selenium, nanoparticles, solubility, drug delivery systems, toxicology, hydrophobicity, free radicals, particle size, nanofabrication, cancer, nanomedicine, drugs, biomedical materials, encapsulation, cellular biophysics, pH, organic compoundsOther keywords: pectin‐decorated selenium nanoparticles, pectin‐stabilised selenium nanoparticles, curcumin encapsulation, Cur‐loaded pectin‐SeNPs, nanocarrier pectin‐SeNPs, physicochemical properties, biological properties, homogeneous spherical structures, monodisperse spherical structures, aqueous solutions, particle size, hydrogen bonding interactions, encapsulation efficiency, loading content, pH‐dependent drug release, in vitro controlled drug release, water solubility, free radical scavenging ability, in vitro antioxidant capacity, in vitro antitumour activity assay, HepG2 cells, cytotoxic activity, in vitro bioactivity, hydrophobic curcumin, Se  相似文献   

7.
Curcumin, the main active constituent of turmeric herb (Curcuma longa L.) have been reported to possess many medicinal values. The application of curcumin in dermatological preparations is limited by their intense yellow color property, which stains the fabric and skin. The objectives of this study were to reduce the color staining effect and enhance the stability of curcumin via microencapsulation using gelatin simple coacervation method. As for curcumin, ethanol and acetone were used as coacervating solvents. Curcumin was dispersed in ethanol while dissolved in acetone. Irrespective of the types of coacervating solvents used, microencapsulation resolved the color-staining problem and enhanced the flow properties and photo-stability of curcumin. Nevertheless, it was found that more spherical curcumin microcapsules with higher yield, higher curcumin loading, and higher entrapment efficiency were obtained with acetone than ethanol. The in vitro release of curcumin after microencapsulation was slightly prolonged. Further evaluation of the effects of solubility of core materials in coacervating solvent or polymeric aqueous solution using six different drug compounds, namely, ketoconazole, ketoprofen, magnesium stearate, pseudoephedrine HCl, diclofenac sodium, and paracetamol, suggested that the solubility of core materials in aqueous polymeric solution determined the successful formation of microcapsules. Microcapsules could only be formed if the core materials were not dissolved in the aqueous polymeric solution while the core materials could either be dissolved or dispersed in the coacervating solvent. In summary, microencapsulation not only circumvents the color-staining problem but also improved the stability and flowability of curcumin. The solubility of core material in aqueous polymeric solution plays a pivotal role in determining the successful formation of microcapsules.  相似文献   

8.
Curcumin, the main active constituent of turmeric herb (Curcuma longa L.) have been reported to possess many medicinal values. The application of curcumin in dermatological preparations is limited by their intense yellow color property, which stains the fabric and skin. The objectives of this study were to reduce the color staining effect and enhance the stability of curcumin via microencapsulation using gelatin simple coacervation method. As for curcumin, ethanol and acetone were used as coacervating solvents. Curcumin was dispersed in ethanol while dissolved in acetone. Irrespective of the types of coacervating solvents used, microencapsulation resolved the color-staining problem and enhanced the flow properties and photo-stability of curcumin. Nevertheless, it was found that more spherical curcumin microcapsules with higher yield, higher curcumin loading, and higher entrapment efficiency were obtained with acetone than ethanol. The in vitro release of curcumin after microencapsulation was slightly prolonged. Further evaluation of the effects of solubility of core materials in coacervating solvent or polymeric aqueous solution using six different drug compounds, namely, ketoconazole, ketoprofen, magnesium stearate, pseudoephedrine HCl, diclofenac sodium, and paracetamol, suggested that the solubility of core materials in aqueous polymeric solution determined the successful formation of microcapsules. Microcapsules could only be formed if the core materials were not dissolved in the aqueous polymeric solution while the core materials could either be dissolved or dispersed in the coacervating solvent. In summary, microencapsulation not only circumvents the color-staining problem but also improved the stability and flowability of curcumin. The solubility of core material in aqueous polymeric solution plays a pivotal role in determining the successful formation of microcapsules.  相似文献   

9.
We report our experimental results of a hybrid which has both the cooling-responsive shape memory effect (SME) and water-responsive SME. The hybrid is designed based on the concept of shape memory hybrid (SMH), and is made of a plastic sponge (as elastic component) filled with Poloxamer 407 (P407) gel (as transition component). It is observed that the hybrid is able to recover its original shape upon immersing into 0 °C water in less than one minute (due to “melting” of P407 gel upon cooling), while upon immersing into 20 °C water, the recovery time is about one hour (due to dissolving of P407 gel in the water). Apparently, cooling for shape recovery is a complement to heating induced SME as in almost all traditional thermo-responsive shape memory materials. Mechanical properties of these samples are characterized by cyclic uniaxial compression test. Our experimental results reveal the compatibility and feasibility of P407 hybrid for biomedical applications inside human body. Potential biomedical applications are further discussed.  相似文献   

10.
Curcumin is a natural pigment that generates singlet oxygen upon light excitation, hence it can be used as a photosensitizer in photodynamic therapy. The extremely low water solubility and poor systemic bioavailability make curcumin a challenging molecule to be used clinically. In this study, two nanocarrier systems for curcumin were prepared and characterized; nanoliposomes and polyvinyl pyrrolidone-capped gold nanoparticles. The dark and photocytotoxicity were investigated as a function of light fluence rate (100 and 200?mW/cm2) on HepG2 cancer cells. In vivo Erlich tumor model was developed and comparison of the tumor volume, survival rate, and histopathological alterations was made for the two nanocarriers. Results showed that both curcumin nanocarriers were successfully prepared and characterized. Light irradiation was able to augment the cytotoxicity of both curcumin liposomes and gold nanoparticles, with the former being superior in cytotoxicity compared to the latter. The tumor size was almost diminished 1 month post-photodynamic treatment for both systems with regression in the number of tumor cells upon histopathological evaluation, with curcumin liposomes producing better tumor regression than gold nanoparticles with comparable survival rate. Liposomes were confirmed to be superior to gold nanoparticles as a photodynamic treatment modality for cancer.  相似文献   

11.
Abstract

Objective: Curcumin, the golden spice from Indian saffron, has shown chemoprotective action against many types of cancer including breast cancer. However, poor oral bioavailability is the major hurdle in its clinical application. In the recent years, self-nanoemulsifying drug delivery system (SNEDDS) has emerged as a promising tool to improve the oral absorption and enhancing the bioavailability of poorly water-soluble drugs. In this context, complexation with lipid carriers like phospholipid has also shown the tremendous potential to improve the solubility and therapeutic efficacy of certain drugs with poor oral bioavailability.

Methods: In the present investigation, a systematic combination of both the approaches is utilized to prepare the phospholipid complex of curcumin and facilitate its incorporation into SNEDDS. The combined use of both the approaches has been explored for the first time to enhance the oral bioavailability and in turn increase the anticancer activity of curcumin.

Results: As evident from the pharmacokinetic studies and in situ single pass intestinal perfusion studies in Sprague–Dawley rats, the optimized SNEDDS of curcumin–phospholipid complex has shown enhanced oral absorption and bioavailability of curcumin. The cytotoxicity study in metastatic breast carcinoma cell line has shown the enhancement of cytotoxic action by 38.7%. The primary tumor growth reduction by 58.9% as compared with the control group in 4T1 tumor-bearing BALB/c mice further supported the theory of enhancement of anticancer activity of curcumin in SNEDDS.

Conclusion: The developed formulation can be a potential and safe carrier for the oral delivery of curcumin.  相似文献   

12.
Curcumin is an active ingredient which is poorly water-soluble, leading to a low oral bioavailability. The aim of this research was to prepare a novel microbead formulation, and to solubilize, solidify, and improve storage stability of curcumin. Firstly, curcumin was solubilized with KolliphorTM RH40 and then microencapsulated by cross linking of sodium alginate with calcium chloride. A three-factor, three-level Box–Behnken design was employed to acquire the optimum microbead formulation, namely the best entrapment efficiency and in vitro curcumin release. The independent variables were sodium alginate concentration, calcium chloride concentration, and the weight of curcumin solution, while the dependent variables were entrapment efficiency and in vitro curcumin release. The optimized microbead formulation was 2.06% sodium alginate, 24.33% calcium chloride, and 1.28 g curcumin solution (containing curcumin and RH40 with a ratio of 1:22, g/g). Results showed that high concentrations of sodium alginate and calcium chloride could increase the entrapment efficiency. In vitro curcumin release decreased with increasing of sodium alginate as well as decreasing of calcium chloride. In conclusion, the optimum microbead formulation increased the solubility of curcumin and enhanced its stability, and achieved a high entrapment efficiency and in vitro curcumin release.  相似文献   

13.
Chitin and chitosan are natural biopolymers that are non-toxic, biodegradable and biocompatible. In the last decade, chitin and chitosan derivatives have garnered significant interest in the biomedical and biopharmaceutical research fields with applications as biomaterials for tissue engineering and wound healing and as excipients for drug delivery. Introducing small chemical groups to the chitin or chitosan structure, such as alkyl or carboxymethyl groups, can drastically increase the solubility of chitin and chitosan at neutral and alkaline pH values without affecting their characteristics; substitution with carboxyl groups can yield polymers with polyampholytic properties. Carboxymethyl derivatives of chitin and chitosan have shown promise for adsorbing metal ions, as drug delivery systems, in wound healing, as anti-microbial agents, in tissue engineering, as components in cosmetics and food and for anti-tumor activities. This review will focus on the preparative methods and applications of carboxymethyl and succinyl derivatives of chitin and chitosan with particular emphasis on their uses as materials for biomedical applications.  相似文献   

14.
As a new kind of 2D material, black phosphorus has gained increased attention in the past three years. Although few‐layered black phosphorus nanosheets (BPs) degrade quickly under ambient conditions to phosphate anions, which greatly hampers their optical and electronic applications, this property also makes BPs highly biocompatible and biodegradable, and is regarded as an advantage for various biomedical applications. This Concept summarizes the state‐of‐art progresses of BPs, from fabrication and surface modification to biomedical applications. It is expected that BPs with such fascinating properties will encourage more scientists to engage in expanding its biomedical applications by tackling the scientific challenges involved in their development.  相似文献   

15.
石墨烯是由碳原子以sp2杂化排列形成的,具有单原子层结构的新型二维原子晶体。迄今为止,石墨烯的量子物理特性及其在纳米电子元件、透明导体、纳米复合材料等方面的潜在应用已被人们研究,但其在生物医药领域的应用却很少有报道。文章制备出功能化的氧化石墨烯具有良好的水溶性和稳定性,通过研究氧化石墨烯与抗感染药物-哌拉西林钠他唑巴坦钠的作用机制,探索其在生物医药领域的应用。  相似文献   

16.
Hydrophobic ultrasmall nanoparticles synthesized in nonpolar solvents exhibit great potential in biomedical applications. However, a major challenge when applying these nanomaterials in biomedical research is the lack of a versatile strategy to render them water dispersible while preserving the hydrodynamic diameter (HD) to be less than 8 nm for efficient renal clearance. To address this problem, tryptone is employed as the novel ligand to fabricate a simple, versatile, and inexpensive strategy for transferring hydrophobic NaGdF4 nanodots (3 nm in diameter) from organic phase into aqueous phase without any complicated organic synthesis. The paramagnetic properties of NaGdF4 nanodots are well retained after the phase transfer process. In particular, the tryptone–NaGdF4 nanodots have ultrasmall HD (ca., 7.5 nm), which greatly improves their tumor accumulation and facilitates renal clearance within 24 h postinjection. The as‐prepared tryptone–NaGdF4 nanodots can also be further functionalized with other molecules for extensively biomedical and bioanalytical applications. Furthermore, the proposed strategy can easily be extended to transfer other types of inorganic nanoparticles from hydrophobic to hydrophilic for facilitating biomedical applications.  相似文献   

17.
Porous metal–organic framework (MOF) liquids with permanent porosity, good fluidity, and fine dispersion attract broad attention in catalysis, transportation, gas storage, and chemical separations. Yet, the design and synthesis of porous MOF liquids for drug delivery remain less explored. Herein, a simple and general strategy is reported to prepare ZIF-91 porous liquid (ZIF-91-PL) via surface modification and ion exchange. The cationic nature of ZIF-91-PL not only renders it antibacterial but also with high curcumin loading capacity and sustained release. More importantly, the acrylate group on the grafted side chain of ZIF-91-PL makes it feasible to crosslink with modified gelatin through light curing, and the obtained hydrogel shows a significantly improved healing effect on the wound of diabetes. This work demonstrates for the first time, a MOF-based porous liquid for drug delivery, and the further fabrication of composite hydrogel may have potential applications in biomedical science.  相似文献   

18.
The novel optical and electrical properties of luminescent semiconductor nanocrystals are appealing for ultrasensitive multiplexing and multicolor applications in a variety of fields, such as biotechnology, nanoscale electronics, and opto-electronics. Luminescent CdSe and CdTe nanocrystals are archetypes for this dynamic research area and have gained interest from diverse research communities. In this review, we first describe the advances in preparation of size- and shape-controlled CdSe and CdTe semiconductor nanocrystals with the organometallic approach. This article gives particular focus to water soluble nanocrystals due to the increasing interest of using semiconductor nanocrystals for biological applications. Post-synthetic methods to obtain water solubility, the direct synthesis routes in aqueous medium, and the strategies to improve the photoluminescence efficiency in both organic and aqueous phase are discussed. The shape evolution in aqueous medium via self-organization of preformed nanoparticles is a versatile and powerful method for production of nanocrystals with different geometries, and some recent advances in this field are presented with a qualitative discussion on the mechanism. Some examples of CdSe and CdTe nanocrystals that have been applied successfully to problems in biosensing and bioimaging are introduced, which may profoundly impact biological and biomedical research. Finally we present the research on the use of luminescent semiconductor nanocrystals for construction of light emitting diodes, solar cells, and chemical sensors, which demonstrate that they are promising building blocks for next generation electronics.  相似文献   

19.
Abstract

The curcumin (CUR)-hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion complex (CUR-HP-β-CD) was prepared to erase its therapeutic restrictions of poor aqueous solubility and low oral bioavailability. CUR-HP-β-CD was prepared by a simple procedure of water-ethanol cosolvent incubation-lyophilization which may be suitable for scale up production, and characterized by Fourier transform-infrared spectroscopy (FT-IR), powder X-ray diffractometry (PXRD), differential scanning calorimetry (DSC), phase solubility method and dissolution study; the in vitro cytotoxicity was assayed by MTT, whereas the in vivo pharmacokinetics was tested by HPLC in rats receiving formulations via intravenous and oral administration, respectively. CUR was successfully encapsulated in HP-β-CD with a loading capacity of about 1:7 of CUR to HP-β-CD mole ratio, which remarkably enhanced drug water solubility and maintained well the antitumour activity of CUR. The CUR-HP-β-CD and free CUR have a similar pharmacokinetic behaviour in rats after intravenous administration; however, the oral bioavailability of CUR was enhanced to 2.77-fold by the HP-β-CD. The CUR-HP-β-CD can be successfully prepared by a simple method, which may be feasible for industrial scaling up, to remarkably increase drug water solubility and oral bioavailability while maintaining its bioactivity and may be a promising therapeutic preparation.  相似文献   

20.
Carvacrol is a known antioxidant molecule and commonly used in food and cosmetics as a flavor and fragrance agent; however, carvacrol has major issues such as high volatility, low water solubility, and stability. In this study, carvacrol/cyclodextrin inclusion complex fibers (carvacrol/CD-IC fibers) were produced via electrospinning in order to enhance thermal stability, water solubility and shelf-life of carvacrol having antioxidant activity. The phase solubility and computational modeling studies showed that carvacrol can form inclusion complexes with two types of modified CDs, hydroxypropyl-β-cyclodextrin (HPβCD) and hydroxypropyl-γ-cyclodextrin (HPγCD). The carvacrol/cyclodextrin inclusion complex electrospun fibers (carvacrol/HPβCD-IC fibers and carvacrol/HPγCD-IC fibers) were obtained as free-standing fibrous webs. Although pure carvacrol is highly volatile, the electrospun carvacrol/CD-IC fibers were quite effective to preserve high amount of carvacrol due to the inclusion complexation. In addition, carvacrol/CD-IC fibers have shown higher temperature stability for carvacrol. Moreover, carvacrol/CD-IC fibers showed more effective antioxidant activity as compared to pure carvacrol. The carvacrol/CD-IC fibrous webs have shown fast-dissolving character in water due to the enhanced water solubility of carvacrol/CD-IC and their ultrafine fiber structure. In short, encapsulation of carvacrol in electrospun CD-IC fibrous webs has shown potentials for food and oral care applications due to free-standing and fast-dissolving character along with high water solubility, high temperature stability and enhanced antioxidant by carvacrol/cyclodextrin inclusion complexation.  相似文献   

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