Antisolvent Precipitation Research Articles

Development, Characterization and Evaluation of Phytosomal Gel of Curcumin for the Treatment of Topical Fungal Infection

An innovative approach to the delivery of phytoconstituents and plant extracts for therapeutic and cosmetic purposes constitutes a herbal medication delivery system. However, their bioavailability is low because of their high molecular size and low lipid solubility. Turmeric (Curcuma longa) and Curcuma xanthorrhiza oil contain the active component curcumin, also known as diferuloylmethane. This medication can kill or inhibit the growth of bacteria, fungi, viruses, and fungi, and it can reduce inflammation, lower blood sugar, and speed the healing of wounds. In this study, we created a phytosomal gel containing Curcumin and analyzed its efficacy. Anti-solvent precipitation was used to create Curcumin phytosomes in three separate batches with varying drug-to-soya lecithin ratios. Several tests, including those of yield, solubility, drug content, entrapment efficiency, and in vitro drug release, were conducted on phytosomal formulations. Based on a number of evaluation criteria, the formulation F1 was chosen as the optimal formulation to include into a gel basis of varying proportions utilizing carbopol 940 and PEG400 as polymers. This formulation contained drug extract: soya lecithin in the ratio 1:1. Maximum drug absorption (98.19%) was observed after 8 hours in the improved formulation (G2). 45 days of stability testing was conducted at 40oC ±20oC, 70±5%.RH The drug's potency, pH, dispersibility, extrudability, viscosity, or in-vitro diffusion profile all remained unchanged. The Curcumin phytosomal gel was found to have a superior diffusion and stability profile, making it an appealing vehicle for the delivery of the various phytoconstituents.

Sustainable, economical and rapid treatment of multiple lung diseases using therapeutic potential of curcumin nanoparticles

The study was designed to prepare pure curcumin nanoparticles in rapid and simple way for target specific drug delivery to kill bacteria lying deep down within the alveoli of lungs via inhaler. Three different methods including evaporation precipitation of nanosuspension (ENP), solid dispersion (SD) and anti-solvent precipitation (ASP) were selected to prepare nanocurcumin in pure form in very simple way. This was done to compare their efficiency in terms of particle size obtained and water solubility and bacterial toxicity of as prepared curcumin nanoparticles. In this comparative study, curcumin NPs obtained from three different methods having particles size 65.3 nm, 98.7 nm and 47.4 nm respectively. The NPs were characterized using various techniques like SEM, XRD, UV–Visible and FTIR for their particle size determination and solubility evaluation. These particles were screened off against five bacterial strains causing lung diseases. AB3 prepared by ASP method, being smallest sized nanostructures, showed maximum solubility in water. These nanoparticles can be used as drug directly via inhaler to the target area without using any support or nano-carrier. In this way minimum dose formulation is required to target bacteria.

Nanoparticles loaded with phlorizin fabricate a fortified yogurt with antioxidant potential

Phlorizin (PHL) has various biological activities, especially powerful antioxidant effects, but its water solubility limits its application. In this study, zein-encapsulated PHL nanoparticles (zein-PHL nanoparticles), as well as zein and gum arabic (GA) co-encapsulated PHL nanoparticles (zein/GA-PHL nanoparticles) were prepared by the antisolvent precipitation method. On this basis, encapsulated PHL nanoparticles were added to yogurt to make fortified yogurt. Fourier transform infrared (FT-IR) spectroscopy and X-ray diffraction (XRD) experiments showed that the main driving forces for nanoparticle formation were electrostatic interactions and hydrogen bonding between compounds. Zein-PHL nanoparticles were more sensitive to temperature and salt ions than zein/GA-PHL nanoparticles. The addition of GA can improve the stability of the nanoparticles. In addition, the nanoparticles encapsulated with PHL were applied to yogurt. It was found that the nanoparticles improved the antioxidant capacity and water-holding capacity of yogurt, which provides a reference for the development of functional yogurt containing flavonoid compounds.

Formulation and Evaluation of Phytosomes of Hydroalcoholic Extract of Adiantum capillus-veneris for Antimicrobial Activity

Pharmacognosy Research,2023,15,3,468-477.DOI:10.5530/pres.15.3.048Published:June 2023Type:Original Article Authors:Supriya Ganesh Jagtap, Vedant Vinay Kajale, Mukta Mahesh Abhyankar, Aditi Shrinivas Kulkarni, and Minal Rushikesh Ghante Author(s) affiliations:Supriya Ganesh Jagtap1,*, Vedant Vinay Kajale2, Mukta Mahesh Abhyankar1, Aditi Shrinivas Kulkarni1, Minal Rushikesh Ghante2 1Department of Pharmacognosy, STES’s, Smt. Kashibai Navale College of Pharmacy, Kondhwa (Bk), Pune, Maharashtra, INDIA. 2Department of Pharmaceutical Quality Assurance, STES’s, Smt. Kashibai Navale College of Pharmacy, Kondhwa (Bk), Pune, Maharashtra, INDIA. Abstract:Background: Natural plant extracts and phytoconstituents have high in vitro bioactivity but low in vivo bioactivity because of poor lipid solubility, multiple ring large molecules, or digestion in the gut. Polyphenolic phytoconstituents were complexed with phospholipids, mainly phosphatidylcholine, which molecularly attaches components to one another to produce novel drug delivery systems like phytosomes. The important constituents of the herbal extract are designed to protect from being disrupted by gastric juices and gut bacteria, as phytosomes have the ability to cross the bio-membranes that which are lipid enriched and boost bioavailability. Objectives: The current work is aimed to formulate and evaluate phytosomes from Adiantum capillus-veneris (ACV) hydroalcoholic extract for antimicrobial activity. Materials and Methods: Antisolvent precipitation method was chosen on the basis of the solubility of hydroalcoholic extract in dichloromethane. The prepared trial batches of the phytosomes complex were characterized by using particle size, zeta potential, drug entrapment efficiency, drug content, and in vitro drug release study. The optimized batch of phytosomes was characterized for compatibility studies by using Infrared Spectrometry (IR), Transmission Electron Microscopy (TSM), Differential Scanning Calorimetry (DSC), and further for stability studies. Results: The results revealed that ACV hydroalcoholic extract and phosphatidylcholine were found to be connected by a non-covalent bond and did not generate a new molecule in the ACV hydroalcoholic extract-phosphatidylcholine complex and showed enhanced in vitro antimicrobial activity as compared to the hydroalcoholic extract. Conclusion: The complex's dissolution profile was found to be improved. As a result, the phospholipid complex of ACV extract can therefore be concluded to have the potential to enhance bioavailability. Keywords:Adiantum capillus-veneris (ACV), Antimicrobial activity., H-ACV extract phytosomes, Hydroalcoholic extract, PhytosomesView:PDF (549.56 KB)

Efficient synergistic combination effect of curcumin with piperine by polymeric magnetic nanoparticles for breast cancer treatment

Although it has been reported that the co-delivery of drugs can be beneficial to patients to kill breast cancer cells, the delivery methods could only be employed to effectively encapsulate individual curcumin (CUR) or piperine (PIP) molecules due to their different molecular polarities. Therefore, in the current research, an attempt was made to overcome the limitation of the co-delivery of CUR and PIP nanoparticles for breast cancer therapy. To manage locoregional breast cancer recurrence, a magnetic co-delivery system of CUR and PIP against MCF-7 breast cancer cells was examined. CUR and PIP demonstrated synergistic effects for breast cancer therapy when utilized together. However, due to the different polarities of CUR and PIP, it was difficult to co-encapsulate them in conventional delivery systems. Moreover, their low bioavailability, hydrophobic nature, and low cellular uptake limit its usage for cancer therapy. In the current study, to overcome the issues and improves its therapeutic efficacy, CUR and PIP-loaded zein/chitosan-coated iron oxide (Chit-PIP/CUR-zein@Fe3O4) were prepared via a combination of anti-solvent precipitation and layer-by-layer deposition. X-ray diffraction (XRD) analysis revealed magnetite cores and also showed that the binding process did not change the Fe3O4 phase. A vibrational sample magnetometer confirmed that the saturation of sample magnetization was 60 and 40 emu/g for pure Fe3O4 and nanocomposite, respectively. Nanoparticles with an average size of 20 nm were prepared. The drug-loading content of CUR and PIP was approximately 18% and 16%, respectively. CUR and PIP release from Chit-PIP/CUR-zein@Fe3O4 was faster at the extracellular pH of around tumors (6.5) than in normal tissues (7.4), an interesting degree of pH sensitivity. The MTT assay exhibited that PIP/CUR-loaded polymeric magnetic nanoparticles had significant synergistic cytotoxicity against MCF-7 cells compared with other groups. These results demonstrate that the combination of dual-drug loaded polymeric magnetic nanoparticles holds promise for the targeted treatment of cancer cells.

Fabrication and optimization of itraconazole-loaded zein-based nanoparticles in coated capsules as a promising colon-targeting approach pursuing opportunistic fungal infections

Itraconazole (ITZ), a broad-spectrum antifungal drug, was formulated into colon-targeting system aiming to treat opportunistic colonic fungal infections that commonly infect chronic inflammatory bowel diseases (IBD) patients due to immunosuppressive therapy. Antisolvent precipitation technique was employed to formulate ITZ-loaded zein nanoparticles (ITZ-ZNPs) using various zein: drug and aqueous:organic phase ratios. Central composite face-centered design (CCFD) was used for statistical analysis and optimization. The optimized formulation was composed of 5.5:1 zein:drug ratio and 9.5:1 aqueous:organic phase ratio with its observed particle size, polydispersity index, zeta potential, and entrapment efficiency of 208 ± 4.29 nm, 0.35 ± 0.04, 35.7 ± 1.65 mV, and 66.78 ± 3.89%, respectively. ITZ-ZNPs were imaged by TEM that revealed spherical core–shell structure, and DSC proved ITZ transformation from crystalline to amorphous form. FT-IR showed coupling of zein NH group with ITZ carbonyl group without affecting ITZ antifungal activity as confirmed by antifungal activity test that showed enhanced activity of ITZ-ZNPs over the pure drug. Histopathological examination and cytotoxicity tests ensured biosafety and tolerance of ITZ-ZNPs to the colon tissue. The optimized formulation was then loaded into Eudragit S100-coated capsules and both in vitro release and in vivo X-ray imaging confirmed the success of such coated capsules in protecting ITZ from the release in stomach and intestine while targeting ITZ to the colon. The study proved that ITZ-ZNPs is promising and safe nanoparticulate system that can protect ITZ throughout the GIT and targeting its release to the colon with effectual focused local action for the treatment of colon fungal infections.Graphical

Hyaluronic acid-engineered Bcl-2 inhibitor nanocrystals for site-specific delivery to breast tumor cells.

Aim: This investigation aims to repurpose venetoclax using hyaluronic acid-coated venetoclax nanocrystals (HA-VEN-NCs) to target breast cancer. Materials & methods: An antisolvent precipitation method was used to fabricate the nanocrystals and optimize them using central composite design. Hyaluronic acid (HA)-coated and -uncoated nanocrystals were compared in terms of in vitro drug release, cell line studies, CD44-expressing breast tumor cell binding capability and anticancer activity. Results: HA-VEN-NCs and venetoclax nanocrystals (VEN-NCs) showed pH-responsive drug-release behavior, exhibiting sustained release at pH 6.8. Our extensive in vitro cell line investigation showed that HA-VEN-NCs efficiently bind to CD44-expressing breast tumor cells and possess excellent anticancer activity (half maximal inhibitory concentration: 2.00μg/ml) compared with VEN-NCs. Conclusion: Our findings anticipate that HA-VEN-NCs could serve as valuable nanoplatforms for cancer treatments in the future.

Fabrication of egg white protein/phosphatidylcholine-EGCG co-assembled nanoparticles with sustained release in simulated gastrointestinal digestion and their transcellular permeability in Caco-2 cultures

Epigallocatechin-3-gallate (EGCG) is a kind of polyphenol with various biological activities but poor stability and bioavailability. The encapsulation of EGCG in a nano-delivery system effectively improves its shortcomings. In this research, co-assembled nanoparticles of egg white protein, phosphatidylcholine (PC), and EGCG (EW/PE1:5 NPs) were prepared by antisolvent precipitation to improve their bioavailability. The constructed EW/PE1:5 NPs had an average particle size of 172 nm, a ζ-potential of −26.1 mV, and a polymerization dispersion index (PDI) of 0.33. The encapsulation efficiency (EE) of EGCG was 88.09% and the loading capacity (LC) was 20.10%. UV spectra, FTIR, XRD and intermolecular force results indicated that hydrophobic, electrostatic and hydrogen bonding interactions contributed to the formation of EW/PE1:5 NPs. EW/PE1:5 NPs exhibited Fick diffusion and sustained release characteristics in simulated gastrointestinal digestion. In addition, the transcellular permeability of EW/PE1:5 NPs was significantly increased compared with free EGCG. At the same time, EW/PE1:5 NPs increased EGCG absorption transport and inhibited MRP2 and P-gp-mediated efflux transport. These results suggest that EW/PE1:5 NPs play a key role in improving the bioavailability of EGCG. Therefore, EW/PE1:5 NPs are expected to provide a theoretical basis for the design and development of functional foods or dietary supplements that synergistically enhance the bioavailability of EW, PC and other flavonoids.

Investigating of zein-gum arabic-tea polyphenols ternary complex nanoparticles for luteolin encapsulation: Fabrication, characterization, and functional performance

Luteolin has extensive biological effects, but its low water-solubility and oral bioavailability have restricted its application. In this study, we successfully prepared new zein-gum arabic (GA)-tea polyphenols (TP) ternary complex nanoparticles (ZGTL) as a delivery system to encapsulate luteolin using an anti-solvent precipitation method. Consequently, ZGTL nanoparticles showed negatively charged smooth spherical structures with smaller particle size and higher encapsulation ability. X-ray diffraction revealed the amorphous state of luteolin in the nanoparticles. Hydrophobic, electrostatic, and hydrogen bonding interactions contributed to the formation and stability of ZGTL nanoparticles, as indicated by fluorescence and Fourier transform infrared spectra analyses. The inclusion of TP improved the physicochemical stability and luteolin retention rate of ZGTL nanoparticles by forming more compact nanostructures under different environmental conditions, including pH, salt ion concentration, temperature, and storage. Additionally, ZGTL nanoparticles exhibited stronger antioxidant activity and better sustainable release capacity under simulated gastrointestinal conditions due to TP incorporation. These findings demonstrate that ZGT complex nanoparticles have potential applications as an effective delivery system for encapsulating bioactive substances in food and medicine fields.

Solubility measurement and modeling of hydroxychloroquine sulfate (antimalarial medication) in supercritical carbon dioxide

A supercritical fluid, such as supercritical carbon dioxide (scCO2) is increasingly used for the micronization of pharmaceuticals in the recent past. The role of scCO2 as a green solvent in supercritical fluid (SCF) process is decided by the solubility information of the pharmaceutical compound in scCO2. The commonly used SCF processes are the rapid expansion of supercritical solution (RESS) and supercritical antisolvent precipitation (SAS). To implement micronization process, solubility of pharmaceuticals in scCO2 is required. Present study is aimed at both measuring and modeling of solubilities of hydroxychloroquine sulfate (HCQS) in scCO2. Experiments were conducted at various conditions (P = 12 to 27 MPa and T = 308 to 338 K), for the first time. The measured solubilities were found to be ranging between (0.0304 × 10–4 and 0.1459 × 10–4) at 308 K, (0.0627 × 10–4 and 0.3158 × 10–4) at 318 K, (0.0982 × 10–4 and 0.4351 × 10–4) at 328 K, (0.1398 × 10–4 and 0.5515 × 10–4) at 338 K. To expand the usage of the data, various models were tested. For the modelling task existing models (Chrastil, reformulated Chrastil, Méndez-Santiago and Teja (MST), Bartle et al., Reddy-Garlapati, Sodeifian et al., models) and new set of solvate complex models were considered. Among the all models investigated Reddy-Garlapati and new solvate complex models are able to fit the data with the least error. Finally, the total and solvation enthalpies of HCQS in scCO2 were calculated with the help of model constants obtained from Chrastil, reformulated Chrastil and Bartle et al., models.

Fortification of chocolates with high-value-added plant-based substances: Recent trends, current challenges, and future prospects.

High consumption of delicious foods, such as chocolates, is considered excellent snacks, capable of converting from health-threatening to great functional foods. The fortification of chocolates with high-value-added plant-based substances might improve their healthful effects, nutritional properties, and shelf life. Chocolate could be an effective carrier for plant-based substances delivery, and it could be an effective vehicle to treat and reduce the indications of disease, such as obesity, overweight, hypertension, stress, cardiovascular failure, congestive heart failure, and diabetes. Referring to the recent studies in chocolate fortification with high-value-added plant-based substances, it seems that the recent trends are toward its therapeutic effects against noncommunicable diseases. Despite the undeniable functional effects of fortified chocolates, there are some challenges in the fortification way of chocolates. In other words, their functional characteristics, such as rheological and sensory attributes, may undesirably change. It seems that encapsulation techniques, such as spray drying, antisolvent precipitation, nanoemulsification, and liposomal encapsulation, could almost overcome these challenges. Thus, several studies focused on designing and fabricating nanoscale delivery systems with the aim of chocolate fortification, which is discussed.

Formulation Strategies of Nanosuspensions for Various Administration Routes.

Nanosuspensions (NSs), which are nanosized colloidal particle systems, have recently become one of the most interesting substances in nanopharmaceuticals. NSs have high commercial potential because they provide the enhanced solubility and dissolution of low-water-soluble drugs by means of their small particle sizes and large surface areas. In addition, they can alter the pharmacokinetics of the drug and, thus, improve its efficacy and safety. These advantages can be used to enhance the bioavailability of poorly soluble drugs in oral, dermal, parenteral, pulmonary, ocular, or nasal routes for systemic or local effects. Although NSs often consist mainly of pure drugs in aqueous media, they can also contain stabilizers, organic solvents, surfactants, co-surfactants, cryoprotectants, osmogents, and other components. The selection of stabilizer types, such as surfactants or/and polymers, and their ratio are the most critical factors in NS formulations. NSs can be prepared both with top-down methods (wet milling, dry milling, high-pressure homogenization, and co-grinding) and with bottom-up methods (anti-solvent precipitation, liquid emulsion, and sono-precipitation) by research laboratories and pharmaceutical professionals. Nowadays, techniques combining these two technologies are also frequently encountered. NSs can be presented to patients in liquid dosage forms, or post-production processes (freeze drying, spray drying, or spray freezing) can also be applied to transform the liquid state into the solid state for the preparation of different dosage forms such as powders, pellets, tablets, capsules, films, or gels. Thus, in the development of NS formulations, the components/amounts, preparation methods, process parameters/levels, administration routes, and dosage forms must be defined. Moreover, those factors that are the most effective for the intended use should be determined and optimized. This review discusses the effect of the formulation and process parameters on the properties of NSs and highlights the recent advances, novel strategies, and practical considerations relevant to the application of NSs to various administration routes.

Reverse-QTY code design of active human serum albumin self-assembled amphiphilic nanoparticles for effective anti-tumor drug doxorubicin release in mice

Human serum albumin (HSA) is a highly water-soluble protein with 67% alpha-helix content and three distinct domains (I, II, and III). HSA offers a great promise in drug delivery with enhanced permeability and retention effect. But it is hindered by protein denaturation during drug entrapment or conjugation that result in distinct cellular transport pathways and reduction of biological activities. Here we report using a protein design approach named reverse-QTY (rQTY) code to convert specific hydrophilic alpha-helices to hydrophobic to alpha-helices. The designed HSA undergo self-assembly of well-ordered nanoparticles with highly biological actives. The hydrophilic amino acids, asparagine (N), glutamine (Q), threonine (T), and tyrosine (Y) in the helical B-subdomains of HSA were systematically replaced by hydrophobic leucine (L), valine (V), and phenylalanine (F). HSArQTY nanoparticles exhibited efficient cellular internalization through the cell membrane albumin binding protein GP60, or SPARC (secreted protein, acidic and rich in cysteine)-mediated pathways. The designed HSArQTY variants displayed superior biological activities including: i) encapsulation of drug doxorubicin, ii) receptor-mediated cellular transport, iii) tumor cell targeting, and iv) antitumor efficiency compare to denatured HSA nanoparticles. HSArQTY nanoparticles provided superior tumor targeting and antitumor therapeutic effects compared to the albumin nanoparticles fabricated by antisolvent precipitation method. We believe that the rQTY code is a robust platform for specific hydrophobic modification of functional hydrophilic proteins with clear-defined binding interfaces.

Hydrodynamics and Transport Mechanism of Microfluidic Mixing in Precipitation of Nanodrugs: A Review

AbstractPoor aqueous solubility drugs are a concern of pharmaceutical industries due to low dissolution rates and low bioavailability. Various approaches and techniques address these issues by customizing drug micro–nanonization, as investigated by many researchers. Establishing a compelling synthesis of tailored nanoparticles with highly variable qualities intended for therapeutic applications needs the flexibility to vary particle size, content, crystallinity, and shape. Such an approach necessitates getting to the desired yield and developing a synthetic process that is durable, reproducible, and scalable. However, precipitation techniques to produce nanoparticles are more convenient than other approaches. Liquid antisolvent precipitation is one of the robust crystal manipulation approaches extensively used for producing nanoparticles, where mixing sets the basis to create supersaturation followed by corresponding quality precipitation. Various process intensification equipments are in use for adequate mixing‐based precipitation. Nowadays, microfluidic precipitation system is gaining interest in the production of nanodrugs. Further, the use of ultrasound in a microfluidic system improves the mixing quality by cavitation phenomena. This review focuses on the transport phenomena and hydrodynamics involved in mixing to enhance the mass transfer during antisolvent precipitation of synthesized nanodrugs in the microfluidic system.

ONE POT DEVELOPMENT OF LIPID-BASED QUERCETIN SPHERICAL AGGLOMERATES FOR BIOAVAILABILITY ENHANCEMENT: IN VITRO AND IN VIVO ASSESSMENTS

Objective: Quercetin, a wonder flavanoid despite numerous pharmacological actions, has limited clinical applications due to solubility and permeability issues and additionally having shorter biological half-life. The goal of the current work was to design Quercetin lipid-based spherical crystals, to improve its oral bioavailability and sustain its in vivo plasma levels. Methods: An anti-solvent precipitation method was employed to prepare quercetin spherical agglomerates using ethanol and distilled water as good and bad solvents, respectively. As bridging liquid chloroform, dichloromethane, hexane and gelucire 43/01, compritol 888 as lipid carrier were screened. The drug-to-lipid polymer proportion and stirring speed effect were optimized by 3-level, 2-factor, experimental design. Numerical optimization function was employed to identify the optimum level of independent variables. Spectroscopic, micromeritic, surface morphology, size distribution, saturated solubility, in vitro dissolution, in vivo pharmackokinetic and stability studies were performed. Results: Surface morphology studies indicated the agglomeration of quercetin needle-like fragments into a spherical shape, which further showed smooth surfaces due to entrapment of QC in lipid carrier. The spherical agglomerates of quercetin showed a four-fold improvement in aqueous solubility compared to pure drug and showed 92.13% release in 8 h. The optimised formulation showed a 3.69-fold enhancement in relative bioavailability in contrast to the marketed preparation in an in vivo pharmacokinetic analysis in male Wistar rats. Conclusion: The obtained lipid-based spherical crystals of quercetin with enhanced bioavailability could be effectively used for its various potential pharmacological applications. The designed system can also be utilized to deliver other phytochemicals with poor bioavailability due to limited solubility and permeability.

Anti-solvent precipitation for the preparation of nobiletin nano-particles under ultrasonication-cis/reverse homogenization

In order to address the issue of nobiletin's limited bioavailability, nobiletin nanoparticles (NNP) were created for the first time in this research employing an anti-solvent under ultrasonication-cis/reverse homogenization. Dimethyl sulfoxide (DMSO) was used as the solvent and deionized water as the anti-solvent to create the nobiletin solution. The optimal surfactant dose of surfactant dose of 0.43%; an ultrasonic period of 8.1 min, ultrasonic at a temperature of 64 °C and a solution concentration of 8.33 mg/mL, the method was optimized to obtain the minimum NNP diameter of 199.89 ± 0.02 nm. A dual optimization process of response surface PBD and BBD was used to minimize the size of HNP particles. Additionally, scanning electron microscopy revealed that the specific surface area of the NNP dramatically increased with the reduction of NNP particle size, and dissolving studies indicated the solubility and dissolution studies showed that NNP had substantially greater solubility and dissolution rates than raw nobiletin per unit time; as a result, the NNP produced by anti-solvent precipitation with a twofold homogenization system supported by ultrasound had a realistic potential for growth.

Morphological and Physicochemical Properties of Pine Seed Starch Nanoparticles

AbstractThis study aims to characterize pine starch (PS) and pine starch nanoparticles (PSNPs) produced by anti‐solvent precipitation (ASP). PS and PSNPs are characterized by particle size, surface charge, morphology, crystalline structure, chemical bonds, thermal properties, moisture content (MC), water activity, solubility in water (SW), swelling factor (SF), water and oil absorption, and stability in water. PS shows typical starch particle size distribution, while PSNPs display a size distribution varying between 230 and 1300 nm. The crystalline structure is modified from A‐type structure (native starch) to V6h structure (PSNPs) after ASP. PSNPs SW at 25 and 90 °C, as well as oil and water absorption capacities are greatly improved when compared with PS. Furthermore, PSNPs have high stability in water at 25 °C, forming homogeneous dispersions. This research provides information about the valorization of pine seed as a possible starch source to produce nanoparticles

Purification and characterization of a chicory polysaccharide and its application in stabilizing genistein for cancer therapy

Genistein is an isoflavone with chemopreventive and therapeutic effects on various types of cancers. Apparently, in contrast to the advantages of multi-target therapy, the poor water solubility of this molecule is a major obstacle to its clinical application. In this work, zein/chicory polysaccharide nanoparticles (G-zein-P NPs) were prepared by pH-induced antisolvent precipitation method for the encapsulation of genistein. Firstly, an acidic polysaccharide (CIP70-2) with a molecular weight of 66.7 kDa was identified from the roots of chicory (Cichorium intybus). This natural macromolecule was identified as a plant pectin, for which the structure included RG-I (rhamnogalacturonan I) and HG (homogalacturonan) regions. Using this polysaccharide, G-zein-P NPs were prepared, in which the water solubility of genistein was improved by encapsulation. The encapsulation efficiency and loading efficiency of genistein by composite nanoparticles reached 99.0 % and 6.96 %, respectively. In vitro tumor inhibition experiments showed that the inhibitory effect of G-zein-P NPs on HepG2 cells was twice that of unencapsulated genistein. Moreover, the significant inhibition of tumor development and metastasis by G-zein-P NPs was observed in zebrafish xenograft models. The results suggested that zein/chicory polysaccharide nanoparticles may be a promising delivery carrier for genistein application in cancer prevention and therapy.

Preparation and characterization of particle-filled microgels by ion induction based on zein and κ-carrageenan for delivering the CoQ10

The aim of this paper was to develop novel particle-filled microgels based on zein and κ-carrageenan for delivering the coenzyme Q10 (CoQ10). The anti-solvent precipitation and potassium ion induction methods were combined to produce the zein-CoQ10-κ-carrageenan particle-filled microgels with different mass ratios (100:10:20, 100:10:40, 100:10:60, 100:10:80, 100:10:100 and 100:10:120). Results showed that zein-CoQ10-κ-carrageenan (100:10:60) particle-filled microgels were the optimized formulation, which exhibited an average particle diameter of 807.4 nm and a zeta-potential of −28.4 mV. Their encapsulation efficiency and loading capacity for CoQ10 reached 84.9% and 2.55%, respectively. The particle-filled microgels effectively reduced the chemical degradation of CoQ10 under intense light irradiation and high temperature. Moreover, the simulated gastrointestinal digestion assay revealed that the particle-filled microgels controlled the release of CoQ10, which might contribute to its improved oral bioavailability. These findings suggested that particle-filled microgels based on zein and κ-carrageenan might be a promising and effective delivery system for CoQ10 as well as other bioactive molecules.

The comparison between zein-anthocyanins complex and nanoparticle systems: Stability enhancement, interaction mechanism, and in silico approaches

This research aimed to compare and characterize the physicochemical properties and interaction mechanism of zein and anthocyanins (ACNs) from experimental and theoretical perspectives. Zein-ACNs complex (ZACP) was prepared by mixing ACNs with different concentrations of zein, and zein-ACNs nanoparticles (ZANPs) were formed using ultrasound-assisted antisolvent precipitation method. The hydrated particle sizes of the two systems were 590.83 nm and 99.86 nm, respectively, and observed to be spherical under transmission electron microscopy (TEM). The multi-spectroscopy approaches confirmed hydrogen bonding and hydrophobic forces were the dominant forces for stabilizing ACNs. The retention of ACNs, color stability and antioxidant activities were also improved in both systems. Furthermore, molecular simulation results were consistent with the multi-spectroscopy findings, which clarified the contribution of van der Waals forces to the binding of zein and ACNs. This study provided a practical approach for stabilizing ACNs and expanding the utilization of plant proteins as stabilization systems.