Regulation of the colon-targeted release rate of lactoferrin by constructing hydrophobic ethyl cellulose/pectin composite nanofibrous carrier and its effect on anti-colon cancer activity.

In order to modify colonic release behavior of lactoferrin (Lf), a hydrophobic composite nanofibrous carrier (CNC) was constructed by emulsion coaxial electrospinning. Ethylcellulose/pectin based water-in-oil emulsion and Lf-contained polyvinyl alcohol solution were used as shell and core fluids, respectively. An electrospinning diagram was first constructed to screen out suitable viscosity (51-82 cP) and conductivity (960-1300 µS/cm) of the dispersed phase of pectin solution for successful electrospinning of shell emulsion. Varying mass fraction of pectin solution (5 %-20 %) of shell emulsion during emulsion coaxial electrospinning obtained CNCs with different micro-structures, labeled as 5&95 CNC, 10&90 CNC, 15&85 CNC, 20&80 CNC. These CNCs all achieved colonic delivery of Lf (>95 %), and the time for complete release of Lf in simulated colon fermentation process were 10, 7, 5 and 3 h, respectively. That is, the greater the pectin content in CNC, the faster the release rate of stabilized Lf in colon. Lf release in simulated colon fermentation fluid involved complex mechanisms, in which diffusion release of Lf was dominant. Increasing colonic release rate of Lf enhanced its regulation effect on the expression levels of cell cycle arrest and apoptosis-related protein and promote its effective inhibition on the proliferation of HCT116 cell.

Synthesis of hydroxyethylcellulose phthalate-modified silver nanoparticles and their multifunctional applications as an efficient antibacterial, photocatalytic and mercury-selective sensing agent.

Water contamination by several aquatic pollutants such as dyes, heavy metal ions and microbes is a prevalent concern to health and environment. Thus, developing facile, economical, and eco-friendly strategies to tackle this problem have become paramount. Hence, this study reports the synthesis of hydroxyethylcellulose phthalate-capped silver nanoparticles (HEC-PA@AgNPs) using a simple sunlight-assisted route. The multifunctional applications of the synthesized particles as an efficient nanoprobe for the selective sensing of Hg2+ as well as their photocatalytic and antimicrobial activities were demonstrated. HEC-PA@AgNPs were systematically characterized by various advanced analytical techniques such as FTIR, UV-Vis spectroscopy, X-ray diffraction (XRD), zeta potential (ZP) and dynamic light scattering (DLS). The successful functionalization of AgNPs with HEC-PA was manifested using FTIR. SEM and XRD revealed the formation of spherical AgNPs with a face centered cubic structure and a crystallite size of 14 nm. The particles demonstrated a hydrodynamic size of 40 nm with a good colloidal stability as evidenced from the ZP value of -35 mV, suggesting the effective role of the negatively charged HEC-PA capping agent in stabilizing the NPs. HEC-PA@AgNPs exhibited fast naked-eye colorimetric detection, high selectivity, and sensitivity to Hg2+ in spiked real water samples over a wide range of pH (3-9) and temperatures (298-328 K), achieving a detection limit of 119 nM. The presence of other diverse metal ions didn't affect the specificity of the particles toward Hg ions. Further, the sensing mechanism is based on a characteristic redox reaction between Hg2+ and AgNPs. Further, HEC-PA@AgNPs showcased a more noxious antimicrobial activity to gram-positive bacteria (B. subtilis and S. aureus) than gram-negative bacteria (E. coli). Besides, AgNPs exhibited high photocatalytic potential under sunlight irradiation with a degradation efficiency of 79 % for methylene blue dye in only 80 min following pseudo-1st order kinetics with a rate constant of 0.019 min-1. The photocatalyst exhibited good reusability after five recycling runs. These results render our approach promising multifunctional analytical probe for environmental and biomedical applications.

Electrospun Tamarindus indica-loaded antimicrobial PMMA/cellulose acetate/PEO nanofibrous scaffolds for accelerated wound healing: In-vitro and in-vivo assessments.

In this work, Tamarindus indica (T. indica)-loaded crosslinked poly(methyl methacrylate) (PMMA)/cellulose acetate (CA)/poly(ethylene oxide) (PEO) electrospun nanofibers were designed and fabricated for wound healing applications. T. indica is a plant extract that possesses antidiabetic, antimicrobial, antioxidant, antimalarial and wound healing properties. T. indica leaves extract of different concentrations were blended with a tuned composition of a matrix comprised of PMMA (10 %), CA (2 %) and PEO (1.5 %), and were electrospun to form smooth, dense and continuous nanofibers as illustrated by SEM investigation. In vitro evaluation of T. indica-loaded nanofibers on normal human skin fibroblasts (HBF4) revealed a high compatibility and low cytotoxicity. T. indica-loaded nanofibers significantly increased the healing activity of scratched HBF4 cells, as compared to the free plant extract, and the healing activity was significantly enhanced upon increasing the plant extract concentration. Moreover, T. indica-loaded nanofibers demonstrated significant antimicrobial activity in vitro against the tested microbes. In vivo, nanofibers resulted in a superior wound healing efficiency compared to the control untreated animals. Hence, engineered nanofibers loaded with potent phytochemicals could be exploited as an effective biocompatible and eco-friendly antimicrobial biomaterials and wound healing composites.

Exposure to cellulose acetate films incorporated with garlic essential oil does not lead to homologous resistance in Listeria innocua ATCC 33090.

Essential oils (EOs) have been considered potential green additives for active food packaging. However, sub-lethal concentrations of EOs may lead to bacterial resistance, which is a concern. In this sense, the effects of 1% (GEO1) and 10% (GEO10) of garlic EO in cellulose acetate-based films regarding homologous resistance in Listeria innocua were investigated after incubation at 37 °C/24 h and 7 °C/10 d. The films were also characterized and tested on sliced mozzarella cheese as interfold packaging for 8-days storage at 7 °C. The EO did not alter the mechanical properties of the films nor their thermal degradation profile. However, GEO10 was less permeable to water vapor than GEO1. When tested against L. innocua, the incubation at 7 °C enhanced the films' antimicrobial effect: log reductions of 4.3 and 5.7 were obtained for GEO1 and GEO10, respectively. Moreover, 86.3% of L. innocua cells were injured at sub-lethal level when exposed to GEO10. Despite this, no occurrence of homologous resistance was found. When the active films were tested on cheese against the natural microbiota, they resulted in slices of mozzarella with fewer contaminants, however the reduction was not significant. Nevertheless, we considered this an important finding to the food industry since this work suggested that GEO is a safe active compound from the point of view of homologous resistance to be used against Listeria.

Bio-packaging based on cellulose acetate from banana pseudostem and containing Butia catarinensis extracts.

Banana (Musa acuminata) pseudostem cellulose was extracted and acetylated (CA) to prepare membranes with potential use as bio-packages. The CA membrane was embedded by Butia seed (CA-BS) or Butia pulp (CA-BP) extracts obtained from Butia catarinenses (Butia). The produced CA, CA-BS, and CA-BP membranes were evaluated for their physical-chemical, mechanical, thermal, and antibacterial properties. The process for obtaining the cellulose yielded a material with about 92.17% cellulose (DS = 2.85). The purity, cellulose degree acetylation, and the incorporation of Butia extracts into the membranes were confirmed by FTIR. The CA-BS and CA-BP membranes showed a smaller contact angle and higher swelling ratio than the CA membrane. Furthermore, Butia seed or pulp extracts reduced the elastic modulus and deformation at break compared to the CA membrane. The DSC analysis suggested the compatibility between sections and the CA matrix, whereas the TGA analysis confirmed the thermal stability of the membranes. Moreover, less than 1% of the Butia seed and pulp extracts were put into a food simulant media from the membrane. Finally, the CA-BS and CA-BP membranes could inhibit the growth of Staphylococcus aureus and Escherichia coli on their surface, confirming the potential use of these membranes as bio-packaging for food preservation.

Study on the antioxidative mechanism of tocopherol loaded ethyl cellulose particles in thermal-oxidized soybean oil.

Our previous study proposed preparation method of tocopherol (Toc) loaded ethyl cellulose (EC) particles as antioxidant due to instability of Toc under high temperature. The present study aimed to explore the antioxidant mechanism of loaded particles. Results showed that loaded particles prepared by EC of different viscosities (EC9, EC70, EC200) had antioxidative effect, and the antioxidant activity increased with EC viscosity. Fourier transform infrared analysis demonstrated that the interaction between EC and tocopherol was mainly hydrogen bond. Loaded particles retained effectively the thermal degradation of Toc and thus enhanced the antioxidant activity. Further investigation into thermal oxidation of EC inferred the possible antioxidative mechanism included two aspects. One was that Toc was fixed in the network structure of loaded particles formed by EC to provide a barrier for avoiding degradation. Another was that EC and Toc acted on different stages of lipid oxidation, playing the antioxidative effect together.

Deacetylated cellulose acetate nanofibrous dressing loaded with chitosan/propolis nanoparticles for the effective treatment of burn wounds.

Every year, about 1 out of 9 get burnt in Egypt, with a mortality rate of 37%, and they suffer from physical disfigurement and trauma. For the treatment of second-degree burns, we aim at making a smart bandage provided with control of drug release (using chitosan nanoparticles) to enhance the healing process. This bandage is composed of natural materials; namely, cellulose acetate (CA), chitosan, and propolis (bee resin) as the loaded drug. Cellulose acetate nanofibers were deacetylated by NaOH after optimizing the reaction time and the concentration of NaOH solution, and the product was confirmed with FTIR analysis. Chitosan/propolis nanoparticles were prepared by ion gelation method with size ranging from 100 to 200 nm and a polydispersity index of 0.3. Chitosan/propolis nanoparticles were preloaded in the CA solution to ensure homogeneity. Loaded deacetylated cellulose nanofibers have shown the highest hydrophobicity measured by contact angle. Cytotoxicity of propolis and chitosan/propolis nanoparticles were tested and the experimental IC50 value was about 137.5 and 116.0 µg/mL, respectively, with p-value ≤0.001. In addition, chitosan/propolis nanoparticles loaded into cellulose nanofibers showed a cell viability of 89.46% in the cell viability test. In-vivo experiments showed that after 21 days of treatment with the loaded nanofibers repairing of epithelial cells, hair follicles and sebaceous glands in the skin of the burn wound were found in albino-mice model.

Electrospun nanofiber based on Ethyl cellulose/Soy protein isolated integrated with bitter orange peel extract for antimicrobial and antioxidant active food packaging.

The present work was aimed to produce a novel bioactive nanofiber (NFs) based on Ethyl cellulose (EC), Soy protein isolated (SPI), and containing Bitter orange peel extract (BOPE) by electrospinning technology. The EC/SPI NFs were formulated with different weight ratios of 1:1, 2:1, and 1:2 denoted as ES11, ES21, and ES12, respectively, and investigated by several analyses. Based on the obtained results, the maximum hydrogen interactions between these two polymers, ES11 NFs offered a uniform morphology without bead with the diameter of 185.33 nm as a result of the compatibility of the polymer solutions of EC and SPI. Moreover, appropriate thermal stability was presented along with more porosity (78%), maximum water vapor transmission rate (657 g/m2.24h), good tensile stress (6.12 MPa), and acceptable water contact angel (82.3°). Therefore, ES11 NFs were selected as the optimal sample for incorporation of the BOPE as the antibacterial and antioxidant agent. According to the antioxidant activity test, the highest concentration (20% wt) of this extract increased the antioxidant activity of NF around 64.7% and also inhibited the growth of pathogenic bacteria (S. areus, and E. coli). Therefore, the ES11 electrospun NFs containing 20% BOPE can be a beneficial system to increase the safety and quality of foods.

Effects of partially replacing animal fat by ethylcellulose based organogels in ground cooked salami.

Partial fat replacement in cooked salamis was formulated using organogels made with canola oil, ethylcellulose (EC; 6, 8, 9, 10, 11, 12 and 14%) and three types of surfactants; i.e., glycerol monostearate (GMS), stearyl alcohol/stearic acid (SOSA) and soybean lecithin (Lec). Texture profile analysis (TPA) and back extrusion tests indicated that increasing EC polymer concentration leads to harder gels regardless of the surfactant used. However, using GMS resulted in the hardest gel, whereas Lec did not strengthen the gel (mechanical stress test), but plasticized it. In general, gel hardness had a distinct effect on the binding of the organogel particle to the meat matrix, with softer gels adhering better under progressive compression. Substituting animal fat with organogel did not affect the main TPA parameters in most salami formulations, and canola oil by itself was also not significantly different from the pork and beef fat control. Using canola oil resulted in very small oil globules compared to the animal fat control, while structuring the oil yielded a microstructure with larger fat particles/globules, similar to the control. Color evaluation revealed a shift to yellow of the treatments with organogels compared to the control, but lightness and redness were not altered. The results demonstrate the potential use of structured vegetable oil to manufacture coarse ground meat products with lower saturated fat and a more favorable nutritional profile while resembling the traditional ground products.

Production and characterization of bio-oils from fast pyrolysis of tobacco processing wastes in an ablative reactor under vacuum.

Application of advanced pyrolysis processes to agricultural waste for liquid production is gaining great attention, especially when it is applied to an economic crop like tobacco. In this work, tobacco residues were pyrolyzed in an ablative reactor under vacuum. The maximum bio-oil yield of 55% w/w was obtained at 600°C with a particle size of 10 mm at a blade rotation speed of 10 rpm. The physical properties of the products showed that the oil produced was of high quality with high carbon, hydrogen, and calorific value. Two-dimensional gas chromatography/time-of-flight mass spectrometric analysis results indicated that the oils were complex mixtures of alkanes, benzene derivative groups, and nitrogen-containing compounds. In addition, 13C NMR results confirmed that long aliphatic chain alkanes were evident. The alkanes were likely converted from furans that were decomposed from hemicelluloses. Ablative pyrolysis under vacuum proved to be a promising option for generating useful amount of bio-oils from tobacco residues.

Dialdehyde Nanocrystalline Cellulose as Antibiotic Substitutes against Multidrug-Resistant Bacteria.

Antibiotic abuse resulted in the emergence of multidrug-resistant Gram-positive pathogens, which pose a severe threat to public health. It is urgent to develop antibiotic substitutes to kill multidrug-resistant Gram-positive pathogens effectively. Herein, the antibacterial dialdehyde nanocrystalline cellulose (DNC) was prepared and characterized. The antibacterial activity and biosafety of DNC were studied. With the increasing content of aldehyde groups, DNC exhibited high antibacterial activity against Gram-positive pathogens in vitro. DNC3 significantly reduced the amounts of methicillin-resistant Staphylococcus aureus (MRSA) on the skin of infected mice models, which showed low cytotoxicity, excellent skin compatibility, and no acute oral toxicity. DNC exhibited potentials as antibiotic substitutes to fight against multidrug-resistant bacteria, such as ingredients in salves to treat skin infection and other on-skin applications.

Improving the nutritional profile of culinary products: oleogel-based bouillon cubes.

Structured fat phases are the basis of many consumer relevant properties of fat-containing foods. To realise a nutritional improvement - less saturated, more unsaturated fatty acids - edible oleogels could be remedy. The feasibility of traditional fat phases structured by oleogel in culinary products has been evaluated in this study. In this contribution the oleogel application in bouillon cubes as model system for culinary products is discussed. Three different gelators (sunflower wax (SFW), a mixture of ß-Sitosterol and γ-Oryzanol (SO) and ethylcellulose (EC)), at two concentration levels (5% and 10% (w/w)) each, were evaluated with respect to their physical properties, in the food matrix and application. The application of pure and structured canola oil (CO) was benchmarked against the reference, palm fat (PO). The assessment of the prototypes covered attempts to correlate the physicochemical analyses and sensory data. Organoleptic and analytical studies covered storage stability (up to 6 months) monitoring texture, color and fat oxidation. The results indicate that the substitution of palm fat by oleogel is essentially possible. The characteristics of the bouillon cubes are tuneable by gelator choice and inclusion level. Most importantly, the data show that the anticipated risk of intolerable effects of oxidation during shelf life is limited if antioxidants are used.

Osteogenesis enhancement using poly (l-lactide-co-d, l-lactide)/poly (vinyl alcohol) nanofibrous scaffolds reinforced by phospho-calcified cellulose nanowhiskers.

Electrospun poly (l-lactide-co-d, l-lactide) (PLDLLA)/poly (vinyl alcohol) (PVA) nanofibers were reinforced by various contents (0-1 wt%) of phospho-calcified cellulose nanowhiskers (PCCNWs) as scaffolds in bone applications. The hydrophilicity and rate of hydrolytic degradation of PLDLLA were improved by introducing 10 wt% of PVA. PCCNWs with inherent hydrophilic properties, high aspect ratio, and large elastic modulus enhanced the hydrophilicity, accelerated the rate of degradation, and improved the mechanical properties of the nanofibrous samples. Moreover, calcium phosphate and phosphate functional groups on the surface of PCCNWs possessing act as stimulating agents for cellular activities such as proliferation and differentiation. Besides the physico-chemical properties investigation of PLDLLA/PVA-PCCNWs nanofibrous samples, their cytotoxicity was also studied and they did not show any adverse side effect. Incorporation of PCCNWs (1 wt%) into the PLDLLA/PVA nanofibrous samples showed more enzymatic activities and deposited calcium. The micrograph images of the morphology of human mesenchymal stem cells (hMSCs) cultured on the nanofibrous sample containing 1 wt% of PCCNWs after 14 days of cell differentiation revealed their high potential for bone tissue engineering.

Synthesis and Spectrophotometric Analysis of Microcapsules Containing Immortelle Essential Oil.

In this study, microcapsules were prepared by solvent evaporation technique using ethyl cellulose component as wall and essential oil as core material. The synthesis of microcapsules was carried out using different oil masses. The analysis of the microcapsules was carried out using field emission scanning electron microscope (FE-SEM) and UV spectrophotometric analysis using absorption spectrophotometer. The obtained results confirm the regular spherical shape and size of the synthesized microcapsules. The qualitative and quantitative spectrophotometric analysis of the microencapsulated immortelle oil was measured at the wavelength of 265 nm. The calibration diagram was used to calculate the unknown concentrations of the microencapsulated oil. The obtained results confirm the application of the presented method as relevant for the possible determination of microencapsulated oil on textile materials.

Synthesis and characterization of osmotic pump capsules containing polyoxyethylene and pH modifier to control the release of nifedipine.

The aim of this study was to formulate osmotic pump capsules (OPCs) to control the release of nifedipine (NP). NP solid dispersion was prepared by solvent evaporation method. The prepared mixture of NP solid dispersion and various excipients were filled into the commercial HPMC hard capsule shells and then coated with cellulose acetate (CA) solution to form NP-OPC. The CA coating solution consisted of CA as semi-permeable membrane, and Poloxamer 188 as pore formers. The impact of addition agents, citric acid and pore formers on in vitro drug release were investigated. Furthermore, the study has highlighted the impact of paddle speed and the pH value of release media, on the release and compared the release with the commercial controlled release tablets. The in vitro drug release study indicated that drug release could reach 95% in 24 h with optimal formulation, and interestingly model fitting showed that the drug release behavior was closely followed to zero-order release kinetics. The pharmacokinetic studies were performed in rabbits with commercial controlled release tablets as reference, both preparations showed a sustained release effect. Compared with traditional preparation methods of OPCs, the new preparation process was simplified without the operation of laser drilling and the sealing process of capsule body and cap, which improved the feasibility of industrial production.

Unique adaptations in neonatal hepatic transcriptome, nutrient signaling, and one-carbon metabolism in response to feeding ethyl cellulose rumen-protected methionine during late-gestation in Holstein cows.

BACKGROUND: Methionine (Met) supply during late-pregnancy enhances fetal development in utero and leads to greater rates of growth during the neonatal period. Due to its central role in coordinating nutrient and one-carbon metabolism along with immune responses of the newborn, the liver could be a key target of the programming effects induced by dietary methyl donors such as Met. To address this hypothesis, liver biopsies from 4-day old calves (n = 6/group) born to Holstein cows fed a control or the control plus ethyl-cellulose rumen-protected Met for the last 28 days prepartum were used for DNA methylation, transcriptome, metabolome, proteome, and one-carbon metabolism enzyme activities. RESULTS: Although greater withers and hip height at birth in Met calves indicated better development in utero, there were no differences in plasma systemic physiological indicators. RNA-seq along with bioinformatics and transcription factor regulator analyses revealed broad alterations in 'Glucose metabolism', 'Lipid metabolism, 'Glutathione', and 'Immune System' metabolism due to enhanced maternal Met supply. Greater insulin sensitivity assessed via proteomics, and efficiency of transsulfuration pathway activity suggested beneficial effects on nutrient metabolism and metabolic-related stress. Maternal Met supply contributed to greater phosphatidylcholine synthesis in calf liver, with a role in very low density lipoprotein secretion as a mechanism to balance metabolic fates of fatty acids arising from the diet or adipose-depot lipolysis. Despite a lack of effect on hepatic amino acid (AA) transport, a reduction in metabolism of essential AA within the liver indicated an AA 'sparing effect' induced by maternal Met. CONCLUSIONS: Despite greater global DNA methylation, maternal Met supply resulted in distinct alterations of hepatic transcriptome, proteome, and metabolome profiles after birth. Data underscored an effect on maintenance of calf hepatic Met homeostasis, glutathione, phosphatidylcholine and taurine synthesis along with greater efficiency of nutrient metabolism and immune responses. Transcription regulators such as FOXO1, PPARG, E2F1, and CREB1 appeared central in the coordination of effects induced by maternal Met. Overall, maternal Met supply induced better immunometabolic status of the newborn liver, conferring the calf a physiologic advantage during a period of metabolic stress and suboptimal immunocompetence.

Dopamine-polyethyleneimine co-deposition cellulose filter paper for α-Glucosidase immobilization and enzyme inhibitor screening.

In this work, cellulose filter paper (CFP), which is inexpensive and commercially available, was used as the carrier, and the immobilized α-glucosidase was obtained by two steps: firstly, the surface of CFP was modified by polydopamine/polyethyleneimine (PDA/PEI) co-deposition method to obtain CFP-PDA/PEI with a uniform coating of rich positive charge; subsequently, α-glucosidase was immobilized on the CFP-PDA/PEI by electrostatic adsorption. The free enzyme and immobilized enzyme have the same optimal temperature (70℃) and pH (8.0), and their Km is similar, which is 2.2 and 2.8, respectively. These results show that the immobilization process does not change the properties of the enzyme greatly. The immobilized enzyme still maintains 75.6% of its initial activity after 10 repeated uses, showing good reusability. The excellent repeatability (RSD = 2.2%, n = 5) and the verification of competitive inhibitor (acarbose) illustrates the reliability of the immobilized enzymes for enzyme inhibitor screening. Finally, combined with CE, a screening method based immobilized α-glucosidase was proposed and applied to screen the α-glucosidase inhibitory from 10 kinds of Traditional Chinese medicines (TCMs) in vitro. The results indicated that the method was a very effective tool for screening potential α-glucosidase inhibitors from TCMs.

Combined effects of hydroxypropylation and alcoholic alkaline treatment on structural, functional and rheological characteristics of sorghum and corn starches.

This study describes the effects of hydroxypropylation (HP) on sorghum and corn cold water soluble (CWS) starches prepared via alcoholic alkaline treatment (AAT). Propylene oxide (5% and 12% on starch weight basis) was used to modify both sorghum and corn starches. SEM analysis revealed that HP modification prior to AAT altered the granular morphology of native CWS starches. The characteristic peaks at 2980.28 cm-1 and 2979.87 cm-1 indicated the presence of hydroxypropyl groups and the complete loss of the granular order for HS12-CWS (hydroxypropylated sorghum CWS starch treated with 12% propylene oxide based on dry starch weight) and HC12-CWS (hydroxypropylated corn CWS starch treated with 12% propylene oxide based on dry starch weight) starches. Increase in swelling power and water binding capacity of HP modified CWS starches was observed. However, Percent transmittance was significantly reduced due to fragmented water-soluble granules. HP-modified CWS starch gels exhibited a more rigid gel network. Broader linear viscoelastic range suggesting greater stability and well dispersed behavior of HP-CWS starches. High G' values of HP-CWS starches were due to the ordered and elastic gel network that resisted deformation. Furthermore, all HP-CWS starches exhibited higher shear and thermal resistance compared to unmodified CWS starches.

Cellulose acetate nanofibers loaded with crude annatto extract: Preparation, characterization, and in vivo evaluation for potential wound healing applications.

In this study we prepared annatto-loaded cellulose acetate nanofiber scaffolds and evaluated both in vitro cytotoxicity and potential for wound healing in a rat model. Annatto extract, which has been used to accelerate wound healing, was added to cellulose acetate polymer and the resulting material was used to produce nanofiber scaffolds via electrospinning. Physicochemical, and thermal evaluation of the resulting nanofiber mats showed that incorporating annatto did not significantly affect the thermal or chemical stability of the polymer. Annatto extract did not demonstrate cytotoxicity in the HET-CAM assay or MTT assay for fibroblast culture. Scanning electron microscopy of the fibroblasts confirmed that cells spread and penetrated into the nanofiber. In vivo experiments confirmed that cellulose acetate retained its biocompatibility when associated with crude annatto extract, and suggested that dose/response modulation occurs between the annatto-functionalized nanofibers and mast cells, indicating the potential of this material for wound healing applications.

Prediction of in vivo performance of oral extended release formulations prior to clinical evaluation: A case study for enteric coated polymeric beads formulation.

To reduce cost and time for product development, an ideal strategy for the development of oral extended release (ER) product is to identify the desired formulation with minimum needsfor clinical evaluation. The aim of this work was to demonstrate the feasibility of adopting a "prediction-then-validation" strategy for the development of oral ER formulations. Instead of the traditional approach using multiple ER formulations for IVIVC development, an enteric-coated fast release formulation was successfully utilized for the development of a biopredictive tool to estimate the drug release from enteric coated polymeric ER formulations in the intestine. A TS1 (time scale factor between Tvitro and Tvivo equals to 1) system was designed and developed, based on which the in vivo pharmacokinetic (PK) performance of ER formulations in dog and in human were well predicted prior to in vivo evaluations. The model further passed a posteriori validation using the criteria for level A IVIVC and, as designed, provided a Tscale value of 1 for the IVIVC model.