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1.
This study is aimed to investigate the nanoliposomal artemisinin preparation, and its implementation on breast cancer cells. Side effects have been one of the common challenges of drug usage, as well as cancer treatment. In order to reduce such effects, nanotechnology has been a great help. Nanoliposomes are provided through reverse phase evaporation. In this method, certain proportions of phosphatidylcholine, cholesterol and artemisinin were mixed together. Besides, the obtained formulation was pegylated by using polyethylene glycol 2000 in order to increase its stability and solubility. The mean diameter of non-pegylated and pegylated liposomal artemisinin was determined by Zeta sizer system. The percent of drug released from liposome was performed by dialysis. The encapsulation efficiency of both formulations was estimated by spectrophotometry method. As a result, encapsulation and drug release of nanoliposomal formulation were more than the pegylation of the same formulation. In addition, this study indicated that cytotoxicity effect of pegylated nanoliposomal artemisinin was more, in comparison with nanoliposomal artemisinin.  相似文献   

2.
Breast cancer is one of the most frequent cancer types within women population. Hydroxyurea (HU) is a chemotherapy compound for treatment of patients with cancer diagnosis, including breast cancer associated with several adverse effects. In this study, we applied nanotechnology to decreased drug side effects along with improvement of therapeutic index. Liposomation is widely used in modern pharmacological developments in order to enhance the effects of the drugs. To achieve this, in this study a mixture of phosphatidylcholine and cholesterol was made up and HU was added to the resultant mixture, was then pegylated using Polyethylene Glycol 2000 to increase resistance, applicability and solubility. The mean diameters of nanoliposomal and pegylated nanoliposomal HU were measured by Zeta sizer device and obtained about 402.5 and 338.2 nm. The efficiency of non-pegylated and pegylated liposomal HU was 70.8 and 64.2, respectively. Releasing HU in both formulations was estimated about 25.8 and 21.7 %. Also, this study investigated the cytotoxicity effect of nanoliposomal and pegylated nanoliposomal HU using MTT assay. Results of this investigation showed that the cytotoxic properties of pegylated HU was 3.6 % more than those non-pegylated form, while was 38.93 % more than ordinary from of HU. This study showed that the stability, releasing pattern and cytotoxicity of the pegylated nanoliposomal HU is better than that of nanoliposomal HU.  相似文献   

3.
It is clear that cancer is one of the most mortal diseases in the world and the most prevalent among women is breast cancer. As hydroxyurea (HU)—a drug which is used in chemotherapy—has many adverse effects in long-term despite of its therapeutic properties, we made use of nano drug delivery technology in order to reduce adverse effects and increase therapeutic index. Thus, liposomation is a novel way in drug delivery systems. In this study a mixture of phosphatidylcholine and cholesterol was mixed and HU was added to the resultant mixture. The mean diameter of the nanoliposomal HU measured with the Zeta Sizer device (equal to 402.5 nm) and its encapsulation efficiency was 70.8 %. Besides, using dialysis, the pattern of drug release from nanoliposomes has been studied and the results showed that the drug release of nanoliposomal drug within 28 h was equal to 25.85 %. This study showed that the cytotoxicity effect of nanoliposomal drug is more than that of the standard drug.  相似文献   

4.
Regarding that the breast cancer is the most prevalent disease among women, paclitaxel, an anti-cancer drug, could be used in treatment of this disease. As paclitaxel has adverse effects, it was used of nanoliposome drug delivery technology in order to reduce adverse effects and improve drug efficacy. Certain ratios of phosphatidylcholine, cholesterol and paclitaxel were synthesized to prepare nanoliposomal paclitaxel. Using Zeta sizer device, the mean diameter of nanoliposomal paclitaxel was obtained 421.4 nm and its encapsulation efficiency was 91.3 %. By dialysis, drug release in nanoliposome paclitaxel formulation within 28 h was studied which was 5.53 %. This study showed that cytotoxicity effect of nanoliposomal paclitaxel is more than that of the standard form.  相似文献   

5.
In the present study, paclitaxel was archaeosomed to reduce side effects and improve its therapeutic index. Carriers have made a big evolution in treatment of many diseases in recent years. Lipid carriers are of special importance among carriers. Archaeosome is one of the lipid carriers. Paclitaxel is one of the drugs used to treat breast cancer which has some unwanted side effects despite its therapeutic effects. Archaeosomes were extracted from methanogenic archi bacteria and synthesized with a certain ratio of paclitaxel in PBS. The mean diameter of archaeosomal paclitaxel was measured by Zeta sizer instrument, Drug releasing of archaeosomal paclitaxel was examined within 26 h which results showed that the most drug releasing occurs during first 3 h. The cytotoxicity effect of archaeosomal paclitaxel on breast cancer’s cell line was evaluated by MTT assay which results showed that the cytotoxicity effect of archaeosomal paclitaxel on breast cancer’s cell line is more than that of the standard paclitaxel formulation. The results indicated that new drug delivery of paclitaxel using archaeosome, increases the therapeutic index of the drug.  相似文献   

6.
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7.
Carboplatin is a chemotherapeutic agent used against various malignancies such as ovarian carcinoma. The aim of this study is to improve the therapeutic efficacy of carboplatin using pegylated liposomal nanocarriers. Nanoparticles were synthesized using thin film hydration technique and characterized for shape morphology, particle size, zeta potential and drug-release properties. In the next step, A2780S and A2780CP ovarian cancer cell lines were used to determine the efficacy of nanodrug by MTT assay. The particle size and zeta potential of nanodrug were measured 244.3 ± 19.6 nm and ?22.9 ± 1.7 mV, respectively. High encapsulation capacity (78.6 ± 3.7 %) confirmed the efficiency of technique. The cytotoxicity results also showed that nanodrug compared to free drug improve the efficacy of carboplatin against both A2780S (P < 0.01) and A2780CP (P < 0.05) cell lines. In conclusion, the findings of our study suggested pegylated liposomal nanocarriers are proper for carboplatin delivery to ovarian cancer cell lines A2780S and A2780CP.  相似文献   

8.
Cisplatinum (Cispt) is an anti-cancer drug with a low level of solubility. One of Cispt’s solvents is dimethyl sulfoxide (DMSO) which can be substituted with chlorine of drug as Cispt’s solvent. Applying such a solvent in biological studies is impossible due to intense reduction in activity. On the other hand, it is specified that Cispt’s stability is increased in aqueous media by increasing sodium chloride (NaCl) concentration up to 0.9 %. Consequently, we intended to study the effect of DMSO on cytotoxicity of Cispt in presence of sodium. MTT assay was employed to study cytotoxicity effect of Cispt + NaCl + DMSO and Cispt + DMSO on G-292 cell line. Cytotoxicity in dilutions of 300 and 9 (p < 0.01) of Cispt in Cispt + NaCl + DMSO formulation was equal to 78 and 7 %. These values were estimated 79 and 18 % for Cispt + DMSO formulation and 79 and 24 % for free drug. IC50 values demonstrated reduction of 45 % in cytotoxicity of Cispt in Cispt + DMSO formulation. Studying chemical structure of Cispt and Cispt dissolved in DMSO showed that NaCl cannot inhibit inactivating effect of DMSO on Cispt and effect of this solvent on Cispt is independent from presence of NaCl. Results represented that using NaCl does not result in stability and keeping cytotoxicity properties of Cispt in DMSO. Findings suggest more studies for using DMSO as a solvent of Cispt.  相似文献   

9.
青蒿素:从中国传统药方到全球抗疟良药   总被引：1，自引：0，他引：1       下载免费PDF全文
青蒿素是从中国传统药物青蒿中提取的抗疟药物。青蒿素及其衍生物、复方的应用为全球疟疾耐药性难题提供了有效的解决方案。青蒿素及其衍生物作为全球疟疾治疗的首选药物,解除了数百万疟疾患者的病痛,因此在青蒿素研制中作出了突出贡献的屠呦呦成为因为在中国本土进行的科学研究而首次获诺贝尔科学奖的中国科学家。青蒿素的发现是在一个特殊的社会文化环境中完成的,是一个任务("523任务")带动科研和学科发展的典型案例,是国家需要与科学研究相互促进的结果。文章回顾青蒿素研发的历史,考察在设备、技术条件相对落后的情况下,如何通过有组织的科研协作、多机构的优势整合而取得突破的经验,探讨社会、政治、文化与基础研究、开发应用之间的互动关系,从中汲取经验与教益。  相似文献   

10.
Schizophrenia is a psychotic disorder with a complex pathophysiology and requires treatment that includes long term administration of antipsychotics that is said to be associated with metabolic syndrome. This study was designed to evaluate the impact of seven different antipsychotics prescribed to schizophrenic patients, on development of metabolic syndrome in the patients. A total of 210 patients with schizophrenia (30 patients in each drug therapy group) were recruited according to ICD-10 criteria and were assigned to receive the drug for 16 weeks. Measurement of anthropometric (body weight, waist circumference, blood pressure) and biochemical parameters (glucose, insulin, HOMA-IR, triglycerides, LDL, HDL) was done and the patients were subjected to ATP-III defined criteria for metabolic syndrome. Patients undergoing treatment with olanzapine were more prone to metabolic syndrome as the drug induces weight gain after 16 weeks of treatment. It also induces dyslipidemia (P < 0.001) and hyperglycemia (P < 0.01). Clozapine was found to be second most potent drug in inducing metabolic syndrome as the weight in clozapine treated patients increased after 16 weeks, along with a significant increase in glycemic (P < 0.001) and lipid parameters (P < 0.01). Aripriazole and amisulphride are comparatively safer drugs as their role in inducing metabolic abnormalities in schizophrenic patients was insignificant, although the impact of long term administration of these drugs needs to be explored. It is clear from the study that antipsychotic treatment induces metabolic syndrome so, it becomes important that the metabolic and cardiovascular risk factors should be surveillance regularly in schizophrenic patients undergoing antipsychotic treatment.  相似文献   

11.
Recently, the combination of lipids and block copolymers has become an alternative to liposomes and polymersomes as nano-sized drug carriers. We synthesize novel block copolymers consisting of poly(cholesteryl acrylate) as the hydrophobic core and poly(N-isopropylacrylamide) (PNIPAAm) as the hydrophilic extensions. Their successful phospholipid-assisted assembly into vesicles is demonstrated using the evaporation-hydration method. The preserved thermo-responsive property of the lipid-polymer hybrids is shown by a temperature dependent adsorption behaviour of the vesicles to poly(l lysine) coated surfaces. As expected, the vesicle adsorption is found to be higher at elevated temperatures. The cellular uptake efficiency of hybrids is assessed using macrophages with applied shear stress. The amount of adhering macrophages is affected by the time and level of applied shear stress. Further, it is found that shorter PNIPAAm extensions lead to higher uptake of the assemblies by the macrophages with applied shear stress. No inherent cytotoxicity is observed at the tested conditions. Taken together, this first example of responsive lipid-polymer hybrids, and their positive biological evaluation makes them promising nano-sized drug carrier candidates.  相似文献   

12.
从标准合作网络中参与主体的重要性评估出发,探讨标准合作网络特征及演化规律和趋势.以我国人工智能产业技术标准为例,采用社会网络分析方法从萌芽期、成长期与成熟初期三阶段构建标准合作网络,基于度数中心度、中介中心度、接近中心度和特征向量中心度4个评价指标,通过TOPSIS熵权法识别我国人工智能产业技术标准重点发展领域的核心主...  相似文献   

13.
Elevated plasma triglyceride and non-esterified fatty acid concentrations may cause insulin resistance and type 2 diabetes mellitus. Lipoprotein lipase (LPL) is a rate-determining enzyme in lipid metabolism. A variant in the LPL gene has been identified which alters the penultimate amino acid Serine at 447 to a stop codon (S447X), and results in a truncated LPL molecule lacking the C-terminal dipeptide Ser–Gly. The present study was designed to evaluate the frequency of S447X variant in the LPL gene and its effect on the lipid and lipoprotein levels in type 2 diabetic subjects. The genotype frequency distributions of type 2 diabetes patients and controls were in Hardy–Weinberg equilibrium. Comparison of the genotype and allelic frequencies of S447X in subjects with type 2 diabetics compared to controls demonstrated no significant difference. In subjects with type 2 diabetics having hypertriglyceridemia (TG ≥ 150 mg/dl) compared to diabetics with TG level <150 mg/dl, significant difference in genotype frequency was found among these groups, while allelic frequency of X was significantly differed. Logistic regression analysis showed the negative association of LPL S447X variant with TG and VLDL cholesterol, while no association with total cholesterol, HDL cholesterol and LDL cholesterol was found. The lipid levels except for HDL cholesterol were found to be significantly lower in carriers for S447X than wild type in diabetes group. The decreased level of TG and TG rich lipoprotein in subjects with SNP S447X in LPL, predicts anti-atherogenic activity of carriers for S447X variant in general population as well as type 2 diabetic patients.  相似文献   

14.
The study has been undertaken as number of sickle cell patients in Chhattisgarh tribal population is 23.7 %. The Co enzyme Q10 is a strong antioxidant and energy producing compound. The patients were divided into three groups group A homozygous (SS), group B heterozygous (AS) and group C controls for TBARS study. The age group is 10–55 years and 200 mg of CoQ10 was given to A and B groups. The hematological parameters, C reactive protein as well as RBC TBARS level were performed by usual and standard techniques. The results were obtained as 25.37 % increased RBC level in group A and 23.24 % in group B. The increased hemoglobin level was observed as 16.73 % in group A and 10.7 % in group B. In case of WBC it was observed increased 24.38 % in group A and 12.0 % in group B. C-reactive protein was observed 7.8 times decreased in group A and 1.54 times in group B. The RBC TBARS level was also found decreased 48 % in group A and 51 % in group B as compared to group C. During the supplementation of coenzyme Q10 the pain caused by vaso-occlusive events has reduced. This significant increase in hematological parameters as well as decreased C-reactive protein and TBARS level suggest that the Q10 should be included in the diet of sickle cell patients.  相似文献   

15.
Finding side effects of drugs, before reaching the animal and clinical test, can decrease the cost and time of developing new drugs. Also, a lot of side effects are reported after going to market and using it by patients (post-marketing). There are some systems to report these events but most of the time, side effects stay hidden. Thus, a lot of computational methods have been developed to predict the side effects of drugs before reaching the clinical test or going to market. These methods are based on different features of drugs like chemical or biological features. Most of these methods can just complete the side effect list of approved drugs or require a great deal of biological information about the drugs. So, it is impossible to find the side effects of a new drug candidate very early. In this paper, we propose a network and domain-based algorithm (NDDSA) that can predict the side effects of new drug candidates by assigning a score to each side effect. Unlike other methods, it needs just the chemical formula of the new drug. We show that NDDSA performs better than the best present method in case of predicting ADRs for a new drug and has acceptable results in case of predicting potential side effects for approved drugs, while it is much faster than the other methods.  相似文献   

16.
The present study was undertaken to evaluate antidiabetic and antioxidant activities of Cayratia trifolia root extract against streptozotocin induced diabetes in experimental rats to scientifically validate its use against diabetes in some parts of India. Ethanolic extract, showing the highest activity in in vitro experiments, was prepared in saline and administered orally to streptozotocin induced albino Wistar diabetic rats for 21 days. Biochemical parameters liver and muscles glycogen and in vivo antioxidant activity in normal, diabetic control, standard (metformin) and treated animals were determined and compared. Attempt was made to isolate, purify and characterize one of the major secondary metabolites in extract by range of chromatographic and spectroscopic techniques. Treatment of streptozotocin induced diabetic rats with ethanolic root extract (500 mg/kg) caused significant (P < 0.01) reduction in blood glucose (312–178 mg/dL), increase in body weight (181–219 g) and serum insulin (1.28–2.26 IU/dL). It also maintained lipid profile and tests of liver and kidney functions within normal range as compared to diabetic control rats and almost at par with standard drug metformin. The oxidative stress induced decline in glutathione and catalase in liver and kidney tissues showed recovery nearly to normal level as a function of treatment. The GC–MS profile of the extract showed relatively high concentration of β-sitosterol which was characterized by different spectroscopic and chromatographic techniques. The result scientifically and comprehensively validate the reported use of roots of this indigenous plant against diabetes. A strong antioxidant activity of the ethanolic root extract suitably compliments the antidiabetic effect.  相似文献   

17.
Obesity is risk factor for insulin resistance, diabetes, and other chronic diseases. Adiponectin, an adipose-specific protein with antiatherogenic and antiinflammatory effects, were found to be associated with obesity, type 2 diabetes, and insulin resistance. Our aim to identify possible relationships between circulating adiponectin and obesity as well as obesity related phenotypes. A total of 642, obese and non-obese individuals were included in this cross-sectional study. Hormone and glucose levels were estimated using standard protocols. The adiponectin levels showed a significant decrease with increasing quartiles of insulin resistance index. Subjects in lowest quartile of adiponectin level had a significantly higher risk than those in the highest quartile, with higher body mass index, waist circumference, blood pressure, percentage body fat, fat mass, fasting insulin, insulin resistance index, total cholesterol (p < 0.001), low density lipoprotein–cholesterol (p = 0.001), very low density lipoprotein–cholesterol (p = 0.002), and Triglyceride (p = 0.002). The present study indicates that adiponectin is significantly associated with obesity, insulin resistance and other obesity related phenotypes.  相似文献   

18.
The present study was undertaken to evaluate antidiabetic and antioxidant activities of Cassia tora (C. tora) seeds extract against streptozotocin induced diabetes in experimental rats to scientifically validate its use against diabetes. Ethanolic extract of C. tora seeds extract and standard drug (glibenclamide) prepared in aqueous gum acacia (2 %, w/v) suspension and fed orally to streptozotocin induced male adult diabetic rats of Charles Foster strain for 15 days. Biochemical parameters in normal, diabetic control, standard (600 μg/kg bw p.o.) and treated (500 mg/kg bw p.o.) animal groups were quantified and compared. Treatment of streptozotocin induced diabetic rats with ethanolic seeds extract caused significant (p < 0.001) reduction in blood glucose (270–220 mg/dl), total cholesterol (140–104 mg/dl), triglyceride (149–99 mg/dl), phospholipids (100–74 mg/dl), free fatty acid (2.39–2.00 μmol/l), lipid peroxide (9–5.63 nmol MDA/dl) and significantly increased post heparin lipolytic activity (11–14 nmol FFA released/h/l plasma) (p < 0.001). Furthermore, the seeds extract (100–400 μg) when tested for its antioxidant activity in vitro, showed significant (p < 0.001) inhibition in the generation of super oxide anions in enzymic system a (46–37, 33, 23, 21 nmol uric acid formed/min), in enzymic system b (113–91, 77, 60, 51 nmol formazon formed/min), non-enzymic system (324–230, 211, 161, 141 nmol uric acid formed/min) and hydroxyl radicals in enzymic system (544–501, 411, 319, 291 nmol 2,3-dihydroxybenzoate formed/h) and non-enzymic system (28–21, 17, 14, 12). The results of the present study demonstrated antidiabetic, antidyslipidemic and antioxidant activities of C. tora seeds which could help in prevention of diabeticdyslipidemia and related complications.  相似文献   

19.
The biological activity of the mineralocorticoid antagonist, spironolactone depend upon its metabolism. In this study the effect of diuretic drug compound spironolactone on the acid and alkaline phosphatase in the testes of albino rat. The drug spironolactone was administered orally daily for 7th, 14th and 21st days at the dose of 100 mg/kg body weight. Among them, the side effects of drug are that the degradation of alkaline phosphatase in the testes; while acid phosphatase increased significantly may be due to 7a-thiospironolactone is a tissue metabolite of spironolactone and may contribute to the testicular enzymes, therapeutic actions and some other side effects. It is suggested that the decrease and increase of alkaline and acid phosphatase in the testes of albino rat are the due to the side effects of spironolactone drug compound.  相似文献   

20.
Voriconazole, an antifungal drug exhibiting wide inter-individual variability, is an ideal candidate for therapeutic drug monitoring (TDM). The aim of the present study was to standardize a simple, sensitive and rapid high performance liquid chromatography (HPLC) method with ultraviolet detection to determine plasma voriconazole concentration. The HPLC method consisted of a combination of acetonitrile and water (7:3) as mobile phase with 1 ml/min flow rate and detection at 255 nm. Plasma protein precipitation was carried out using perchloric acid and the filtered supernatant was passed through C18 column (250 × 4.6 mm, 5 μm) for the separation of voriconazole. The limit of quantification of voriconazole was 0.2 mg/L. The assay was validated with a linearity of 0.2–15 mg/L and used clinically for TDM in patient samples. The inter-assay precision was below 15 % for routine quality control samples. Weight based voriconazole doses were prescribed to 26 patients for empirical treatment of invasive fungal infections. Voriconazole therapy was managed from the baseline drug levels and follow up analysis reflected achievement in clinical efficacy. Routine TDM of voriconazole may reduce adverse events and improve the treatment response in invasive fungal infections.  相似文献   

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