Enhanced gastrointestinal absorption of N3-O-toluyl-fluorouracil by cationic solid lipid nanoparticles

This study was aimed to prepare N₃-O-toluyl-fluorouracil (TFu) loaded cationic solid lipid nanoparticles (TFu-SLNs) and evaluate the potential of a novel lipid-based drug delivery system to enhance the oral absorption of TFu. TFu-SLNs were prepared by the film dispersion-ultrasonication method, using hexadecyltrimethylammonium bromide as cationic tenside. The formulation and manufacture parameters were optimized concerning the drug encapsulation efficiency and the particle size. The in vitro release characteristics, in vivo pharmacokinetic properties and bioavailability, and in situ intestinal absorption features were investigated. The morphology of TFu-SLNs was approximately spherical and the mean particle size was 178.8 ± 9.99 nm; the zeta potential was +19.54 ± 0.32 mV. The mean entrapment efficiency and drug loading were 71.03 ± 1.19% and 3.57 ± 0.08%, respectively. The release behaviors of TFu from TFu-SLNs in PBS were fitted to the bioexponential model, while in artificial gastric juice, artificial intestinal juice and artificial gastric juice (2 h) followed by artificial intestinal juice (2–48 h) were fitted to the Weibull equation. The results of the pharmacokinetic studies in mice showed that the bioavailability of TFu-SLNs was significantly increased compared with that of the TFu suspensions after oral administration. The absorption of TFu-SLNs in intestine of rat was fitted to first-order kinetics with passive diffusion mechanism and the main segments of TFu-SLNs absorbed in intestine were duodenum and jejunum for the bioadhesion mediated by electrostatic interaction between the positively charged colloidal particles and the negatively charged mucosal surface. These results indicated that cationic SLNs would offer a promising delivery system for the facilitation of the bioavailability of poorly oral absorption drugs by enhancing the bioadhesion between the absorption mucosal surface and the drug carriers.     

Micronization of Pharmaceutical Substances by Rapid Expansion of Supercritical Solutions (RESS): Experiments and Modeling

An increasing number of newly developed pharmaceutical substances are poorly soluble in both aqueous and organic media. Thus, the application of oral or injectable drugs is often limited by its low bioavailability. An alternative and promising method to improve the bioavailability of pharmaceutical agents is the production of nanoscale particles by the rapid expansion of supercritical solutions (RESS). Our research is aimed towards an improved understanding of the underlying physical phenomena of the relationship between the process conditions and the particle characteristics. Therefore, experimental investigations and numerical simulations were performed. RESS experiments with the pharmaceutical substances β‐sitosterol, griseofulvin, and ibuprofen led to particle sizes in the range of 240±80 nm. In addition, as one step towards intravenous application of poorly soluble drugs, β‐sitosterol was used to produce aqueous suspensions of a water‐insoluble drug with a particle size smaller than or equal to those produced by RESS into air. RESS modeling is focused on the flow through the nozzle, the supersonic free jet, the mach shock, and particle growth in the expansion unit. The comparison with experimental results shows a good agreement in the general trends but does not match exactly the measured mean particle sizes.     

Template-directed hydrothermal synthesis of hydroxyapatite as a drug delivery system for the poorly water-soluble drug carvedilol

In order to improve the dissolution rate and increase the bioavailability of a poorly water-soluble drug, intended to be administered orally, the biocompatible and bioactive mesoporous hydroxyapatite (HA) was successfully synthesized. In the present study, mesoporous HA nanoparticles were produced using Pluronic block co-polymer F127 and cetyltrimethylammonium bromide (CTAB) as templates by the hydrothermal method. The obtained mesoporous HA was employed as a drug delivery carrier to investigate the drug storage/release properties using carvedilol (CAR) as a model drug. Characterizations of the raw CAR powder, mesoporous HA and CAR-loaded HA were carried out by the scanning electron microscopy (SEM), transmission electron microscopy (TEM), X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), Fourier transform infrared (FT-IR) spectroscopy, N₂ adsorption/desorption, thermogravimetric analysis (TGA), and UV-VIS spectrophotometry. The results demonstrated that CAR was successfully incorporated into the mesoporous HA host. In vitro drug release studies showed that mesoporous HA had a high drug load efficiency and provided immediate release of CAR compared with micronized raw drug in simulated gastric fluid (pH 1.2) and intestinal fluid (pH 6.8). Consequently, mesoporous HA is a good candidate as a drug carrier for the oral delivery of poorly water-soluble drugs.     

Mixing thiols on the surface of silver nanoparticles: preserving antibacterial properties while introducing SERS activity

The purpose of the study was to prepare and characterize nanosuspensions that can maintain high and extended supersaturation to improve the dissolution and absorption of poorly soluble 10-hydroxycamptothecin (10-HCPT). 10-HCPT oral nanosuspensions (HCPT-Nanosuspensions) were produced on a laboratory-scale by microprecipitation- high pressure homogenization method. The particle morphology and the physical state were studied using transmission electron microscopy, X-ray powder diffraction (XRPD), and differential scanning calorimetry (DSC). Supersaturated dissolution tests were carried out with the paddle method. Caco-2 cell experiments were performed to imitate the oral absorption. The in vivo pharmacokinetics studies were undertaken in rats following oral administration. The 10-HCPT nanoparticles were 135 nm in dimension before lyophilization and were claviform or lump in shape. XRPD and DSC both confirmed that a portion of 10-HCPT was present in a crystalline state in nanosuspension. Supersaturated dissolution tests showed HCPT-Nanosuspensions could maintain high supersaturated level for an extended period time. The cell experiment on HCPT-Nanosuspensions showed a significantly higher uptake and greater membrane permeability compared with the other formulations. The pharmacokinetic test exhibited HCPT-Nanosuspensions had a similar pharmacokinetic performance with 10-HCPT solution. In conclusion, highly and extendedly supersaturated HCPT-Nanosuspensions have been prepared which could result in high peak concentration (C _max) and great exposure (AUC) after oral administration.

     

Fabrication of amorphous pharmaceutical materials by electrospraying into reduced pressure

It is estimated that more than 95% of new drug candidates suffer from limited bioavailability [1]. Particle size reduction and formation of amorphous form are commonly used techniques in modifying bioavailability of such drugs. In the present study, electrospraying was used in drug particle production. Three poorly soluble drugs were electrosprayed. Particle size was reduced down to micrometre range. Electrospraying was carried out in both atmospheric and reduced pressure, the latter in order to increase the proportion of amorphous content. The aim of the study was to examine the degree of crystallinity of the produced particles for both pressures.     

Functional and unmodified MWNTs for delivery of the water-insoluble drug Carvedilol - A drug-loading mechanism

The purpose of this study was to develop carboxyl multi-wall carbon nanotubes (MWNTs) and unmodified MWNTs loaded with a poorly water-soluble drug, intended to improve the drug loading capacity, dissolubility and study the drug-loading mechanism. MWNTs were modified with a carboxyl group through the acid treatment. MWNTs as well as the resulting functionalized MWNTs were investigated as scaffold for loading the model drug, Carvedilol (CAR), using three different methods (the fusion method, the incipient wetness impregnation method, and the solvent method). The effects of different pore size, specific surface area and physical state were systematically studied using scanning electron microscopy (SEM), thermogravimetric analysis (TGA), Fourier transformation infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), nitrogen adsorption, X-ray diffraction (XRD) and X-ray photoelectron spectroscopy (XPS). The functional MWNTs allowed a higher drug loading than the unmodified preparations. The methods used to load the drug had a marked effect on the drug-loading, dissolution, and physical state of the drug as well as its distribution. In addition, the solubility of the drug was increased when carried by both MWNTs and functional MWNTs, and this might help to improve the bioavailability.     

Effect of ultrasonic treatment on the stability and release of selenium-containing peptide TSeMMM-encapsulated nanoparticles in vitro and in vivo

Rice selenium-containing peptide TSeMMM (T) with immunomodulatory functions was isolated from selenium-enriched rice protein hydrolysates. However, its biological activity is difficult to be protected in complex digestive environments. In this study, T was encapsulated within zein and gum arabian (GA) through ultrasound treatment to improve its bioactivity and bioavailability. The zein@T/GA nanoparticles were formed using ultrasonic treatment at 360 W for 5 min with a 59.9% T-encapsulation efficiency. In vitro digestion showed that the cumulative release rate of zein@T/GA nanoparticles reached a maximum of 80.69% after 6 h. In addition, short-term animal studies revealed that the nanoparticles had an effect on the levels of tissue glutathione and improved peptides’ oral bioavailability. Conclusively, these findings suggest that the ultrasonicated polysaccharide/protein system is suitable for encapsulating active small molecular peptides. Furthermore, it provides a novel foundation for studying the bioavailability of active substances in functional foods.     

Enhancement of transport of curcumin to brain in mice by poly(n-butylcyanoacrylate) nanoparticle

Curcumin, a widely used coloring agent and spice in food, has a potential in blocking brain tumor formation and curing Alzheimer’s disease. Due to the specific properties of blood–brain barrier (BBB), only traces of curcumin were transported across BBB. The aim of the present study was to design and characterize curcumin loaded polybutylcyanoacrylate nanoparticles (PBCN) coated with polysorbate 80, and to evaluate the effect of PBCN as a delivery system on carrying curcumin across BBB. Curcumin loaded nanoparticles were prepared by an anionic polymerization method, and they presented in a core–shell spherical shape under transmission electron microscopy, with an average diameter of 152.0 nm. The average drug loading was 21.1%. Physicochemical status of curcumin in the nanoparticles was confirmed with differential scanning colorimetry and Fourier transform infrared spectroscopy. The in vitro release behavior of drug from the nanoparticles was fitted to a double phase kinetics model. The studies of pharmacokinetic and bio-distribution to brain were conducted in mice after intravenous administration of the nanoparticle formulation at the dose of 5 mg/kg and curcumin solution at the dose of 10 mg/kg via the tail vein. The results showed that in plasma, the area under concentration–time curve (AUC_0–∞) for curcumin loaded nanoparticles was greater than that for the control solution, moreover, the mean residence time of curcumin loaded nanoparticles was 14-fold that of the control solution. In brain, AUC_0–∞ for curcumin loaded nanoparticles was 2.53-fold that for the control solution. In conclusion, the present study demonstrated that PBCN could enhance the transport of curcumin to brain and have a potential as a delivery system to cross the BBB.     

Fabrication of fucoxanthin/2-hydroxypropyl-β-cyclodextrin inclusion complex assisted by ultrasound procedure to enhance aqueous solubility,stability and antitumor effect of fucoxanthin

Fucoxanthin (Fx) possesses multiple bioactivities such as antitumor, antioxidant and anti-inflammatory activities, but its application is limited due to the poor water solubility, low bioavailability, and instability to some external harsh conditions. In this study, a stable inclusion complex of Fx and 2-hydroxypropyl-β-cyclodextrin (2-HP-β-CD) was prepared with the aid of ultrasound, which was characterized by scanning electron microscope, Fourier transform infrared spectroscopy, powder X-ray diffraction, and differential scanning calorimetry techniques. The phase solubility analysis and absorption spectroscopy results showed that Fx formed stoichiometry 1:2 inclusion complex with 2-HP-β-CD, and this could be well proved by molecular simulation. Structural analyses and molecular docking study indicated that Fx was successfully encapsulated into the cavity of 2-HP-β-CD, promoting it soluble in water and stable against heat, storage and gastrointestinal environments. In addition, Fx/2-HP-β-CD inclusion complex exhibited excellent antitumor activity against HCT116 and Caco-2 cell lines with IC₅₀ values of 12.0 μΜ and 14.86 μΜ, respectively. Therefore, it could be a potentially promising way to promote the application of Fx in pharmaceuticals and functional foods by HP-β-CD encapsulation strategy.     

Fish oil based vitamin D nanoencapsulation by ultrasonication and bioaccessibility analysis in simulated gastro-intestinal tract

Recently, nanoemulsions have been employed for different applications including food and drug industries for efficient nutrient delivery system. In this study, vitamin D (a lipophilic molecule) was encapsulated in fish oil for higher oral bioavailability. The oil-in-water nanoemulsion was formulated by ultrasonication technique with a droplet size range of 300–450 nm and a shelf life of more than 90 days. The influence of oil, water and surfactant concentration was investigated by phase diagram. The formulated nanoemulsion had encapsulation efficiency in the range of 95.7–98.2%. Further, nanoemulsion passed through simulated gastro-intestinal tract revealed an increased bioavailability than non-encapsulated vitamin. Thus, the formulation can be used as a drug delivery vehicle for various lipophilic compounds. Till date, no one have fabricated an efficient nano-vehicle for the delivery of vitamin D as well as analyzed the efficient delivery system in simulated GI-tract, this is first of its kind study in this regard. This can be scaled up further after analyzing the safety aspects.     

Au–Pt bimetallic nanoparticles supported on nest-like MnO2: synthesis and application in HCHO decomposition

Major research issues in oral protein delivery include the stabilization of protein in delivery devices which could increase its oral bioavailability. The study deals with development of oral insulin delivery system utilizing biodegradable poly(lactic-co-glycolic acid) (PLGA) nanoparticles and modifying its surface with Concanavalin A to increase lymphatic uptake. Surface-modified PLGA nanoparticles were characterized for conjugation efficiency of ligand, shape and surface morphology, particle size, zeta potential, polydispersity index, entrapment efficiency, and in vitro drug release. Stability of insulin in the developed formulation was confirmed by SDS-PAGE, and integrity of entrapped insulin was assessed using circular dichroism spectrum. Ex vivo study was performed on Wistar rats, which exhibited the higher intestinal uptake of Con A conjugated nanoparticles. In vivo study performed on streptozotocin-induced diabetic rats which indicate that a surface-modified nanoparticle reduces blood glucose level effectively within 4?h of its oral administration. In conclusion, the present work resulted in successful production of Con A NPs bearing insulin with sustained release profile, and better absorption and stability. The Con A NPs showed high insulin uptake, due to its relative high affinity for non-reducing carbohydrate residues i.e., fucose present on M cells and have the potential for oral insulin delivery in effective management of Type 1 diabetes condition.     

仿生技术在转基因大豆中镍形态分析和生物可给性评价中的应用

转基因的食品安全问题一直是科学家和公众关注的焦点,其微量元素的生物可给性研究可为转基因食品的安全评价提供参考。以“胃肠仿生消化、肠道微生物代谢、脂质体仿生物膜亲合吸附”构建胃肠功能模型,用于大豆(转基因大豆和普通大豆)的样品前处理,以脂质体亲合态、水溶态界定消化食糜中镍化合物的形态, 以人体可吸收部分的脂质体亲合态评价大豆中镍的生物可给性。经胃肠消化和微生物代谢,大豆食糜中镍配合物以水溶态为主;胃肠消化、肠道微生物代谢均对镍配合物的生物可给性起促进作用;转基因大豆和普通大豆中镍的生物可给性分别为4.1%和3.3%,即大豆转基因后镍生物可给性提高24%;但转基因大豆中脂质体结合态镍含量122.3 ng·g-1,仅为普通大豆的36%。     

Ionic liquid-assisted synthesis of carbon nanotube/platinum nanocomposites

A novel solution-enhanced dispersion by supercritical CO₂ (SEDS) was employed to prepare silk fibroin (SF) nanoparticles. The resulting SF nanoparticles exhibited a good spherical shape, a smooth surface, and a narrow particle size distribution with a mean particle diameter of about 50?nm. The results of X-ray powder diffraction, thermo gravimetry-differential scanning calorimetry, and Fourier transform infrared spectroscopy analysis of the SF nanoparticles before and after ethanol treatment indicated conformation transition of SF nanoparticles from random coil to ??-sheet form and thus water insolubility. The MTS assay also suggested that the SF nanoparticles after ethanol treatment imposed no toxicity. A non-steroidal anti-inflammatory drug, indomethacin (IDMC), was chosen as the model drug and was encapsulated in SF nanoparticles by the SEDS process. The resulting IDMC?CSF nanoparticles, after ethanol treatment, possessed a theoretical average drug load of 20%, an actual drug load of 2.05%, and an encapsulation efficiency of 10.23%. In vitro IDMC release from the IDMC?CSF nanoparticles after ethanol treatment showed a significantly sustained release over 2?days. These studies of SF nanoparticles indicated the suitability of the SF nanoparticles prepared by the SEDS process as a biocompatible carrier to deliver drugs and also the feasibility of using the SEDS process to reach the goal of co-precipitation of drug and SF as composite nanoparticles for controlled drug delivery.     

Drug nanocrystals for the formulation of poorly soluble drugs and its application as a potential drug delivery system

Formulation of poorly soluble drugs is a general intractable problem in pharmaceutical field, especially those compounds poorly soluble in both aqueous and organic media. It is difficult to resolve this problem using conventional formulation approaches, so many drugs are abandoned early in discovery. Nanocrystals, a new carrier-free colloidal drug delivery system with a particle size ranging from 100 to 1000 nm, is thought as a viable drug delivery strategy to develop the poorly soluble drugs, because of their simplicity in preparation and general applicability. In this article, the product techniques of the nanocrystals were reviewed and compared, the special features of drug nanocrystals were discussed. The researches on the application of the drug nanocrystals to various administration routes were described in detail. In addition, as introduced later, the nanocrystals could be easily scaled up, which was the prerequisite to the development of a delivery system as a market product.     

Development of polymethacrylate nanospheres as targeted delivery systems for catechin within the gastrointestinal tract

In this study, pH-sensitive nanospheres were fabricated using a polymethacrylate-based copolymer to encapsulate, protect, and release catechin, and thereby overcome its poor water solubility and low oral bioaccessibility. The polymer used was a polymethacrylic acid-co-ethyl acrylate 1:1 copolymer that dissolves above pH 5.5, and so can be used to retain and protect bioactives within the stomach but releases them in the small intestine. Catechin-loaded nanospheres were fabricated using the solvent displacement method. Physicochemical characterization of the nanospheres indicated that they were relatively small (d = 160 nm) and had a high negative charge (ζ = ? 36 mV), which meant that they had good stability to aggregation under physiological conditions (pH 7.2). Catechin was trapped within the nanospheres at an encapsulation efficiency of about 51% in an amorphous state. A simulated gastrointestinal study showed that catechin was slowly released under gastric conditions (pH 2.5), but rapidly released under small intestine conditions (pH 7.2). The observed improvement in the antioxidant activity and bioaccessibility of catechin after encapsulation was attributed to the fact that it was in an amorphous state and had good water dispersibility. This study provides useful information for the formulation of novel delivery systems to improve the dispersibility, bioaccessibility, and bioactivity of catechin and potentially other active components. These delivery systems could be used to improve the efficacy of bioactive components in foods, supplements, and pharmaceutical products.     

Gold nanoflowers with mesoporous silica as “nanocarriers” for drug release and photothermal therapy in the treatment of oral cancer using near-infrared (NIR) laser light

In this experiment, we successfully developed nanocarriers in the form of gold nanoflowers coated with two layers of silica for the purposes of drug loading and NIR (near-infrared) photothermal therapy for the treatment of oral cancer. The gold nanoflowers converted NIR laser energy into heat energy. The cores were coated with a thin silica layer (AuNFs@SiO₂) to protect the gold nanoflowers from intraparticle ripening. The second layer was mesoporous silica (AuNFs@SiO₂@mSiO₂), which acted as a nanocarrier for anticancer drug (DOX) loads. The mean effective diameter of the nanoparticles was approximately 150–200 nm, whereas the peak absorption of the AuNFs was 684 nm. After the AuNFs were encapsulated by the silica shells, the plasmonic absorption peak of AuNFs@SiO₂ and AuNFs@SiO₂@mSiO₂ exhibited a red shift to 718 nm. When exposed to an 808 nm NIR laser, these crystals showed an obvious photothermal conversion in the NIR region and a highly efficient release of DOX. Biocompatibility was assessed in vitro using Cell Counting Kit-8 assays, and the results showed that the nanocarriers induced no obvious cytotoxicity. This nanomaterial could be considered a new type of material that shows promising potential for photothermal-chemotherapy against malignant tumours, including those of oral cancers.     

RSM and ANN modeling-based optimization approach for the development of ultrasound-assisted liposome encapsulation of piceid

Piceid, a naturally occurring derivative of resveratrol found in many plants, has recently been considered as a potential nutraceutical. However, its poorly water-soluble property could cause a coupled problem of biological activities concerning drug dispersion and absorption in human body, which is still unsolved now. Liposome, a well-known aqueous carrier for water-insoluble ingredients, is commonly applied in drug delivery systems. In this study, a feasible approach for solving the problem is that the targeted piceid was encapsulated into a liposomal formula as aqueous substrate to overcome its poor water-solubility. The encapsulation process was assisted by ultrasound, with investigation of lipid content, ultrasound power and ultrasound time, for controlling encapsulation efficiency (E.E%), absolute loading (A.L%) and particle size (PS). Moreover, both RSM and ANN methodologies were further applied to optimize the ultrasound-assisted encapsulation process. The data indicated that the most important effects on the encapsulation performance were found to be of lipid content followed by ultrasound time and ultrasound power. The maximum E.E% (75.82%) and A.L% (2.37%) were exhibited by ultrasound assistance with the parameters of 160 mg lipid content, ultrasound time for 24 min and ultrasound power of 90 W. By methodological aspects of processing, the predicted E.E% and A.L% were respectively in good agreement with the experimental results for both RSM and ANN. Moreover, RMSE, R² and AAD statistics were further used to compare the prediction abilities of RSM and ANN based on the validation data set. The results indicated that the prediction accuracy of ANN was better than that of RSM. In conclusion, ultrasound-assisted liposome encapsulation can be an efficient strategy for producing well-soluble/dispersed piceid, which could be further applied to promote human health by increased efficiency of biological absorption, and the process of ultrasound-mediated liposome encapsulation can be well established by a methodological approach using either RSM or ANN, but it is worth mentioning that the ANN model used here showed the superiority over RSM for predicting and optimizing encapsulation.     

Ultrasound influence on the solubility of solid dispersions prepared for a poorly soluble drug

Solid dispersions have been successfully used to enhance the solubility of several poorly water soluble drugs. Solid dispersions are produced by melting hydrophilic carriers and mixing in the poorly water soluble drug. Supersaturation is obtained by quickly cooling the mixture until it solidifies, thereby entrapping the drug. The effects of using ultrasound to homogenize the molten carrier and drug mixture were studied. In particular, the increase in drug solubility for the resulting solid dispersions was analyzed. Piroxicam, which has very low water solubility, was used as a model drug. A full factorial design was used to analyze how sonication parameters affected the solubility and in vitro release of the drug. The results show that the use of ultrasound can significantly increase the solubility and dissolution rate of the piroxicam solid dispersion. Pure piroxicam presented a solubility of 13.3 μg/mL. A maximum fourfold increase in solubility, reaching 53.8 μg/mL, was observed for a solid dispersion sonicated at 19 kHz for 10 min and 475 W. The in vitro dissolution rate test showed the sonicated solid dispersion reached a maximum rate of 18%/min, a sixfold increase over the piroxicam rate of 2.9%/min. Further solid state characterization by thermal, X-ray diffraction and Fourier transform infrared analyses also showed that the sonication process, in the described conditions, did not adversely alter the drug or significantly change its polymorphic form. Ultrasound is therefore an interesting technique to homogenize drug/carrier mixtures with the objective of increasing the solubility of drugs with poor water solubility.     

Identification of furo[3′, 2′:3,4]naphtho[1,2-d]imidazole derivatives as orally active and selective inhibitors of microsomal prostaglandin E2 synthase-1 (mPGES-1)

This study describes the synthesis and anti-inflammatory effects of furo[3', 2':3,4]naphtho[1,2-d] imidazole derivatives. Among these furo[3', 2':3,4]naphtho[1,2-d]imidazole derivatives, 2-(4-methoxyphenyl)furo [3', 2':3,4]naphtho[1,2-d]imidazole (12) exhibited a strong inhibitory activity against LPS-induced PGE(2) production, with an IC(50) value of 47?nM. Compound 12 is then further examined for its inhibitory effects in the protein expression of COX-2 and microsomal prostaglandin E(2) synthase-1 (mPGES-1) in Raw 264.7 cells. Our results indicate that compound 12 was capable against inhibiting LPS-induced mPGES-1 protein expression at a concentration of 1.0?μM and no inhibitory effect in COX-2 expression. The sepsis-induced PGE(2) production in rat serum decreased ~250% by the pretreatment of 12 at 10?mg/kg. These results are especially important since compound 12 exhibited good oral bioavailability (72%) and was not cytotoxic at a concentration of 10.0?μM. Therefore, compound 12 is a highly selective mPGES-1 inhibitor that can serve as a lead for the development of novel oral anti-inflammatory drug candidates.     

Preparation,characterization, and biological activity of Cinnamomum cassia essential oil nano-emulsion

To solve the problems of low bioavailability and unstable properties of Cinnamomum cassia Essential oil (CCEO), encapsulation technology was introduced as an effective means to improve its shortcomings. In this study, Cinnamomum cassia Essential oil nano-emulsion (CCEO-NE) was successfully synthesized by the oil-in-water method and characterized by standard analytical methods, including dynamic light scattering (DLS), Scanning electron microscopy (SEM), and Transmission electron microscopy (TEM). The results show that the synthesized CCEO is spherical, smooth in surface, and uniform in shape, with an average particle size of 221.8 ± 1.95 nm, which is amorphous. In this experiment, by simulating the digestion of CCEO-NE in the gastrointestinal tract, it was found that CCEO-NE was undigested in the oral cavity, mainly in the stomach, followed by the small intestine. By understanding the digestion of CCEO-NE, we can improve the potential of CCEO bioavailability in food and drug applications. In addition, through the study of ABTS and DPPH free radicals by CCEO and CCEO-NE, it was found that the antioxidant activity of CCEO-NE was more potent than that of CCEO. When the concentration of CCEO-NE and CCEO is 400 μg/mL, the DPPH free radical scavenging rate is 92.03 ± 0.548% and 80.46 ± 5.811%, respectively. In comparison, ABTS free radical scavenging rate is 90.35 ± 0.480% and 98.44 ± 0.170% when the concentration of CCEO- NE, and CCEO is 75 μg/mL, respectively. The antibacterial test shows that CCEO-NE can inhibit both Gram-positive and Gram-negative bacteria. Among them, CCEO-NE has a stronger antibacterial ability than CCEO, and the maximum inhibition zone diameter of CCEO can reach 15 mm, while that of CCEO-NE can reach 18 mm. Meanwhile, SEM and TEM showed that CCEO-NE treatment destroyed the ultrastructure of bacteria. Generally speaking, we know the situation of CCEO in the gastrointestinal tract. CCEO-NE has more potent antioxidant and antibacterial ability than CCEO. Our research results show that whey protein is an effective packaging strategy that can improve the effectiveness, stability, and even bioavailability of CCEO in various applications, including food and health care industries.