Enhanced Water Solubility Research Articles

Biochemical characterization of synthesized fisetin glucoside by dextransucrase from Leuconostoc mesenteroides NRRL B-1299CB4 with enhanced water solubility

Fisetin (7,3',4'-flavon-3-ol) is a flavonol found in plants, fruits, and vegetables. It exhibits diverse biological activities, including antioxidant, anti-inflammatory, and anti-cancer effects. However, the low water solubility and bioavailability of fisetin restrict its pharmaceutical applications. In this work, we synthesized a novel fisetin-4'-O-α-D-glucopyranoside (FST-G1) using transglucosylation with sucrose, fisetin, and dextransucrase from Leuconostoc mesenteroides NRRL B-1299CB4. The water solubility of FST-G1 (109.8 ± 6.3 mg/L) was enhanced compared to fisetin (13.6 ± 1.3 mg/L). The antioxidant activities of FST-G1 in non-cellular assays, including ORAC, ABTS•+, and FRAP assays, were lower compared to fisetin. However, FST-G1 exhibited higher nitric oxide inhibition (62.5 µM; 92.3 %) in lipopolysaccharide-stimulated RAW 264.7 murine macrophage cells compared to fisetin (81.4 %). Anti-lipid accumulation in mouse 3T3-L1 cells treated with FST-G1 was similar to that in cells treated with fisetin. Taken together, the novel synthesized FST-G1 is expected to become a promising functional material for using in the pharmaceutical industry.

Downstream Processing of Amorphous and Co-Amorphous Olanzapine Powder Blends.

The work evaluates the stability of amorphous and co-amorphous olanzapine (OLZ) in tablets manufactured by direct compression. The flowability and the compressibility of amorphous and co-amorphous OLZ with saccharin (SAC) and the properties of the tablets obtained were measured and compared to those of tablets made with crystalline OLZ. The flowability of the amorphous and mostly of the co-amorphous OLZ powders decreased in comparison with the crystalline OLZ due to the higher cohesiveness of the former materials. The stability of the amorphous and co-amorphous OLZ prior to and after tableting was monitored by XRPD, FTIR, and NIR spectroscopies. Tablets presented long-lasting amorphous OLZ with enhanced water solubility, but the release rate of the drug decreased in comparison with tablets containing crystalline OLZ. In physical mixtures made of crystalline OLZ and SAC, an extent of amorphization of approximately 20% was accomplished through the application of compaction pressures and dwell times of 155 MPa and 5 min, respectively. The work highlighted the stability of amorphous and co-amorphous OLZ during tableting and the positive effect of compaction pressure on the formation of co-amorphous OLZ, providing an expedited amorphization technique, given that the process development-associated hurdles were overcome.

Heterodinuclear Ru-Pt Complexes Bridged with 2,3-Bis(pyridyl)pyrazinyl Ligands: Studies on Kinetics, Deoxyribonucleic Acid/Bovine Serum Albumin Binding and Cleavage, In Vitro Cytotoxicity, and In Vivo Toxicity on Zebrafish Embryo Activities.

Di- and poly-homo/heteronuclear complexes have great potential as anticancer drugs. Here, we report their reactivity, deoxyribonucleic acid (DNA)/bovine serum albumin (BSA) binding and cleavage interactions, in vitro cytotoxicity, and in vivo zebrafish embryo toxicity of [(phen)2Ru(μ-L)PtCl2]2+ (phen = 1,10-phenanthroline and L = 2,3-bis(2-pyridyl)pyrazine, bpp, C1; 2,3-bis(2-pyridyl)quinoxaline, bpq, C2ial; 2,3-bis(2-pyridyl)benzo[g]quinoxaline, bbq, C3) anticancer prodrugs. The substitution reactivity increases from C1 to C3 owing to an increase in the π-conjugation on the bridging chelate which facilitates π-back bonding. As a result, the electrophilicity index on the C3 complex increases than that on the complex C2 followed by C1 which leads to higher rates of substitution and thus the reactivity order follows C1 < C2 < C3. The coordination of Ru at one end of each of the complexes enhances water solubility. Moreover, the charge addition of the two metal ions increases their reactivity toward substitution in addition to ensuring electrostatic interactions at target sites such as the DNA/BSA. Spectroscopic (UV–vis absorption and fluorescence quenching) titration and viscosity measurement results of the interactions of C1/2/3 with CT-DNA established the formation of stable, nonconvent C1/2/3-DNA adducts with DNA most likely via the intercalative binding mode. Furthermore, studies with BSA showed a good binding affinity of these complexes owing to hydrophobic interactions with the coordinated ligands. The interactions of these complexes with DNA/BSA are in line with the reactivity trend, and all these experimental findings were further supported by molecular docking analysis. In vitro MTT cytotoxic activities on human breast cancer cell line MCF-7 revealed that all the complexes have high cytotoxicity activity (IC50 > 9 μM); furthermore, the selectivity index and SI values were higher (>3). Complex C3 showed the highest cytotoxicity with IC50 = 3.1 μM and SI value (5.55) against MCF7 cell lines and these values were comparable to those of the cisplatin (IC50 and SI values are 5.0 μM and 4.02, respectively). In vivo toxicological assessments on zebrafish embryos revealed that all the Ru–Pt complexes (CI/2/3) have poor embryo acute toxic effects over 96 h postfertilization, hpf with LC50 > 65.2 μM. The complex C3 has shown the lowest embryo toxicity (LC50 = 148.8 μM), which is comparable to that of commercial cisplatin (LC50 = 181.1 μM). Based on the cytotoxicity results, complexes C2 and C3 could be considered for further development as chemotherapeutic agents against MCF breast cancer cells.

Peptide-Mediated Targeted Delivery of Aloe-Emodin as Anticancer Drug.

Breast cancer is one of the most diffuse cancers in the world and despite the availability of the different drugs employed against it, the need for new and particularly more specific molecules is ever growing. In this framework, natural products are increasingly assuming an important role as new anticancer drugs. Aloe-emodin (AE) is one of the best characterized molecules in this field. The functionalization of bioactive natural products with selected peptide sequences to enhance their bioavailability and specificity of action is a powerful and promising strategy. In this study, we analyzed the cell specificity, cell viability effects, intracellular distribution, and immune cell response of a new peptide conjugate of Aloe-emodin in SKBR3 and A549 cell lines by means of viability tests, flow cytometry, and confocal microscopy. The conjugate proved to be more effective at reducing cell viability than AE in both cell lines. Furthermore, the results showed that it was mainly internalized within the SKBR3 cells, showing a nuclear localization, while A459 cells displayed mainly a cytoplasmic distribution. A preserving effect of the conjugate on NKs’ cell function was also observed. The designed conjugate showed a promising specific activity towards HER2-expressing cells coupled with an enhanced water solubility and a higher cytotoxicity; thus, the resulting proof-of-concept molecule can be further improved as an anticancer compound.

Synthesis, Physical Properties, and In Vitro-Simulated Gastrointestinal Digestion of Hydrophilic β-Sitosterol Sugar Esters.

Hydrophilic β-sitosterol sugar esters were synthesized by a two-step biocatalytic approach using β-sitosterol vinyl adipate as an intermediate. The maximum conversion (above 90%) of β-sitosterol vinyl adipate was achieved using the saccharides glucose, sucrose, and raffinose. The chemical structure of the synthesized esters was confirmed by various techniques. The investigation of physical properties revealed that β-sitosterol sugar esters had enhanced water solubility (3.0-8.0 mM at 35 °C), reduced crystallinity, and high wettability. Their lyotropic liquid crystal properties were observed by polarized light microscopy. Furthermore, β-sitosterol sugar esters could be hydrolyzed into β-sitosterol adipate under simulated intestinal conditions at a low rate (2.83-18.14%). Most β-sitosterol sugar esters probably entered into intestinal bile salt micelles with ester bonds intact and showed up to 10-fold higher in vitro bioaccessibility than free β-sitosterol in non-fat systems. The excellent physical and functional characteristics of β-sitosterol sugar esters suggested their great potential application in the food industry.

Complete regression of xenografted breast tumors by dextran-based dual drug conjugates containing paclitaxel and docosahexaenoic acid

In this study, a novel carboxymethyl dextran (CMD)-based dual drug delivery system that delivering two water insoluble drugs to tumor sites was developed and evaluated for anticancer activities. Paclitaxel (PTX) and docosahexaenoic acid (DHA) were covalently coupled with CMD to generate CMD-DHA-PTX conjugate S and conjugate L with different linkers containing amino acids Gly-Gly or Lys-Gly-Gly, respectively. Both conjugates possessed high PTX loading contents and enhanced water solubility, as well as the ability of being self-assembled into nanoparticles with the nanoparticle size ranged from 88.7 nm to 94.7 nm. These two conjugates released free PTX continuously in plasma and cancer cells. The conjugate S exhibited improved pharmacokinetic parameters and higher distribution extent in tumor sites than the parent PTX, Abraxane and the conjugate L. The antitumor efficacy of these two conjugates outperformed parent PTX formulation and Abraxane in nude mice bearing breast cancer cells MCF-7. More importantly, the conjugate S treatment eliminated all the xenograft tumors without causing any mice body weight loss in mice model. This study revealed that the dextran-based dual drug conjugates may represent an effective and innovative way to deliver anticancer agents to a variety of tumors.

Creating diverse glycosides of 2′-hydroxyflavone through microbial glycosylation

Four new 2′-hydroxyflavone glycosides, namely hydroxyflavone-2′-O-β-D-glucuronide (1), hydroxyflavone-2′-O-α-L-rhamnoside (2), hydroxyflavone-2′-O-β-D-glucoside (3), and hydroxyflavone-2′-O-4″-O-methyl-β-D-glucoside (4), were biosynthesized through microbial glycosylation using Streptomyces coeruleorubidus NRRL B-2569, Streptomyces toxytricini NRRL 15443, Escherichia coli BL21(DE3)/pWZ8, and Beauveria bassiana ATCC 7159, respectively. Compounds 1–4 were structurally characterized through extensive analysis of 1D and 2D NMR spectroscopic data. The water solubility of glycosylated products 1–4 were enhanced by 7 to 15 times compared to the substrate 2′-hydroxyflavone. Moreover, antioxidant assays revealed that compounds 1 and 2 exhibited stronger 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity than the substrate, decreasing the logIC50 by 68.7% and 80.7%, respectively. Therefore, this research provides several effective biocatalysts that can be used for structural modification of flavonoids for enhanced water solubility and biological activities.

Enzymatic glucosylation of citrus flavonoids to enhance their bioactivity and taste as new food additives

Cyclodextrin glucosyltransferase (CGTase) is commonly used to produce cyclodextrins but its utility in flavonoids modification is rarely found. In the present study, an enzymatic transformation of citrus flavonoids by applying CGTase as the catalyst was investigated to produce a number of novel polyglucosylated derivatives from monoglucoside metabolites of citrus flavonoid diglycosides. Under the optimized conditions, the yield of glucosylated products achieved 80%. The water solubility and water partition coefficient of citrus flavonoids before and after the structural modification were compared. The results revealed that the water solubility of the flavonoids modified by glucosylation was significantly increased while the oil-water partition coefficient was just slightly reduced. Moreover, after glucosylation, the products have good anti-inflammatory and antioxidant effects. Interestingly, the taste property (bitterness and sweetness) of the glucosylated products was ameliorated. An evaluation with a Taste-Sensing System showed that the taste of the glucosylated products was strongly correlated with the attached rhamnosyl group (bitter taste) and glucosyl group (sweet taste), indicating that the amelioration of taste of flavonoids could be mainly attributed to the addition of glycosyl groups. The present study demonstrated a novel molecular engineering approach for the enhancement of water solubility and amelioration of taste for some citrus flavonoids, which may have potential applications in the functional food industry.

Development of the Antithrombotic Peptide LEKNSTY Targeting the Collagen Surface: I. Design and Validation.

Exposed collagen on the diseased vessel wall is crucial for arterial thrombosis. The currently developed antithrombotic drugs mostly target blood components such as platelets and suffer from the risk of bleeding. Therefore, anticollagen therapy of covering the collagen surface was proposed as an alternative in our previous study, and an antithrombotic peptide LWWNSYY was designed and validated. However, its application was hindered due to the poor water solubility. In the present study, in order to develop a novel antithrombotic peptide with enhanced water solubility, redesigning of LWWNSYY to LEKNSTY using the EK pattern was proposed. Improved solubility was obtained for LEKNSTY. Moreover, the binding of LEKNSTY on the collagen surface was confirmed by molecular docking, molecular dynamics simulations, and experimental validation. A Kd of 0.91 ± 0.44 μM was observed. The effective inhibition of platelet adhesion on the collagen surface by LEKNSTY was demonstrated at an IC50 of 2.48 ± 0.59 μg/mL. Therefore, the successful design of the antithrombotic peptide LEKNSTY was confirmed, which would facilitate the research into the interface involving thrombus and the development of antithrombotic agents.

Physicochemical properties and solubility of sweet potato starch-based edible films

This study aimed to develop a sweet potato starch (SPS)-based edible film with improved water solubility. Initially, types of sweet potatoes were used, and their characteristics were analyzed to select the most appropriate variety for edible films. Shingeonmi was finally selected, and a chemical modification of starch, acetylation with different concentrations of acetic anhydride (1, 5, and 9 mL), was conducted to improve the water solubility. During the film-forming process, amidated pectin (AP) and calcium chloride (CaCl2) were also compounded to enhance the solubility. The developed native and acetylated SPS films, with or without the two substances, were further used to investigate various physicochemical properties and water solubility. Acetylated SPS-based films with AP and CaCl2 showed excellent water solubility (99.16%) than the native SPS one, indicating the beneficial effect of variables (acetylation, AP, and CaCl2) for enhanced water solubility. These results imply the potential use of the developed water-soluble film to package food ingredients and products such as vegetables, bakery, meat, or seafood due to the enhanced solubility and edibility.

Exploration of Fulvic Acid as a Co-Former in Crystal Engineering

The aim of the project was to investigate Peat-derived Fulvic acid for its propensity to form co-crystals with quercetin and curcumin and characterize it by using different analytical techniques. The formation of co-crystals generally enhances water solubility and the overall bioavailability of molecules. Co-crystals were synthesized using a 1:1 stoichiometric ratio of fulvic acid with quercetin and curcumin, respectively, using solvent crystallization techniques taking tetrahydrofuran and water in a 1:1 v/v ratio. The co-crystals were characterized by spectroscopic methods, FTIR and Differential scanning calorimetry. Further confirmation was made by morphological studies using SEM. A structural analysis was also carried out, using 13C solid-state NMR analysis. The studies confirmed the formation of semi crystalline forms. Furthermore, the saturation solubility displayed the enhancement in solubility of up to 10, 5-folds for Quercetin and Curcumin, respectively. The in vitro dissolution results showed that T50% was achieved within 30 min for both the drugs. The literature supports that the nutraceutical co-crystals offer advantages, particularly in the improvement of biopharmaceutical properties and addressing the challenges of the lab and manufacturing scale process. Both the semi crystalline powders exhibited enhanced solubility and a better dissolution profile.

Effect of microcrystalline cellulose under different hydrolysis durations on the stability of thyme oil emulsion.

The thyme oil emulsion was prepared using a novel type of nanocellulose obtained under different hydrolysis durations. The effect of different cellulose structures on interfacial adsorption properties of emulsion and loading efficiency of thyme oil were analyzed. The results showed that the cellulose particles became more homogeneous and hydrophilic after hydrolysis duration for 10 h. The loading efficiency of thyme oil for all emulsions reached about 80%. The retention rate of thyme oil decreased during the storage period, and rising temperatures will exacerbate the loss of thyme oil. Compared to Hd2, emulsions stabilized by Hd10 exhibited better stability and higher retention at all storage conditions. Cellulose emulsion can increase the dispersion and improve the stability of thyme oil. A smaller cellulose particle could make the emulsion become more stable. The experimental results confirmed that cellulose can be used as a stabilizer to encapsulate and transport hydrophobic active ingredient. PRACTICAL APPLICATION: The study results demonstrated that the emulsion transport system was developed using cellulose nanoparticles prepared by hydrolysis. The system can be used to load hydrophobic active substances (active peptides, curcumin, β-carotene, essential oils, etc.). It can protect the active substance from environmental damage, enhance water solubility and stability, and improve the bioavailability of the active substance.

Development of amorphous solid dispersions of cannabidiol: Influence of the carrier, the hot-melt extrusion parameters and the use of a crystallization inhibitor

Hot-melt extrusion has been widely used to manufacture amorphous solid dispersion to enhance water solubility of molecules. In this study, the influence of the polymer, the extrusion parameters and the use of a crystallization inhibitor were investigated for the production of amorphous solid dispersions.Three polymers, namely Kollidon® VA 64, Parteck® MXP and Eudragit® EPO, were first investigated to manufacture amorphous solid dispersions with cannabidiol as a model poor water-soluble drug. Selected mixtures were extruded at three temperatures and two screw speeds. Eudragit® NM 30D, was added to the formulation which had the most appropriated dissolution behavior in order to highlight the prevention of the recrystallization.Dissolution tests first showed a difference between polymers regarding the dissolution of cannabidiol. Eudragit® EPO allowed the highest and the quickest dissolution of CBD (80% after 30 min), so it was selected for the rest of the study. The dissolution tests on the ASD produced with different extrusion parameters showed that the temperature had an influence on the cannabidiol concentration upkeep during the test.Finally, it was observed that Eudragit® NM 30D was able to maintain the elevated CBD concentration during at least 4 h, while the same formulation without this inhibitor was subjected to a drop of cannabidiol concentration.This study showed the importance of first, the choice of polymers for the manufacture of amorphous solid dispersions containing cannabidiol. Secondly, the influence of the extrusion temperature on the upkeep of the cannabidiol concentration was highlighted. Finally, it was shown that the use of a crystallization inhibitor prevents the cannabidiol recrystallization during at least 4 h of dissolution.

Targeted Drug Delivery Using Graphene Quantum Dots: Approaches, Limitations and Future Perspectives.

This mini-review centers on the framework of GQDs to function as a drug delivery system (DDS), that is both target-specific and efficient. Researchers exploit GQDs for the unique pharmacokinetic properties they possess, that make them an ideal multi-functional drug delivery vehicle. We cannot enhance the therapeutic efficacy of drugs merely by focusing on drug delivery mechanisms. The conjugation of the drug with GQD allows more flexibility in controlling the kinetics and circulation time of drug in the body, the characteristic which is highly regarded in modern therapeutics. GQDs possess properties such as enhanced water solubility, lower cytotoxicity, tunable photoluminescence properties, larger specific surface area, large surface to volume ratio, and ease of surface functionalization, which make them highly effective drug molecular loading cores. Also, the review addresses the various methods of synthesis of GQDs, that include top-down and bottom-up approaches; top-down modes being more feasible and advantageous. The review touches on the various modes of GQD drug-loaded delivery- release systems (DDRS). The review also addresses the limitations associated with drug delivery using GQDs. Insufficient information about the translocation of GQDs limits their application in biomedical field and make it difficult for GQD-based carriers to pass clinical trials. Through this review, we look to summarize the important concepts of drug delivery using GQDs, and their biomedical applications and scope in nanomedicine in foreseeable future

Polyisocyanide Quaternary Ammonium Salts with Exceptionally Star-Shaped Structure for Enhanced Antibacterial Properties.

The development of non-polluting and non-hazardous polymeric antimicrobial agents has become a hot issue in current research and development. Among them, polymer quaternary ammonium salts are thought to be one of the most promising materials for antibacterial efficacy. Here, we present an efficient strategy for synthesizing polyisocyanide quaternary ammonium salts (PQASs) with a novel star-shaped structure. Benefitting from the novel structure, increased cation density and enhanced water solubility, the prepared star polyisocyanide quaternary ammonium salts (S-PQASs) exhibit excellent antibacterial properties against Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus). In particular, S-POcQAS-M50 (where M stands for isonitrile monomer and 50 stands for the initial feeding ratio) showed the best antimicrobial activity with minimum inhibitory concentration (MIC) of 17 and 20 µg/mL against E. coli and S. aureus, respectively. It was also found that the unique star-shaped structure can give QASs with improved antimicrobial performance compared with our previously prepared linear quaternary ammonium salts (L-PQASs). These results demonstrated that the antibacterial activity of QASs is closely related to its structure. This work provides an idea for the design of efficient polymeric antimicrobial agents.

Phosphorylated walnut protein isolate as a nanocarrier for enhanced water solubility and stability of curcumin

The low solubility and poor dispersion of alkaline-extracted walnut protein isolate (AWPI) limit its application as a protein-based carrier for the delivery of poorly soluble nutraceuticals, including curcumin. This work investigated the physicochemical characteristics of phosphorylated walnut protein isolate (PWPI) extracted using sodium tripolyphosphate (STP) and evaluated its encapsulation ability. The results of phosphorus determination, X-ray photoelectron spectroscopy (XPS), and Fourier transform infrared (FTIR) spectroscopy confirmed the phosphorylation of the extracted PWPI. Circular dichroism (CD) analysis indicated that PWPI contained higher α-helix and lower β-sheet contents than AWPI. The PWPI prepared at pH 9.0 and 11.0 showed significantly improved solubility, similar surface hydrophobicity, and increased surface charges compared to the AWPI. Fluorescence quenching experiments indicated that the binding affinity of curcumin to PWPI was significantly higher than that of AWPI. When bound to PWPI, the solubility of curcumin in aqueous solution was greatly enhanced, with an 8,700-fold increase at a nanocomplex concentration of 10 mg/mL. The complexation of curcumin with PWPI significantly improved the storage stability of curcumin. Additionally, the PWPI-curcumin nanocomplexes showed significantly increased antioxidant capacity. Phosphorylated walnut protein isolate showed greatly improved solubility and strong encapsulation ability, making it a promising nanocarrier for curcumin. This article is protected by copyright. All rights reserved.

Improvement of chitosan water solubility by fumaric acid modification

Chitosan is a natural biopolymer with widespread availability. Its absorption, biodegradability, and biocompatibility make it ideal for extensive application. However, the high molecular weight and the high degree of polymerization limit its water solubility at neutral pH. Water solubility can be improved through the transformation in chitosan properties. We aimed to enhance the physicochemical properties through the modification of low, medium, and high molecular weight chitosan by using fumaric acid. With increasing molecular weight of native chitosan, the modified chitosan showed a decrease in water solubility and thermal properties. According to the pH dependence study, the modified products showed higher water solubility than native chitosan in a wide pH range. Fourier transform infrared (FTIR) spectroscopy results proved the effectiveness of modification by fumaric acid. The enhanced water solubility of modified chitosan can maximize its application to the food, biomedical, and cosmetic industry.

Tailoring protein intrinsic charge by enzymatic deamidation for solubilizing chicken breast myofibrillar protein in water

Inspired by the salt-in effect, the potential use of protein-glutaminase (PG) to increase the intrinsic charges of chicken breast myofibrillar proteins (CMPs) for enhanced water solubility was tested. The degree of deamidation (DD) and solubility of CMPs increased with PG reaction time. Over 60% of CMPs were soluble in water under a DD of 6.5% due to specific conversion of glutamine to glutamic acid. PG deamidation could remarkably increase the net charge of CMPs with a merit in maintaining most of the amino acid and protein subunit compositions. Such a high electrostatic repulsion exerted a transformation of β-sheet into α-helix, unfolded the structure to expose hydrophobic residues, and allowed the dissociation of myofibril and release of subunits (myosin, actin or their oligomers), leading to a stable colloidal state. This work may foster the engineering advances of protein micro-modification in the tailor manufacture of muscle protein-based beverages.

Fabrication of poly(AA)-chitosan nanoparticles graft copolymer via microwave irradiation system for enhancing water solubility and antimicrobial properties

PurposeThis paper aims to study previously prepared and fully characterized chitosan nanoparticles (CNPs) as a starting substrate and microwave initiation technique for grafting acrylic acid (AA). This was done to see the influence of both CNPs with respect to well-dispersed nanosized particles, large surface areas, biodegradability, biocompatibility and reactivity and microwave initiation technique with respect to reduction in organic solvents, toxic chemical initiator and exposer time on exploiting the graft yield % and enhancing water solubility and antibacterial properties.Design/methodology/approachFor evaluating the best accurate standard metrological method for calculating the graft yield %, the grafting parameters were stated in terms of graft yield percent and measured gravimetrically (based on dry weight method) and titrimetrically (based on carboxyl content). Microwave power, AA and CNPs concentrations and reaction duration were shown to be the most important parameters influencing the grafting process.FindingsThe optimum reaction conditions were obtained when CNPs 1.5 g, AA 150 bows, microwave irradiation power 500 W and reaction duration 120 s were used. Various analytical methods were used to characterize CNPs and poly(AA)–CNPs graft copolymers. According to the findings, Fourier transform infrared spectroscopy examination determines the attachment of carboxyl groups to CNPs chains. The thermogravimetric analysis revealed that the copolymers were more thermally stable than CNPs counterparts. Furthermore, the resulting copolymers were shown to have greater water solubility biodegradability resistance and antibacterial properties than CNPs counterpart. Finally, a preliminary mechanism demonstrating all occasions that occur during the polymerization reaction has been proposed.Originality/valueThe advancement addressed here is undertaken using previously prepared and fully characterized CNPs as a green bio-nanocompatible polymer and microwave initiation technique as green and efficient tool with respect to reduction in organic solvents toxic chemical initiator and exposer time for grafting AA.

Synergic Antitumor Effect of Photodynamic Therapy and Chemotherapy Mediated by Nano Drug Delivery Systems.

This review provides a summary of recent progress in the development of different nano-platforms for the efficient synergistic effect between photodynamic therapy and chemotherapy. In particular, this review focuses on various methods in which photosensitizers and chemotherapeutic agents are co-delivered to the targeted tumor site. In many cases, the photosensitizers act as drug carriers, but this review, also covers different types of appropriate nanocarriers that aid in the delivery of photosensitizers to the tumor site. These nanocarriers include transition metal, silica and graphene-based materials, liposomes, dendrimers, polymers, metal–organic frameworks, nano emulsions, and biologically derived nanocarriers. Many studies have demonstrated various benefits from using these nanocarriers including enhanced water solubility, stability, longer circulation times, and higher accumulation of therapeutic agents/photosensitizers at tumor sites. This review also describes novel approaches from different research groups that utilize various targeting strategies to increase treatment efficacy through simultaneous photodynamic therapy and chemotherapy.