Single Factor Investigation Research Articles

A finasteride patch for the treatment of androgenetic alopecia: A study of promoting permeability strategy using synthetic novel O-acylmenthols combined with ion-pair

Currently, finasteride (FIN) is approved to treat androgenetic alopecia only orally, and the application of FIN in transdermal drug delivery system (TDDS) has introduced a new approach for treating the disease. This study was aimed to develop a FIN transdermal patch for the treatment of androgenetic alopecia（AGA） by combing ion-pair and O-acylmenthols (AM) as chemical permeation enhancers (CPEs). The formulation of patch was optimized though single-factor investigation and Box-Behnken design. The pharmacokinetics and androgenetic alopecia pharmacodynamics of the patch were evaluated. Additionally, the permeability enhancement mechanisms of ion-pair and AMs were explored at both the patch and skin levels. The effects of ion-pair and AMs on the patch were characterized by rheology study, FTIR, and molecular docking, and the effects on the skin were assessed through ATR-FTIR, Raman study, DSC, CLSM and molecular dynamics. The finalized formulation of FIN patches was consisted of 5 % (w/w) synthetic FIN-CA (Citric Acid), 6 % MT-C6 as CPEs, 25-AAOH as a pressure-sensitive adhesive (PSA), with a patch thickness of 80 ± 5 μm. The final Q24 h is 78.22 ± 5.18 μg/cm2. Based on the high FIN permeability, the pharmacokinetic analysis revealed that the FIN patch group exhibited a slower absorption rate (tmax = 7.3 ± 2.7 h), lower peak plasma concentration and slower metabolic rate (t1/2 = 6.2 ± 0.8 h, MRT0-t = 26.0 ± 7.8 h) compared to the oral group. Moreover, the FIN patch also demonstrated the same effect as the oral group in promoting hair growth in AGA mice. The results indicated that both FIN-CA and AMs could enhance the fluidity of the PSA and weaken the interaction between FIN-CA and PSA, thereby promoting the release of the FIN from the patch. The interaction sites on the skin for ion-pair and the four AMs were found in the stratum corneum (SC) of the skin, disrupting the tight arrangement of stratum corneum lipids. This study serves as a reference for the multi-pathway administration of FIN and the combination of ion-pair with AMs to enhance drug permeation.

Construction of Lactobacillus casei-loaded Water-in-oil High Internal Phase Emulsion and its Study on Anti-breast Cancer Properties

Objective: To prepare an oil-in-water high internal phase emulsion containing Lactobacillus casei, and to optimize and characterize the preparation process. To explore the therapeutic effect of the probiotic-carrying emulsion on in situ breast cancer in mice. Methods: Using corn oil, sodium alginate, polyglycerin ricinoleate and L. casei as raw materials, the high internal phase emulsion containing probiotic oil-in-water was prepared by high-speed homogenization method. The optimal preparation process was obtained through single factor investigation, microstructure characterization, stability investigation and in vitro simulation digestion experiment. Ten female BALB/c mice (SPF grade, 18–20 g) were selected. After the in situ breast cancer model was successfully established, the mice were randomly divided into experimental group and control group, with 5 mice in each group. The mice were administrated with probiotic-loaded emulsion and normal saline respectively, and were administrated with the stomach every other day for 10 days. The change of tumor volume during treatment and tumor mass at the end of treatment were recorded. Results: The optimum process of emulsion was: With the concentration of 5% Polyglycerin ricinolate, 75% aqueous volume, 3000r/min homogenizing speed, 30 s homogenizing time and 2% aqueous sodium alginate concentration, a high internal phase emulsion with a particle size of 9.33 ± 1.74 μm and an appearance of milky paste was prepared. The inclusion rate of probiotics reached 90.97 ± 27.09%. Breast cancer anti-tumor experiment showed that the tumor inhibition rate of the experimental group reached 33.78% compared with the control group. Conclusion: Water-in-oil high internal phase emulsion can effectively protect L. casei and reduce the loss of live probiotic when probiotics pass through the digestive fluid environment. Oral intragastric high internal phase emulsion containing L. casei oil-in-water has a certain therapeutic effect on breast cancer.

Deep eutectic solvent combined with permeation enhancer strategy to convert tandospirone from oral to transdermal formulations improving drug bioavailability

Tandospirone(Tan) is a commonly used drug for anxiety treatment. However, it has a significant first-pass effect and needs to be taken three times a day. To increase the bioavailability of the drug and reduce the number of administrations, this work amid to prepare a Tan patch that can be administered once a day by using the strategy of therapeutic deep eutectic solvent(THEDES) in cooperation with chemical permeation enhancer(CPE). In this study, four organic acids and five permeation enhancers were selected, and the optimized formulation was obtained by single-factor investigation and Box-Behnken design. The optimized formulation could significantly enhance drug loading by 2.5-fold and skin permeation up to 586.6 ± 17 μg/cm2 in rats. Based on pharmacokinetic results, compared to oral administration, the drug exhibited a substantially elevated bioavailability, registering a 17-fold increase(from 3.01 % to 52.17 %), alongside a 10-fold rise in the mean residence time(MRT). Meanwhile, the patch was not irritating. The results of the mechanistic study showed that levulinic acid(LeA) acted as a bridge to increase the interaction between the Tan and the matrix and inhibited the crystallization of the drug in the patch, and THEDES together with CPE improved the matrix fluidity and skin permeability. This study provides a reference for the joint application of THEDES and CPEs in patch development.

Osmotic absorption behaviors of imidazolium ILs in digestive system and their effective removal way

Considering the controversial safety and risk solutions of ionic liquids (ILs), more essential basic researches are required as their applied fields become broader and applied scale grows larger. Under this background, the permeation behaviors of six common imidazole ILs on porcine gastric and enteric membranes together with the feasibility of their removal by adsorption with montmorillonite were investigated in vitro. Through the single-factor investigation of different cations, anions and ionic liquid concentrations, the current results show that the IL of 1-ethyl-3-methylimidazolium bromide ([Emim]Br) has the strongest permeation capacity on the gastric membrane during the tests. The cumulative permeation amount of Qn can reach 0.72 mg/cm2, and the cumulative permeation percentage alsoreaches 95.77 %; the whole permeation process conforms to the Hixcon-Crowell model. As comparison, the maximum cumulative penetration percentage of [Emim]Br on enteric member was determined as 89.11 %, and related models was also compared. In order to remove the potential IL in digestive tract, montmorillonite was screened out from those popularily used antidotes in clinic and the adsorption of [Emim]Br in gastric fluid by montmorillonite has been proved more consistent with the second-order kinetics and Langmuir model. The results of molecular simulation, infrared spectrum (IR), X-ray diffraction (XRD) and thermogravimetric (TG) characterization exhibit that [Emim]Br has been successfully adsorbed into the interlayer of montmorillonite. As a whole, the study provided a scientific and effective way to diminish the hidden danger of ionic liquid entering the blood through the digestive system.

Preparation of copolymer 7-hydroxyethyl chrysin loaded PLGA nanoparticles and the in vitro release.

To prepare 7-hydroxyethyl chrysin (7-HEC) loaded poly (lactic-co-glycolic acid) (PLGA) nanoparticles and to detect the in vitro release. The 7-HEC/PLGA nanoparticles were prepared by emulsification solvent volatilization method. The particle size, polydispersity index (PDI), encapsulation rate, drug loading and zeta potential were measured. The prescription was optimized by single factor investigation combined with Box-Behnken response surface method. Mannitol was used as protectant to prepare lyophilized powder, and the optimal formulation was characterized and studied for the in vitro release. The optimal formulation of 7-HEC/PLGA nanoparticles was as follows: drug loading ratio of 2.12∶20, oil-water volume ratio of 1∶14.7, and 2.72% soybean phospholipid as emulsifier. With the optimal formulation, the average particle size of 7-HEC/PLGA nanoparticles was (240.28±0.96) nm, the PDI was 0.25±0.69, the encapsulation rate was (75.74±0.80)%, the drug loading capacity was (6.98±0.83)%, and the potentiostatic potential was (－18.17±0.17) mV. The cumulative in vitro release reached more than 50% within 48 h. The optimized formulation is stable and easy to operate. The prepared 7-HEC/PLGA nanoparticles have uniform particle size, high encapsulation rate and significantly higher dissolution rate than 7-HEC.

Salen-based ionic polymers as efficient heterogeneous catalysts for CO2 cycloaddition

A Salen-functionalized ionic polymer (Zn-Salen-IP) was synthesized through a metal-assisted method. The structure and microstructure were characterized by using different characterization methods. Subsequently, the cycloaddition of CO2 with epoxide was used to investigate the catalytic activity of Zn-Salen-IP. The relationship between the types of ions within Zn-Salen-IP and its catalytic performance was thoroughly explored. Single-factor investigations were used to determine the optimal reaction conditions for catalytic CO2 cycloaddition used Zn-Salen-IP. The universality and recyclability of Zn-Salen-IP were systematically studied under the optimized conditions. Finally, Density functional theory calculations were employed to research the mechanism and pathway of the CO2 cycloaddition reaction catalyzed by Zn-Salen-IP with dual functional active sites. This provided a deep understanding for the rate-determining step and the influence of the nucleophilicity of the halogen anion in cycloaddition reaction of CO2 and epoxide.

Hot water washing processing technology of Euodiae Fructus based on change laws of active components and tastes

In order to establish the standardized processing technology of the hot water washing of Euodiae Fructus, this study, based on the traditional processing method of hot water washing of Euodiae Fructus recorded in ancient works and modern processing specifications of traditional Chinese medicine decoction pieces, took the yield of decoction pieces and the content of main components as the indicators and optimized the processing conditions by orthogonal test based on the results of single factor investigation. At the same time, electronic tongue technology was used to analyze the change law of the taste index of Euodiae Fructus during the hot water washing. The results of the single factor investigation showed that the content of the main components in Euodiae Fructus showed some regular changes during the processing. Specifically, the content of chlorogenic acid, hyperin, isorhamnetin-3-O-rutinoside, isorhamnetin-3-O-galactoside, and dehydroevodiamine decreased significantly, with average decreases of-23.75%,-27.80%,-14.04%,-14.03%, and-13.11%, respectively. The content of limonin increased significantly with an average increase of 19.83%. The content of evodiamine, rutaecarpine, evocarpine, and dihydroevocarpine showed fluctuating changes and generally increased, with average variation amplitudes of 0.54%,-3.78%, 2.69%, and 5.13%, respectively. The orthogonal test results showed that the optimum processing parameters for the hot water washing of Euodiae Fructus were as follows: washing time of 2 min, the solid-to-liquid ratio of 1∶10 g·mL~(-1), washing temperature of 80 ℃, washing once, and drying at 50 ℃. After the hot water washing processing, the average yield of Euodiae Fructus pieces was 94.80%. The content of limonin, evodiamine, and rutaecarpine was higher than those of raw pro-ducts, and the average transfer rates were 102.56%, 103.15%, and 105.16%, respectively. The content of dehydroevodiamine was lower than that of the raw products, and the average transfer rate was 83.04%. The results of taste analysis showed that the hot water washing could significantly reduce the salty, astringent, and bitter tastes of Euodiae Fructus. This study revealed the influence of the hot water washing on the content of main components and taste of Euodiae Fructus, and the processing technology of the hot water was-hing of Euodiae Fructus established in this study was stable, feasible, and suitable for industrial production, which laid a foundation for clarifying its processing principle and improving the quality standard and clinical application value of decoction pieces.

A multiparametric fluorescent visualization approach for detecting drug resistance in living cancer cells

Drug resistance is a worldwide health care crisis which impedes disease treatment and increases financial burden, especially for its multifactorial nature and high complexity. Herein, we developed a multiparametric approach to visualize and detect drug resistance in living cancer cells, through the combination of DNA-templated covalent protein labeling strategy and fluorescent resonance energy transfer technique. Gefitinib resistance in non-small cell lung cancer caused by mesenchymal-epidermal transition factor (Met) overexpression and hyperactivation was investigated as a proof-of-concept. Unlike the traditional single-factor investigation, the proposed approach evaluated the contribution of three important parameters towards the resistance, including the changes of Met expression level, the homodimerization of Met with itself and the heterodimerization of Met with epidermal growth factor receptor (EGFR). A multiple regression model based on these three parameters was tentatively established for evaluation of the resistance level of laboratory-developed resistant cells and evaluation of the resistance level of patient-derived cells. Such an approach facilitates a quick identification of a drug resistance, to evaluate not only the resistance level but also the resistance mechanism.

Combination of ion-pair strategy and chemical enhancers for design of dexmedetomidine long-acting patches: Dual action mechanism induced longer controlled release and better delivery efficiency

The purpose of this study was to prepare a dexmedetomidine (Dex) 72 h long-acting patch by the combined use of ion-pair strategy and chemical enhancers (CEs), and to investigate molecular mechanisms of drug-loading enhancement and controlled release. The formulation of patch was optimized by single-factor investigation and Box-Behnken design. The pharmacokinetics, analgesic pharmacodynamics and irritation of the formulation were evaluated, respectively. Moreover, the effects of ion-pairs and CEs on the patch were characterized by DSC, rheology study, FTIR, and molecular docking, and the effects on the skin were evaluated by Attenuated Total Reflection Fourier Transform Infrared Spectroscopy (ATR-FTIR), Raman study, and molecular dynamics, respectively. The optimized formulation was 17.00 % (w/w) Dex-NA (Naphthoic acid), 7.20 % Polyglyceryl-3 dioleate (POCC), 25-AAOH as pressure sensitive adhesives (PSA) and 66.50 μm in thickness. Compared with the control group (Cmax = 62.02 ± 16.55 ng/mL, MRT0-t = 26.74 ± 1.27 h), the pharmacokinetics behavior of the optimization group was more stable and durable (Cmax = 31.22 ± 13.26 ng/mL, MRT0-t = 33.62 ± 1.62 h). Besides, it also showed good analgesic effect and no obvious irritation. The results indicated that Dex-NA both increased the drug-PSA interactions and inhibited the penetration of the drug into the skin. POCC increased the molecular mobility of the PSA and disrupted skin lipids thereby improving the drug penetration rate. In summary, the Dex long-acting patch was developed, which provided a reference for the combined application of ion-pair strategy and CEs in other long-acting transdermal delivery.

The effects of solvent–based ultrasonic–assisted extraction of bioactive compounds and antioxidant activities from pigmented rice bran

Rice is one of the staple grains that most people consume. Pigmented rice is a highly nutritious rice bran, and it is abundant in bioactive compounds like phenolic compounds, which have antioxidant activities. In order to effectively extract bioactive compounds for adoption, it is essential to select the optimal solvent–based extraction method. The study's objective was to optimize the solvent–based ultrasonic–assisted extraction of bioactive compounds and antioxidant activities from pigmented rice bran. A single factor investigation was used to study the effects of duration time (20–40 min), UAE temperature (30–60 °C), and sample–to–solvent ratio (1:10–1:30 g/mL). The bioactive compounds were determined using total anthocyanin content (TAC), total phenolic content (TPC), and total flavonoid content (TFC) assays. The DPPH radical scavenging activity assay was used to assess antioxidant activities. According to the results of the experiments, extraction conditions had a significant effect on bioactive compound extraction and antioxidant activities. The optimum solvent extraction was 60% (v/v) aqueous methanol with 0.1% citric acid solvent, yielding values of 2.32 ± 0.14 mg C3G/g DW for TAC, 13.36 ± 0.89 mg GAE/g DW for TPC, 2.99 ± 0.87 mg QE/g DW for TFC and 398.29 ± 96.08 µg/mL for 50% inhibition concentration on DPPH (IC50). The ultrasonic–assisted extraction (UAE) of pigmented rice bran bioactive compounds under optimal conditions at 30 °C for 30 min with a material-to-solvent ratio of 1:20 g/mL resulted in an extract with 3.15 ± 0.15 mg C3G/g DW of TAC, 16.13 ± 0.82 mg GAE/g DW of TPC, 4.04 ± 0.11 mg QE/g DW of TFC and 413.90 ± 47.46 µg/mL of IC50. It shows that, under optimal conditions, solvent–based ultrasonic–assisted extraction could be used to maximize the extraction of bioactive phytochemicals from pigmented rice bran.

Construction and Evaluation of Hyaluronic Acid-Coated Flurbiprofen-Layered Double Hydroxide Ocular Drug Delivery System.

In this study, flurbiprofen (FB) was selected as the model drug, and hyaluronic acid-coated flurbiprofen-layered double hydroxide ophthalmic drug delivery system (HA-FB-LDH) was designed and prepared. In this system, the model drug flurbiprofen was intercalated in layered double hydroxide and coated with hyaluronic acid (HA), so as to prolong the cornealresidencetime and increase the corneal permeability of the drug. Layered double hydroxide (LDH) was prepared by alcohol-water coprecipitation method. Through single factor investigation, the optimum preparation conditions were obtained as follows: The Mg/Al ratio was 2:1, the reaction pH was 11.0, the hydrothermal reaction time was 24h, and the hydrothermal reaction temperature was 100°C. Under these conditions, the particle size of LDH was 116.4 ± 0.8nm, the potential was 42.2 ± 1.2mV, and a relatively regular crystal structure could be had. Then FB was intercalated into the LDH layer to prepare flurbiprofen-layered double hydroxide (FB-LDH). In the end, HA-FB-LDH was prepared by the stirring-ultrasonic method, in which through prescription screening, the molecular weight of HA was 200-400kDa and the concentration of HA solution was 1.25mg·mL -1, the final particle size of HA-FB-LDH was 185.8 ± 3.3nm, and potential of - 31.4 ± 0.7mV. The successful loading of FB and the coating of HA were verified by XRD, FTIR, TGA, TEM, and other characterization methods. The results of in vitro stability experiment indicated that the coating of HA could significantly enhance the stability of LDH in the presence of electrolytes. The in vitro release results suggested that the cumulative release amounts of FB-LDH and HA-FB-LDH within 12h were 92.99 ± 0.37% and 74.82 ± 0.29% respectively, showing a certain sustained release effect. At the same time, the release mechanism of FB-LDH was preliminarily explored by in vitro release experiment, which proved that the release mechanism of FB-LDH was mainly ion exchange. The results of in vivo ocular irritation experiments demonstrated that the ophthalmic preparation studied in this paper was safe and non-irritating. The results of tear pharmacokinetics in rabbits showed that the area under the curve(AUC), the average residence time (MRT), and the highest concentration (Cmax) in tears in the HA-FB-LDH group were 4.43, 4.48, and 2.27 times higher than those in eye drops group separately. Furthermore, the AUC of the HA-FB-LDH group was 1.48 times higher than that of the FB-LDH group. The above results suggested that HA-FB-LDH could improve the precorneal residence time. The results of aqueous humor pharmacokinetics in rabbits indicated that the AUC, MRT, and maximum concentration (Cmax) in aqueous humor in the HA-FB-LDH group were 6.88, 2.15, and 4.08 times of those in the eye drop group respectively. Additionally, the AUC and MRT of the HA-FB-LDH group were 1.55 and 1.63 times those of the FB-LDH group separately. These mentioned findings verified that HA-FB-LDH could enhance the corneal permeability of the drug. The fluorescent substance-fluoresce isothiocyanate (FITC) was substituted for FB intercalation in LDH for in vitro tissue imaging study of rabbits, whose results stated clearly that FITC-LDH and HA-FITC-LDH could both prolong the precorneal residence time of drugs, and HA-FITC-LDH could increase the corneal permeability of the drug to a certain extent. To sum up, HA-FB-LDH, which can overcome the shortcomings of low bioavailability of traditional eye drops to a certain degree, is a safe and effective ophthalmic drug delivery system.

Non-metal and non-halide enol PENDI catalysts for the cycloaddition of CO2 and epoxide

A series of non-metal and high-efficiency PENDIs with hydrogen bond donor, which were prepared by condensation reaction of β-diketone and imine, are used for cycloaddition of CO2 and epoxides. The influences of different structure of catalysts and hydrogen bonds on catalytic performance were studied by experiments and density functional theory. The results showed that PENDIs which possess -OH of β-diketone and -NH- exhibit excellent catalytic performance for cycloaddition of CO2 and epichlorohydrin, and the record yield is 97.26 %. The single factor investigation and response surface methodology were used for obtaining optimal reaction conditions of PENDIs. A possible mechanism for CO2 cycloaddition that catalyzed by PENDIs is proposed, it includes epoxide adsorption, ring-opening of epoxide, CO2 insertion and the formation of cyclic carbonate. It is proved that the synergy between -OH of β-diketone and -NH- can promote the catalytic performance of PENDIs for CO2 cycloaddition.

Preparation of astragaloside IV (AS-IV) nanoparticles via SAS process for anticancer efficacy: Optimization based on Box-Behnken Design

Despite significant advances in drug formulation, the clinical application of most active pharmaceutical ingredients from traditional Chinese herbs remained a significant challenge due to their poor solubility. To address this crucial issue, astragaloside-IV (AS-IV) was selected as a model drug to prepare nanoparticles with a large specific surface area via a constant, steady, and well-organized supercritical antisolvent (SAS) method. Initially, the optimal range of nanoparticle nucleation was determined by a single-factor investigation under altered critical conditions. Under the optimized conditions obtained from the Box-Behnken Design model analysis (AS-IV solution flow rate (F): 0.85 mL/min, Temperature (T): 42 ℃, Pressure (P): 120 bar), the SAS process resulted in nanospheres with smooth surface and narrow particle size distribution. After the SAS process treatment, AS-IV with altered physical states presented improved solubility and enhanced in vitro antiproliferative effects compared to untreated AS-IV, illustrating the potential application of the SAS method in promoting the bioavailability of low water-soluble drugs.

Optimization of preparation technology for Acanthopanax senticosus total saponins microemulsion by D-optimal mixture design and intestinal absorption characteristics

Following the preparation of Acanthopanax senticosus total saponins microemulsion, the formulation and preparation technology were optimized and the quality was evaluated. The absorption characteristics of A. senticosus total saponins microemulsion by the self-microemulsifying drug delivery system(SMEDDS) were investigated in the unidirectional intestinal perfusion model in vivo. The oil phase, mass ratio(K_m), number of revolutions, and drug concentration were subjected to single-factor investigation with the area of pseudo-ternary phase diagram as the index. The process was optimized by D-optimal mixture design with the particle size as the index, and then the appearance, morphology, and particle size were investigated. The mass concentrations of eleutherosides B and E in the microemulsion were determined. The results showed that the optimum formulation of A. senticosus total saponins microemulsion was determined as follows: 20.8% of water phase, 31.2% of isopropyl palmitate, and 48.0% of soybean phospholipid and absolute ethanol(K_m=1∶1). As revealed by the observation under a transmission electron microscope, the microemulsion exhibited homogeneous dispersion and was a spherical emulsion droplet in the water-in-oil type. At room temperature, the pH value was 5.19, the refractive index 1.416 5, the average particle size(26.47±0.04)nm, and the polydispersity index(PDI) 0.118±0.03. The content of the eleutherosides B and E was 0.038 9 and 0.166 4 mg·mL~(-1), respectively. The preliminary stability study showed that the solution was clear and transparent within 30 d, without stratification or content change, indicating good stability. The absorption of microemulsion in each intestinal segment was significantly improved as compared with that of the A. senticosus total saponins, with the best absorption effect detected in the ileum, which has laid a foundation for further development and utilization of A. senticosus.

Microwave-Assisted Extraction of Anticancer Flavonoid, 2',4'-Dihydroxy-6'-methoxy-3',5'-dimethyl Chalcone (DMC), Rich Extract from Syzygium nervosum Fruits.

2′,4′-Dihydroxy-6′-methoxy-3′,5′-dimethyl chalcone (DMC) is a biological flavonoid that is present in the fruits of Syzygium nervosum (Ma-Kiang in Thai). Microwave-assisted extraction (MAE), which utilizes microwave radiation to heat the extraction solvent quickly and effectively, was used to recover DMC-rich extract from Syzygium nervosum fruit. To determine the DMC content, a highly accurate and precise HPLC technique was developed. The influences of MAE conditions, including the solid–liquid ratio, microwave power, and microwave duration on the content of DMC, were sequentially employed by a single factor investigation and response surface methodology (RSM) exploratory design. The predicted quadratic models were fitted due to their highly significant (p < 0.0001) and excellent determination coefficient (R2 = 0.9944). The optimal conditions for producing DMC-rich extract were a ratio of sample to solvent of 1:35 g/mL, a microwave power of 350 W, and a microwave time of 38 min. Under the optimal MAE setting, the DMC content reached 1409 ± 24 µg/g dry sample, which was greater than that of the conventional heat reflux extraction (HRE) (1337 ± 37 µg/g dry sample) and maceration (1225 ± 81 µg/g dry sample). The DMC-rich extract obtained from MAE showed stronger anticancer activities against A549 (human lung cancer cells) and HepG2 (human liver cancer cells) than the individual DMC substance, which makes MAE an effective method for extracting essential phytochemicals from plants in the nature.

Optimization of Phenol Sulfuric Acid Method for the Polysaccharide Content of Wine-steamed Polygonatum cyrtonema Hua

Objectives: To establish the optimal method of phenol-sulfuric acid method to determine polysaccharides from wind-steamed Polygonatum cyrtonema Hua. Methods: The anthrone-sulfuric acid method and phenol-sulfuric acid method were used at the same time to measure the polysaccharide content of wine-steamed Polygonatum cyrtonema Hua. For the phenol-sulfuric acid method, the concentration of phenol, the amount of phenol, the amount of sulfuric acid, the heating time and the heating temperature were selected for single-factor investigation. And the response surface method was used for analysis and optimization. Results: Analyzing the F value by response surface method, the influence of each factor on the absorbance was: The amount of sulfuric acid>the concentration of phenol>the amount of phenol. The heating temperature and time had no obvious effect. The best process obtained was 1.5 mL of phenol, 4.5% of phenol and 6.5 mL of sulfuric acid. Measuring by this condition, the average content of polysaccharides was 8.50% and the relative standard deviation was 0.87%. Conclusion: The phenol-sulfuric acid method after the optimization could accurately measure the polysaccharide content in the wine-steamed Polygonatum cyrtonema Hua, which would provide reference value for further study of quality standard.

Application of Implantable Polylactic-Co-Glycolic Acid Microcapsule in Repairing Alveolar Bone Defects.

Alveolar bone defects (ABDs) were a perennial problem, especially in the aged. Bisphosphonates, especially etidronate sodium (ET), were frequently used in clinical treatment of ABD. However, the oral administration of ET had poor absorption (<1%). Therefore, optimization of a suitable dosage form substituted with ET to locally repair the ABD was a straightforward approach. Polylactide-co-glycolide (PLGA) is a biodegradable material and had been used in locally implanted medical devices. Therefore, an ET-PLGA microcapsule may help local delivery and prolong the activity of healing ABD. In this paper, a preparation method of ET-PLGA microcapsule was optimized by the single-factor investigation and response surface method. Subsequently, the rat ABD model was used to evaluate the enhancement effect of these microcapsules. Finally, the optimum parameters were determined as follows: 40% dichloromethane, 160 mg/mL PLGA, 10% internal aqua/oil phase, 4% PVA, and emulsifying for 10 min. These microcapsules were spherical in shape and fairly monodisperse in a particle size of 27,51 μm (PDI = 0.3), encapsulation rate 96.6%, and drug loading 4.58%. Compared with the ET groups, the total healing volume of ABD in ET-PLGA groups was significantly increased (P < 0.05). ET-PLGA microcapsules significantly enhanced the effect of ET on ABD. This study provided important technical support for the treatment of ABD with bisphosphonates by local administration. This paper has an exploratory significance for the development of water-soluble bioactive components with low bioavailability for ABD.

Dummy molecularly imprinted membranes based on an eco-friendly synthesis approach for recognition and extraction of enrofloxacin and ciprofloxacin in egg samples

In this work, novel dummy molecularly imprinted membranes (MIMs) were fabricated using the nylon-66 (NY-66) membranes as the subtracts based on an eco-friendly “sandwich” technology with less consumption of organic reagents at mild conditions for recognition and extraction of enrofloxacin (ENR) and ciprofloxacin (CIP) in egg samples. The prepared MIMs were characterized by SEM, ATR-FTIR and TGA, showing the successful construction of uniform and porous polymers on the surface of membranes. A series of adsorption affinity tests were investigated, indicating the prepared materials had specific recognition capacity and excellent stability as novel sorbents. Furthermore, Box-Benhnken design (BBD) and single factor investigations were applied to optimize pretreatment procedures, coupling with Ultra High Performance Liquid Chromatograph (UHPLC) detection. The method showed a good correlation (r2>0.9999) within the linear range of 5.0~5000.0 µg kg−1, and limit of detection (LOD) of ENR and CIP were 0.3 and 0.7 µg kg−1, respectively. The mean recovery ranged from 84.5% to 97.0% within relative standard deviations (RSDs) of 10.2%. Finally, ENR and CIP were not detected in 3 batches of egg samples. The current study developed the dummy MIMs as sorbents combined with UHPLC analysis for extraction and detection of target analytes in food matrices.

Optimization of canthaxanthin extraction from fermented biomass of Paracoccus carotinifacuens VTP20181 bacteria strain isolated in Vietnam

Introduction. The bacterium strain Paracoccus carotinifaciens VTP20181 isolated in Vietnam produces canthaxanthin, a carotenoid widely used in the food and pharmaceutical industries. The aim of this work was to determine optimal parameters for canthaxanthin extraction from fermented biomass of P. carotinifaciens VTP20181.&#x0D; Study objects and methods. First, a series of single factor investigations were carried out in regard to maximal carotenoid content in the biomass extract obtained by using ultrasonic waves. Four parameters of the extraction process, such as extraction temperature, solvent/material ratio, extraction time, and ultrasonic output power, were studied. The obtained results were then optimized by using Response Surface Methodology (RSM) and Box-Behnken experimental design.&#x0D; Results and discussion. The optimal technological parameters of the extraction process included extraction temperature of 35°C, solvent/material ratio of 9.5:1 (v/w), extraction time of 90 min, and ultrasonic output power of 145 W. Under optimal conditions, canthaxanthin and total carotenoid contents were determined as 14.95 ± 0.12 and 18.21 ± 0.11 mg/g respectively, which were compatible with theoretical calculations ‒ 15.074 and 18.263 mg/g, respectively.&#x0D; Conclusion. Current results confirmed that the strain of halophilic P. carotinifaciens VTP20181 is a potential source for canthaxanthin biosynthesis.

A study of the freeze-drying process and quality evaluation of Angelica sinensis

Abstract The freeze-drying process of Angelica sinensis (Oliv.) Diels was studied and evaluated. Using a single factor investigation, drying temperature and pressure were determined as the main factors affecting the drying process. The central composite design (CCD) combined with response surface method was employed to optimize the drying process. Optimal conditions were determined to be 52 Pa, 63 °C, and a slice thickness of 5 mm. Subsequently, samples were compared in terms of chemical constituents, microstructure, and in vitro absorption profiles under different drying operations. The freeze-drying process was effective for the preservation of ferulic acid (1.82 mg/g), Z-ligustilide (13.91 mg/g), and other compositions. The porous and loose characteristic structure enabled rapid release of ferulic acid (71%, 60 min) and Z-ligustilide (32%, 60 min). Therefore, the freeze-drying method is a reasonable and efficient drying method for the dehydration of A. sinensis.