In the present study,we aimed to prepare sustained-release microspheres for injection of neurokinin-1(NK-1)receptor antagonist APT011,and to evaluate their physicochemical properties,in vitro sustained-release effect ...In the present study,we aimed to prepare sustained-release microspheres for injection of neurokinin-1(NK-1)receptor antagonist APT011,and to evaluate their physicochemical properties,in vitro sustained-release effect and preliminary stability.APT011-loaded sustained-release microspheres were prepared using W/O/W double emulsion-solvent evaporation technique.The L9(34)orthogonal experiment was used to optimize the APT011 sustained-release microsphere formulation.Microscope photographs showed that APT011-loaded microspheres were spherical,and the particle size was^90μm with uniform size distribution.XRD results indicated that APT011 existed in the microspheres in an amorphous form.DSC results showed that there was no significant interaction between APT011 and blank microspheres.APT011-loaded microspheres had a significant sustained-release effect,which maintained release for at least 2 months.Preliminary study results indicated that the loading content and release percentage at 0.5 h were not markedly altered below 40°C and under high lighting condition.APT011-loaded microspheres prepared in our study exhibited excellent physicochemical properties and sustained-release characteristics and preliminary stability,demonstrating real potential for the clinical practice.展开更多
A highly porous Ta-10%Nb alloy was successfully prepared for tissue engineering via the methods of the sponge impregnation and sintering techniques.The porous Ta-10%Nb alloy offers the capability of processing a pore ...A highly porous Ta-10%Nb alloy was successfully prepared for tissue engineering via the methods of the sponge impregnation and sintering techniques.The porous Ta-10%Nb alloy offers the capability of processing a pore size of 300-600μm,a porosity of(68.0±0.41)%,and open porosity of(93.5±2.6)%.The alloy also shows desirable mechanical properties similar to those of cancellous bone with the elastic modulus and the comprehensive strength of(2.54±0.5)GPa and(83.43±2.5)MPa,respectively.The morphology of the pores in the porous Ta-Nb alloy shows a good interconnected three-dimension(3D)network open cell structure.It is also found that the rat MC3T3-E1 cell can well adhere,grow and proliferate on the porous Ta-Nb alloy.The interaction of the porous alloy on cells is attributed to its desirable pore structure,porosity and the great surface area.The advanced mechanical and biocompatible properties of the porous alloy indicate that this material has promising potential applications in tissue engineering.展开更多
Laboratory cultures of freshwater cyanobacterium (blue-green alga) Microcystis aeruginosa PCC 7806 was cvaluated for its hepatotoxic effects in rats. The lyophilized cell extract injected intraperitoneally at 1 and 2 ...Laboratory cultures of freshwater cyanobacterium (blue-green alga) Microcystis aeruginosa PCC 7806 was cvaluated for its hepatotoxic effects in rats. The lyophilized cell extract injected intraperitoneally at 1 and 2 LD50 (15.8 and 31.6 mg/kg, respectively) produced significant increase in liver-specific enzymes viz. plasma alkaline phosphatase,γ-glutamyl transferase, lactate dehydrogenase with a concomitant decrease in hepatic glutamic pyruvic transaminase. A corresponding increase in liver body weight index and histopathological changes in liver (degeneration of hepatocytes, congestion and hemorrhage etc.) are indicative of a dose and time dependent hepatotoxic nature of the algal extract展开更多
The aim of the present study was to develop tamsulosin hydrochloride sustained-release pellets using two-layered membrane techniques.Centrifugal granulator and fluidizedbed coater were employed to prepare drug-loaded ...The aim of the present study was to develop tamsulosin hydrochloride sustained-release pellets using two-layered membrane techniques.Centrifugal granulator and fluidizedbed coater were employed to prepare drug-loaded pellets and to employ two-layered membrane coating respectively.The prepared pellets were evaluated for physicochemical characterization,subjected to differential scanning calorimetry(DSC)and in vitro release of different pH.Different release models and scanning electron microscopy(SEM)were utilized to analyze the release mechanism of Harnual■ and home-made pellets.By comparing the dissolution profiles,the ratio and coating weight gain of Eudragit■ NE30D and Eudragit■ L30D55 which constitute the inside membrane were identified as 18:1 and 10%-11%.The coating amount of outside membrane containing Eudragit■ L30D55 was determined to be 0.8%.The similarity factors(f_(2))of home-made capsule and commercially available product(Harnual■)were above 50 in different dissolution media.DSC studies confirmed that drug and excipients had good compatibility and SEM photographs showed the similarities and differences of coating surface between Harnual■ and self-made pellets before and after dissolution.According to Ritger-Peppas model,the two dosage form had different release mechanism.展开更多
A recombinant skin model is a model in which skin cells are grown in vitro on a bioactive scaffold and provided with adequate nutrition to promote cell proliferation and differentiation to produce a mock skin structur...A recombinant skin model is a model in which skin cells are grown in vitro on a bioactive scaffold and provided with adequate nutrition to promote cell proliferation and differentiation to produce a mock skin structure and biological features. The development of recombinant skin models allows for effective and scientifically sound in vitro evaluation tests. This review briefly summarizes the overview of recombinant skin models and the progress of their application in in vitro evaluation which focuses on three aspects: skin irritation, skin corrosivity, and anti-skin aging. Moreover, an outlook on the future development of recombinant skin models is also provided in this review.展开更多
Chronic respiratory diseases, cardiovascular and cerebrovascular diseases, diabetes, and tumors are called the "four chronic diseases" in the world, and they are one of the main causes of mortality and morbi...Chronic respiratory diseases, cardiovascular and cerebrovascular diseases, diabetes, and tumors are called the "four chronic diseases" in the world, and they are one of the main causes of mortality and morbidity in the world. Among them, chronic obstructive pulmonary disease (COPD) and asthma are the most common among all chronic respiratory diseases. COPD is a group of lung diseases characterized by airflow restriction, which is not completely reversible and develops progressively, mainly involving the lungs. The main causes and pathogenesis include environmental reasons and organism reasons. Bad living habits such as smoking, poor air quality and long-term exposure to dust may all induce COPD. In addition, there are also organic reasons, such as the weak defense function of the body, which cant defend against external sensitization factors. With the increase of age, the disease is often aggravated. Bronchial asthma is a chronic inflammatory disease of airway involving many cells (such as eosinophils, mast cells, T lymphocytes, neutrophils, airway epithelial cells, etc.) and cell components. Its main causes are genetic factors and environmental factors. If both parents have increased airway responsiveness, the probability of relatives suffering from asthma is higher, followed by dust mites, fungi, dander, infection, food, medicine, climate change, exercise and air pollution. Due to the aggravation of global air pollution and the aging of population, the number of patients with COPD and asthma is increasing year by year.展开更多
Biodegradable metals have been increasingly utilized clinically due to their biosafety and pro-osteogenic prop-erties.However,conventional monolayer cell-based preclinical safety evaluation methods based on ISO10993-5...Biodegradable metals have been increasingly utilized clinically due to their biosafety and pro-osteogenic prop-erties.However,conventional monolayer cell-based preclinical safety evaluation methods based on ISO10993-5 consistently indicate significant cytotoxicity that contradicts in vivo outcomes.In this study,we aimed to establish an in vitro evaluation model that better correlates with in vivo performance.Three-layer BMSC cell sheets were constructed using layer-by-layer assembly.Histological analyses revealed a stable three-dimensional structure with elevated cell-cell interaction proteins,including N-Cadherin,Fibronectin,and Vinculin,along with enhanced osteogenic potential.The cytotoxicity of 4N pure Mg was evaluated in both cell sheet and monolayer co-culture models.Flow cytometry showed higher Ki67 expression and lower ROS levels and apoptosis rate in cell sheets.ShRNA-mediated silencing of N-Cadherin in cell sheets significantly compromised their cytopro-tective capacity against Mg metal-induced toxicity.Osteogenesis-related gene expression correlation analysis between in vitro co-culture models and in vivo femur implantation models was conducted using RNA-seq and qRT-PCR.Results showed that 4N pure Mg enhanced osteogenic genes(BMP2R,RUNX2,and SP7)in cell sheets,consistent with in vivo patterns but contrary to monolayer models.Various Mg-based metals(4N/5N Pure Mg,ZE21B,and WE43)were evaluated in cell sheet defect,monolayer defect,and cranial defect models.5N Pure Mg,ZE21B,and WE43 promoted defect healing in both cranial defect and cell sheets,but showed no positive effect in monolayers.Collectively,cell sheet models correlated well with in vivo results,suggesting their potential as alternative in vitro evaluation models,thereby accelerating clinical translation of Mg-based biomaterials.展开更多
About 80%of population in developing countries use traditional remedies in their usual health care and plants used in traditional medicine are an interesting alternative to expensive and hardly available modern medici...About 80%of population in developing countries use traditional remedies in their usual health care and plants used in traditional medicine are an interesting alternative to expensive and hardly available modern medicines,mainly in rural areas.Moreover,they are a promising source of new drugs structurally innovative.Therefore it is important to investigate their biological properties and we focused on5 beninese plants:Byrsocarpus coccineus Schumach.&Thonn(Connaraceae),Carpolobia lutea G.Don(Polygalaceae),展开更多
Oral mucositis due to chemotherapy and irradiation continues to be an important clinical problem. The effectiveness of hyaluronic acid-based compounds in accelerated healing and helping manage pain in patients with or...Oral mucositis due to chemotherapy and irradiation continues to be an important clinical problem. The effectiveness of hyaluronic acid-based compounds in accelerated healing and helping manage pain in patients with oral mucositis was demonstrated. It was investigated a protective and regenerative effect of hyaluronic acid based gel formulation enriched with NAG （N-acetyl glucosamine） loaded solid lipid nanoparticles against degenerative process of the oral mucosa. Gel formulations were obtained by adding sHA （sodium hyaluronate） into SLN aqueous suspension. Gel performances were evaluated by multi-methodological approach： mucoadhesive and barrier properties evaluation, cell viability. It was shown that gel formulation based sHA, enriched with NAG loaded SLNs, when added as suspension, demonstrated to have a good mucoadhesion profile comparable in terms of tensile work and fracture strength to Carbomer 934 2%. The presence of NAG encapsulated and not in gel formulation enhances also the biocompatibility of the system, demonstrating also to have a proliferative effect. Finally, any barrier property was altered. Finally, results demonstrated that sHA based gel formulation enriched SLNs, demonstrated good mucoadeshion property, comparable to carbopol gel, positive control. The proposed gel formulation enriched with SLNs setting up in this work could be used as innovation strategy to treat oral mucositis.展开更多
基金National Science&Technology Major Project“Key New Drug Creation and Manufacturing”(Grant No.2019ZX09201001-003-007)。
文摘In the present study,we aimed to prepare sustained-release microspheres for injection of neurokinin-1(NK-1)receptor antagonist APT011,and to evaluate their physicochemical properties,in vitro sustained-release effect and preliminary stability.APT011-loaded sustained-release microspheres were prepared using W/O/W double emulsion-solvent evaporation technique.The L9(34)orthogonal experiment was used to optimize the APT011 sustained-release microsphere formulation.Microscope photographs showed that APT011-loaded microspheres were spherical,and the particle size was^90μm with uniform size distribution.XRD results indicated that APT011 existed in the microspheres in an amorphous form.DSC results showed that there was no significant interaction between APT011 and blank microspheres.APT011-loaded microspheres had a significant sustained-release effect,which maintained release for at least 2 months.Preliminary study results indicated that the loading content and release percentage at 0.5 h were not markedly altered below 40°C and under high lighting condition.APT011-loaded microspheres prepared in our study exhibited excellent physicochemical properties and sustained-release characteristics and preliminary stability,demonstrating real potential for the clinical practice.
基金Projects(51404302,51274247) supported by the National Natural Science Foundation of ChinaProject supported by "125 Talent Project" of the Third Xiangya Hospital of Central South University,China
文摘A highly porous Ta-10%Nb alloy was successfully prepared for tissue engineering via the methods of the sponge impregnation and sintering techniques.The porous Ta-10%Nb alloy offers the capability of processing a pore size of 300-600μm,a porosity of(68.0±0.41)%,and open porosity of(93.5±2.6)%.The alloy also shows desirable mechanical properties similar to those of cancellous bone with the elastic modulus and the comprehensive strength of(2.54±0.5)GPa and(83.43±2.5)MPa,respectively.The morphology of the pores in the porous Ta-Nb alloy shows a good interconnected three-dimension(3D)network open cell structure.It is also found that the rat MC3T3-E1 cell can well adhere,grow and proliferate on the porous Ta-Nb alloy.The interaction of the porous alloy on cells is attributed to its desirable pore structure,porosity and the great surface area.The advanced mechanical and biocompatible properties of the porous alloy indicate that this material has promising potential applications in tissue engineering.
文摘Laboratory cultures of freshwater cyanobacterium (blue-green alga) Microcystis aeruginosa PCC 7806 was cvaluated for its hepatotoxic effects in rats. The lyophilized cell extract injected intraperitoneally at 1 and 2 LD50 (15.8 and 31.6 mg/kg, respectively) produced significant increase in liver-specific enzymes viz. plasma alkaline phosphatase,γ-glutamyl transferase, lactate dehydrogenase with a concomitant decrease in hepatic glutamic pyruvic transaminase. A corresponding increase in liver body weight index and histopathological changes in liver (degeneration of hepatocytes, congestion and hemorrhage etc.) are indicative of a dose and time dependent hepatotoxic nature of the algal extract
文摘The aim of the present study was to develop tamsulosin hydrochloride sustained-release pellets using two-layered membrane techniques.Centrifugal granulator and fluidizedbed coater were employed to prepare drug-loaded pellets and to employ two-layered membrane coating respectively.The prepared pellets were evaluated for physicochemical characterization,subjected to differential scanning calorimetry(DSC)and in vitro release of different pH.Different release models and scanning electron microscopy(SEM)were utilized to analyze the release mechanism of Harnual■ and home-made pellets.By comparing the dissolution profiles,the ratio and coating weight gain of Eudragit■ NE30D and Eudragit■ L30D55 which constitute the inside membrane were identified as 18:1 and 10%-11%.The coating amount of outside membrane containing Eudragit■ L30D55 was determined to be 0.8%.The similarity factors(f_(2))of home-made capsule and commercially available product(Harnual■)were above 50 in different dissolution media.DSC studies confirmed that drug and excipients had good compatibility and SEM photographs showed the similarities and differences of coating surface between Harnual■ and self-made pellets before and after dissolution.According to Ritger-Peppas model,the two dosage form had different release mechanism.
文摘A recombinant skin model is a model in which skin cells are grown in vitro on a bioactive scaffold and provided with adequate nutrition to promote cell proliferation and differentiation to produce a mock skin structure and biological features. The development of recombinant skin models allows for effective and scientifically sound in vitro evaluation tests. This review briefly summarizes the overview of recombinant skin models and the progress of their application in in vitro evaluation which focuses on three aspects: skin irritation, skin corrosivity, and anti-skin aging. Moreover, an outlook on the future development of recombinant skin models is also provided in this review.
文摘Chronic respiratory diseases, cardiovascular and cerebrovascular diseases, diabetes, and tumors are called the "four chronic diseases" in the world, and they are one of the main causes of mortality and morbidity in the world. Among them, chronic obstructive pulmonary disease (COPD) and asthma are the most common among all chronic respiratory diseases. COPD is a group of lung diseases characterized by airflow restriction, which is not completely reversible and develops progressively, mainly involving the lungs. The main causes and pathogenesis include environmental reasons and organism reasons. Bad living habits such as smoking, poor air quality and long-term exposure to dust may all induce COPD. In addition, there are also organic reasons, such as the weak defense function of the body, which cant defend against external sensitization factors. With the increase of age, the disease is often aggravated. Bronchial asthma is a chronic inflammatory disease of airway involving many cells (such as eosinophils, mast cells, T lymphocytes, neutrophils, airway epithelial cells, etc.) and cell components. Its main causes are genetic factors and environmental factors. If both parents have increased airway responsiveness, the probability of relatives suffering from asthma is higher, followed by dust mites, fungi, dander, infection, food, medicine, climate change, exercise and air pollution. Due to the aggravation of global air pollution and the aging of population, the number of patients with COPD and asthma is increasing year by year.
基金financially funded by National Key Research and Development Program of China(2021YFC2400703)the National Nat-ural Science Foundation of China(NSFC)(52171234)+1 种基金Beijing Municipal Science and Technology Project(Z211100002921066)Peking Univer-sity National Clinical Key Specialty Translation Support Project(PKUSSNKP-Т202104).
文摘Biodegradable metals have been increasingly utilized clinically due to their biosafety and pro-osteogenic prop-erties.However,conventional monolayer cell-based preclinical safety evaluation methods based on ISO10993-5 consistently indicate significant cytotoxicity that contradicts in vivo outcomes.In this study,we aimed to establish an in vitro evaluation model that better correlates with in vivo performance.Three-layer BMSC cell sheets were constructed using layer-by-layer assembly.Histological analyses revealed a stable three-dimensional structure with elevated cell-cell interaction proteins,including N-Cadherin,Fibronectin,and Vinculin,along with enhanced osteogenic potential.The cytotoxicity of 4N pure Mg was evaluated in both cell sheet and monolayer co-culture models.Flow cytometry showed higher Ki67 expression and lower ROS levels and apoptosis rate in cell sheets.ShRNA-mediated silencing of N-Cadherin in cell sheets significantly compromised their cytopro-tective capacity against Mg metal-induced toxicity.Osteogenesis-related gene expression correlation analysis between in vitro co-culture models and in vivo femur implantation models was conducted using RNA-seq and qRT-PCR.Results showed that 4N pure Mg enhanced osteogenic genes(BMP2R,RUNX2,and SP7)in cell sheets,consistent with in vivo patterns but contrary to monolayer models.Various Mg-based metals(4N/5N Pure Mg,ZE21B,and WE43)were evaluated in cell sheet defect,monolayer defect,and cranial defect models.5N Pure Mg,ZE21B,and WE43 promoted defect healing in both cranial defect and cell sheets,but showed no positive effect in monolayers.Collectively,cell sheet models correlated well with in vivo results,suggesting their potential as alternative in vitro evaluation models,thereby accelerating clinical translation of Mg-based biomaterials.
文摘About 80%of population in developing countries use traditional remedies in their usual health care and plants used in traditional medicine are an interesting alternative to expensive and hardly available modern medicines,mainly in rural areas.Moreover,they are a promising source of new drugs structurally innovative.Therefore it is important to investigate their biological properties and we focused on5 beninese plants:Byrsocarpus coccineus Schumach.&Thonn(Connaraceae),Carpolobia lutea G.Don(Polygalaceae),
文摘Oral mucositis due to chemotherapy and irradiation continues to be an important clinical problem. The effectiveness of hyaluronic acid-based compounds in accelerated healing and helping manage pain in patients with oral mucositis was demonstrated. It was investigated a protective and regenerative effect of hyaluronic acid based gel formulation enriched with NAG （N-acetyl glucosamine） loaded solid lipid nanoparticles against degenerative process of the oral mucosa. Gel formulations were obtained by adding sHA （sodium hyaluronate） into SLN aqueous suspension. Gel performances were evaluated by multi-methodological approach： mucoadhesive and barrier properties evaluation, cell viability. It was shown that gel formulation based sHA, enriched with NAG loaded SLNs, when added as suspension, demonstrated to have a good mucoadhesion profile comparable in terms of tensile work and fracture strength to Carbomer 934 2%. The presence of NAG encapsulated and not in gel formulation enhances also the biocompatibility of the system, demonstrating also to have a proliferative effect. Finally, any barrier property was altered. Finally, results demonstrated that sHA based gel formulation enriched SLNs, demonstrated good mucoadeshion property, comparable to carbopol gel, positive control. The proposed gel formulation enriched with SLNs setting up in this work could be used as innovation strategy to treat oral mucositis.
