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Development and Ex vivo evaluation of Rasagiline Mesylate mucoadhesive microemulsion for intranasal delivery using Box-Behnken design Box-Behnken设计甲磺酸雷沙吉兰黏附微乳鼻内给药的研制及体外评价
Pub Date : 2019-03-04 DOI: 10.21746/APS.2018.8.3.4
Krishnaveni Janapareddi, A. Kandhula
Rasagiline mesylate (RM), an irreversible, selective inhibitor of MAO-B enzyme, is used in the treatment of Parkinson’s disease as oral tablets. It has low oral bioavailability (36%) due to hepatic first pass metabolism. Oral route of administration is associated with nausea and vomiting. Hence present research work was aimed to develop intranasal RM- loaded mucoadhesive microemulsions for brain targeting via olfactory pathway. The microemulsions were developed using Box Behnken design and evaluated for globule size, PDI, Zeta potential, pH, viscosity and ex vivo permeation on excised porcine nasal mucosa. Based on drug solubility, Capmul MCM, Tween 20 and Transcutol P were selected as oil, surfactant and cosurfactant respectively. Microemulsions were prepared by water titration method. Pseudoternary phase diagrams were constructed and the levels of surfactants, oil were selected. The influence of independent variables such as oil, Smix and water on responses size, zeta potential and flux were studied with the help of polynomial equations, contour plots and 3D response surface plots generated by design expert software. Optimized microemulsion formulation (ME18) was composed of oil (Capmul MCM), Smix (Tween 20: Transcutol P; 1:1), water and drug in the ratio 5:42:65:5.The globule size, zeta potential and flux of the optimized microemulsion was 150 nm, -29.6 mV and 291.7 μg/cm2/h respectively. Mucoadhesive agent (Chitosan) was added at 0.5% concentration to optimized microemulsion formulation (MME18). The size, zeta potential and flux of the MME18 was 176.4 nm, 12.1 mV and 323.1 μg/cm2/h respectively. The flux of ME18 and MME 18 was significantly higher than drug solution. The enhancement ratio of MME 18 was 4.2 times to that of drug solution, indicating potential advantage of microemulsion formulation.
由于肝脏首过代谢,口服生物利用度较低(36%)。口服给药可引起恶心和呕吐。因此,本研究旨在开发经鼻经嗅觉途径靶向脑的含RM的黏附微乳。采用Box Behnken设计研制微乳,并对微乳的粒径、PDI、Zeta电位、pH值、黏度和体外对猪鼻黏膜的渗透性进行评价。根据药物溶解度,选择Capmul MCM、Tween 20和Transcutol P分别作为油、表面活性剂和助表面活性剂。采用水滴定法制备微乳。建立了伪三元相图,选择了表面活性剂、油的含量。利用多项式方程、等高线图和设计专家软件生成的三维响应面图,研究了油、Smix和水等自变量对响应尺寸、zeta电位和通量的影响。优化后的微乳液配方(ME18)由油(Capmul MCM)、Smix (Tween 20: Transcutol P;1:1),水和药物的比例为5:42:65:5。优化后的微乳液粒径为150 nm, zeta电位为-29.6 mV,通量为291.7 μg/cm2/h。优化后的微乳液配方(MME18)中加入0.5%浓度的黏合剂(壳聚糖)。MME18的粒径为176.4 nm, zeta电位为12.1 mV,通量为323.1 μg/cm2/h。ME18和mme18的通量显著高于药物溶液。mme18对药物溶液的增强率为4.2倍,说明微乳制剂具有潜在的优势。
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引用次数: 2
Bioactive potential of Pseudomonas alcaliphila isolated from a marine sponge against human pathogens 从海绵中分离的嗜酸假单胞菌对人类病原体的生物活性潜力
Pub Date : 2019-03-03 DOI: 10.21746/IJBPR.2019.8.3.2
K. Sathiyamurthy, H Bavithra
Metabolite extraction is considered as one of the important steps in metabolomics, the marine metabolite are the new source of the most antimicrobial agents used in both pharmacological and biological applications. In the present study, sponge associated bacterial metabolites was investigated. A total of 20 bacterial strains were isolated from the sponge Haliclona sp., All the strains were screened primarily with cross streaking method against human bacterial pathogens. The potent isolate was chosen based on the good inhibitory activity and metabolite extraction was achieved using chloroform: methanol mixture. The metabolites were then checked for their antimicrobial activity by disk diffusion and also minimum inhibitory concentration was determined. Out of 20 bacterial strains, only one strain selected based on the good inhibitory activity against pathogens and the strain was identified as Pseudomonas alcaliphila based on the biochemical and16S rRNA sequencing. The results revealed that the metabolites exhibited high activity and it was found that Klebsiella pneumoniae was inhibited high with the diameter of 22 mm followed by Salmonella Typhi (15 mm), E.coli (12 mm), and Bacillus subtilis (15 mm). The MIC was observed at 31.25 µg/ml against all pathogens. Results of TLC exhibited the Rf value at 0.86 and the FTIR results revealed the presence of C=o, amide bond, amino acids and methoxy groups. In GC-MS results showed that the metabolites mostly contain fatty acids and alkenes compounds. Thus, this marine active compound was considered as a novel compound for biological applications and may be a potential drug for therapeutic use.
代谢物的提取是代谢组学研究的重要步骤之一,海洋代谢物的提取是大多数抗菌药物的新来源,在药理学和生物学上都有广泛的应用。在本研究中,研究了海绵相关的细菌代谢物。从海绵菌中分离到20株细菌,采用交叉条纹法对所有菌株进行初步筛选。筛选出抑菌活性较好的有效分离物,并用氯仿-甲醇混合萃取代谢物。然后用圆盘扩散法检测代谢物的抑菌活性,并确定最低抑菌浓度。在20株菌株中,根据对病原菌的良好抑制活性筛选出1株菌株,经生化和16s rRNA测序鉴定为假单胞菌alcaliphila。结果表明,代谢产物表现出较高的活性,其中肺炎克雷伯菌(22 mm)受抑制程度最高,其次是伤寒沙门菌(15 mm)、大肠杆菌(12 mm)和枯草芽孢杆菌(15 mm)。对所有病原菌的MIC均为31.25µg/ml。薄层色谱结果显示其Rf值为0.86,FTIR结果显示存在C= 0、酰胺键、氨基酸和甲氧基。气相色谱-质谱分析结果表明,代谢产物主要含有脂肪酸和烯烃类化合物。因此,这种海洋活性化合物被认为是一种具有生物应用价值的新型化合物,可能是一种潜在的治疗药物。
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引用次数: 1
Effect of vagbhattokta tambula sevana as per ayurveda on mukha roga 根据阿育吠陀,vagbhattokta tambula sevana对mukha roga的影响
Pub Date : 2019-03-03 DOI: 10.21746/IJBPR.2019.8.3.1
N. Rathore, S. Paul, A. Jain
The diseases of oral cavity termed as Mukharoga in Ayurveda which involve various pathological conditions such as; Danta Gata Roga and Austha Gata Roga etc. Ayurveda described that Mukharogas may occur at different site of oral cavity and Acharya Charaka has mentioned 64 Mukha rogas in Swayathu Chikitsa Adhyaya depended on Doshik predominance. Vatika Mukha Roga, Paittik Mukha Roga, Kaphaja Mukha Roga and Sannipatika Mukha Roga are some disease of oral cavity emphasized in Ayurveda classic. Vagbhattokta Tambula Sevana is an Upkrama of Dinacharya practices since long in India and it alter pathological manifestation of Mukha rogas. Considering this fact present article described effect of Vagbhattokta Tambula Sevana as an Upkrama of Dinacharya.
在阿育吠陀中被称为Mukharoga的口腔疾病涉及各种病理状况,例如;Danta Gata Roga和Austha Gata Roga等。阿育吠陀描述了Mukharogas可能发生在口腔的不同部位,Acharya Charaka提到了Swayathu Chikitsa Adhyaya的64个Mukharogas依赖于Doshik优势。贪食症、贪食症、贪食症和散食症是阿育吠陀经典中强调的一些口腔疾病。Vagbhattokta Tambula Sevana是印度长期以来Dinacharya实践的Upkrama,它改变了Mukha rogas的病理表现。考虑到这一事实,本文描述了Vagbhattokta Tambula Sevana作为Dinacharya的Upkrama的作用。
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引用次数: 0
Preparation and characterizations of Graphene oxide and Graphene NPs 氧化石墨烯和石墨烯纳米粒子的制备与表征
Pub Date : 2019-02-03 DOI: 10.21746/IJBPR.2019.8.2.2
G Prabhavathi, A. Saleem, A. Ayeshamariam, M Karunanithy, M. Jayachandran
An eco-friendly and inexpensive process of reduction of Graphene oxide using extract of Amla juices is here in reported. The objective is to reduce Graphene oxide to Graphene nanoparticles. The crystallite size of nanoparticles Graphene was confirmed by XRD analysis. FTIR spectral analysis revealed the reduction of Graphene oxide using extract of Amla juices. The morphology of the synthesized Graphene was examined by TEM analysis and SAED pattern. From Graphene oxide which was prepared by Hummer method is reduced to Graphene by using Amla juices as reducing agent. To synthesize Graphene nanoparticles using a cost effective green method and to analyze how Graphene improves a device with respect to cost, production and efficiency. The toxicity of the Graphene nanoparticles will be reduced through the green method.
本文报道了一种利用Amla果汁提取物还原氧化石墨烯的环保且廉价的工艺。目标是将氧化石墨烯还原为纳米石墨烯。通过XRD分析证实了纳米石墨烯的晶粒尺寸。FTIR光谱分析显示,使用Amla果汁的提取物可以还原氧化石墨烯。通过TEM分析和SAED图对合成石墨烯的形貌进行了表征。以Amla果汁为还原剂,将Hummer法制备的氧化石墨烯还原为石墨烯。使用具有成本效益的绿色方法合成石墨烯纳米颗粒,并分析石墨烯如何在成本,生产和效率方面改善设备。石墨烯纳米颗粒的毒性将通过绿色方法降低。
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引用次数: 3
Clinical efficacy of Ashwattha Choorna Lepa in the management of Mukhapaka 枳实治疗木卡帕卡的临床疗效
Pub Date : 2019-02-03 DOI: 10.21746/IJBPR.2019.8.2.1
U. Bhadoriya, Krishan Kumar, A. Jain, S. Paul
Mukha (mouth) is one of the important parts of body and it is exposed to various risk factors due to the bad habits like tobacco chewing and smoking etc. Mukhapaka is pathological condition related to Mukha which occurs due to the simple cut, eating hot food items, unhygienic cleaning, vitamins deficiencies and adverse reaction of antibiotics. Lalasrava, Glani, Dugdha Dwesha, Vyatha and Nasa Shwasa etc. are general symptoms of Mukhapaka. As per ayurveda Mukha Rogas is Pittaja Nanatmaja and Rakta Pradoshaja Vikara and around 20% of population is suffering with this problem. Ayurveda described various treatment modalities for the management of Mukhapaka; Ashwattha Choorna Lepa is one of them, present article established efficacy of Ashwattha Choorna Lepa in Mukhapaka. The study concluded that Lepan-Karma with ayurveda formulation Ashwattha Choorna offers beneficial effects in mouth ulcer.
口部是人体的重要部位之一,由于咀嚼烟草、吸烟等不良习惯,口部暴露在各种危险因素中。Mukhapaka是一种与Mukha有关的病理状况,它是由于简单的伤口、吃热的食物、不卫生的清洁、维生素缺乏和抗生素的不良反应而发生的。Lalasrava、Glani、Dugdha Dwesha、Vyatha和Nasa Shwasa等都是Mukhapaka的一般症状。根据阿育吠陀,Mukha Rogas是Pittaja Nanatmaja和Rakta Pradoshaja Vikara,大约20%的人口患有这个问题。阿育吠陀描述了治疗Mukhapaka的各种治疗方式;Ashwattha Choorna Lepa是其中之一,本文确定了Ashwattha Choorna Lepa在Mukhapaka中的功效。该研究得出结论,乐盘羯磨与阿育吠陀配方Ashwattha Choorna对口腔溃疡有有益的作用。
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引用次数: 1
Morpho-Anatomical studies of Atalantia racemosa Wight ex Hook., an important medicinal plant of Chittoor Dt. of Andhra Pradesh, India. 总状花序Atalantia的形态解剖学研究。是Chittoor属的重要药用植物。位于印度安得拉邦。
Pub Date : 2019-02-03 DOI: 10.21746/IJBPR.2019.8.2.3
V. Padmavathi, K. M. Chetty
Atalantia racemosa Wight ex Hook., belongs to the family Rutaceae and is widely used as ethnomedicine in and around chittoor district of Andhra Pradesh for various ailments. In this paper we attempted for authenticity in morphological identification of Atalantia racemosa with the Morpho-anatomical studies of root, stem and leaf inorder to provide a scientific basis for this important medicinal plant. The observations on taxonomical, macroscopical and microscopical characters confirmed that A. racemosa has apparent anatomical distinctiveness and peculiarities which differentiate with any adulterant taxa.
亚特兰大总状花序怀特前胡克。它属于芸香科,在安得拉邦chittoor地区及其周边地区被广泛用作民族药,用于治疗各种疾病。本文通过对总状花序的根、茎、叶的形态解剖研究,试图对总状花序进行形态鉴定的真实性,以期为这一重要药用植物的鉴定提供科学依据。通过对其分类学、宏观和微观特征的观察,证实了总状花序在解剖学上具有明显的特殊性,与任何掺假类群都有明显的区别。
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引用次数: 2
Isolation and characterization of Arbuscular Mycorrhizal (AM) fungi from the rhizospheric soil of some medicinal plants 药用植物根际土壤丛枝菌根(AM)真菌的分离与鉴定
Pub Date : 2019-01-01 DOI: 10.21746/IJBPR.2018.7.12.2
Dhritiman Chanda, M. Dey
The present investigation was carried out to estimate the colony forming units of indigenous fungi and to study the diversity and Arbuscular mycorrhizal (AM) of some medicinal plants. The study was also aimed to estimate and isolate the Arbuscular mycorrhizal (AM) spore population from the rhizospheric soil of some important medicinal plants from the Botanical garden of College campus. All the selected medicinal plants i.e., Mentha sp. Ocimum sanctum, Bryophyllum sp. Adhatoda vasica, and Andrographis paniculata showed a very good diversity of rhizospheric soil fungi. The highest number of Colony forming unit (c.f.u) was estimated in Mentha sp (162/10-1) followed by Bryophyllum sp. (156/10-1), Andrographis paniculata (91/10-1), Adhatoda vasica (72/10-1) and Ocimum sanctum (68/10-1). Arbuscular mycorrhizal (AM) spore population was also estimated in all the medicinal plants. The higest number of AM spores was estimated in Andrographis paniculata (121/50gm-1) followed by Ocimum sanctum (112/50gm-1), Adhatoda vasica (94/50gm-1), Bryophyllum sp.(89/50gm-1) and Mentha sp (75/ 50gm-1). The rhizospheric soil fungal diversity including mycorrhizal fungi (Glomus sp.) also was found to be beneficial for increasing the photosynthetic activity and uptake of phosphorus in medicinal plants. Thus, the use of AM inoculum can increase the yield of medicinal plants along with their secondary metabolites to utilize on a sustainable basis as a traditional and herbal medicine for the human welfare.
本研究旨在估计本地真菌的菌落形成单位,并研究一些药用植物的丛枝菌根(AM)多样性。本研究还对大学校园内一些重要药用植物根际土壤中的丛枝菌根(AM)孢子数量进行了估算和分离。所选药用植物薄荷(Mentha sp. Ocimum sanctum)、苔藓(Bryophyllum sp. Adhatoda vasica)和穿心莲(Andrographis paniculata)的根际土壤真菌多样性都很好。菌落形成单位(c.f.u)以薄荷(162/10-1)最多,其次为苔藓(156/10-1)、穿心莲(91/10-1)、水仙(72/10-1)和蜜露(68/10-1)。对所有药用植物的丛枝菌根(AM)孢子数量进行了估计。AM孢子数最多的是穿心莲(121/50gm-1),其次是蜜露(112/50gm-1)、灰苔(94/50gm-1)、苔藓(89/50gm-1)和薄荷(75/ 50gm-1)。包括菌根真菌(Glomus sp.)在内的根际土壤真菌多样性也被发现有利于提高药用植物的光合活性和磷的吸收。因此,使用AM接种物可以增加药用植物及其次生代谢物的产量,从而作为传统和草药为人类福利可持续利用。
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引用次数: 1
Prediction of high CPT yielding ecotypes of Nothapodytes nimmoniana (Graham) Mabb. in Western Ghats using Ecological Niche Modeling Nothapodytes nimmonana (Graham) mab .)高产生态型的预测。西高止山脉生态位模型研究
Pub Date : 2018-12-01 DOI: 10.21746/IJBPR.2018.7.12.1
C. Hannah, J. Priya, N Kasthuri Bhai
Camptothecin (CPT) is one of anticancer drug that is widely used for treating various cancers. In India, the drug is primarily sourced from natural habitats of the red listed species Nothapodytes nimmoniana. Ecological niche models are potential tools to define and predict the “ecological niche” of a species that exhibit ecological variations. The predicted ecological niche of a species indicates their survival fitness against Bioclimatic variables. The habitat suitability was predicted using Maxent for different ecotypes of Nothapodytes nimmoniana (Graham.) Mabb. In this study the synonymised populations of N. nimmoniana in the Western Ghats were cogitated as five different ecotypes. The predicted habitat suitability of different ecotypes were evaluated and correlated against CPT content using high performance thin layer chromatography. The study shows a significant positive correlation between the predicted habitat quality and chemical content. The ecotypes growing in sites predicted as highly suitable showed high content of camptothecin compared to those growing in poorly suitable sites. Thereby enabling precise identification of “chemical hot-spots” which will eventually establish a strong foot hold on monoculture of the species, an effort towards conservation.
喜树碱(CPT)是一种广泛用于治疗各种癌症的抗癌药物。在印度,这种药物主要来自红色物种Nothapodytes nimmonana的自然栖息地。生态位模型是定义和预测表现出生态变化的物种的“生态位”的潜在工具。预测的生态位反映了物种对生物气候变量的生存适应性。利用Maxent对不同生态型Nothapodytes nimmonana (Graham.)生境适宜性进行了预测。Mabb。本研究将西高止山脉的N. nimmonana同义种群划分为5种不同的生态型。利用高效薄层色谱法对不同生态型的预测生境适宜性进行了评价,并与CPT含量进行了相关性分析。研究表明,预测生境质量与化学物质含量呈显著正相关。生长在高适宜地点的生态型喜树碱含量高于生长在低适宜地点的生态型。因此,能够精确地识别“化学热点”,最终将建立一个牢固的立足点,对物种的单一栽培,努力保护。
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引用次数: 0
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International Journal of Bio-Pharma Research
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