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Assessment of the effects of an aqueous extract of the leaves, flowers, and seeds of Crotalaria retusa L (Fabaceae) on the glycemia in rats 蚕豆科植物叶、花和种子水提物对大鼠血糖的影响
Pub Date : 2022-12-23 DOI: 10.24018/ejpharma.2022.2.3.50
Bi Lane Adrien Goh, Goore Guy Charles Gole Nanti, Stanislas Ouga Zahoui, Semi Anthelme Nene-Bi, F. Traoré
The aim of this study was to evaluate the effects of an aqueous extract of Crotalaria retusa L (Fabaceae) (EACr) on glycemia in Wistar rats, to contribute to the valorization of plants used in traditional medicine for the improvement of people’s health. A phytochemical screening and pharmacological study of the aqueous extract of Crotalaria retusa L (Fabaceae) on glycemia in rats, were carried out. The administration of the substances in animals was made orally. The qualitative phytochemical study carried out with the aqueous extract of the leaves, the flowers, and the pods of Crotalaria retusa L (Fabaceae) made to highlight the presence of polyphenols, flavonoids, catechic, and gallic tannins, quinonic compounds, alkaloids, sterols, and polyterpenes. This extract showed hypoglycemic activity in the normoglycemic animals, treated with the dose of 1000 mg/kg BW with a percentage of reduction of the glycemia of 21.04%. After an overload of glucose, EACr (1000 mg/kg BW) and the glibenclamide (10-2g/kg BW) showed better antihyperglycemic activity in the rats post-treated, with respective percentages of reduction of 41.90 and 50.39%. EACr has hypoglycemic and antihyperglycemic properties which would be probably related to the presence of alkaloids, tannins, and flavonoids. These compounds, generally recognized for their hypoglycemic and antihyperglycemic effects, confer to this extract similar properties to those of certain insulin-secretors. These results support the use of this plant for the treatment of diabetes in traditional medicine and bring a scientific base.
本研究旨在探讨蚕豆科(Crotalaria retusa L,简称EACr)水提物对Wistar大鼠血糖水平的影响,以期为传统药用植物的健康发展提供参考。采用植物化学筛选和药理学方法研究了蚕豆科水提物对大鼠血糖的影响。这些物质是口服给动物服用的。定性的植物化学研究进行了叶,花,豆荚的水提取物的Crotalaria retusa L (Fabaceae),以突出的存在多酚,类黄酮,儿茶素,没食子单宁,醌化合物,生物碱,甾醇和多萜。该提取物对正常血糖动物具有降血糖作用,给药剂量为1000 mg/kg BW,降血糖率为21.04%。葡萄糖过载后,EACr (1000 mg/kg BW)和格列本脲(10-2g/kg BW)对大鼠的降糖活性较好,分别降低41.90%和50.39%。EACr具有降血糖和抗高血糖的特性,这可能与生物碱、单宁和类黄酮的存在有关。这些化合物,通常被认为具有降糖和抗高血糖的作用,赋予这种提取物与某些胰岛素分泌物相似的特性。这些结果支持了该植物在传统医学中治疗糖尿病的应用,并为其提供了科学依据。
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引用次数: 0
Formulation and Evaluation of Orodispersible Tablet of Sulindac 舒林达多孔分散片的研制及评价
Pub Date : 2022-12-23 DOI: 10.24018/ejpharma.2022.2.3.41
Bhavna B. Gaikwad, B. Rane, Ashish Jain
Oral administration of dosage form is the most recommended mode of administration, because of its self-medication, accurate dose of the drug, and ease of administration. However, trouble swallowing in geriatric patients is one major negative of this route, which can mentally disrupt patients. The goal of this study was to use the direct compression method to make orodispersible tablets of sulindac utilizing various doses of super disintegrant agents such as Sodium starch glycolate Crospovidone and Croscarmellose sodium. Three distinct super disintegrants were used to create nine formulations with varying concentration levels. The preformulation, precompression, and post-compression properties of the powder combinations were assessed. In comparison to the other formulations, tablets from batch F3 containing crospovidone had superior organoleptic qualities, as well as outstanding drug release and in-vitro disintegration time. The super disntegrants addition technique was shown to be a viable method for manufacturing orodispersible tablets using the direct compression method.
口服给药是最推荐的给药方式,因为它可以自行给药,剂量准确,给药方便。然而,老年患者的吞咽困难是这条路线的一个主要负面影响,它可能会扰乱患者的精神。本研究的目的是利用不同剂量的高崩解剂如淀粉乙醇酸钠、交联维酮和交联纤维素钠,采用直接加压法制备舒林酸非分散片。三种不同的超级崩解剂被用来制造9种不同浓度水平的配方。评估了粉末组合的配方前、压缩前和压缩后的性能。与其他制剂相比,F3批含交叉维酮片具有较好的感官品质,且具有较好的药物释放和体外崩解时间。超级分散剂的加入技术是一种可行的直接压缩法制备非分散片剂的方法。
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引用次数: 1
Drug Promising Effect for Diabetic Mice of CARICA PAPAYA Leaves 木瓜叶对糖尿病小鼠的药物前景研究
Pub Date : 2022-12-04 DOI: 10.24018/ejpharma.2022.2.3.47
Md. Rokibul Hasan Bhuiyan, Md. Maniruzzaman, Sabina Akter, Sanzia Mehjabin, Md. Rakib Rased Rana, M. Jaman
Diabetics Mellitus is a major problem for city people worldwide. The objective of this study is finding the anti-diabetic and anti-hyper lipidaemic activity by using Carica papaya leaves. This leaves are not generally eaten but this leaves were eaten during dengue fever. The leaves extract is used for the treatment of diabetes and cancer. This leaves were collected from different place of Bangladesh and made methanolic extract then this extract was feed four groups of mice. The results showed that there was a significant (p<0.001 to p<0.05) reduction in blood glucose concentration (mmol/L) by the methanolic extract of C. papaya leaves at dose 100 mg/kg, 200 mg/kg and glibenclamide (used as standard) 5mg/kg body weight. C. papaya leaves extract also regulated the serum lipid profile levels significantly (p<0.001) at same dose in experimental model of diabetes mellitus. The level of serum SGPT, SGOT and CRP were also seen change to the normal level notably (p<0.001) by the oral administration of methanolic extract of C. papaya leaves. In conclusion this research finding indicate that the methanolic extract of Carica papaya leaves contains bioactive substances with hypoglycemic potency.
糖尿病是世界范围内城市人口的主要问题。本研究的目的是研究番木瓜叶的抗糖尿病和抗高血脂活性。这种叶子一般不被食用,但在登革热期间被食用。叶子提取物用于治疗糖尿病和癌症。这些叶子是从孟加拉国不同的地方采集的,并制成甲醇提取物,然后用这种提取物喂养四组小鼠。结果表明:番木瓜叶甲醇提取物在100、200 mg/kg和格列本脲(标准品)5mg/kg体重剂量下,可显著降低大鼠血糖浓度(mmol/L) (p<0.001 ~ p<0.05)。木瓜叶提取物在相同剂量下对糖尿病大鼠血脂水平也有显著调节作用(p<0.001)。口服番木瓜叶甲醇提取物后血清SGPT、SGOT和CRP水平也明显恢复到正常水平(p<0.001)。本研究结果表明,番木瓜叶甲醇提取物中含有具有降血糖作用的生物活性物质。
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引用次数: 1
The Role of an Aqueous Extract of Cactus on Histopancreatic Architecture in Streptozotocin Induced Diabetes Mellitus in Wistar Rats 仙人掌水提物对链脲佐菌素诱导糖尿病Wistar大鼠胰腺组织结构的影响
Pub Date : 2022-08-01 DOI: 10.24018/ejpharma.2022.2.2.30
Uthman Yusuf, Francine Kafula, Kalande Kaimba, Wandi Kalipenta, Hellen Kabwe, J. A. Mulemena, K. Kamvuma, Sam Beza Phiri, M. Miyoba, B. S. Mesole, Adrian Phiri, B. B. Bwalya, W. Zimba
Herbs have been used as medicinal for several years to cure or rather manage different ailments such as diabetes mellitus. This is very common in rural settings of sub-saharan Africa and is now being adopted in urban areas. Opunta species have widely been seen to contain antihyperglycaemic effects. To evaluate the antihyperglycaemic and histopancreatic effect of aqueous extract of prickly pear cactus (Opuntia species) cladodes in streptozotocin-induced diabetic male Wistar rats in vivo.This was a laboratory based research conducted at Mulungushi University involving 30 wistar rats (Rattus norvegicus) that weighed between 160-200 g which were randomly selected into five groups (6 per cage); normal control, diabetic control, diabetic +metformin, diabetic +cactus and cactus only group. Initial blood glucose levels were obtained from the tail and record then Diabetes mellitus was induced using a single intraperitoneal dose of streptozotocin (70mg/kg BW) and established a persistent state of hyperglycemia after 72hours. The aqueous cactus extract of 100 mg/kg BW and metformin of 100 mg/kg BW was administered orally using intragastric cannula daily for a period of 4 weeks.At the end of the fourth week, Diabetes + cactus and diabetes + metformin groups body weights were statistically significant when compared to the diabetic group (P<0.05). While diabetic group was statistically significant when compared to normal control (P<0.05). The relative weight of the pancreas in diabetic group was statistically significant to other groups (P<0.05). The blood glucose in diabetic + cactus was normoglycaemic at 3rd week, Diabetic + metformin group when compared to diabetic group was statistically significant (P<0.05). The normal control and cactus only groups maintained normoglycaemic till the end of the 4th week. The histological findings of the normal control and cactus only group showed normal pancreatic cytoarchitecture. Diabetes group showed high degree of disorganization in the cytoarchitecture in the islet with reduction in β cell mass and deposition of elastic fibres. The Diabetic+Metformin group showed slight decrease in the cell mass (β cells) and elastic fibres were extensively deposited. Diabetic+Cactus treated group exhibited normal histology of the pancreas with increased number of β cells.Opuntia species are able to lower elevated blood glucose levels and ameliorate the effects of STZ on the pancreatic morphology
多年来,草药一直被用作药物来治疗或更确切地说,是治疗不同的疾病,如糖尿病。这在撒哈拉以南非洲的农村地区非常普遍,现在正在城市地区采用。Opunta物种已被广泛认为含有抗高血糖作用。观察刺梨仙人掌水提液对链脲佐菌素诱导的糖尿病雄性Wistar大鼠体内的降糖和组织胰腺作用。这是一项在Mulungushi大学进行的实验室研究,涉及30只体重在160-200 g之间的褐家鼠(Rattus norvegicus),随机分为五组(每笼6只);正常对照组、糖尿病对照组、糖尿病+二甲双胍组、糖尿病+仙人掌组和仅仙人掌组。取尾测初始血糖水平,记录单次腹腔注射链脲佐菌素(70mg/kg BW)诱导糖尿病,72小时后进入持续高血糖状态。给予仙人掌水提物100 mg/kg BW和二甲双胍100 mg/kg BW,每天灌胃给药,连续4周。第4周末,糖尿病+仙人掌组、糖尿病+二甲双胍组体重与糖尿病组比较,差异均有统计学意义(P<0.05)。糖尿病组与正常对照组比较,差异有统计学意义(P<0.05)。糖尿病组胰腺相对重量与其他组比较,差异有统计学意义(P<0.05)。糖尿病+仙人掌组第3周血糖正常,糖尿病+二甲双胍组与糖尿病组比较,差异有统计学意义(P<0.05)。正常对照组和仅仙人掌组血糖维持正常至第4周结束。正常对照组和仙人掌组胰腺细胞结构正常。糖尿病组胰岛细胞结构高度紊乱,β细胞数量减少,弹性纤维沉积。糖尿病+二甲双胍组细胞质量(β细胞)轻微减少,弹性纤维广泛沉积。糖尿病+仙人掌治疗组胰腺组织学正常,β细胞增多。机会鱼能够降低升高的血糖水平,改善STZ对胰腺形态的影响
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引用次数: 0
Medicinal Plants Used in Composition of Anti-Viral Hepatitis Recipes in Burkina Faso: Ethnobotanical Study 布基纳法索抗病毒肝炎配方中使用的药用植物:民族植物学研究
Pub Date : 2022-07-29 DOI: 10.24018/ejpharma.2022.2.2.34
M. Sawadogo, M. J. Bangou, Armandine Lema, Mindiempo Hyacinthe Thiombiano, H. Ouoba, Béboila Ouoba
Viral hepatitis is an inflammatory disease of the liver cells caused by cytopathic viruses. It constitutes a major public health problem. The aim of the present study was to identify the recipes used in the treatment of viral hepatitis in four cities of Burkina Faso and to select the most requested recipe for further analysis. Semi-structured interviews in the local language were conducted by the "snowball" technique among traditional medicine practitioners from May to October 2021. A total of 280 traditional healers (80.35% men) were interviewed and 74 species of medicinal plants belonging to 42 botanical families used in composition of 168 anti-viral hepatitis recipes were identified. The most frequently used organs were roots, followed by barks and then leaves with proportions of 34.64%, 26.07% and 20% respectively. Decoction (54,29%) and drinking (77,14%) are respectively the main method of preparation and administration of drugs. The study allowed the selection of one recipe that will be subjected to phytochemical and pharmacological analyses in order to isolate the molecules with hepatoprotective properties.
病毒性肝炎是一种由细胞病变病毒引起的肝细胞炎症性疾病。它构成了一个重大的公共卫生问题。本研究的目的是确定布基纳法索四个城市用于治疗病毒性肝炎的配方,并选择最需要的配方进行进一步分析。采用“滚雪球”技术,于2021年5月至10月对传统医学从业者进行当地语言半结构化访谈。共采访了280名传统治疗师(男性占80.35%),鉴定了168种抗病毒肝炎配方中使用的42个植物科74种药用植物。使用频率最高的器官是根,其次是树皮和叶片,分别占34.64%、26.07%和20%。煎煮(54,29%)和饮饮(77,14%)分别是主要的制备方法和给药方法。该研究允许选择一个配方,将进行植物化学和药理学分析,以分离具有肝保护特性的分子。
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引用次数: 0
A Review of Medicinal Plants with Anti-Dengue Virus Activity 抗登革病毒活性药用植物研究进展
Pub Date : 2022-03-30 DOI: 10.24018/ejpharma.2022.2.2.20
Joshua John Akwayamai, M. Ahmed, Galaya Tirah, Kadauyina Samuel, W. Usman, Hezekiah Bulus
Dengue virus is an arthropod-borne infectious agent that causes dengue disease. The virus spreads by Aedes aegypti and Aedes albopictus mosquitos. Due to the neglegent care given to the infection, the vectors as well as the virus have expanded globally and millions have already been affected by dengue infection as regards reports by ECDC, CDC and WHO. Dengue virus infection have been alleviated by erratic treatments since there is no precise formulation against it. However, there are plenteous clinical risks alongside using the drugs, this leaves human with no other choices than to reason for other alternative means of treatment to decrease the deleterious effects to minimal level. To introduce newer candidate anti-dengue pharmaceutical agent with minimal/ or no therapeutic lapses, botanical treatments have highly been recognized. Medicinal plants have been observed to be of health benefit in dengue virus infection through promoting immunocompetence, supplying pharmacological aids such as prophylactic effects, decrease viral amplification and lowering morbid condition. The potential anti-dengue activity of medicinal plants have been exemplified in the literature as the principal interest. We tried to find the existing factors behind virucidal activity of plants in the context of anti-dengue virus and the consulted publications indicated that certain flavonoids (Kaempferol-3-Orutinoside, Rutin, Hyperoside, Epicatechin Resveratrol, Quercetin, Emodin, Emodin-8-beta-D-glucoe and Polydatin), Tannins (Galic acid, Tannic acids), Alkaloids (Artesonic Acid, Homoegonol, Myristicin), Fatty acids (Methyldodecanoic acid, Dodecanoic acid, Tridecanoic acid, 12-methyl-methyl-esters, n-hexadecanoic acid), Terpenoids (Beta-asarone, Acoric acid, Andrographolide, Caryophyllene, Cyclododocane) and many others could be the major antiviral factors. This study will assist in giving better insights on anti-dengue activity of medicinal plants divulging dengue virus reliable combaters eventually. However, it is needful to conduct heightened critical clinical studies in this vein for proper verification.
登革病毒是引起登革热的节肢动物传播的传染因子。该病毒通过埃及伊蚊和白纹伊蚊传播。根据疾控中心、疾控中心和世卫组织的报告,由于对感染的忽视,媒介和病毒在全球范围内扩大,数百万人已经受到登革热感染的影响。由于没有针对登革热病毒的精确配方,不稳定的治疗减轻了登革热病毒感染。然而,在使用这些药物的同时,也存在着大量的临床风险,这使得人类别无选择,只能寻找其他替代治疗方法,将有害影响降至最低。为了引入新的候选抗登革热药物,植物治疗已得到高度认可。药用植物已被观察到通过提高免疫能力、提供药物辅助如预防作用、减少病毒扩增和降低疾病状况等对登革热病毒感染的健康有益。药用植物潜在的抗登革热活性已在文献中作为主要兴趣例证。我们试图在抗登革病毒的背景下寻找植物杀毒活性背后的存在因素,并咨询出版物表明,某些黄酮类化合物(山奈酚-3-芦丁苷、芦丁、金丝桃苷、表儿茶素白藜芦醇、槲皮素、大黄素、大黄素-8- β -d -葡萄糖和聚datatin)、单宁(没食子酸、单宁酸)、生物碱(己烯酸、同质戊二醇、肉豆素)、脂肪酸(甲基十二烷酸、十二烷酸、三烯酸、12-甲基甲基酯、正十六烷酸)、萜类(-asarone、Acoric acid、穿心莲内酯、石竹烯、环dodocane)和许多其他可能是主要的抗病毒因子。该研究将有助于更好地了解药用植物的抗登革热活性,最终揭示登革热病毒的可靠战斗者。然而,有必要在这方面进行严格的临床研究,以进行适当的验证。
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引用次数: 0
Evaluation of the Anti-ulcer Effect of Extra Virgin Avocado (Persea americana) Oil in Rats 特级初榨鳄梨油对大鼠抗溃疡作用的评价
Pub Date : 2022-01-03 DOI: 10.24018/ejpharma.2022.2.1.15
S. Offor, Adedayo A. Tologbonse, S. Akpan, Victor U. Anah, Enobong Anietie Edward
Peptic ulcer disease is a gastrointestinal disorder of high mortality and morbidity. Therapy of this disease condition with conventional drugs presents therapeutic challenge due to incidents of unwanted side effects, and the high cost of these medications. The use of products from natural sources will provide useful alternatives due to their minimal side effects, being inexpensive, and readily available, especially in resource-challenged nations of the continent of Africa and other developing economies. Oils derived from plants are increasingly being used in management of several disease conditions. This study aims at evaluating the antiulcer activity of extra virgin avocado oil in rodents using ethanol-induced, and indomethacin-induced ulcer models. Test group was given extra virgin avocado oil (1ml per 250g weight) for 7 days before induction of ulcer. Positive controls received omeprazole 30 mg/kg, while negative control animals were given distilled water (10ml/kg) for 7 days respectively, before induction of ulcer. The stomachs were excised and their histopathological examinations carried out. Avocado oil significantly reduced the ulcer index in both models when compared to the negative control group, and histopathological findings corroborate that the oil ameliorates ulcerations in both models. The present study has demonstrated that extra virgin avocado oil possesses significant antiulcer activity.
消化性溃疡是一种死亡率和发病率高的胃肠道疾病。由于不良副作用的发生和这些药物的高成本,用传统药物治疗这种疾病提出了治疗挑战。使用来自自然资源的产品将提供有用的替代品,因为它们副作用最小,价格低廉,而且容易获得,特别是在非洲大陆资源匮乏的国家和其他发展中经济体。从植物中提取的油越来越多地用于几种疾病的管理。本研究旨在通过乙醇诱导和吲哚美辛诱导的溃疡模型来评估特级初榨鳄梨油对啮齿动物的抗溃疡活性。试验组在溃疡诱导前7天给予特级初榨鳄梨油(每250g重量1ml)。阳性对照组给予奥美拉唑30 mg/kg,阴性对照组分别给予蒸馏水10ml/kg,连续7天诱导溃疡。切除胃并进行组织病理学检查。与阴性对照组相比,牛油果油显著降低了两种模型的溃疡指数,组织病理学结果证实了牛油果油改善了两种模型的溃疡。目前的研究表明,特级初榨鳄梨油具有显著的抗溃疡活性。
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引用次数: 1
Assessment of Anti-oxidant Activity of Aerial Parts of Mangrove Plant, Derris trifoliata ( Leguminosae) 红树植物三叶草(Derris trifoliata,豆科)地上部分抗氧化活性评价
Pub Date : 2021-09-27 DOI: 10.24018/ejpharma.2021.1.1.4
Arif Hossin, B. Chakma, M. Raju
The current study was conducted to verify the traditional medicinal use and to carry out the in-vitro antioxidant activity of various solvent extracts of Derris trifoliata (aerial part). The percentage yield of ethanol, ethyl acetate and n-hexane extracts were found 2.5% w/w. Freshly prepared extracts were subjected to preliminary phytochemical screening. All extracts revealed the presence of several important phytochemicals which might be responsible for its medicinal properties. In vitro Electron transfer (ET) reaction-based assays of ethanol, ethyl acetate and n-hexane extracts have been investigated using various model systems viz., DPPH, total phenolic, tannin and flavonoid content, ferric ion reducing antioxidant power (FRAP) and reducing power assay. Hydrogen atom transfer (HAT) reaction-based assays have been conducted using Nitric Oxide (NO) scavenging and hydrogen peroxide scavenging activity assay methods. Ethanol extract was found to possess highest DPPH (IC50=16.824 µg/ml), total phenolic content (44.51 GAE/g of dried plant extract), reducing power assay (0.387±0.0006), FRAF assay (IC50=133.51 µg/ml), hydrogen peroxide scavenging (IC50=144.888 µg/ml) and nitric oxide scavenging activities (IC50=152.655 µg/ml). Whereas ethyl acetate extract was found to possess the highest total tannin content (42.56 GAE/g of dried plant extract) and total flavonoid content (78.08 QE/g of dried plant extract). In vitro antioxidant study was also performed in terms of chelation power on ferrous ions. The highest chelation power was found for ethyl acetate extract (IC50=62.489 µg/ml). The above study suggests that Derris trifoliata may be a vital source of nutraceuticals.
本研究旨在验证三叶霉(地皮部分)的传统药用价值,并对其各种溶剂提取物进行体外抗氧化活性研究。乙醇、乙酸乙酯和正己烷提取物的产率为2.5% w/w。新鲜制备的提取物进行了初步的植物化学筛选。所有提取物都显示出几种重要的植物化学物质的存在,这些化学物质可能是其药用特性的原因。利用DPPH、总酚、单宁和类黄酮含量、铁离子还原抗氧化能力(FRAP)和还原能力测定等多种模型体系,研究了乙醇、乙酸乙酯和正己烷提取物的体外电子转移(ET)反应。基于氢原子转移(HAT)反应的测定采用了一氧化氮(NO)清除和过氧化氢清除活性测定方法。乙醇提取物具有最高的DPPH (IC50=16.824µg/ml)、总酚含量(44.51 GAE/g)、还原力(0.387±0.0006)、frf (IC50=133.51µg/ml)、过氧化氢清除能力(IC50=144.888µg/ml)和一氧化氮清除能力(IC50=152.655µg/ml)。乙酸乙酯提取物的总单宁含量最高(42.56 GAE/g),总黄酮含量最高(78.08 QE/g)。体外抗氧化研究了其对亚铁离子的螯合能力。乙酸乙酯提取物的螯合能力最高(IC50=62.489µg/ml)。上述研究表明,三连木可能是营养保健品的重要来源。
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引用次数: 0
Inaugural Issue Editorial Note 创刊号编辑说明
Pub Date : 2019-03-13 DOI: 10.34154/2019-EJPR.01(01).PP-01-01/EURAASS
N. Anton
Welcome to the Inaugural Issue of European Journal of Pharmaceutical Research, launched in March 2019!
欢迎来到2019年3月推出的《欧洲药物研究杂志》创刊号!
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引用次数: 0
Spontaneous nano-emulsification with tailor-made amphiphilic polymers and related monomers 与定制的两亲性聚合物和相关单体自发纳米乳化
Pub Date : 2019-03-13 DOI: 10.34154/2019-EJPR.01(01).PP-27-36/EURAASS
A. Rehman, Mayeul Collot, A. Klymchenko, S. Akram, B. Mustafa, T. Vandamme, N. Anton
In general, nano-emulsions are submicron droplets composed of liquid oil phase dispersed in liquid aqueous bulk phase. They are stable and very powerful systems when it regards the encapsulation of lipophilic compounds and their dispersion in aqueous medium. On the other hand, when the properties of the nano-emulsions aim to be modified, e.g. for changing their surface properties, decorating the droplets with targeting ligands, or modifying the surface charge, the dynamic liquid / liquid interfaces make it relatively challenging. In this study, we have explored the development of nano-emulsions which were not anymore stabilized with a classical low-molecular weight surfactant, but instead, with an amphiphilic polymer based on poly(maleic anhydride-alt-1-octadecene) (PMAO) and Jeffamine®, a hydrophilic amino-terminated PPG/PEG copolymer. Using a polymer as stabilizer is a potential solution for the nano-emulsion functionalization, ensuring the droplet stabilization as well as being a platform for the droplet decoration with ligands (for instance after addition of function groups in the terminations of the chains). The main idea of the present work was to understand if the spontaneous emulsification –commonly performed with nonionic surfactants– can be transposed with amphiphilic polymers, and a secondary objective was to identify the main parameters impacting on the process. PMAO was modified with two different Jeffamine®, additionally different oils and different formulation conditions were evaluated. As a control, the parent monomer, octadecyl succinic anhydride (OSA) was also modified and studied in the similar way as that of polymer. The generated nano-emulsions were mainly studied by dynamic light scattering and electron microscopy, that allows discriminating the crucial parameters in the spontaneous process, originally conducted with polymers as only stabilizer.
一般来说,纳米乳液是由分散在液水体相中的液油相组成的亚微米液滴。当涉及到亲脂化合物的包封和它们在水介质中的分散时,它们是稳定和非常强大的系统。另一方面,当纳米乳液的性质被修改时,例如改变其表面性质,用靶向配体修饰液滴,或修改表面电荷,动态液/液界面使其相对具有挑战性。在这项研究中,我们探索了纳米乳液的开发,不再使用传统的低分子量表面活性剂,而是使用基于聚马来酸酐-1-十八烯(PMAO)和杰弗明(一种亲水的氨基端PPG/PEG共聚物)的两亲性聚合物。使用聚合物作为稳定剂是纳米乳液功能化的潜在解决方案,既保证了液滴的稳定,又为液滴的配体修饰提供了平台(例如在链的末端添加官能团后)。本工作的主要思想是了解自发乳化-通常用非离子表面活性剂进行-是否可以用两亲性聚合物转位,第二个目标是确定影响该过程的主要参数。用两种不同的Jeffamine®对PMAO进行改性,并对不同的油脂和不同的配方条件进行了评价。作为对照,对母单体十八烷基丁二酸酐(OSA)也进行了类似于聚合物的修饰和研究。所生成的纳米乳液主要通过动态光散射和电子显微镜进行研究,可以区分自发过程中的关键参数,最初仅以聚合物作为稳定剂进行。
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引用次数: 5
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European Journal of Pharmaceutical Research
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