Controlling release of astaxanthin in ß-sitosterol oleogel-based emulsions via different self-assembled mechanisms and composition of the oleogelators.

In this study, three types of ß-sitosterol-based oleogels (ß-sitosterol + Î³-oryzanol oleogels, ß-sitosterol + lecithin, oleogels and ß-sitosterol + monostearate oleogels), loaded with astaxanthin, were employed as the oil phase to create oleogel-based emulsions (SO, SL, and SM) using high-pressure homogenization. The microstructure revealed that fine-scale crystals were dispersed within the oil phase of the droplets in the ß-sitosterol oleogel-based emulsion. The bioaccessibility of astaxanthin was found to be 58.13 %, 51.24 %, 36.57 %, and 45.72 % for SM, SL, SO, and the control group, respectively. Interestingly, the release of fatty acids was positively correlated with the availability of astaxanthin (P = 0.981). Further analysis of FFAs release and kinetics indicated that the structural strength of the oil-phase in the emulsions influenced the degree and rate of lipolysis. Additionally, the micellar fraction analysis suggested that the nature and composition of the oleogelators in SM and SL also impacted lipolysis and the bioaccessibility of astaxanthin. Furthermore, interfacial binding of lipase and isothermal titration calorimetry (ITC) measurements revealed that the oleogel network within the oil phase of the emulsion acted as a physical barrier, hindering the interaction between lipase and lipid. Overall, ß-sitosterol oleogel-based emulsions offer a versatile platform for delivering hydrophobic molecules, enhancing the bioavailability of active compounds, and achieving sustained release.

Formulation design and characterization of silymarin liposomes for enhanced antitumor activity.

Liposomes, a nanoscale carrier, plays an important role in the delivery of drug, affects the in vivo efficacy of drugs. In this paper, silymarin(SM)-loaded liposomes was optimized using the response surface method (RSM), with entrapment efficiency (EE%) as an index. The formulation was optimized as follow: lecithin (7.8mg/mL), SM/lecithin (1/26) and lecithin/cholesterol (10/1). The optimized SM liposomes had a high EE (96.58 ±3.06%), with a particle size of 290.3 ±10.5nm and a zeta potential of +22.98 ±1.73mV. In vitro release tests revealed that SM was released in a sustained-release manner, primarily via diffusion mechanism. In vitro cytotoxicity studies demonstrated that the prepared SM liposomes had stronger inhibitory effects than the model drug. Overall, these results indicate that this liposome system is suitable for intravenous delivery to enhance the antitumor effects of SM.

Chitosan lecithin nanocomposite based electrochemical biosensor for glycine detection in biological matrices.

Increased glycine concentrations are associated with altered metabolism of cancer cells and is reflected in the bodily fluids of the brain cancer patients. Various studies have been conducted in past to detect glycine as an imaging biomarker via NMR Spectroscopy tools. However, the use is limited because of the low concentration and different in vivo detection due to overlapping of peaks with myo-inositol in same spectral position. Alongside, little is known about the electrochemical potential of Glycine as a biomarker for brain cancer. The prime impetus of this study was to check the feasibility of glycine as non-invasive biomarker for brain cancer. A divergent approach to detect glycine "non-enzymatically" via unique chitosan lecithin nanocomposite has been utilised during this study. The electrochemical inactivity at provided potential that prevented glycine to get oxidized or reduced without mediator was compensated utilising the chitosan-lecithin nanocomposite. Thus, a redox mediator (Prussian blue) was used for high sensitivity and indirect detection of glycine. The chitosan nanoparticles-lecithin nanocomposite is used as a matrix. The electrochemical analysis of the onco-metabolomic biomarker (glycine) utilizing cyclic voltammetry in glycine spiked multi-Purpose artificial urine was performed to check distribution of glycine over physiological range of glycine. A wide linear range of response varying over the physiological range from 7 to 240 µM with a LOD 8.5 µM was obtained, showing potential of detection in biological samples. We have further evaluated our results via simulating the interaction of mediator and matrix with Glycine by HOMO-LUMO band fluctuations.

Polyglycerol polyricinoleate and lecithin stabilized water in oil nanoemulsions for sugaring Beijing roast duck: Preparation, stability mechanisms and color improvement.

Traditional Beijing roast duck often suffers from uneven color and high sugar content after roasting. Water-in-oil (W/O) nanoemulsion is a promising alternative to replace high concentration of sugar solution used in sugaring process according to similarity-intermiscibility theory. Herein, 3% of xylose was embedded in the aqueous phase of W/O emulsion to replace 15% maltose solution. W/O emulsions with different ratios of lecithin (LEC) and polyglycerol polyricinoleate (PGPR) were constructed by high-speed homogenization and high-pressure homogenization. Distribution and penetration extent of solutions and emulsions through the duck skin, as well as the color uniformity of Beijing roast duck were analyzed. Emulsions with LEC:PGPR ratios of 1:3 and 2:2 had better stability. Stable interfacial film and spatial structure were important factors influencing emulsion stabilization. The stable W/O emulsions could more uniformly distribute onto the surface of duck skin and longitudinally penetrate through the skin than solutions.

Subcritical water-assisted fish gelatin hydrolysis for astaxanthin-loaded fish oil emulsion stability.

Though gelatin emulsifying properties have been intensively studied, how low-molecular-weight (LMW) fish gelatin affects astaxanthin (AST)-loaded fish oil emulsion stability remains elusive. In this study, subcritical water hydrolysis (SWH)-modified LMW fish gelatin (SWHG) was produced from 110 °C to 180 °C and used to enhance the AST steadiness in oil/water emulsions in the presence of an emulsifier, lecithin. In the prepared emulsions, the surface charge increased while droplet size decreased with the decrease in gelatin MW due to the reduced thickness of the adsorbed gelatin membrane. LMW gelatin and lecithin could form a firm-absorbed layer on the droplet surface by electrostatic interaction between amide groups of gelatin molecules and phosphate groups of lecithin, thus stabilizing the emulsions. SWHG improved the creaming stability of the emulsions and hindered the oxygen- and light-induced AST degradation for 11 months compared to high MW gelatin. Whereas, the control emulsion showed noticeable phase separation after two weeks of storage. These findings prove the advantage of the SWH approach and propose the use of SWHG in oil-in-water emulsions for AST stabilization.

Modulating edible-oleogels physical and functional characteristics by controlling their microstructure.

The influence of co-oleogelators like lecithin or hydrogenated lecithin together with the addition of dispersed water droplets to modulate the microstructure and thus the physical properties of glyceryl stearate (GS)-corn oil oleogels was investigated by thermal profile, microstructure, hardness, and oil binding capacity (OBC). The addition of ß-carotene (ßC) was also assessed. With lecithin, crystallization and melting temperatures were reduced, resulting in less-ordered crystal networks with a lower hardness and OBC, while with hydrogenated lecithin, the opposite effect was observed. In the presence of water, oleogels became harder but more brittle. Finally, ßC acted as a crystal modifier increasing the hardness and OBC in the presence of lecithin, but decreased these parameters in hydrogenated lecithin-containing and water-filled oleogels. This study provides a better understanding on how the composition of GS-based oleogels can affect their physical properties.

Design, development, and evaluation of CDK-4/6 inhibitor loaded 4-carboxy phenyl boronic acid conjugated pH-sensitive chitosan lecithin nanoparticles in the management of breast cancer.

Our main aim to design and develop a novel 4-carboxy phenyl boronic acid (4-CPBA) conjugated Palbociclib (PALB) loaded pH-sensitive chitosan lipid nanoparticles (PPCL) to enhance the anti-cancer efficacy of the PALB in in-vitro cell line studies by loading into 4-CPBA conjugated chitosan lipid nanoparticles. 4-CPBA was conjugated to chitosan by carbodiimide chemistry and formation of conjugate was confirmed by 1HNMR, ATR-FTIR spectroscopic techniques. Ionic-gelation method was used for the fabrication of PPCL and particles size, PDI, zeta potential were found to be 226.5 ± 4.3 nm, 0.271 ± 0.014 and 5.03 ± 0.42 mV. Presence of pH-sensitive biological macromolecule i.e. chitosan in the carrier system provides pH-sensitivity to PPCL and sustainedly released the drug upto 144 h. The PPCL exhibited approximately 7.2, 6.6, and 5-fold reduction in IC50 values than PALB in MCF-7, MDA-MB-231 and 4T1 cells. Receptor blocking assay concluded that the fabricated nanoparticles were internalized into MCF-7 cells might be through sialic acid-mediated endocytosis. PPCL caused extensive mitochondrial depolarization, enhanced ROS generation, apoptosis (DAPI nuclear staining, acridine orange/ ethidium bromide dual staining), and reduced % cell migration than pure PALB. It was concluded that the hybrid lipid-polymer nanoparticles provides an optimistic approach for the treatment of breast cancer.

Surfactant-free oleogel-based emulsion stabilized by co-assembled ceramide/lecithin crystals with controlled digestibility.

BACKGROUND: There is increasing interest in the development of oleogel-based emulsions. However, they usually contained surfactants for stabilization, especially small-molecular weight surfactants, which may have adverse health impacts. RESULTS: Herein, a surfactant-free oleogel-based emulsion stabilized by co-assembled ceramide/lecithin (CER/LEC) crystals was developed. The formation and stabilization mechanisms were explored. The different molar ratios of gelator (LEC and CER) in emulsions resulted in different crystal morphology, crystallinity as well as different emulsion properties. This suggested that appropriate crystallinity, crystal size, and interfacial distribution of these crystals provided higher surface coverage against droplets coalescence, thus better emulsion stabilization. Both X-ray diffractograms and contact angle results confirmed that the crystals which were primarily responsible for emulsion stabilization, are co-assembled crystals consisted of both gelators (CER and LEC). Furthermore, the percentage of free fatty acids (FFAs%) results revealed a negative relationship between lipid digestibility and crystal concentration. CONCLUSIONS: This strategy greatly enriched surfactant-free oleogel-based emulsion formulations, as well as their potential applications in healthy lipid-based products and novel food delivery systems with controlled lipid digestibility. © 2022 Society of Chemical Industry.

Fabrication and characterization of nanoemulsions for encapsulation and delivery of vitexin: antioxidant activity, storage stability and in vitro digestibility.

BACKGROUND: Nanoemulsions were prepared as an encapsulation and delivery system for vitexin, a poorly water-soluble antioxidant. This study evaluated how the type and concentration of the dispersed oil phase and vitexin loading impacted droplet characteristics and nanoemulsion stability. The influences of storage temperature on antioxidant activity and in vitro gastrointestinal digestion on nanoemulsion stability were also investigated. RESULTS: Nanoemulsions prepared at different dispersed oil concentrations showed diverse characteristics and stability. Highest stability against droplet aggregation and phase separation with small oil droplets (< 150 nm) was observed for nanoemulsions prepared using 300 g kg-1 medium-chain triglyceride oil. These nanoemulsions are able to entrap and deliver vitexin with high encapsulation efficiency (88-90%) with no significant effect on emulsion stability. Vitexin-loaded nanoemulsions were stable during storage when refrigerated (4 °C) and at room temperature (25 °C) for up to 45 days with no effect on their antioxidant activity. Significantly delayed lipolysis rate and decreased extent of lipid digestion were observed in vitexin-loaded nanoemulsions. CONCLUSIONS: Stable vitexin-loaded nanoemulsions were successfully produced by high-pressure homogenization using a mixture of Tween 80 and lecithin as emulsifiers. Vitexin-loaded nanoemulsions stabilized with a mixture of these two emulsifiers were effective in retaining antioxidant activity during storage and protecting vitexin from changes during gastrointestinal digestion. Our results suggested that nanoemulsions were effective vitexin delivery systems for food applications. © 2022 Society of Chemical Industry.

Physical, morphological and storage stability of clove oil nanoemulsion based delivery system.

Clove oil based Nanoemulsions (NE) were prepared ultrasonically using Tween 80 and soy lecithin as synthetic and natural surfactants, respectively. The developed NEs were characterized for various parameters (particle size, polydispersity index, zeta potential, morphology, viscosity, colour, turbidity and pH) and the comparative effect of both the surfactants at variable levels (oil:tween 80-1:1, 1:2, 1:3 and 1:4 and oil: soy lecithin- 1:1, 1:1.5 and 1:2) was assessed. It was found that the type of surfactant and oil to surfactant ratio significantly affected particle size and stability of NEs. The NE prepared using tween 80 @1:3 had smallest average droplet diameter (40.9 nm). The formulated NEs were stored at 25 °C and 4 °C and analyzed for turbidity, pH and phase separation up to 90 days. Results revealed that the type and concentration of the surfactant significantly influenced the particle size and stability of NEs. NEs prepared using tween 80 were found to be more viscous than those prepared with soy lecithin. The prepared clove oil NEs have important implication to be used as a natural delivery system to increase the shelf life of food products.

Sugar-sugar interactions in oil suspensions containing surfactants and effects on macroscopic phenomena.

Surfactants are used in confectionery production to control the viscosity and yield value of molten chocolate. To develop a deeper understanding of the structure-function relationship of surfactants in food-related particle suspensions, the apparent viscosity, yield value, sedimentation, and particle interactions of 10 wt% confectioner's sugar-in-canola oil suspensions were investigated in the presence of up to 1 wt% commercial soy lecithin, polyglycerol polyricinoleate (PGPR), citric acid esters of monoacylglycerols (CITREM) or ammonium phosphatides (AMP). Atomic force microscopy (AFM) was used to measure attractive forces at the nano-Newton scale between a sugar substrate and a sugar crystal-functionalized AFM cantilever in an oil environment. For all but PGPR, addition of surfactant reduced the adhesion force between sugar surfaces up to a critical concentration above which the force increased, implying the presence of additional interactions. This critical concentration was assumed to be when monolayer coverage of the sugar surfaces by surfactant occurred (0.05 wt% for lecithin, 0.10 wt% for CITREM and AMP). No critical concentration was found for PGPR, with its greatest effect for each analysis occurring at the highest concentrations tested (0.60 and 1.00 wt%). The significance of these interactions on macroscopic phenomena such as apparent viscosity and sedimentation was also assessed. Like with the AFM data, there was an optimal concentration of added surfactant above which viscosity increased. Sedimentation rate greatly decreased with addition of PGPR while being only slightly affected by addition of lecithin, CITREM and AMP. An argument regarding their efficacy was made based on the relative sizes of the polar headgroup and nonpolar tail groups of the molecules, which contributed to how they adsorbed to the sugar surface. Overall, these results suggested that surfactant properties such as molecular weight and head group properties played an important role in modifying the interactions between sugar crystals in an oil-continuous environment.

Middle purity soy lecithin is appropriate for food grade nanoliposome: Preparation, characterization, antioxidant and anti-inflammatory ability.

The purity of soy lecithin exerts significant impact on nanoliposome (NL) properties for food applications. In this study, three soy lecithin of different purity were used to prepare NL. LC-MS analysis confirmed soy lecithin of relatively low purify (50% and 70%) contains multiple natural phospholipids. NL produced by soy lecithin of middle purity (70%) is smaller and more stable than other counterparts. Ultimately, soy lecithin of 70% purity was selected to develop NL encapsulated crocetin (CR) as model payload and further coated by chitosan (CS). The structure characteristic, physicochemical properties, antioxidant activity and anti-inflammatory activity of crocetin nanoliposome (CR-NL) and chitosan coated crocetin nanoliposome (CS-CR-NL) were evaluated. NL encapsulation and CS coating significantly improve antioxidant and anti-inflammatory ability of CR, and prolong storage period of CR (p < 0.05). For food applications, soy lecithin of middle purity (70%) is cheaper and more appropriate than soy lecithin of high purity.

The Influence of Tea Tree Oil on Antifungal Activity and Pharmaceutical Characteristics of Pluronic® F-127 Gel Formulations with Ketoconazole.

Fungal skin infections are currently a major clinical problem due to their increased occurrence and drug resistance. The treatment of fungal skin infections is based on monotherapy or polytherapy using the synergy of the therapeutic substances. Tea tree oil (TTO) may be a valuable addition to the traditional antifungal drugs due to its antifungal and anti-inflammatory activity. Ketoconazole (KTZ) is an imidazole antifungal agent commonly used as a treatment for dermatological fungal infections. The use of hydrogels and organogel-based formulations has been increasing for the past few years, due to the easy method of preparation and long-term stability of the product. Therefore, the purpose of this study was to design and characterize different types of Pluronic® F-127 gel formulations containing KTZ and TTO as local delivery systems that can be applied in cases of skin fungal infections. The influence of TTO addition on the textural, rheological, and bioadhesive properties of the designed formulations was examined. Moreover, the in vitro release of KTZ, its permeation through artificial skin, and antifungal activity by the agar diffusion method were performed. It was found that obtained gel formulations were non-Newtonian systems, showing a shear-thinning behaviour and thixotropic properties with adequate textural features such as hardness, compressibility, and adhesiveness. Furthermore, the designed preparations with TTO were characterized by beneficial bioadhesive properties. The presence of TTO improved the penetration and retention of KTZ through the artificial skin membrane and this effect was particularly visible in hydrogel formulation. The developed gels containing TTO can be considered as favourable formulations in terms of drug release and antifungal activity.

Formulation of liposomes loading lentisk oil to ameliorate topical delivery, attenuate oxidative stress damage and improve cell migration in scratch assay.

Pistacia lentiscus L. is a sclerophyllous shrub capable of growing under harsh climatic conditions especially in the Mediterranean Basin. Different products can be obtained from this plant, such as essential oil, mastic gum or even fixed oil. The last is well known for its flavor which is mainly exploited in the food industry. Additionally, it has been traditionally used in the treatment of skin diseases, but, at the moment, any suitable formulation for skin delivery has been formulated and its biological effects was not deeply confirmed. Given that, in the present study, the lentisk oil has been formulated in liposomes at different concentrations (10, 20, 30 mg/ml) and their physicochemical, technological and main biological properties have been evaluated. Vesicles were prepared by using natural soy lecithin and a green and organic solvent free method, thus obtaining spherical, small (~ 118 nm), homogeneously dispersed (0.27) and highly negatively charged (~ -62 mV) vesicles. The used amount of oil loaded in liposomes (10, 20, 30 mg/ml) modulated the penetration ability of vesicles in the skin, favoring the deposition of the payload in the deeper strata. The loading in the vesicles potentiated the ability of oil to counteract the damaging effects caused by hydrogen peroxide in keratinocytes and fibroblasts and facilitate their migration in a cell monolayer lesion. Overall findings suggested that the incorporation of lentisk oil in liposomes made from soy lecithin can be an alternative and natural approach to exploit it in pharmaceutical ad cosmetical applications and manufacturing natural products suitable for the treatment of skin lesions.

Fabrication and characterization of ß-carotene emulsions stabilized by soy oleosin and lecithin mixtures with a composition mimicking natural soy oleosomes.

Natural soy oleosomes are known to have a remarkable stability, given the advantage of their sophisticated membrane. The aim of the present study is to examine the concept of fabricating a ß-carotene emulsion stabilized by soy oleosin (OLE) and lecithin (LEC) mixtures mimicking the membrane composition of soy oleosomes while providing preferable stability and bioaccessibility. For this, the fabricated emulsion was characterized in terms of droplet size distribution, and emulsion structure, stability and digestion (release and absorption of lipophilic ß-carotene). Compared to SPI/LEC (10 : 1) stabilized emulsions, the OLE/LEC (10 : 1) mixture stabilized emulsion exhibited the highest emulsifying activity index (EAI) and emulsifying stability index (ESI) values, and higher encapsulation efficiency. Results show that the ß-carotene emulsion stabilized by OLE and LEC mixtures at the ratio of 10 : 1 (w/w) has the most uniform droplet distribution and highest stability. The in vitro gastrointestinal digestion test revealed that the ß-carotene emulsion stabilized by OLE and LEC mixtures was digested more rapidly than the emulsion stabilized by soy protein isolate (SPI) and LEC mixtures. In turn, the bioaccessibility and cellular uptake of ß-carotene were enhanced, resulting in a higher absorption, a desirable feature of nutrition delivery systems. Our results demonstrated a promising way to fabricate emulsions mimicking natural soy oleosomes.

Oil-gelling properties of soy lecithin fractions.

Lecithin is a mixture of amphiphilic lipids with health benefits. In this study, four different fractions (ethanol soluble, ethanol insoluble, phospholipid and glycolipid fractions) from soy lecithin were obtained and evaluated as oleogelators. As with the parent lecithin, the ethanol insoluble fraction (EIF) was unable to function as an oleogelator. The ethanol soluble fraction (ESF) and phospholipid fraction (PLF) formed oleogels at 30% (wt%), while the glycolipid fraction (GLF) formed oleogels at 15%. ESF resulted in an oleogel with a similar appearance and microstructure, but a harder and less cohesive texture than the PLF-supported oleogel. The oleogels formed with GLF were different from those formed with ESF and PLF in appearance and microstructure. GLF at 20% formed an oleogel with better texture characteristics (in the light of hardness) and oil-holding capacity than those formed with 30% of ESF and PLF. This is the first study to investigate the oil-gelling properties of fractions from soy lecithin. Our results show that the naturally occurring glycolipids from soy lecithin exhibit great potential as oleogelators.

Hybrid chitosan-lipid nanoparticles of green tea extract as natural anti-cellulite agent with superior in vivo potency: full synthesis and analysis.

The aim of this work is to exploit the advantages of chitosan (CS) as a nanocarrier for delivery of anti-cellulite drug, green tea extract (GTE), into subcutaneous adipose tissue. Primarily, analysis of herbal extract was conducted via newly developed and validated UPLC method. Ionic gelation method was adopted in the preparation of nanoparticles where the effect lecithin was investigated resulting in the formation of hybrid lipid-chitosan nanoparticles. Optimal formula showed a particle size of 292.6 ± 8.98 nm, polydispersity index of 0.253 ± 0.02, zeta potential of 41.03 ± 0.503 mV and an entrapment efficiency percent of 68.4 ± 1.88%. Successful interaction between CS, sodium tripolyphosphate (TPP) and lecithin was confirmed by Fourier-transform infrared spectroscopy, differential scanning calorimetry and X-ray diffraction. Morphological examination was done using transmission electron microscope and scanning electron microscope confirmed spherical uniform nature of GTE load CS-TPP nanoparticles. Ex vivo permeation study revealed permeability enhancing activity of the selected optimal formula due to higher GTE deposition in skin in comparison to GTE solution. Moreover in vivo study done on female albino Wistar rats carried out for 21 days proved successful potential anti-cellulite activity upon its application on rats' skin. Histological examination showed significant reduction of adipocyte perimeter and area and fat layer thickness. Results of the current study demonstrated that the developed GTE-loaded CS-TPP nanoparticle comprised of chitosan and lecithin showed permeability enhancing activity along with the proven lipolytic effect of green tea represent a promising delivery system for anti-cellulite activity.

Metformin-loaded lecithin nanoparticles induce colorectal cancer cytotoxicity via epigenetic modulation of noncoding RNAs.

BACKGROUND: Colorectal cancer (CRC) is major aliment around the word, with a cumulative rate of mortality. Metformin (MT) was recently approved as anticancer drug against solid tumors, such as CRC. Resistance to MT therapy remains to be a challenging matter facing the development of possible anti-cancer strategy. To circumvent this problem, MT nano-encapsulation has been introduced to sensitize resistant cancer cells. The purpose of the current study is to explore the MT's aptitude encapsulated in lecithin (LC) and chitosan (CS) nanoparticles to inhibit CRC proliferation through modulations of long noncoding RNAs (lncRNAs), micro RNAs (miRNAs), and some biochemical markers. METHODS AND RESULTS: Cytotoxic screenings of the newly synthesized MT-based regimens; MT, MT-LC NPs (NP1), MT-CS NPs (NP2), and MT-LC-CS NPs (NP3) against colorectal cancerous Caco-2 and HCT116 cell lines versus normal WI-38 cells were performed. The epigenetic mechanistic effects of these proposed regimens on lncRNAs and miRNAs were investigated. Additionally, some protein levels were assessed in CRC cells upon treatments; YKL-40, PPARγ, E-cadherin (ECN), and VEGF. We resulted that NP1 recorded the highest significant cytotoxic effect on CRC cells. HCT116 cells were more sensitive to the NP1 compared to Caco-2 cells. Intriguingly, it was suggested that NP1 tackled the CRC cells through down-regulation of the H19, HOTTIP, HULC, LINC00641, miR-200, miR-92a, miR-21, YKL-40, PPARγ, and VEGF expressions, as well as up-regulation of the miR-944 and ECN expressions. CONCLUSIONS: We concluded that the NP1 can potentially be cytotoxic to CRC cells in-vitro by modulating noncoding RNA.

Electro-hydrodynamic assisted synthesis of lecithin-stabilized peppermint oil-loaded alginate microbeads for intestinal drug delivery.

Peppermint oil (PO) is the most prominent oil using in pharmaceutical formulations with its significant therapeutic value. In this sense, this oil is attracting considerable attention from the scientific community due to its traditional therapeutic claim, biological and pharmacological potential in recent research. An organic solvent-free and environment-friendly electrohydrodynamic assisted (EHDA) technique was employed to prepared PO-loaded alginate microbeads. The current study deals with the development, optimization, in vitro characterization, in vivo gastrointestinal tract drug distribution and ex-vivo mucoadhesive properties, antioxidant, and anti-inflammatory effects of PO-loaded alginate microbeads. The optimization results indicated the voltage and flow rate have a significant influence on microbeads size and sphericity factor and encapsulation efficiency. All these optimized microbeads showed a better drug release profile in simulated intestinal fluid (pH 6.8) at 2 h. However, a minor release was found in acidic media (pH 1.2) at 2 h. The optimized formulation showed excellent mucoadhesive properties in ex-vivo and good swelling characterization in intestine media. The microbeads were found to be well distributed in various parts of the intestine in in vivo study. PO-loaded alginate microbeads similarly showed potential antioxidant effects with drug release. The formulation exhibited possible improvement of irritable bowel syndrome (IBS) in MO-induced rats. It significantly suppressed proinflammatory cytokines, i.e., interleukin- IL-1ß, and upregulated anti-inflammatory cytokine expression, i.e., IL-10. It would be a promising approach for targeted drug release after oral administration and could be considered an anti-inflammatory therapeutic strategy for treating IBS.

Preparation of Catechin Nanoemulsion from Oolong Tea Leaf Waste and Its Inhibition of Prostate Cancer Cells DU-145 and Tumors in Mice.

Anti-cancer activity of catechin nanoemulsions prepared from Oolong tea leaf waste was studied on prostate cancer cells DU-145 and DU-145-induced tumors in mice. Catechin nanoemulsions composed of lecithin, Tween-80 and water in an appropriate proportion was prepared with high stability, particle size of 11.3 nm, zeta potential of -67.2 mV and encapsulation efficiency of 83.4%. Catechin nanoemulsions were more effective than extracts in inhibiting DU-145 cell growth, with the IC50 being 13.52 and 214.6 µg/mL, respectively, after 48 h incubation. Furthermore, both catechin nanoemulsions and extracts could raise caspase-8, caspase-9 and caspase-3 activities for DU-145 cell apoptosis, arresting the cell cycle at S and G2/M phases. Compared to control, catechin nanoemulsion at 20 µg/mL and paclitaxel at 10 µg/mL were the most effective in reducing tumor volume by 41.3% and 52.5% and tumor weight by 77.5% and 90.6% in mice, respectively, through a decrease in EGF and VEGF levels in serum.