This paper reviewed the unique biological function of trehalose and its mechanism of stabilizing biological macromolecules and the research progress in the protective effect of trehalose on lactic acid bacteria fermen...This paper reviewed the unique biological function of trehalose and its mechanism of stabilizing biological macromolecules and the research progress in the protective effect of trehalose on lactic acid bacteria fermentation starters during lyophilization in food production.The application of trehalose in food industry was prospected.展开更多
Nifedipine-solid-lipid nanoparticles lyophilized with trehalose (NI-SLN-Tre) were prepared by the high pressure homogenization of a roll mixture consisting of NI and hydrogenated soybean phosphatidylcholine and dipalm...Nifedipine-solid-lipid nanoparticles lyophilized with trehalose (NI-SLN-Tre) were prepared by the high pressure homogenization of a roll mixture consisting of NI and hydrogenated soybean phosphatidylcholine and dipalmitoylphosphatidylglycerol, and in vivo pharmacokinetic properties and their hemocompatibility were determined and compared with those of a NI-SLN suspension. The resulting pharmacokinetic data demonstrated that although no significant differences were observed between the time of peak concentration (Tmax), peak plasma concentration (Cmax), and the area under the curve (AUC0→∞) values of both administrated samples, NI tended to be absorbed to a much greater extent from the lyophilized NI-SLN-Tre suspensions because of the enhanced solvation of NI-SLN in gastrointestinal fluid, derived from formation of hydrogen bonds between the polar head groups of the lipids and the O-H groups of trehalose. Furthermore, the results of a hemolysis assay revealed that the NI-SLN and NI-SLN-Tre suspensions showed good hemocompatibility properties with hemolysis values of less than 5%. Taken together, the results of this study demonstrate that NI-SLN-Tre exhibits suitable pharmacokinetic properties and good biocompatibility.展开更多
Pre-freezing is an important stage in freeze-drying processes.For the lyophilization of a cell,freezing not only plays a role for primary dehydration,but it also determines the amount of residual(intracellular or extr...Pre-freezing is an important stage in freeze-drying processes.For the lyophilization of a cell,freezing not only plays a role for primary dehydration,but it also determines the amount of residual(intracellular or extracellular)water,which in turn can influence the solution properties and the choice of operation parameters.The freezing of human platelets in lyoprotectant solution is theoretically investigated here.A two-parameter model and an Arrhenius expression are used to describe cell membrane permeability and its temperature dependency.It is assumed that the intracellular solution is composed of four components:sodium chloride,trehalose,serum protein and water,while the extracellular solution consists of three components.Non-ideal solution behaviors are predicted using measured data.The concentration of maximally freeze-concentrated solution is estimated on the basis of an assumption of solute hydration.The impacts of lyoprotectant composition and extracellular sub-cooling on intracellular supercooling and residual water content in the cell are analyzed.The values of activation energy of hydraulic permeability at low temperatures are tested to study their impact on the critical cooling rate.As the mass fraction extracellular lyoprotectant(trehalose+bovineserum albumin)increases from 5 wt%to 20 wt%,the intracellular water content at the end of freezing does not change,but the intracellular solution undergoes much higher super-cooling degree.Increasing the mass ratio of trehalose to bovine serum albumin does not change the intracellular water content,but can mitigate intracellular super-cooling.While 0.05 mol/kg trehalose is loaded into platelet,the total quantity of residual water at the end of freezing may raise by 4.93%.The inclusion of dimethyl sulfoxide(Me2SO)in protectant may bring negative impacts to the drying stage by increasing the residual water content and lowering the drying temperature.展开更多
Objectives: To improve the aqueous solubility and dissolution of fexofenadine HCl, an attempt was made to prepare its fast dissolving tablets by lyophilization technique. Methods: For the preparation of lyophilized ta...Objectives: To improve the aqueous solubility and dissolution of fexofenadine HCl, an attempt was made to prepare its fast dissolving tablets by lyophilization technique. Methods: For the preparation of lyophilized tablets (F1-F32), the drug was dispersed in a hydrated solution of water-soluble polymers (gelatin/maltodextrin/acacia) containing glycine and mannitol. The blend was pelted down into the patches of a blister pack, frozen down and then lyophilized. Different characterization parameters viz. differential scanning calorimetry, hardness, weight variation, X-ray diffraction (XRD), scanning electron microscopy (SEM), mercury porosimetry, solubility, wetting time and water absorption ratio, lyophilization tablet index, drug content, in vitro dissolution and stability were evaluated. Key findings: Tablets (F32) containing acacia were found to have fast disintegration and relatively higher mechanical strength with improved drug solubility. X-ray diffractogram and scanning electron micrograph indicated decrease in crystallinity of drug and a good porous structure property for prepared tablet, respectively. Dissolution study showed complete drug released within 5 min. Moreover, tablets (F32) were found to be stable for one month at 25 ± 2 °C/60 ± 5% relative humidity.展开更多
The aim of present study was to use QbD approaches to evaluate the effect of independent product variables and their interaction on particle size of sodium fluoride and then obtain the optimized experimental condition...The aim of present study was to use QbD approaches to evaluate the effect of independent product variables and their interaction on particle size of sodium fluoride and then obtain the optimized experimental condition for predefined particle size of sodium fluoride. The sodium fluoride is mainly used in dental preparation for delivering the fluoride ion to the tooth enamel for that nano-particle size is required. Nowadays the milling process is used to reduce the particle size. But that process has some limitations due to crystalline nature of sodium fluoride;for overcoming those limitations, lyophilization method is used. A 4<sup>3</sup> level full factorial design was used to study the significant influence of process and product variables i.e. 1) Concentration of sodium fluoride, 2) Concentration of PVP, 3) Sample volume, 4) Drying surface, on particle size of sodium fluoride. The experimental design result shows that independent product variables significantly modify the structure and improve particle size reduction of sodium fluoride.展开更多
[Objectives]To enhance the skin permeability of hydroxypropyl tetrahydropyrantriol and provide a reference for the subsequent prevention or treatment of skin aging.[Methods]The lyophilization process of hydroxypropyl ...[Objectives]To enhance the skin permeability of hydroxypropyl tetrahydropyrantriol and provide a reference for the subsequent prevention or treatment of skin aging.[Methods]The lyophilization process of hydroxypropyl tetrahydropyrantriol liposomes was investigated using a single factor method,and a quality evaluation system was established based on the appearance,particle size,PDI,and re-dispersibility of the lyophilized samples.[Results]The lyophilization process of hydroxypropyl tetrahydropyrantriol liposomes was determined by single factor experiments.The pre-freezing period was 16 h at-80℃,the total drying time was 36 h,and the addition of 10%mannitol-sucrose was used as the lyoprotectant.[Conclusions]The product prepared by the lyophilization method exhibits a fluffy and full appearance,with minimal shrinkage and collapse.The volume remains consistent before and after lyophilization,and the re-dispersibility is satisfactory.The re-dissolution process is rapid,and the particle size and polydispersity index(PDI)remain largely unchanged before and after lyophilization.展开更多
基金Supported by School-based Scientific Research Project of Hebi Polytechnic in 2022 (2022-KJZD-001).
文摘This paper reviewed the unique biological function of trehalose and its mechanism of stabilizing biological macromolecules and the research progress in the protective effect of trehalose on lactic acid bacteria fermentation starters during lyophilization in food production.The application of trehalose in food industry was prospected.
文摘Nifedipine-solid-lipid nanoparticles lyophilized with trehalose (NI-SLN-Tre) were prepared by the high pressure homogenization of a roll mixture consisting of NI and hydrogenated soybean phosphatidylcholine and dipalmitoylphosphatidylglycerol, and in vivo pharmacokinetic properties and their hemocompatibility were determined and compared with those of a NI-SLN suspension. The resulting pharmacokinetic data demonstrated that although no significant differences were observed between the time of peak concentration (Tmax), peak plasma concentration (Cmax), and the area under the curve (AUC0→∞) values of both administrated samples, NI tended to be absorbed to a much greater extent from the lyophilized NI-SLN-Tre suspensions because of the enhanced solvation of NI-SLN in gastrointestinal fluid, derived from formation of hydrogen bonds between the polar head groups of the lipids and the O-H groups of trehalose. Furthermore, the results of a hemolysis assay revealed that the NI-SLN and NI-SLN-Tre suspensions showed good hemocompatibility properties with hemolysis values of less than 5%. Taken together, the results of this study demonstrate that NI-SLN-Tre exhibits suitable pharmacokinetic properties and good biocompatibility.
基金supported by the National Natural Science Foundation of China[grant number 51876185]archaeological artifact protection technology project of Zhejiang Province grant number 2017008].
文摘Pre-freezing is an important stage in freeze-drying processes.For the lyophilization of a cell,freezing not only plays a role for primary dehydration,but it also determines the amount of residual(intracellular or extracellular)water,which in turn can influence the solution properties and the choice of operation parameters.The freezing of human platelets in lyoprotectant solution is theoretically investigated here.A two-parameter model and an Arrhenius expression are used to describe cell membrane permeability and its temperature dependency.It is assumed that the intracellular solution is composed of four components:sodium chloride,trehalose,serum protein and water,while the extracellular solution consists of three components.Non-ideal solution behaviors are predicted using measured data.The concentration of maximally freeze-concentrated solution is estimated on the basis of an assumption of solute hydration.The impacts of lyoprotectant composition and extracellular sub-cooling on intracellular supercooling and residual water content in the cell are analyzed.The values of activation energy of hydraulic permeability at low temperatures are tested to study their impact on the critical cooling rate.As the mass fraction extracellular lyoprotectant(trehalose+bovineserum albumin)increases from 5 wt%to 20 wt%,the intracellular water content at the end of freezing does not change,but the intracellular solution undergoes much higher super-cooling degree.Increasing the mass ratio of trehalose to bovine serum albumin does not change the intracellular water content,but can mitigate intracellular super-cooling.While 0.05 mol/kg trehalose is loaded into platelet,the total quantity of residual water at the end of freezing may raise by 4.93%.The inclusion of dimethyl sulfoxide(Me2SO)in protectant may bring negative impacts to the drying stage by increasing the residual water content and lowering the drying temperature.
文摘Objectives: To improve the aqueous solubility and dissolution of fexofenadine HCl, an attempt was made to prepare its fast dissolving tablets by lyophilization technique. Methods: For the preparation of lyophilized tablets (F1-F32), the drug was dispersed in a hydrated solution of water-soluble polymers (gelatin/maltodextrin/acacia) containing glycine and mannitol. The blend was pelted down into the patches of a blister pack, frozen down and then lyophilized. Different characterization parameters viz. differential scanning calorimetry, hardness, weight variation, X-ray diffraction (XRD), scanning electron microscopy (SEM), mercury porosimetry, solubility, wetting time and water absorption ratio, lyophilization tablet index, drug content, in vitro dissolution and stability were evaluated. Key findings: Tablets (F32) containing acacia were found to have fast disintegration and relatively higher mechanical strength with improved drug solubility. X-ray diffractogram and scanning electron micrograph indicated decrease in crystallinity of drug and a good porous structure property for prepared tablet, respectively. Dissolution study showed complete drug released within 5 min. Moreover, tablets (F32) were found to be stable for one month at 25 ± 2 °C/60 ± 5% relative humidity.
文摘The aim of present study was to use QbD approaches to evaluate the effect of independent product variables and their interaction on particle size of sodium fluoride and then obtain the optimized experimental condition for predefined particle size of sodium fluoride. The sodium fluoride is mainly used in dental preparation for delivering the fluoride ion to the tooth enamel for that nano-particle size is required. Nowadays the milling process is used to reduce the particle size. But that process has some limitations due to crystalline nature of sodium fluoride;for overcoming those limitations, lyophilization method is used. A 4<sup>3</sup> level full factorial design was used to study the significant influence of process and product variables i.e. 1) Concentration of sodium fluoride, 2) Concentration of PVP, 3) Sample volume, 4) Drying surface, on particle size of sodium fluoride. The experimental design result shows that independent product variables significantly modify the structure and improve particle size reduction of sodium fluoride.
基金Youth Science Foundation Project of Sichuan Provincial Department of Science and Technology(2022NSFSC1437)Special Project of Scientific and Technological Research of Sichuan Provincial Administration of Traditional Chinese Medicine(2021MS121)Fundamental Research Funds for the Central Universities of Southwest Minzu University(ZYN2022040).
文摘[Objectives]To enhance the skin permeability of hydroxypropyl tetrahydropyrantriol and provide a reference for the subsequent prevention or treatment of skin aging.[Methods]The lyophilization process of hydroxypropyl tetrahydropyrantriol liposomes was investigated using a single factor method,and a quality evaluation system was established based on the appearance,particle size,PDI,and re-dispersibility of the lyophilized samples.[Results]The lyophilization process of hydroxypropyl tetrahydropyrantriol liposomes was determined by single factor experiments.The pre-freezing period was 16 h at-80℃,the total drying time was 36 h,and the addition of 10%mannitol-sucrose was used as the lyoprotectant.[Conclusions]The product prepared by the lyophilization method exhibits a fluffy and full appearance,with minimal shrinkage and collapse.The volume remains consistent before and after lyophilization,and the re-dispersibility is satisfactory.The re-dissolution process is rapid,and the particle size and polydispersity index(PDI)remain largely unchanged before and after lyophilization.
