Encapsulation of HRP-Immobilized Silica Particles into Hollow-Type Spherical Bacterial Cellulose Gel: A Novel Approach for Enzyme Reactions within Cellulose Gel Capsules.

We revealed that the encapsulation of enzyme-immobilized silica particles in hollow-type spherical bacterial cellulose (HSBC) gels enables the use of the inside of HSBC gels as a reaction field. The encapsulation of horseradish peroxidase (HRP)-immobilized silica particles (Si-HRPs, particle size: 40-50 µm) within HSBC gels was performed by using a BC gelatinous membrane produced at the interface between Komagataeibacter xylinus suspension attached onto an alginate gel containing Si-HRPs and silicone oil. After the biosynthesis of the BC gelatinous membrane, formed from cellulose nanofiber networks, the alginate gel was removed via immersion in a phosphate-buffered solution. Si-HRP encapsulated HSBC gels were reproducibly produced using our method with a yield of over 90%. The pore size of the network structure of the BC gelatinous membrane was less than 1 µm, which is significantly smaller than the encapsulated Si-HRPs. Consequently, the encapsulated Si-HRPs could neither pass through the BC gelatinous membrane nor leak from the interior cavity of the HSBC gel. The activity of the encapsulated HRPs was detected using the 3,3',5,5'-tetramethylbenzidine (TMB)-H2O2 system, demonstrating that this method can encapsulate the enzyme without inactivation. Since HSBC gels are composed of a network structure of biocompatible cellulose nanofibers, immune cells cannot enter the hollow interior, thus, the enzyme-immobilized particles encapsulated inside the HSBC gel are protected from immune-cell attacks. The encapsulation technique demonstrated in this study is expected to facilitate the delivery of enzymes and catalysts that are not originally present in the in vivo environment.

Preparation of novel sulfated polysaccharide-carboxymethyl-5-fluorouracil-folic acid conjugates for targeted anticancer drug delivery.

GFP1, a sulfated polysaccharide extracted from Grateloupia filicina, exhibits remarkable immunomodulatory activity. To reduce the side effects of 5-fluorouracil (5-FU), GFP1 was employed as a macromolecular carrier to synthesize of GFP1-C-5-FU by reacting with carboxymethyl-5-fluorouracil (C-5-FU). Subsequently, this new compound was reacted with folic acid (FA) through an ester bond, forming novel conjugates named GFP1-C-5-FU-FA. Nuclear magnetic resonance analysis confirmed the formation of GFP1-C-5-FU-FA. In vitro drug release studies revealed that the cumulative release rate of C-5-FU reached 46.9 % in phosphate buffer (pH 7.4) after 96 h, a rate significantly higher than that of the control groups, indicating the controlled drug release behavior of GFP1-C-5-FU-FA. Additionally, in vitro anticancer assays demonstrated the potent anticancer activity of GFP1-C-5-FU-FA conjugates, as evidenced by the reduced viability of HeLa and AGS cancer cells, along with increased levels of apoptosis and cellular uptake. Western blot analysis indicated that the GFP1-C-5-FU-FA conjugate effectively enhanced phosphorylation in cancer cells through the NF-kB and MAPK pathways, thereby promoting apoptosis. These findings highlight the potential of folate-targeted conjugates in efficiently treating HeLa and AGS cancer cells in vitro and lay a robust theoretical groundwork for future in vivo anti-cancer research involving these cells.

Preparation and drug release performance of different gelation type polysaccharide/ß-lactoglobulin fiber composite gels.

Self-assembled protein fibers have attracted much attention in the fields of medicine and food because of their high aspect ratio, polymorphic structure and strong surface hydrophobicity. In this study, three different gelation types of polysaccharides/ß-lactoglobulin fiber (Fblg) composite gels, including ionic alginate-Fblg gels, synergistic xanthan-Fblg gels, and double network agar-Fblg gels, were first prepared. The interactions between the polysaccharides and the Fblgs, the microstructure and mechanical properties of the composite gels were investigated using the light scattering, scanning electron microscopy, rheology and texture analysis in order to reveal their formation mechanisms. Then the loading and release properties of the water-soluble drug 5-fluorouracil (5-FU) and the hydrophobic drug curcumin (Cur) through these composite gels were further studied with release mechanisms determined by fitting different release models. It was found that the mechanical properties of the composite gels were determined by the mesh density of the three-dimensional networks formed inside the gels. The network structure and mechanical strength of the alginate-Fblg gels became weaker with the increase of Fblg content at pH 4 due to their attractive interaction which hindered the binding of Ca2+ to ALG, while the network and the strength of the alginate-Fblg gels didn't change much at pH 7 due to the repulsion between Alg and Fblg. The xanthan-Fblg gels formed lamellar structures with enhanced gel network and mechanical strength due to the hydrogen bonding and the electrostatic interaction with Fblg. The Agar-Fblg composite gel formed at 60 °C (above the gelation temperature of agar of 40 °C) had a denser double network structure and higher mechanical strength than that formed at 0 °C due to inhibition of diffusion of Ca2+ as salt bridges for Fblg. The hydrophilic drugs were loaded in the meshes of the composite gels and their release was determined by the structure of the composite gel networks, whereas the hydrophobic drugs were loaded by attaching to the Fblgs in the composite gels and their release was determined by the loading ability and strength of the gels. The study not only provided a new idea for the preparation and application of polysaccharide-protein fiber composite hydrogels, but also provided insights for improving the efficiency of drug carriers.

Properties and release behavior of sodium alginate-based nanocomposite active films: Effects of particle size of IRMOF-3.

Nanoparticles are used as fillers to improve the properties of biopolymers, and their particle size is an important parameter. This work aims to investigate the effect of particle size of isoreticular metal-organic framework-3 (IRMOF-3) on the mechanical, physical, and release properties of sodium alginate (SA)-based composite active film. In our study, IRMOF-3 with six different particle sizes was synthesized by introducing additives. IRMOF-3 loading with carvacrol (IRMOF-3/CA nanoparticles) was incorporated into the SA matrix to prepare the composite film. The characterization and testing results of films showed that the particle size of nanoparticles affected the physical morphology and chemical structure of the film. Especially smaller nanoparticles uniformly dispersed into the SA matrix more easily, forming a denser and more stable spatial network structure with SA, which could more significantly improve the tensile strength, water vapor barrier, and hydrophobic properties of the film (P < 0.05). In addition, the CA release rate from the active film could be significantly reduced by about 33.90 % even when the smallest particle size of the IRMOF-3/CA nanoparticles was added. Therefore, when IRMOF-3/CA is used as the nano-filler to develop SA-based active film, its particle size has a potential influence on the properties of the film.

Development of cinnamon essential oil-loaded PBAT/thermoplastic starch active packaging films with different release behavior and antimicrobial activity.

The poly (butylene adipate-co-terephthalate)/thermoplastic starch (PBAT/TPS) active packaging films containing cinnamon essential oil (CEO) were fabricated by melting blending and extrusion casting method. The effects of TPS content (0 %, 10 %, 20 %, 30 %, 40 % and 50 %) on the properties of the films and their application in largemouth bass preservation were studied. As TPS content increased from 0 % to 50 %, the water vapor permeability increased from 7.923 × 10-13 (g•cm/(cm2•s•Pa)) to 23.967 × 10-13 (g•cm/(cm2•s•Pa)), the oxygen permeability decreased from 8.642 × 10-11 (cm3•m/(m2•s•Pa)) to 3.644 × 10-11 (cm3•m/(m2•s•Pa)), the retention of CEO in the films increased. The release rate of CEO from the films into food simulant (10 % ethanol) accelerated with increasing TPS. The films exhibited different antibacterial activity against E. coli, S. aureus, and S. putrefaciens. It was closely related with the release behavior of the CEO. The films containing CEO could efficiently inhibit the decomposition of protein and the growth of microorganisms in largemouth bass. It showed that the higher TPS in the films, the better inhibitory effect. This study provided a new idea for developing PBAT/TPS active films with different release behavior of active agents and different antibacterial activity for food packaging.

Bile salt-enriched vs. non-enriched nanoparticles: comparison of their physicochemical characteristics and release pattern.

Bile salts were first used in the preparation of nanoparticles due to their stabilizing effects. As time went by, they attracted much attention and were increasingly employed in fabricating nanoparticles. It is well accepted that the physicochemical properties of nanoparticles are influential factors in their permeation, distribution, elimination and degree of effectiveness as well as toxicity. The review of articles shows that the use of bile salts in the structure of nanocarriers may cause significant changes in their physicochemical properties. Hence, having information about the effect of bile salts on the properties of nanoparticles could be valuable in the design of optimal carriers. Herein, we review studies in which bile salts were used in preparing liposomes, niosomes and other nanocarriers. Furthermore, the effects of bile salts on entrapment efficiency, particle size, polydispersity index, zeta potential, release profile and stability of nanoparticles are pointed out. Finally, we debate how to take advantage of bile salts potential for preparing desirable nanocarriers.

Predicting the binding configuration and release potential of heavy metals on iron (oxyhydr)oxides: A machine learning study on EXAFS.

Heavy metals raise a global concern and can be easily retained by ubiquitous iron (oxyhydr)oxides in natural and engineered systems. The complex interaction between iron (oxyhydr)oxides and heavy metals results in various mineral-metal binding configurations, such as outer-sphere complexes and edge-sharing inner-sphere complexes, which determine the accumulation and release of heavy metals in the environment. However, traditional experimental approaches are time-consuming and inadequate to elucidate the complex binding relationships and configurations between iron (oxyhydr)oxides and heavy metals. Herein, a workflow that integrates the binding configuration data of 11 heavy metals on 7 iron (oxyhydr)oxides and then trains machine learning models to predict unknown binding configurations was proposed. The well-trained multi-grained cascade forest models exhibited high accuracy (> 90%) and predictive performance (R2 ∼ 0.75). The underlying effects of mineral properties, metal ion species, and environmental conditions on mineral-metal binding configurations were fully interpreted with data mining. Moreover, the metal release rate was further successfully predicted based on mineral-metal binding configurations. This work provides a method to accurately and quickly predict the binding configuration of heavy metals on iron (oxyhydr)oxides, which would provide guidance for estimating the potential release behavior of heavy metals and remediating heavy metal pollution in natural and engineered environments.

Sustained drug release behavior of captopril-incorporated chitosan/carboxymethyl cellulose biomaterials for antihypertensive therapy.

Captopril (CTP) is an oral drug widely used to treat high blood pressure and congestive heart failure. In this study, CTP-incorporated biomaterials for antihypertensive therapy were synthesized from chitosan, carboxymethyl cellulose, and plasticizers. The physicochemical properties of the prepared biomaterials were characterized using FE-SEM, FT-IR analysis, and physical properties. CTP release experiments were carried out in buffer solutions at various pH values and temperatures. Results indicated that above 99.0 % of CTP was released within 180 min. Optimization of the experimental conditions for CTP release was analyzed by using response surface methodology (RSM). Results of CTP release through artificial skin indicated that CTP was continuously released above 95.0 % from the prepared biomaterials for 36.0 h. The CTP release mechanisms into a buffer and through artificial skin followed pseudo-Fickian diffusion mechanism and non-Fickian diffusion mechanisms, respectively. Moreover, angiotensin-converting enzyme (ACE) inhibition (related to cardiovascular disease) via the released CTP clearly reveals that the prepared biomaterials have a high potential as a transdermal drug delivery agent in antihypertensive therapy.

Encapsulation of pomegranate polyphenols by ionic gelation: Strategies for improved retention and controlled release.

This study aimed at producing pectin hydrogel beads by ionic gelation proce to carry pomegranate extract (PE) evaluating approaches to increase its retention and protect the polyphenols from environmental conditions that interfere in the stability and color of these compounds, such as the pH of the medium. Several strategies were tested to reduce the mass transfer and consequently increase its retention. The insertion of a filler (gelatinized starch), the employment of different concentrations from the external environment, the adsorption using blank pectin-starch beads, and the electrostatic coating using chitosan were performed. The release of entrapped compounds over time was employed to evaluate the release pattern of PE in water media. Diffusion coefficients calculated from these experiments were then used to estimate the PE release behavior. The encapsulation efficiency (EE) was significantly improved (42 % to 101 %) when equalizing the concentration of the external medium with that from the beads formulation. Furthermore, the increase in the PE concentration was proportional to the rise in the mechanical strength (MS) of the beads which indicates a modification of internal structure due to the presence of polyphenols. The adsorption was efficient in entrapping the active compound, and despite the high PE content observed for all beads (average value of 2960.26 mg of gallic acid equivalent/100 g sample), they had the lowest diffusion coefficient from the release in water media. Finally, the coating was able to reduce the release rate in most of the tests (DAB uncoated = 0.5 DAB coated), however, during the electrostatic deposition a loss of about 32 % of the phenolic compounds in the chitosan solution was observed which led to a reduced EE. Despite the obtention of retarded release, coating studies need to be improved. Some adjustments in the execution of this technique are necessary so that the losses are reduced and the process becomes viable for the use of beads in food.

The Release Behavior of Anthraquinones Encapsulated into Casein Micelles during In Vitro Digestion.

The degradation of anthraquinones extracted from aloe vera plants can be prevented by encapsulating them in casein micelles (CMs). The oral, gastric, and intestinal digestion behavior of spray-dried microcapsules of casein micelles loaded with aloe vera-extracted anthraquinone powder (CMAQP), freeze-dried powder (CMFDP), and whole-leaf aloe vera gel (CMWLAG) obtained through ultrasonication was investigated. The results found that CMAQP and CMFDP dissolved slowly and coagulated into large curds during gastric digestion, improving the retention of anthraquinones in the digestive tract. In contrast, CMWLAG structure was destroyed and increased amounts of anthraquinones were released during oral and gastric digestion phases, indicating increased amounts of surface anthraquinones instead of the encapsulation of anthraquinones in the interior of CMs. The strong hydrophobic interactions protected anthraquinones within the core of CM for CMAQP and delayed diffusion. However, during SIF digestion, both CMAQP and CMFDP released significant amounts of anthraquinones, although CMAQP showed a much more controlled release for both aloin and aloe-emodin over SIF digestion time. The release behavior of anthraquinones from CM microcapsules was a function of the type of anthraquinone that was used to encapsulate. The present study provides insight into the release behavior of loaded bioactive compounds using food-grade CMs as the wall material during in vitro digestion and highlights the importance of the type of bioactive component form that will be encapsulated.

The First Discovery of a Microstructure in Black Plaster and Its Performance Characterization.

Background: Black plaster is one of the classic dosage forms of traditional Chinese medicine for external use and has been widely utilized since the Tang and Song Dynasties. In this paper, we take Goupi Gao as the research object and discuss the scientific characteristics of the black plaster dosage form. Goupi Gao ointment is a plaster for external use of traditional Chinese medicine. Methods: Methods for the morphological and quantitative characterization of black plaster's microstructure, based on FESEM-IPP (Field Emission Scanning Electron Microscope IPP Image Processing) technology, were established. According to the actual operating temperature of Goupi Gao, three temperatures were selected: 28°C, 35°C, and 45°C. A UPLC analysis method was applied to the cinnamaldehyde and eugenol in Goupi Gao, and the release behavior of Goupi Gao from three samples at three temperatures was investigated using the paddle over disk method. Preparation of rabbit model of knee osteoarthritis of cold blood stasis type by cold stimulation combined with drug induction. Results: In terms of morphology, Goupi Gao and the blank black plaster matrix both formed a double continuous phase system with a thicker vegetable oil phase and crossed "branched" soap crystal fibers. Based on the IPP image quantification parameters, the pore area (A) was highly positively correlated with temperature. After the 28 °C treatment, A1 = (216.8±59.5) µm2; after the 35 °C treatment, A2 = (259.7±52.8) µm2; after the 45 °C treatment, A3 = (408.0±57.7) µm2, and there were no significant differences in other pore parameters. Conclusion: The black plaster matrix's unique structure makes it highly applicable in numerous medications; it exhibits slow-release and performs well in extreme temperatures, with good adhesion and peeling properties.

Self-assembled low molecular weight chitosan-based cationic micelle for improved water solubility, stability and sustained release of α-tocopherol.

New amphiphilic low molecular weight chitosan-graft-nicotinic acid bearing decyl groups (LCND) was synthesized by two-step reaction and spontaneously assembled into cationic micelle by ultra-sonication method to improve water solubility and photostability properties of α-tocopherol. The chemical structure of LCND was characterized and physical properties of cationic micelle were evaluated. Results displayed that cationic micelle exhibited strong self-assemble ability with nanoscale spherical morphology and showed best loading ability with loading content of 18.50% when the feeding ratio of LCND to α-tocopherol reached 10:3. Meanwhile, the greatly enhanced water solubility, photostability and sustained release behavior of α-tocopherol in cationic micelle were observed. The cumulative release of α-tocopherol in cationic micelle reached up 82.18% within 96 h while free α-tocopherol was completely released within 10 h. Additionally, release kinetics models were also fitted. The LCND cationic micelle could be promising nanocarrier for improving the physicochemical properties of α-tocopherol in food fields.

Formation, Structural Characterization, and Functional Properties of Corn Starch/Zeaxanthin Composites.

Zeaxanthin is a natural xanthophyll carotenoid and the main macular pigment that protects the macula from light-initiated oxidative damage, but it has poor stability and low bioavailability. Absorption of this active ingredient into starch granules as a carrier can be used to improve both zeaxanthin stability and controlled release. Optimization using three variables judged important for optimizing the system (reaction temperature of 65 °C, starch concentration of 6%, and reaction time of 2 h) was conducted for incorporation of zeaxanthin into corn starch granules, aiming for high zeaxanthin content (2.47 mg/g) and high encapsulation efficiency (74%). Polarized-light microscopy, X-ray diffraction, differential scanning calorimetry, and Fourier transform infrared spectroscopy showed that the process partially gelatinized corn starch; additionally, it showed the presence of corn starch/zeaxanthin composites, with the zeaxanthin successfully trapped in corn starch granules. The half-life time of zeaxanthin in corn starch/zeaxanthin composites increased to 43 days as compared with that of zeaxanthin alone (13 days). The composites show a rapid increase in zeaxanthin release with in vitro intestinal digestion, which is favorable for possible use in living systems. These findings could have application in designing effective starch-based carriers of this bioactive ingredient with enhanced storage stability and improved intestines-targeted controlled-release delivery.

Preparation and characterization of inclusion complex of Myristica fragrans Houtt. (nutmeg) essential oil with 2-hydroxypropyl-ß-cyclodextrin.

Nutmeg essential oil (NEO) is a natural condimentwith versatile biological activities. However, the application of NEO in food has several limitations due to its poor stability and low aqueous solubility. To overcome the shortcomings, this paper focused on the preparation of the inclusion complex (IC) of NEO with 2-hydroxypropyl-ß-cyclodextrin (HP-ß-CD) by the coprecipitation method. The optimal condition was inclusion temperature 36 ℃, time 247 min, stirring speed 520 r/min, and wall-core ratio 12:1, resulting in a recovery of 80.63%. The formation of IC was verified by various methods such as scanning electron microscopy, Fourier transform infrared spectroscopy and nuclear magnetic resonance. The improvement of thermal stability, antioxidant, and nitrite scavenging activities of NEO after encapsulation was proven. Moreover, the controlled release of NEO from IC can be implemented by regulating the temperature and relative humidity. Overall, NEO/HP-ß-CD IC has great application potential in food industries.

pH-Shifting combined with ultrasound treatment of emulsion-filled ß-conglycinin gels as ß-carotene carriers: Effect of emulsion concentration on gel properties.

In this work, emulsion-filled gels were prepared from natural and pH-shifting combined with ultrasound ß-conglycinin (7S) as emulsifiers. The emulsifier modification and emulsion concentrations (5, 10, 15, 20 wt%) were evaluated on the structural and ß-carotene release properties of the gels. Compared to the 7S hydrogel, the emulsion-filled gels exhibited better water-holding and textural properties. The 7S modification and the increase in emulsion concentration resulted in altered water distribution and improved microstructure and rheological properties of the emulsion-filled gels. The dense and homogeneous gel network was formed at an emulsion content of 15 wt%. The gels were regulated by different release kinetics in a simulated gastrointestinal environment. M-15 showed the highest bioaccessibility and chemical stability (72.25% and 89.87%) with good slow-release properties of ß-carotene. These results will guide the development of encapsulated delivery systems for gel food products.

The release analysis of As and Cr metals in lead-zinc smelting slag: Mineralogical analysis, bioavailability and leachability analysis.

Mining and smelting are the main sources of soil heavy metal pollution. Leaching and release of heavy metals in soils has been extensively studied. However, there are few researches on the release behavior of heavy metals from the Angle of mineralogy of smelting slag. This study focuses on the pollution of arsenic and chromium by traditional pyrometallurgical lead-zinc smelting slag in southwest China. Based on the mineralogy of smelting slag, the release behavior of heavy metals in smelting slag was studied. As and Cr deposit minerals were identified by MLA analysis, and the weathering degree and bioavailability of As and Cr deposit minerals were analyzed. The results showed that the weathering degree of slag was positively correlated with the bioavailability of heavy metals. The leaching experiment results showed that the higher pH was beneficial to the release of As and Cr. It was found that the chemical forms of As and Cr changed from relatively stable forms to easily released forms (As5+ to As3+ and Cr3+ to Cr6+) by characterizing the metallurgical slag during leaching. In the transformation process, the S in the pyrite as the enclosing layer is eventually oxidized to SO42-, which will accelerate the dissolution of the enclosing mineral. SO42- will occupy the adsorption site of As on the mineral surface, thus reducing the adsorption amount of As on the mineral surface. Fe is finally oxidized to Fe2O3, and the increase of Fe2O3 content in the waste residue will produce strong adsorption effect on Cr6+ and slow down the release of Cr6+. The results show that the release of As and Cr is controlled by the pyrite coating.

Construction and application of nano ZnO/eugenol@yam starch/microcrystalline cellulose active antibacterial film.

The goal of this study was to develop new biocomposite films that can better protect and prolong the shelf life of food. Here, a ZnO: eugenol@yam starch/microcrystalline cellulose (ZnO:Eu@SC) antibacterial active film was constructed. Because of the advantages of metal oxides and plant essential oils, codoping with these can effectively improve the physicochemical and functional properties of composite films. The addition of an appropriate amount of nano-ZnO improved the compactness and thermostability, reduced the moisture sensitivity, and enhanced the mechanical and barrier properties of the film. ZnO:Eu@SC exhibited good controlled release of nano-ZnO and Eu in food simulants. Nano-ZnO and Eu release was controlled by two mechanisms: diffusion (primary) and swelling (secondary). After loading Eu, the antimicrobial activity of ZnO:Eu@SC was significantly enhanced, resulting in a synergistic antibacterial effect. Z4:Eu@SC film extended the pork shelf life by 100 % (25 °C). In humus, the ZnO:Eu@SC film was effectively degraded into fragments. Therefore, the ZnO:Eu@SC film has excellent potential in food active packaging.

A novel sulfated mannan-carboxymethyl-5-fluorouracil-folic acid conjugates for targeted anticancer drug delivery.

CFP2 is a sulfated polysaccharide isolated from Codium fragile that shows excellent immunomodulatory activity. To reduce the side effects of 5-fluorouracil (5-FU), CFP2 was used as a macromolecular carrier to react with carboxymethyl-5-fluorouracil (C-5-FU) to form CFP2-C-5-FU, which further reacted with folic acid (FA) via an ester bond to form novel conjugates (CFP2-C-5-FU-FA). CFP2-C-5-FU-FA was confirmed by nuclear magnetic resonance (NMR) analysis. In vitro drug release results showed that the cumulative release rate of C-5-FU was 49.9% in phosphate buffer (pH 7.4) after 96 h, which was much higher than that of the other groups, indicating that CFP2-C-5-FU-FA showed controlled drug release behavior. CFP2-C-5-FU-FA also exhibited enhanced apoptosis and cellular uptake in vitro. Further, intravenous administration of CFP2-C-5-FU-FA in an HCT-116 cell-bearing xenograft mouse showed that the conjugates were safe and effective drug delivery systems. These results suggest that folate-targeted conjugates can be used effectively for efficient chemotherapy of colorectal cancer.

Mechanistic insights of different release behaviors dominated by drug physicochemical properties in polyisobutylene pressure sensitive adhesive.

The purpose of this study was to investigate the effect of the physicochemical parameters of drugs on their own release behaviors in polyisobutylene pressure sensitive adhesive (PIB PSA), which provided a theoretical guidance for the application of PIB in transdermal drug delivery system (TDDS). Seven drugs with different physicochemical parameters including clonidine (CLO), flurbiprofen (FLU), diclofenac (DIC), ibuprofen (IBU), zolmitriptan (ZOL), lidocaine (LID), tulobuterol (TUL) and the mixed adhesive (7:3, w/w) of Oppanol® B 15 N (M.W. = 108,000 Da) and Oppanol® N 50 (M.W. = 565,000 Da) were selected for in vitro drug release and skin permeation studies. Regression analysis was used to study the relationship between physicochemical parameters and release behaviors. The release behaviors of drugs were a negative correlation with polarizability and dipole moment per molecular volume (µ/V), which represented van der Waals and dipole-dipole interaction, respectively. Fourier transform infrared spectroscopy (FT-IR), modulated temperature differential scanning calorimetry (MDSC) and molecular dynamics simulation were used to provide molecular details of the interaction between the drug and PIB. The free volume and molecular mobility of PIB were characterized using mechanical property tests, rheology study, MDSC and molecular dynamics simulation. Based on the above results, drugs with high polarizability and µ/V had stronger van der Waals and dipole-dipole interaction with PIB, reducing the free volume and molecular mobility of PIB, so that the drug struggled to release from PIB. In addition, the diffusion activation energy of the drug was calculated by using the variable temperature release study to characterize the ease of drug release from the kinetic aspect. And the trends of in vitro drug release and skin penetration profiles were basically similar. Thus, it was thought that the physicochemical parameters of the drug played a vital role in the drug release behavior of PIB PSAs and would affect the skin penetration process, which provided a reference for the design and application of patches based on PIB PSAs in TDDS.

Drying Technique Providing Maximum Benefits on Hydrogelling Ability of Avocado Seed Protein: Spray Drying.

The current study focused on creating natural hydrogels consisting of mixtures of avocado seed proteins dried with different techniques and locust bean gum. Proteins were extracted from avocado seed by alkali and isoelectric precipitation methods. Avocado seed proteins were dried by five different drying methods, namely ambient drying, oven drying, vacuum drying, freeze drying, and spray drying. FT-IR spectra were used to analyze the chemical structure of proteins dried using various techniques. Additionally, hydrogel models were constructed in the presence of avocado seed proteins and locust bean gum to clarify the effect of drying techniques on their hydrogelling ability. The impact of drying techniques on the functional behavior of hydrogels was notable. The maximum water holding capacity values were detected in the hydrogel system containing spray-dried proteins (93.79%), followed by freeze-dried (86.83%), vacuum-dried (76.17%), oven-dried (72.29%), and ambient-dried (64.8%) counterparts. The swelling ratio was 34.10, 33.51, 23.05, 18.93, and 14.39% for gels in the presence of freeze-dried, spray-dried, vacuum-dried, oven-dried, and ambient-dried proteins, respectively. Additionally, the desirable values for the amount of protein leaking from the systems prepared using spray-dried (7.99%) and freeze-dried (12.14%) proteins were obtained compared to others (ambient-dried: 24.03%; oven-dried: 17.69%; vacuum-dried: 19.10%). Superior results in terms of textural properties were achieved in hydrogel models containing spray-dried and freeze-dried proteins. In general, hydrogel models exhibited elastic behavior rather than viscous properties; however, the magnitudes of elasticity varied. Furthermore, the success of gels containing hydrogel models containing spray-dried protein and locust bean gum in the bioactive compound delivery system was obvious compared with protein ones alone.