Cadmium(Cd)contamination in soil can lead to food chain accumulation and greatly impacts on human health.Bioremediation has gained more and more attention due to its environment-friendly,high efficiency and low-cost.I...Cadmium(Cd)contamination in soil can lead to food chain accumulation and greatly impacts on human health.Bioremediation has gained more and more attention due to its environment-friendly,high efficiency and low-cost.In this work,we studied the impact of phosphate solubilizing bacterial agent(PSBA)on Cd bioavailability,microbial communities in soil and Cd accumulation in lettuce plants with pot experiment and field trial.Results of pot experiment showed that PSBA could decrease the bioavailability of Cd(Cd-acid extractable from 3.30 to 2.34mg/kg,Cd-reducible from 1.94 to 1.56 mg/kg),promote lettuce plants growth(increased by 33.85%height and by 33.65%fresh weight)and reduce the accumulation of Cd(from 5.85 to 3.73 mg/kg)in lettuce plants.High-throughput sequencing identified that PSBA could change the composition and structure of the soil microbial communities.The relative abundances of the three ecologically beneficial bacterial families of Pseudomonadaceae,Burkholderiaceae,and Enterobacteriaceae increased from 2.29%to 5.13%,0.56%to 5.24%,and 1.87%to 16.93%,respectively.And the former two were positively correlated with redox potential(Eh)(R^(2)=0.474,p<0.05,R^(2)=0.590,p<0.01,respectively).The bacterial networks were more complex in PSBA treatment,reflecting through more links(from 1893 to 2185)and a higher average degree(from 38.242 to 45.052)and density(from 0.390 to 0.469).Results of field trial demonstrated that PSBA could also decrease Cd content in lettuce plants and microbial composition in soil.This study indicated that PSBA could be served as an alternative material in bioremediation of Cd contamination in soil.展开更多
Traditional Chinese medicine(TCM)offers diverse therapeutic compounds but faces challenges like poor bioavailability and instability.Recent innovations in drug delivery systems,including nanotechnology-based drug deli...Traditional Chinese medicine(TCM)offers diverse therapeutic compounds but faces challenges like poor bioavailability and instability.Recent innovations in drug delivery systems,including nanotechnology-based drug delivery systems have shown potential to enhance solubility,stability,and therapeutic efficacy.This review examines these advancements,focusing on their mechanisms and applications in improving TCM formulations.Cutting-edge techniques,such as microneedles,iontophoretic patches,and self-orienting applicators,are also discussed for their potential to revolutionize TCM delivery.By bridging traditional wisdom with modern innovations,this review emphasizes the transformative role of these strategies in advancing TCM's integration into contemporary medicine.展开更多
Algal copper uptake(i.e.,Cu bioavailability)in the euphotic zone plays a vital role in algal photosynthesis and respiration,affecting the primary productivity and the source and sink of atmospheric carbon.Algal Cu upt...Algal copper uptake(i.e.,Cu bioavailability)in the euphotic zone plays a vital role in algal photosynthesis and respiration,affecting the primary productivity and the source and sink of atmospheric carbon.Algal Cu uptake is controlled by natural dissolved organic Cu(DOCu)speciation(i.e.,complexed with the dissolved organic matter)that conventionally could be tested by model prediction or molecular-level characterizations in the lab,while DOCu uptake are hardly directly assessed.Thus,the new chemistrybiology insight into the mechanisms of the Cu uptake process in algae is urgent.The DOCu speciation transformation(organic DOCu to free Cu(II)ions),enzymatic reduction-induced valence change(reduction of free Cu(II)to Cu(I)ions),and algal Cu uptake at the algae-water interface are imitated.Herein,an intelligent system with DOCu colorimetric sensor is developed for real-time monitoring of newly generated Cu(I)ions.Deep learning with whole sample image-based characterization and powerful feature extraction capabilities facilitates colorimetric measurement.In this context,the Cu bioavailability with 7 kinds of organic ligands(e.g.,amino acids,organic acids,carbohydrates)can be predicted by the mimetic intelligent biosensor within 15.0min,i.e.,the DOCu uptake and speciation is successfully predicted and streamlined by the biomimetic approach.展开更多
Propolis is a resinous complex mixture made from plant resins collected by worker bees and mixed with their own secretions.It is rich in polyphenols and flavonoids and thus has a wide range of biological activities an...Propolis is a resinous complex mixture made from plant resins collected by worker bees and mixed with their own secretions.It is rich in polyphenols and flavonoids and thus has a wide range of biological activities and is considered a functional source for promoting human health.However,propolis and its bioactive compounds have poor water solubility,rapid and intense metabolism,and low oral bioavailability,which limits their wide application.In this paper,the main bioactive substances in propolis were summarized,and the biological characteristics and therapeutic potential of propolis and its bioactive substances were discussed.In addition,this paper discussed the factors affecting the bioavailability of propolis and its functional ingredients,focusing on the research progress in improving the bioavailability and bioactivity of propolis and its functional ingredients using nanoencapsulation technology.Finally,the current situation of the global propolis market and the applications of propolis products in the pharmaceutical,food,cosmetic and other industrial fields were discussed,providing useful references for promoting the development of the propolis industry.展开更多
In this paper,the vegetable field in the teaching base of College of Agriculture,Yangtze University was taken as the research object.The indoor simulation method was used to explore the effects of temperature and mois...In this paper,the vegetable field in the teaching base of College of Agriculture,Yangtze University was taken as the research object.The indoor simulation method was used to explore the effects of temperature and moisture on the phosphorus(P)bioavailability of vegetable soil.Three temperature gradients[T1(15℃),T2(25℃),T3(35℃)]and three humidity gradients[W1(40%),W2(70%),W3(100%)]were set in the test.The results showed that it could improve the contents of HCl-P,Enzyme-P,Citrate-P,and Olsen-P in vegetable soil by increasing soil moisture content;temperature rise was helpful to increase the contents of HCl-P and Olsen-P,but it could reduce the content of Citrate-P.The contents of Enzyme-P and CaCl 2-P were significantly affected by hydrothermal interaction.Within a certain range of soil temperature and humidity,temperature and moisture had a positive coupling effect on soil P bioavailability components,and significantly affected soil P supply capacity.展开更多
Given the severe toxicity and widespread presence of cadmium(Cd)in staple foods such as rice,accurate dietary exposure assessments are imperative for public health.In vitro bioavailability is commonly used to adjust d...Given the severe toxicity and widespread presence of cadmium(Cd)in staple foods such as rice,accurate dietary exposure assessments are imperative for public health.In vitro bioavailability is commonly used to adjust dietary exposure levels of risk factors;however,traditional planar Transwell models have limitations,such as cell dedifferentiation and lack of key intestinal components,necessitating a more physiologically relevant in vitro platform.This study introduces an innovative three-dimensional(3D)intestinal organoid model using a microfluidic chip to evaluate Cd bioavailability in food.Caco-2 cells were cultured on the chip to mimic small intestinal villi's 3D structure,mucus production,and absorption functions.The model's physiological relevance was thoroughly characterized,demonstrating the formation of a confluent epithelial monolayer with well-developed tight junctions(ZO-1),high microvilli density(F-actin),and significant mucus secretion(Alcian blue staining),closely resembling the physiological intestinal epithelium.Fluorescent particle tracking confirmed its ability to simulate intestinal transport and diffusion.The Cd bioavailability in rice measured by the 3D intestinal organoid model((9.07±0.21)%)was comparable to the mouse model((12.82±3.42)%)but significantly lower than the Caco-2 monolayer model((26.97±1.11)%).This 3D intestinal organoid model provides a novel and reliable strategy for in vitro assessment of heavy metal bioavailability in food,with important implications for food safety and risk assessment.展开更多
Previous study has shown that 10-hydroxycamptothecin（HCPT） has well-established pharmacological effects in vitro.However,its in vivo bioavailability is very poor due to various problems,which severely restricts its ...Previous study has shown that 10-hydroxycamptothecin（HCPT） has well-established pharmacological effects in vitro.However,its in vivo bioavailability is very poor due to various problems,which severely restricts its clinical applications.In the present study,phospholipid complex（PC） technology was employed to improve the solubility and bioavailability of HCPT.XRD data confirmed the formation of HCPT-PC.However,our previously prepared HCPT-PC is too sticky,which may result in the slow dissolution rate and negative effects on its absorption.Therefore,we prepared HCPT-PC-solid dispersion（HCPT-PC-SD）and lipid-based formulations of HCPT-PC through simple preparation process.The results showed that the dissolution rate of HCPT-PC was effectively improved by solid dispersion technology,which reached 91.73%in 45 min.Pharmacokinetic study revealed that the AUC_（0-t） of HCPT-PC-SD and HCPT-PC lipid-based formulations was effectively further increased compared with HCPT-PC.Moreover,we found that the combination of SD technology and lipid-base formulations could be a promising drug-delivery system to improve the oral bioavailability of HCPT-PC.In addition,we showed that the bioavailability of HCPT-PC lipid-base formulations was even greater than that of HCPT-PC-SD.In particular,lipid-base formulations could be prepared just by a simple method,suggesting its feasibility of industrialization.展开更多
A new HPLC MS method to determine loratadine in human plasma was established. The method involved extracting drug with organic solvent under basic conditions. The samples were seperated by ODS column and determined ...A new HPLC MS method to determine loratadine in human plasma was established. The method involved extracting drug with organic solvent under basic conditions. The samples were seperated by ODS column and determined by mass detector. The calibration curve of loratadine was linear within the range of 0.4～100 ng·mL -1 with r=0.9995 . The recovery of this method was within 95%～104%, within day and between day RSD were less than 12%. To study the pharmacokinetics and relative bioavailability of loratadine tablets, two formulations of loratadine tablets were given to 18 healthy male volunteers according to a randomized 2 way cross over design. The C max , AUC 0 t and T max values of the two formulations were 51.89±20.18 ng·mL -1 and 52.48±22.35 ng·mL -1 ; 140.75±88.42 ng·h·mL -1 and 147.24±92.33 ng·h·mL -1 ; 0.81±0.35 h and 0.81±0.27 h respectively. Results from statistic analysis showed that there were no significant difference between the C max , AUC 0-t and T max values of the two formulations. The relative bioavailability of tablets I with respect to tablets II was 97%±13% from the AUC 0 t measurement. Bioequivalance was observed between the two tablets.展开更多
Many active constituents from herbal plants have well-established pharmacological effects in vitro. But they demonstrate less or no activities in vivo due to various problems of themselves, which severely restricts th...Many active constituents from herbal plants have well-established pharmacological effects in vitro. But they demonstrate less or no activities in vivo due to various problems of themselves, which severely restricts their clinical applications. After forming phytosomes with phospholipids in aprotic solvent, the active constituents exhibit different physicochemical properties from the free form. In particular, the bioavailability of the active constituent-phytosomes is enhanced greatly due to the improved capacity to cross the biomembrane and reach circulation. Therefore, increasing attention has been attracted to the use of phytosomes in recent years. Based on the published reports, we reviewed the recent progress in the research of phytosomes including preparation, characterization, structure verification and clinical applications.展开更多
The pharmacokinetics and absolute bioavailability of the sublingual naloxone tablet were studied with HPLC-electrochemical detection. Eight male dogs received single 5 mg dose of naloxone intravenously, the plasma con...The pharmacokinetics and absolute bioavailability of the sublingual naloxone tablet were studied with HPLC-electrochemical detection. Eight male dogs received single 5 mg dose of naloxone intravenously, the plasma concentration-time curves could be fitted to two-compartment open model, with 12.0 min of t1/2( , 143.4 min of t1/2( and 7.92 mg(min/L of AUC. The same eight dogs received 5 mg dose of the sublingual naloxone tablet after an interval of a week. The main pharmacokinetic parameters were: t1/2ka = 11.0 min, t1/2( = 15.4 min, t1/2( = 164.1 min, Tmax = 27.7 min, Cmax = 34.2 ng / ml, and AUC = 6.79 mg(min / L, respectively. The plasma concentration-time curves were fitted to the first order absorption two-compartment open model also. The mean absolute bioavailability of the sublingual naloxone tablet was 86.8 ( 10.9%. No statistically significant differences were found with t1/2(, t1/2(, ( and ( between the two routes of administration. These results indicated that the course of disposition for naloxone in dogs was similar for the two routes of administration, and the absolute bioavailability of the sublingual naloxone tablet was high. Thus satisfactory clinical effects could be expected.展开更多
Aim To establish a sensitive and specific liquid chromatography-mass spectrometry (HPLC-MS) method for measuring lovastatin level in human plasma and the relative bioavailability. Methods Lovastatin in the plasma was ...Aim To establish a sensitive and specific liquid chromatography-mass spectrometry (HPLC-MS) method for measuring lovastatin level in human plasma and the relative bioavailability. Methods Lovastatin in the plasma was extracted with acetoacetate. Simvastatin was added as internal standard (IS). Samples were separated on a C_ 18 column with a mobile phase consisting of methanol and 50 mmol·L~ -1 sodium acetate (88 ∶ 12). The flow rate was 1 mL·min~ -1 . Sample was detected using an electrospray ionization (ES...展开更多
Aim To investigate whether modified-release cefaclor capsules could lead to a more suitable pharmacokinetic profile in the plasma. Methods Cefaclor pellets were prepared by extrusion/spheronization and coated by Eudra...Aim To investigate whether modified-release cefaclor capsules could lead to a more suitable pharmacokinetic profile in the plasma. Methods Cefaclor pellets were prepared by extrusion/spheronization and coated by Eudragit L30D-55 or Eudragit NE30D, then the two sorts of pellets were filled to capsules in a 35：65 ratio to made a modified-release （MR） capsules. The bioavailability of the MR capsules was studied in 24 healthy volunteers after oral administration in a fast state using a commercially available immediate release （IR） capsule as a reference. Results The results showed that the MR formulation had a relatively good bioavailability compared with the commercial capsules, as well as a longer time keeping drug level above MIC than immediate release capsule. The relative bioavailability of the MR capsules was 97.4- 12.1%. Conclusion The data of the present study indicate that time of cefaclor plasma concentration above MIC can be substantially prolonged if cefaclor is administered as a modified- release product.展开更多
Alantolactone, as the principal constituent oflnula Helenium L, has been shown various pharmacologic activities, such as anti-inflammatory and deworming. In the present study, we developed a high performance liquid ch...Alantolactone, as the principal constituent oflnula Helenium L, has been shown various pharmacologic activities, such as anti-inflammatory and deworming. In the present study, we developed a high performance liquid chromatography （HPLC） method for the determination of alantolactone in rat plasma, and pharmacokinetics of alantolactone was investigated after intravenous and oral administrations to Wistar rats. Separation was achieved on C18 column （4.6 mm×250 mm, 5.0 μm） using a mobile phase consisting of methanol-water （70：30, v/v） at a flow rate of 1.0 mL/min. The wavelength of the ultraviolet detector was set at 239 nm. The excellent linearity was found over a concentration range of 0.08-10 μg/mL （R2 = 0.9998）. The intra- and inter-day precisions were good, and the RSD was lower than 2.27%. The mean absolute recovery of alantolactone in plasma ranged from 88.09% to 95.57%. After intravenous administration, alantolactone showed rapid systemic clearance （CL （0.11±0.014） L/h/kg） and small volume of distribution （Vd （0.71±0.14） L/kg）. The biological half life （t1/2） was 56.24 min. After oral administration, alantolactone showed rapid oral absorption in rats, with a short Tmax of （45.02±0.88） and （45.13±0.39） min for 14 and 28 mg/kg, respectively. The bioavailability of alantolactone in rats was 50.88%, indicating that alantolactone was orally available.展开更多
A new pre-column derivation HPLC method with solid-phase extraction to determine captopril in human plasma was established. Derivation products were extracted by a solid-phase extraction method after the reagent, p-a-...A new pre-column derivation HPLC method with solid-phase extraction to determine captopril in human plasma was established. Derivation products were extracted by a solid-phase extraction method after the reagent, p-a-dibromoacetophenone(p-BPB), was added in the plasma samples. The samples were analyzed in a VP-ODS column with UV-detector. The calibration curve of captopril was linear within the range of 5~1000 ngmL-1 with r=0.9987, the recovery of this method was 98.652.04%, within day and between day RSD were no more than 3.4% and 8.4% respectively. To study the pharmacokinetics and the relative bioavailability of captopril tablets, two formulations of captopril tablets were given to 18 healthy male volunteers according to a randomized 2-way cross-over design with a 1-week washout period. The respective AUC0~6 , Cmax and Tmax values of the two formulations were 424.5125.7 and 439.4113.3 mghL-1; 505.9244.6 and 504.8172.2 mgL-1; 0.6620.181 and 0.5280.176 h. Results from statistics analysis showed that there were no significant difference between the AUC0~6 , Cmax and Tmax values of the two formulations, The relative bioavailability of tablets I with respect to II was 96.114.6% from AUC0~6 measurement. Bioequivalance was observed between the two tablets.展开更多
Sorafenib is a novel antitumor drug,which is poorly absorbed in the gastrointestinal tract due to its low solubility in water.To improve the bioavailability of sorafenib,a self-microemulsifying drug delivery system(SM...Sorafenib is a novel antitumor drug,which is poorly absorbed in the gastrointestinal tract due to its low solubility in water.To improve the bioavailability of sorafenib,a self-microemulsifying drug delivery system(SMEDDS) formulation of sorafenib was prepared and its relative bioavailability in rats was evaluated.The blank SMEDDS was prepared from a mixture of ethyl oleate(oil phase,20%,w/w),Cremophol EL(surfactant,48%,w/w),PEG-400(co-surfactant,16%,w/w) and ethanol (co-surfactant,16%,w/w).Sorafenib was subsequently dissolved in the blank SMEDDS to obtain a sorafenib SMEDDS formulation with a final sorafenib concentration at 20 mg/mL.The particle size of the emulsified sorafenib SMEDDS was about 20-25 nm. Compared with sorafenib suspension,the prepared SMEDDS formulation exhibited no effect on the T_(max),but significantly increased the AUC,C_(max) and MRT and decreased the drug clearance.Most importantly,the oral bioavailability based on AUC_(0-72h) increased about 25 times after formulating sorafenib in SMEDDS.We concluded that SMEDDS could be a promising vesicle for the oral delivery of the poorly soluble antitumor drug sorafenib.展开更多
The pharmacokinetics of a sustained- release formulation and an enteric- coated tablet of diclofenac sodium were studied on 8 healthy male volunteers in an open,randomized crossover study.Drug level in serum was assay...The pharmacokinetics of a sustained- release formulation and an enteric- coated tablet of diclofenac sodium were studied on 8 healthy male volunteers in an open,randomized crossover study.Drug level in serum was assayed by HPLC method.The changes in serum concentration were conformed to a l-compartment open model.The t_1/2 (Ke)averaged 2.15±0.17 and ll.60 ± l.95 h,and the areas under the drug concentration curves were 5.87 ± 0.67 and 5.55 ± 0.57μgh/ml for enteric-coated and sustained-release tablet of diclofenac sodium,respectively. The mean relative bioavailability of sustained-release tablet was 0.95 to that of enteric-coated tablet.展开更多
The relative bioavailability of famotidine sustained release (SR) tablets was studied in 16 healthy male volunteers. Famotidine plasma concentration was determined by HPLC method, and the plasma concentration time d...The relative bioavailability of famotidine sustained release (SR) tablets was studied in 16 healthy male volunteers. Famotidine plasma concentration was determined by HPLC method, and the plasma concentration time data were processed with the method provided by USP XXIII. For single dose administration the peak plasma concentration occurring at 8 13±0 34 h was 69 52±3 00 ng/ml and the relative bioavailability was 112 4±8 6%. For multiple dose administration the peak plasma concentration of SR tablet was 86 14±2 95 ng/ml and the degree of fluctuation (DF) was 140 6±13 5% at steady state. Two one sided tests were performed in bioequivalence assessment. The results showed that the sustained release tablets were basically bioequivalent to the immediate release (IR) tablets on sale.展开更多
Solid dispersion of fenofibrate （FNB）, a poorly water-soluble drug, was prepared by a fluid-bed coating technique with PEG 6000 as the carrier. The physical state was characterized by DSC and X-ray powder diffractom...Solid dispersion of fenofibrate （FNB）, a poorly water-soluble drug, was prepared by a fluid-bed coating technique with PEG 6000 as the carrier. The physical state was characterized by DSC and X-ray powder diffractometry, which indicated the existence of fenofibrate in crystalline form in the solid dispersion. In vitro dissolution was studied in water containing 1% sodium lauryl sulfate, FASSIF and FESSIF. Significant enhancement in dissolution was achieved at PEG/FNB ratio of 4/1 with near complete dissolution within 30 min. Moderate improvement in dissolution rate was observed at smaller PEG/FNB ratios. Oral bioavailability was studied in beagle dogs after oral administration of fenofibrate solid dispersion pellets by monitoring fenofibric acid in plasma. The oral bioavailability of PEG/FNB 3/1 and 4/1 solid dispersion pellets was improved by 3.4 and 4.4-fold as compared to Lipanthyl, a commercial micronized fenotibrate formulation. There was a strong dependence of oral bioavailability on the in vitro dissolution rate. Good correlation was observed between the in vivo absorption fraction and the in vitro dissolution rate in each of the dissolution media, water containing 1% sodium lauryl sulfate, FASSIF and FESSIF. It could be concluded that PEG/FNB solid dispersion pellets were able to improve the dissolution and oral bioavailability of fenofibrate.展开更多
Baicalein(BE) is one of the main active flavonoids representing the variety of pharmacological effects including anticancer, anti-inflammatory and cardiovascular protective activities, but it's very low solubility...Baicalein(BE) is one of the main active flavonoids representing the variety of pharmacological effects including anticancer, anti-inflammatory and cardiovascular protective activities, but it's very low solubility, dissolution rate and poor oral absorption limit the therapeutic applications. In this work, a nano-cocrystal strategy was successfully applied to improve the dissolution rate and bioavailability of BE. Baicalein-nicotinamide(BE-NCT) nanococrystals were prepared by high pressure homogenization and evaluated both in vitro and in vivo. Physical characterization results including scanning electron microscopy, dynamic light scattering, powder X-ray diffraction and differential scanning calorimetry demonstrated that BE-NCT nano-cocrystals were changed into amorphous state with mean particle size of 251.53 nm. In the dissolution test, the BE-NCT nano-cocrystals performed 2.17-fold and 2.54-fold enhancement than BE coarse powder in FaSSIF-V2 and FaSSGF. Upon oral administration, the integrated AUC0-t of BE-NCT nano-cocrystals(6.02-fold) was significantly higher than BE coarse powder(1-fold), BE-NCT cocrystals(2.87-fold) and BE nanocrystals(3.32-fold). Compared with BE coarse powder, BE-NCT cocrystals and BE nanocrystals, BENCT nano-cocrystals possessed excellent performance both in vitro and in vivo evaluations.Thus, it can be seen that nano-cocrystal is an appropriate novel strategy for improving dissolution rate and bioavailability of poor soluble natural products such as BE.展开更多
Although active constituents extracted from plants show robust in vitro pharmacological effects, low in vivo absorption greatly limits the widespread application of these compounds. A strategy of using phyto-phospholi...Although active constituents extracted from plants show robust in vitro pharmacological effects, low in vivo absorption greatly limits the widespread application of these compounds. A strategy of using phyto-phospholipid complexes represents a promising approach to increase the oral bioavailability of active constituents, which is consist of ‘‘label-friendly'phospholipids and active constituents. Hydrogen bond interactions between active constituents and phospholipids enable phospholipid complexes as an integral part. This review provides an update on four important issues related to phyto-phospholipid complexes: active constituents, phospholipids, solvents, and stoichiometric ratios. We also discuss recent progress in research on the preparation, characterization, structural verification, and increased bioavailability of phyto-phospholipid complexes.展开更多
基金supported by the Science and Technology Programs of Department of Natural Resources of Zhejiang Province,China(No.2020006)the Zhejiang Provincial Natural Science Foundation of China(No.LGF22D030001)the Key R&D Program of Zhejiang Province,China(No.2021C04020)。
文摘Cadmium(Cd)contamination in soil can lead to food chain accumulation and greatly impacts on human health.Bioremediation has gained more and more attention due to its environment-friendly,high efficiency and low-cost.In this work,we studied the impact of phosphate solubilizing bacterial agent(PSBA)on Cd bioavailability,microbial communities in soil and Cd accumulation in lettuce plants with pot experiment and field trial.Results of pot experiment showed that PSBA could decrease the bioavailability of Cd(Cd-acid extractable from 3.30 to 2.34mg/kg,Cd-reducible from 1.94 to 1.56 mg/kg),promote lettuce plants growth(increased by 33.85%height and by 33.65%fresh weight)and reduce the accumulation of Cd(from 5.85 to 3.73 mg/kg)in lettuce plants.High-throughput sequencing identified that PSBA could change the composition and structure of the soil microbial communities.The relative abundances of the three ecologically beneficial bacterial families of Pseudomonadaceae,Burkholderiaceae,and Enterobacteriaceae increased from 2.29%to 5.13%,0.56%to 5.24%,and 1.87%to 16.93%,respectively.And the former two were positively correlated with redox potential(Eh)(R^(2)=0.474,p<0.05,R^(2)=0.590,p<0.01,respectively).The bacterial networks were more complex in PSBA treatment,reflecting through more links(from 1893 to 2185)and a higher average degree(from 38.242 to 45.052)and density(from 0.390 to 0.469).Results of field trial demonstrated that PSBA could also decrease Cd content in lettuce plants and microbial composition in soil.This study indicated that PSBA could be served as an alternative material in bioremediation of Cd contamination in soil.
文摘Traditional Chinese medicine(TCM)offers diverse therapeutic compounds but faces challenges like poor bioavailability and instability.Recent innovations in drug delivery systems,including nanotechnology-based drug delivery systems have shown potential to enhance solubility,stability,and therapeutic efficacy.This review examines these advancements,focusing on their mechanisms and applications in improving TCM formulations.Cutting-edge techniques,such as microneedles,iontophoretic patches,and self-orienting applicators,are also discussed for their potential to revolutionize TCM delivery.By bridging traditional wisdom with modern innovations,this review emphasizes the transformative role of these strategies in advancing TCM's integration into contemporary medicine.
基金supported by the National Natural Science Foundation of China(No.22074058,S.Li).
文摘Algal copper uptake(i.e.,Cu bioavailability)in the euphotic zone plays a vital role in algal photosynthesis and respiration,affecting the primary productivity and the source and sink of atmospheric carbon.Algal Cu uptake is controlled by natural dissolved organic Cu(DOCu)speciation(i.e.,complexed with the dissolved organic matter)that conventionally could be tested by model prediction or molecular-level characterizations in the lab,while DOCu uptake are hardly directly assessed.Thus,the new chemistrybiology insight into the mechanisms of the Cu uptake process in algae is urgent.The DOCu speciation transformation(organic DOCu to free Cu(II)ions),enzymatic reduction-induced valence change(reduction of free Cu(II)to Cu(I)ions),and algal Cu uptake at the algae-water interface are imitated.Herein,an intelligent system with DOCu colorimetric sensor is developed for real-time monitoring of newly generated Cu(I)ions.Deep learning with whole sample image-based characterization and powerful feature extraction capabilities facilitates colorimetric measurement.In this context,the Cu bioavailability with 7 kinds of organic ligands(e.g.,amino acids,organic acids,carbohydrates)can be predicted by the mimetic intelligent biosensor within 15.0min,i.e.,the DOCu uptake and speciation is successfully predicted and streamlined by the biomimetic approach.
基金supported by the National Natural Science Foundation of China(31972087)the earmarked fund for China Agriculture Research System-Bee(CARS-44-KXJ17)the Science and Technology Innovation Project of Chinese Academy of Agricultural Sciences(CAAS-ASTIP-2021-IAR)。
文摘Propolis is a resinous complex mixture made from plant resins collected by worker bees and mixed with their own secretions.It is rich in polyphenols and flavonoids and thus has a wide range of biological activities and is considered a functional source for promoting human health.However,propolis and its bioactive compounds have poor water solubility,rapid and intense metabolism,and low oral bioavailability,which limits their wide application.In this paper,the main bioactive substances in propolis were summarized,and the biological characteristics and therapeutic potential of propolis and its bioactive substances were discussed.In addition,this paper discussed the factors affecting the bioavailability of propolis and its functional ingredients,focusing on the research progress in improving the bioavailability and bioactivity of propolis and its functional ingredients using nanoencapsulation technology.Finally,the current situation of the global propolis market and the applications of propolis products in the pharmaceutical,food,cosmetic and other industrial fields were discussed,providing useful references for promoting the development of the propolis industry.
基金Supported by Open Fund of Engineering Research Center of Ministry of Education for Wetland Ecology and Agricultural Utilization(KF202015).
文摘In this paper,the vegetable field in the teaching base of College of Agriculture,Yangtze University was taken as the research object.The indoor simulation method was used to explore the effects of temperature and moisture on the phosphorus(P)bioavailability of vegetable soil.Three temperature gradients[T1(15℃),T2(25℃),T3(35℃)]and three humidity gradients[W1(40%),W2(70%),W3(100%)]were set in the test.The results showed that it could improve the contents of HCl-P,Enzyme-P,Citrate-P,and Olsen-P in vegetable soil by increasing soil moisture content;temperature rise was helpful to increase the contents of HCl-P and Olsen-P,but it could reduce the content of Citrate-P.The contents of Enzyme-P and CaCl 2-P were significantly affected by hydrothermal interaction.Within a certain range of soil temperature and humidity,temperature and moisture had a positive coupling effect on soil P bioavailability components,and significantly affected soil P supply capacity.
基金supported by National key research and development program of China(2022YFF1102500)。
文摘Given the severe toxicity and widespread presence of cadmium(Cd)in staple foods such as rice,accurate dietary exposure assessments are imperative for public health.In vitro bioavailability is commonly used to adjust dietary exposure levels of risk factors;however,traditional planar Transwell models have limitations,such as cell dedifferentiation and lack of key intestinal components,necessitating a more physiologically relevant in vitro platform.This study introduces an innovative three-dimensional(3D)intestinal organoid model using a microfluidic chip to evaluate Cd bioavailability in food.Caco-2 cells were cultured on the chip to mimic small intestinal villi's 3D structure,mucus production,and absorption functions.The model's physiological relevance was thoroughly characterized,demonstrating the formation of a confluent epithelial monolayer with well-developed tight junctions(ZO-1),high microvilli density(F-actin),and significant mucus secretion(Alcian blue staining),closely resembling the physiological intestinal epithelium.Fluorescent particle tracking confirmed its ability to simulate intestinal transport and diffusion.The Cd bioavailability in rice measured by the 3D intestinal organoid model((9.07±0.21)%)was comparable to the mouse model((12.82±3.42)%)but significantly lower than the Caco-2 monolayer model((26.97±1.11)%).This 3D intestinal organoid model provides a novel and reliable strategy for in vitro assessment of heavy metal bioavailability in food,with important implications for food safety and risk assessment.
基金Science and Technology Department of Henan province Fund Project(Grant No.144300510019)
文摘Previous study has shown that 10-hydroxycamptothecin（HCPT） has well-established pharmacological effects in vitro.However,its in vivo bioavailability is very poor due to various problems,which severely restricts its clinical applications.In the present study,phospholipid complex（PC） technology was employed to improve the solubility and bioavailability of HCPT.XRD data confirmed the formation of HCPT-PC.However,our previously prepared HCPT-PC is too sticky,which may result in the slow dissolution rate and negative effects on its absorption.Therefore,we prepared HCPT-PC-solid dispersion（HCPT-PC-SD）and lipid-based formulations of HCPT-PC through simple preparation process.The results showed that the dissolution rate of HCPT-PC was effectively improved by solid dispersion technology,which reached 91.73%in 45 min.Pharmacokinetic study revealed that the AUC_（0-t） of HCPT-PC-SD and HCPT-PC lipid-based formulations was effectively further increased compared with HCPT-PC.Moreover,we found that the combination of SD technology and lipid-base formulations could be a promising drug-delivery system to improve the oral bioavailability of HCPT-PC.In addition,we showed that the bioavailability of HCPT-PC lipid-base formulations was even greater than that of HCPT-PC-SD.In particular,lipid-base formulations could be prepared just by a simple method,suggesting its feasibility of industrialization.
文摘A new HPLC MS method to determine loratadine in human plasma was established. The method involved extracting drug with organic solvent under basic conditions. The samples were seperated by ODS column and determined by mass detector. The calibration curve of loratadine was linear within the range of 0.4～100 ng·mL -1 with r=0.9995 . The recovery of this method was within 95%～104%, within day and between day RSD were less than 12%. To study the pharmacokinetics and relative bioavailability of loratadine tablets, two formulations of loratadine tablets were given to 18 healthy male volunteers according to a randomized 2 way cross over design. The C max , AUC 0 t and T max values of the two formulations were 51.89±20.18 ng·mL -1 and 52.48±22.35 ng·mL -1 ; 140.75±88.42 ng·h·mL -1 and 147.24±92.33 ng·h·mL -1 ; 0.81±0.35 h and 0.81±0.27 h respectively. Results from statistic analysis showed that there were no significant difference between the C max , AUC 0-t and T max values of the two formulations. The relative bioavailability of tablets I with respect to tablets II was 97%±13% from the AUC 0 t measurement. Bioequivalance was observed between the two tablets.
基金The National Science and Technology Major Projects"Major New Drugs Innovation and Development"(Grant No.2009ZX09103-007)
文摘Many active constituents from herbal plants have well-established pharmacological effects in vitro. But they demonstrate less or no activities in vivo due to various problems of themselves, which severely restricts their clinical applications. After forming phytosomes with phospholipids in aprotic solvent, the active constituents exhibit different physicochemical properties from the free form. In particular, the bioavailability of the active constituent-phytosomes is enhanced greatly due to the improved capacity to cross the biomembrane and reach circulation. Therefore, increasing attention has been attracted to the use of phytosomes in recent years. Based on the published reports, we reviewed the recent progress in the research of phytosomes including preparation, characterization, structure verification and clinical applications.
文摘The pharmacokinetics and absolute bioavailability of the sublingual naloxone tablet were studied with HPLC-electrochemical detection. Eight male dogs received single 5 mg dose of naloxone intravenously, the plasma concentration-time curves could be fitted to two-compartment open model, with 12.0 min of t1/2( , 143.4 min of t1/2( and 7.92 mg(min/L of AUC. The same eight dogs received 5 mg dose of the sublingual naloxone tablet after an interval of a week. The main pharmacokinetic parameters were: t1/2ka = 11.0 min, t1/2( = 15.4 min, t1/2( = 164.1 min, Tmax = 27.7 min, Cmax = 34.2 ng / ml, and AUC = 6.79 mg(min / L, respectively. The plasma concentration-time curves were fitted to the first order absorption two-compartment open model also. The mean absolute bioavailability of the sublingual naloxone tablet was 86.8 ( 10.9%. No statistically significant differences were found with t1/2(, t1/2(, ( and ( between the two routes of administration. These results indicated that the course of disposition for naloxone in dogs was similar for the two routes of administration, and the absolute bioavailability of the sublingual naloxone tablet was high. Thus satisfactory clinical effects could be expected.
文摘Aim To establish a sensitive and specific liquid chromatography-mass spectrometry (HPLC-MS) method for measuring lovastatin level in human plasma and the relative bioavailability. Methods Lovastatin in the plasma was extracted with acetoacetate. Simvastatin was added as internal standard (IS). Samples were separated on a C_ 18 column with a mobile phase consisting of methanol and 50 mmol·L~ -1 sodium acetate (88 ∶ 12). The flow rate was 1 mL·min~ -1 . Sample was detected using an electrospray ionization (ES...
文摘Aim To investigate whether modified-release cefaclor capsules could lead to a more suitable pharmacokinetic profile in the plasma. Methods Cefaclor pellets were prepared by extrusion/spheronization and coated by Eudragit L30D-55 or Eudragit NE30D, then the two sorts of pellets were filled to capsules in a 35：65 ratio to made a modified-release （MR） capsules. The bioavailability of the MR capsules was studied in 24 healthy volunteers after oral administration in a fast state using a commercially available immediate release （IR） capsule as a reference. Results The results showed that the MR formulation had a relatively good bioavailability compared with the commercial capsules, as well as a longer time keeping drug level above MIC than immediate release capsule. The relative bioavailability of the MR capsules was 97.4- 12.1%. Conclusion The data of the present study indicate that time of cefaclor plasma concentration above MIC can be substantially prolonged if cefaclor is administered as a modified- release product.
基金The National Natural Science fund of China(Grant No.31360379)the open fund of the Key Laboratory of the New Animal Drug Project of Gansu Provincethe Key Laboratory of Veterinary Pharmaceutical Development of the Ministry of Agriculture(Grant No.2014)
文摘Alantolactone, as the principal constituent oflnula Helenium L, has been shown various pharmacologic activities, such as anti-inflammatory and deworming. In the present study, we developed a high performance liquid chromatography （HPLC） method for the determination of alantolactone in rat plasma, and pharmacokinetics of alantolactone was investigated after intravenous and oral administrations to Wistar rats. Separation was achieved on C18 column （4.6 mm×250 mm, 5.0 μm） using a mobile phase consisting of methanol-water （70：30, v/v） at a flow rate of 1.0 mL/min. The wavelength of the ultraviolet detector was set at 239 nm. The excellent linearity was found over a concentration range of 0.08-10 μg/mL （R2 = 0.9998）. The intra- and inter-day precisions were good, and the RSD was lower than 2.27%. The mean absolute recovery of alantolactone in plasma ranged from 88.09% to 95.57%. After intravenous administration, alantolactone showed rapid systemic clearance （CL （0.11±0.014） L/h/kg） and small volume of distribution （Vd （0.71±0.14） L/kg）. The biological half life （t1/2） was 56.24 min. After oral administration, alantolactone showed rapid oral absorption in rats, with a short Tmax of （45.02±0.88） and （45.13±0.39） min for 14 and 28 mg/kg, respectively. The bioavailability of alantolactone in rats was 50.88%, indicating that alantolactone was orally available.
文摘A new pre-column derivation HPLC method with solid-phase extraction to determine captopril in human plasma was established. Derivation products were extracted by a solid-phase extraction method after the reagent, p-a-dibromoacetophenone(p-BPB), was added in the plasma samples. The samples were analyzed in a VP-ODS column with UV-detector. The calibration curve of captopril was linear within the range of 5~1000 ngmL-1 with r=0.9987, the recovery of this method was 98.652.04%, within day and between day RSD were no more than 3.4% and 8.4% respectively. To study the pharmacokinetics and the relative bioavailability of captopril tablets, two formulations of captopril tablets were given to 18 healthy male volunteers according to a randomized 2-way cross-over design with a 1-week washout period. The respective AUC0~6 , Cmax and Tmax values of the two formulations were 424.5125.7 and 439.4113.3 mghL-1; 505.9244.6 and 504.8172.2 mgL-1; 0.6620.181 and 0.5280.176 h. Results from statistics analysis showed that there were no significant difference between the AUC0~6 , Cmax and Tmax values of the two formulations, The relative bioavailability of tablets I with respect to II was 96.114.6% from AUC0~6 measurement. Bioequivalance was observed between the two tablets.
基金The 973 Project(Grant No.2009CB930300)Scientific and Technological Major Special Project -"Significant Creation of New Drugs"(Grant No.2009ZX09310-001).
文摘Sorafenib is a novel antitumor drug,which is poorly absorbed in the gastrointestinal tract due to its low solubility in water.To improve the bioavailability of sorafenib,a self-microemulsifying drug delivery system(SMEDDS) formulation of sorafenib was prepared and its relative bioavailability in rats was evaluated.The blank SMEDDS was prepared from a mixture of ethyl oleate(oil phase,20%,w/w),Cremophol EL(surfactant,48%,w/w),PEG-400(co-surfactant,16%,w/w) and ethanol (co-surfactant,16%,w/w).Sorafenib was subsequently dissolved in the blank SMEDDS to obtain a sorafenib SMEDDS formulation with a final sorafenib concentration at 20 mg/mL.The particle size of the emulsified sorafenib SMEDDS was about 20-25 nm. Compared with sorafenib suspension,the prepared SMEDDS formulation exhibited no effect on the T_(max),but significantly increased the AUC,C_(max) and MRT and decreased the drug clearance.Most importantly,the oral bioavailability based on AUC_(0-72h) increased about 25 times after formulating sorafenib in SMEDDS.We concluded that SMEDDS could be a promising vesicle for the oral delivery of the poorly soluble antitumor drug sorafenib.
文摘The pharmacokinetics of a sustained- release formulation and an enteric- coated tablet of diclofenac sodium were studied on 8 healthy male volunteers in an open,randomized crossover study.Drug level in serum was assayed by HPLC method.The changes in serum concentration were conformed to a l-compartment open model.The t_1/2 (Ke)averaged 2.15±0.17 and ll.60 ± l.95 h,and the areas under the drug concentration curves were 5.87 ± 0.67 and 5.55 ± 0.57μgh/ml for enteric-coated and sustained-release tablet of diclofenac sodium,respectively. The mean relative bioavailability of sustained-release tablet was 0.95 to that of enteric-coated tablet.
文摘The relative bioavailability of famotidine sustained release (SR) tablets was studied in 16 healthy male volunteers. Famotidine plasma concentration was determined by HPLC method, and the plasma concentration time data were processed with the method provided by USP XXIII. For single dose administration the peak plasma concentration occurring at 8 13±0 34 h was 69 52±3 00 ng/ml and the relative bioavailability was 112 4±8 6%. For multiple dose administration the peak plasma concentration of SR tablet was 86 14±2 95 ng/ml and the degree of fluctuation (DF) was 140 6±13 5% at steady state. Two one sided tests were performed in bioequivalence assessment. The results showed that the sustained release tablets were basically bioequivalent to the immediate release (IR) tablets on sale.
基金Shanghai Municipal Committee of Science and Technology (Grant No. 0852nm04400)
文摘Solid dispersion of fenofibrate （FNB）, a poorly water-soluble drug, was prepared by a fluid-bed coating technique with PEG 6000 as the carrier. The physical state was characterized by DSC and X-ray powder diffractometry, which indicated the existence of fenofibrate in crystalline form in the solid dispersion. In vitro dissolution was studied in water containing 1% sodium lauryl sulfate, FASSIF and FESSIF. Significant enhancement in dissolution was achieved at PEG/FNB ratio of 4/1 with near complete dissolution within 30 min. Moderate improvement in dissolution rate was observed at smaller PEG/FNB ratios. Oral bioavailability was studied in beagle dogs after oral administration of fenofibrate solid dispersion pellets by monitoring fenofibric acid in plasma. The oral bioavailability of PEG/FNB 3/1 and 4/1 solid dispersion pellets was improved by 3.4 and 4.4-fold as compared to Lipanthyl, a commercial micronized fenotibrate formulation. There was a strong dependence of oral bioavailability on the in vitro dissolution rate. Good correlation was observed between the in vivo absorption fraction and the in vitro dissolution rate in each of the dissolution media, water containing 1% sodium lauryl sulfate, FASSIF and FESSIF. It could be concluded that PEG/FNB solid dispersion pellets were able to improve the dissolution and oral bioavailability of fenofibrate.
文摘Baicalein(BE) is one of the main active flavonoids representing the variety of pharmacological effects including anticancer, anti-inflammatory and cardiovascular protective activities, but it's very low solubility, dissolution rate and poor oral absorption limit the therapeutic applications. In this work, a nano-cocrystal strategy was successfully applied to improve the dissolution rate and bioavailability of BE. Baicalein-nicotinamide(BE-NCT) nanococrystals were prepared by high pressure homogenization and evaluated both in vitro and in vivo. Physical characterization results including scanning electron microscopy, dynamic light scattering, powder X-ray diffraction and differential scanning calorimetry demonstrated that BE-NCT nano-cocrystals were changed into amorphous state with mean particle size of 251.53 nm. In the dissolution test, the BE-NCT nano-cocrystals performed 2.17-fold and 2.54-fold enhancement than BE coarse powder in FaSSIF-V2 and FaSSGF. Upon oral administration, the integrated AUC0-t of BE-NCT nano-cocrystals(6.02-fold) was significantly higher than BE coarse powder(1-fold), BE-NCT cocrystals(2.87-fold) and BE nanocrystals(3.32-fold). Compared with BE coarse powder, BE-NCT cocrystals and BE nanocrystals, BENCT nano-cocrystals possessed excellent performance both in vitro and in vivo evaluations.Thus, it can be seen that nano-cocrystal is an appropriate novel strategy for improving dissolution rate and bioavailability of poor soluble natural products such as BE.
文摘Although active constituents extracted from plants show robust in vitro pharmacological effects, low in vivo absorption greatly limits the widespread application of these compounds. A strategy of using phyto-phospholipid complexes represents a promising approach to increase the oral bioavailability of active constituents, which is consist of ‘‘label-friendly'phospholipids and active constituents. Hydrogen bond interactions between active constituents and phospholipids enable phospholipid complexes as an integral part. This review provides an update on four important issues related to phyto-phospholipid complexes: active constituents, phospholipids, solvents, and stoichiometric ratios. We also discuss recent progress in research on the preparation, characterization, structural verification, and increased bioavailability of phyto-phospholipid complexes.
