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Abstract Curcumin is a plant-derived compound with polypharmacological properties that are hampered by its poor solubility, fast degradation, etc. Wound closure complications that follow tooth extraction are numerous, and relatively frequently additional treatment is needed to prevent unwanted process chronification. The present study aims to compare the effects of free and the nanoliposome-encapsulated curcumin on tooth extraction wound closure. The experiments were performed on Wistar rats where both forms of curcumin were applied topically on a tooth extraction wound for seven days. Changes in tissue oxidative stress (malondialdehyde and oxidized proteins concentrations, and catalase activity) and inflammation (nitric oxide levels and myeloperoxidase activity) related parameters were studied three and seven days following the tooth extraction. Also, the extent of pathohistological changes and osteopontin immunohistochemical expression were studied. The obtained results indicate that both forms of curcumin prevent an increase in oxidative stress and inflammation-related parameters in the studied samples at 3-and 7-day time points. Additionally, we found that curcumin diminished tissue inflammatory response and osteopontin expression, while at the same time it caused faster granulation tissue maturation. The encapsulation of curcumin in nanoliposomes proved to be better in improving the extraction wound healing process than the free curcumin, giving this formulation a potential in the pharmaceutical industry.
Subject(s)
Animals , Male , Female , Rats , Tooth Extraction/classification , Wound Infection/classification , Wounds and Injuries/drug therapy , Curcumin/analysis , Wound Closure Techniques/classification , Inflammation/drug therapy , Wound Healing/drug effects , Oxidative StressABSTRACT
Abstract The objective of this study was to evaluate the influence of vitamin C (VC) on the stability of stored liposomes under different climatic conditions. Liposomal formulations containing 1 mg/mL of VC (LIP-VC) and blank formulations (LIP-B) were prepared by the reverse-phase evaporation method. After preparation, they were characterized according to their refractive index, average vesicle diameter, polydispersity index (PDI), zeta potential, pH, content, encapsulation efficiency (EE%), morphology, stability and antioxidant activity. For stability, LIP-VC and LIP-B were stored in different climatic conditions (4 °C, 25 °C and 40 °C) for 30 days. The LIP-VC presented 1.3365 refractive index, 161 nm of mean diameter, 0.231 PDI, -7.3 mV zeta potential, 3.2 pH, 19.4% EE%, spherical morphology, 1 mg/mL of VC content, and antioxidant activity of 12 and 11.4 μmol of TE/mL for the radical DPPH and ABTS+, respectively. During stability, the LIP-B stored in 40 °C showed an instability in the parameters: PDI, vesicle size and zeta potential after 15 days, while the LIP-VC remained stable in its size and PDI for 30 days. After that, it is shown that VC can be used as an antioxidant and stabilizer in liposomes to increase the stability and shelf-life of vesicles.
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Objective To compare the differences in the anti-tumor growth effects of organisms with different injections of CT26 tumor cell RNA loaded into nanoliposomes. Methods The extracted tumor RNA was loaded into nanoliposomes to prepare tumor RNA nanoliposome vaccines, and the related properties of nanoliposome vaccines were investigated. The particle size of nanoliposome vaccines was （120.0±12.1）nm and zeta potential was （3.39±0.56）mV. Tumor RNA nanoliposome vaccines were injected into different parts of the mice to test and analyze the influence of different injections on the growth of colon cancer transplanted tumors in mice. Results Tumor RNA nanoliposome vaccines were used to inject tumor-transplanted mice in different ways. Compared with underarm injection, intraperitoneal injection enhanced the organism's anti-tumor immune response and inhibited the growth of transplanted tumors more effectively. The H&E staining of important organs in mice was compared and no obvious organic lesions were found in the organs. Conclusion Intraperitoneal injections of nanoliposome loaded with tumor RNA can enhance the body's anti-tumor immune response more effectively than underarm injections.
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Objective@#To investigate the effects of modified acidic fibroblast growth factor (MaFGF) mediated by nanoliposomes combined with ultrasound-targeted microbubble destruction (UTMD) on left ventricular systolic function in early diabetes mellitus(DM) rats.@*Methods@#The nanoliposomes containing MaFGF(MaFGF-nlip) were prepared by reverse phase evaporation method. Among 60 male Sprague Dawley (SD) rats, 50 rats were randomly selected and were induced to be DM models by streptozotocin(STZ) through intraperitoneal injecting, the other 10 rats as control group. Then DM rats were randomly divided into 4 groups: DM model group, MaFGF solution group, MaFGF-nlip group and MaFGF-nlip+ UTMD group. After the successful induction of DM model, the intervention was performed twice a week.After 12 weeks of intervention, all rats underwent conventional echocardiography and velocity vector imaging (VVI). Left ventricular ejection fraction (LVEF) and left ventricular fraction shortening(LVFS) were measured by conventional echocardiography. The mean peak systolic radial velocity (Vs), radial strain (Sr) and radial strain rate (SRr) of six walls at the papillary muscle level were measured in left ventricular short-axis view by VVI. At last, myocardial tissue of all rats were stained with Sirius red to evaluate myocardial interstitial fibrosis. The level of myocardial apoptosis was evaluated by TUNEL staining, and the changes of myocardial ultrastructure were observed by transmission electron microscopy.@*Results@#The prepared MaFGF-nlip were more rounded, evenly dispersed, and of good stability and high encapsulation efficiency. Twelve weeks later after intervention, LVEF, LVFS, Vs, Sr and SRr in the DM model group were significantly lower than those in the control group (all P<0.05). LVEF, LVFS, Vs, Sr and SRr in the MaFGF-nlip+ UTMD group were significantly higher than those of the DM model group and other intervention groups (all P<0.05). The results of Sirius red staining and Tunel staining showed that CVF and AI in the DM model group were significantly higher than those in the control group (all P<0.05). For MaFGF-nlip+ UTMD group, CVF and AI were significantly decreased compared with the DM model group and other intervention groups(all P<0.05). According to the results of transmission electron microscopy, compared with the DM model group, the improvement of myocardial ultrastructure was the most obvious in the MaFGF-nlip+ UTMD group.@*Conclusions@#MaFGF delivered by using nanoliposomes combined with UTMD can improve the left ventricular systolic function in diabetic rats by inhibiting the myocardium cardiac fibrosis and reducing the cardiomyocyte apoptosis.
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Objective To study the antitumor effect of natural active compound usenamine (C18H17NO6, 6-acety1-2- (1-amino-ethylidene)-7,9-dihydroxy-8,9b-dimethy1-9bH-dibenzofuran-1,3-dione) nano-liposomes in vitro and in vivo. Methods Nano-liposomes were prepared by thin film dispersion-ultrasonic method. The drug loading of nano-liposomes was determined by HPLC. The cancer cells were cultured in vitro, and the absorbance values were measured by MTT method to evaluate the anticancer effect in vitro. A nude mouse xenograft model was established to observe the growth inhibitory effect of drug-loaded nano-liposomes on tumor growth in nude mice. Results The drug loading of drug-loaded nano-liposomes was 1.26 mg/mL. The IC50 of the drug-loaded nano-liposomes in the XWLC-05, HCT-116, and HepG2 cells were 2.48 μg/mL, 0.86 μg/mL, and 1.86 μg/mL, respectively, and the inhibition rates of XWLC-05, HCT-116, and HepG2 cells administered at a dose of 4 μg/mL were 85.59%, 99.95%, and 96.91%, respectively (P < 0.01). The minimum relative tumor proliferation rate of nude mice was 50.98%, and usenamine nano-liposomes had antitumor effect in vivo. Conclusion The natural active compound usenamine can be prepared as a nano-liposome.In vitro cell experiments showed that usenamine nano-liposomes had a dose-effect relationship with cancer cells. In vivo experiments in nude mice found that drug-loaded nano-liposomes had inhibitory effect on tumors.
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OBJECTIVE： To establish a methaod for content determination of doxorubicin hydrochloride nano-liposomes， and to optimize its preparation technology. METHODS： The contents of doxorubicin hydrochloride nano-liposomes was determined by UV spectrophotometry. The membrane dispersion method was used to prepare doxorubicin hydrochloride nano-liposomes. Using particle size， encapsulation efficiency and drug-loading amount as indexes， the weight ratio of phospholipid to drug （mg/mg）， the weight ratio of phospholipid to cholesterol （mg/mg） and ultrasonic time （min） as factors， central composite design-response surface methodology was used to optimize the preparation technology. The photothermal conversion effect of doxorubicin hydrochloride nano-liposomes was investigated by near infrared irradiation. RESULTS： The linear range of doxorubicin hydrochloride were 1.01-16.16 μg/mL（r＝0.999 7）； precision， stability and reproducibility tests were all in line with the requirments of Chinese Pharmacopoeia. The optimal preparation technology included that the weight ratio of phospholipid to drug was 13.30 ∶ 1（mg/mg）； the weight ratio of phospholipid to cholesterol was 4.09 ∶ 1 （mg/mg）； the ultrasonic time was 10 min. Under this technology， the particle size and drug-loading amount of doxorubicin hydrochloride nano-liposomes were （200.5±25.1） nm and （11.02±0.20）％， relative errors of which to predicted value （196.3 nm， 10.68％） were 1.82％ and 1.63％. The consistency between measured value and predicted value was good. Doxorubicin hydrochloride nano-liposomes exhibited concentration- dependent and time-dependent photothermal conversion characteristics under near infrared irradiation at 808 nm. CONCLUSIONS： Established method is simple and good accuracy. The optimized preparation technology is simple and feasible.
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Objective To investigate the advanced preventive effect of acid fibroblast growth factor (aFGF) on diabetic cardiomyopathy(DCM) by using heparin-modified nano-liposomes combined with ultrasoundtargeted microbubble destruction technique (UTMD).Methods aFGF-loaded nano-liposomes (aFGF-lips) were prepared by lyophilization technique.Type Ⅰ diabetes model was induced by intraperitoneal injection of streptozotocin (STZ,70 mg/kg) in male SD rats.Before and twelve weeks after intervention,all rats underwent the transthoracic echocardiography.The segmental mean peak systolic radial velocity (Vs),systolic circumferential strain (Sc),and systolic circumferential strain rate (SRc) were measured.The expression of aFGF in DCM rats was detected by western blot.The rats were sacrificed and myocardial tissue were stained with masson staining and Tunel staining to quantify myocardial collagen fraction(CVF) and cardiac myocyte apoptosis index(AI).Results aFGF-lips showed good morphology and aFGF encapsulation efficiency (89.4±1.2)％ with high stability.From the animal experiments,the echocardiographic indexes including Vs,Sc and SRc had significantly improvements over DM group (P＜0.05) and all other treatment group (P＜0.05).The Masson's trichrome staining demonstrated that CVF was significantly higher in DM group than in the control group and was significantly lower in the aFGF-loaded nano-liposome+UTMD group than other groups(all P＜0.05).The TUNEL results showed that AI was significantly higher in DM group than in the control group and was significantly lower in aFGF-loaded nano-liposome +UTMD group than other groups (all P＜0.05).Conclusion aFGF nano-liposome combining with UTMD technique can improve the functions and pathologies of the hearts in type 1 diabetes mellitus model,which might provide a novel technique for aFGF in DCM prevention.
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Objective To investigate the prevention effect of curcumin loaded nano - liposomes on diabetic cardiomyopathy. Methods The curcumin-loaded nano-liposomes were prepared by Film dispersion and ultrasonic hydration technology and their quality inspections were also investigated.Sixty SD rats were randomly divided into normal control group,model control group,blank and curcumin-loaded nano-liposomes group ( n＝15). Diabetes model was induced by intraperitoneal single injection of STZ(70 mg·kg-1).After two weeks of STZ injection,the rats with model control were used for this study.The curcumin loaded nano-liposomes treatment group rats were treated with curcumin loaded nano-liposomes ( 5 mg·kg-1) via caudal vein administration for 12 weeks (three times a week).Rats of normal control group,blank nano-liposomes treated group and model control group were administrated equivalent volume of 0. 9% sodium chloride solution or blank nano-liposomes solution. After treatment for 12 weeks,the experimental animals underwent ultrasonic heart function examination.Then the rats were sacrificed and their hearts were arrested after saline perfusion. The myocardial cell collagen volume fraction ( CVF) and apoptosis index were detected. Results Curcumin loaded nano-liposomes showed good morphology and curcumin encapsulation efficiency ( 88. 37 ± 1.21) %with high stability and dispersibility. From the animal experiments, the evaluation indexes in curcumin loaded nano-liposomes treated group including LVIDd and LVFS were significantly higher than model control group and nano-liposomes treated group(P<0.05),and the LVPW,CVF and apoptosis index were significantly lower than model control group and nano-liposomes treated group(P<0.05). Conclusion Curcumin loaded nano-liposomes can improve the cardiac function of diabetic rats by reducing the fibrosis and apoptosis index of myocardial cells in diabetic rats, which could be used to prevent the diabetic cardiomyopathy.
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Objective To prepare palmatine-loaded flexible nano-liposomes (PFL) films with Bletilla striata polysaccharide (BSP) as membrane material, and evaluate its pharmacy related performance in order to lay the foundation for further application. Methods The PFL was prepared by injection method and the films of PFL based on Bletilla striata polysaccharide (PFL-BPF) was prepared by homogenate coating method. The PFL-BPF was characterized and evaluated by electron microscopy, differential scanning calorimeter (DSC), and in vitro transmucosal membrane experiment. Results The PFL and BSP had good compatibility and easy to film with BSP as membrane material. The appearance of PFL-BPF obtained was smooth, non-bubble, flexible, and suitable stiffness; PFL-BPF had good biological adhesion. The time of scouring the film agent from mucous membrane with normal saline was (130 ± 7) min. At 0.5 h, the dose of PFL-BPF promoting palmatine (PA) infiltration to mucosa was 32.41 μg/g. It was 3.17 times higher than those of PA solution based on BSP (PL-BPF) and 1.9 times for PA common liposomes based on BSP (BLP + PA-BPF) (t-test, P < 0.05); At 2.5 h, it was 2.67 times and 1.89 times higher than those of PL-BPF and BLP + PA-BPF, respectively. It showed that PFL-BPF could significantly promote the water-soluble drug PA through mucosa membrane and release it slowly. The results of DSC showed that the possible mechanism for promoting the absorption of PA through mucosa membrane was that the flexible liposomes disturbed the mucosal epithelial cells and carried the drug into the mucosal tissue. Conclusion The PFL-BPF had the advantages of good film-forming property, lasting adhesive attraction, strong scour resistance, simple and feasible preparation process, and could promote drug permeation into mucosa obviously. Therefore, the flexible nano-liposomes film is a good drug carrier for the transmucosal drug delivery applications and has a wide application prospect.
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OBJECTIVE:To prepare the Albendazole nanoliposomes freeze-dried power and study its properties. METHODS:Freeze-drying method was conducted to prepare Albendazole nanoliposomes freeze-dried power,using the particle size,encapsula-tion efficiency,appearance,redispersibility as indexes,single factor test was combined with orthogonal test to screen freeze-drying preparation technology. The morphological changes,particle size,Zeta potential,moisture content,12 months stability at 4 ℃ be-fore and after freeze-drying were detected. RESULTS:Plus a total content of freeze-dried protective agent was 10%,the ratio of glucose-trehalose-mannitol was 1.0:1.0:3.0,using quick-freeze,pre-freezing 18 h in -35 ℃ refrigerator,dry-freezing 48 h to ob-tain freeze-dried powder. Compared with before freeze-drying,the freeze-dried liposomal morphology had no obvious changes, showing clear phospholipid bilayer membrane structure;the particle sizes before and after freeze-drying were (208.63 ± 1.04) nm and (223.04 ± 2.02) nm,Zeta potentials were (-15.6 ± 0.04) mV and (-19.4 ± 0.06) mV,encapsulation efficiencies were (94.62±0.49)%and(91.10±0.46)%(n=3),respectively. Compared with liposomes,liposomes freeze-dried power had good sta-bility in 12 months at 4 ℃. CONCLUSIONS:Albendazole nanoliposomes freeze-dried power is prepared successfully,its stability is superior to albendazole nanoliposomes,and the freeze-drying technology is feasible.
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Objective:To study the in vitro corneal permeation and antibacterial activity of N-trimethyl chitosan(TMC)-coated sparfloxacin lactate(SL)nanoliposomes. Methods:Franz diffusion cells were used with rabbit cornea as the barrier to study the in vitro corneal permeation of TMC-coated SL nanoliposomes,and the permeation parameters were calculated. Eseheriehia eoli,staphylo-eoeeus aureus,pseudomonas aeruginosa and baeillus subtilis were used as the tested bacterial strains and the in vitro antibacterial activity of the SL preparations was investigated to obtain the minimum inhibitory concentration(MIC),the minimum bactericidal concentration (MBC)and the relationship of bacterial inhibitory rate and time. Results:The order of steady permeation rate(J),corneal perme-ation coefficient(P)and corneal retention rate was TMC-coated SL nanoliposomes > SL nanoliposomes > SL eye drop. The order of lag time(τ)and corneal diffusion coefficient(D)was SL nanoliposomes > SL eye drop > TMC-coated SL nanoliposomes. The in vitro an-tibacterial activity showed the order of TMC-coated SL nanoliposomes > SL nanoliposomes > SL eye drop. Conclusion:Compared with the eye drop,liposomes can enhance the corneal permeation and storage of SL with improved antibacterial activity,and TMC-coating can further improve the permeation and antibacterial activity,which is worthy of further study.
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Objective:To prepare N-trimethyl chitosan (TMC)-coated sparfloxacin (SL) nanoliposomes in situ gels(ISG)and in-vestigate the drug release in vitro.Methods:SL liposomes were prepared by a pH gradient method , and then homogenized to nanolipo-somes by high pressure .TMC was used as the coating material to prepare TMC-coated SL nanoliposomes .Poloxamer 407 was used as the gel base, and the optimal amount was selected according to the gelation temperature .TMC-coated SL nanoliposomes ISG was pre-pared using a cold method , and the morphology , size, zeta potential and entrapment efficiency of TMC-coated SL nanoliposomes were studied.A membraneless model was used to study the drug release in vitro, and the result was compared with that of TMC-coated SL nanoliposomes.Results:The optimal amount of poloxamer 407 in the formula was 25%, and the gelation temperature was 23.6℃in the artificial tears and 33 .5℃in the diluted artificial tears .The morphology of TMC-coated SL nanaoliposomes in the ISG was spherical with the mean diameter of (96.8 ±1.5) nm, zeta potential of (46.2 ±1.4) mV and entrapment efficiency of (76.6 ±2.4) %, and the indices had no significant difference when compared with those of TMC-coated SL nanoliposomes .Both the drug release in vitro and gel dissolution profile of TMC-coated SL nanoliposomes ISG exhibited the characteristics of zero-order kinetics, and compared with that of TMC-coated SL nanoliposomes , the sustained release property of the ISG was more significant .Conclusion:TMC-coated SL nanoli-posomes ISG has promising gelation temperature and notable sustained release property .
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Objective: To optimize the preparation method of triptolide-nano-liposomes (TP-NLS). Methods High pressure homogeneous method was used to prepare TP-SLN. According to even design U7(73), the preparation method of TP-SLN was optimized with the factors including weight ratio of phosphorlipid and cholesterol (A), quantity of Poloxamer 188 (B), and homogeneous pressure (C), using the encapsulation efficiency (EE), particle size, and Zeta potential of NLS as indexes. Results: The optimum prescription of TP-NLS was A1B5C7, i.g. lipid matrix a : b was 6 : 1, the dosage of Poloxamer 188 was 1.3 g, and the homogeneous pressure was 70 MPa, high pressure homogeneous method for 15 min. The TP-NLS prepared with the optimal method had good appearance. The EE was 83.52%, the average particle size was 117 nm, and the Zeta potential was 31.7 mV. TP-NLS solution was kept in avoiding light environment at 4℃ for 30 d, and the preservation stability was good. Conclusion: The formula is reasonable and the preparation method of TP-NLS is feasible, which is valuable to further study.
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Objective: To explore the optimum preparation process of triptolide nanometer coating agent. Methods: Optimum preparation process was investigated by uniform design with the amount of film forming material such as polyethylene glycol 124 (PVA124), carbomer, CMC-Na, and the mixing time as investigating factors, and with uniformity, film-forming ability, and peeling strength as indexes. We conducted sc simulation experiment in vitro to investigate the percutaneous penetration process of triptolide nanometer coating agent. Results: The best way to prepare triptolide nanometer coating agent is that we use glycerol monostearate 1.6 g, glycerin 0.25 g, PVA124 3.9 g, Carbomer 0.6 g, CMC-Na 0.9 g, and mix them in 150 min. With above preparation process, we can achieve better coating agent. JS was 0.350 µg/(cm2·h) and the cumulative permeation quantity in 24 h was 11.534 µg/cm2. Conclusion: Using the optimum preparation process, we can get better triptolide nanometer coating agent, which is uniform, easy coating,good adhesion with skin, strong flexibility, and drying soon.
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At present, there is no specific antidote for local anesthetic toxicity, which seriously hindered therapeutic efficts of clinical treatment. It is increasingly urgent for finding find the effective antidote to local anesthetic. This article at-tempts to interpret the molecular pharmacological mechanism from fat pool, energy metabolism, NO, ion channel and solubili-zation for the role of fatty acids in reversal of myocardial toxicity of local anesthetics. And the different characteristics of the structure and function of nano liposome and fat emulsion were compared.
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AIM: To compare brucine with the mixed solution of brucine and nano-liposomes to observe analgesic and anti-inflammatory effects of the brucine nano-liposome for local use on skin were studied. METHODS: The effects of brucine,brucine and nano-liposomes mixed solution,brucine nano-liposome,on the edema of mouse ear induced by dimethylbenzene and the writhing induced by acetic acid were investigated. RESULTS: The results showed that brucine nano-liposomes exhibited better anti-inflammatory and analgesic activities than the brucine.(P