Drug Invention Today最新文献_第6页

Compressed glyceryl monostearate based biodegradable implant of Gentamicin using melt granulation technique: In vitro evaluation & biocompatibility in animals 基于熔融造粒技术的压缩单硬脂酸甘油可生物降解庆大霉素植入物:体外评价及动物生物相容性

Drug Invention Today Pub Date : 2013-03-01 DOI: 10.1016/j.dit.2013.03.006

Ashish Y. Pawar , Kiran B. Erande , Deepak D. Sonawane , Vikas R. Asawale , Yogesh S. Harak , Deelip V. Derle

{"title":"Compressed glyceryl monostearate based biodegradable implant of Gentamicin using melt granulation technique: In vitro evaluation & biocompatibility in animals","authors":"Ashish Y. Pawar , Kiran B. Erande , Deepak D. Sonawane , Vikas R. Asawale , Yogesh S. Harak , Deelip V. Derle","doi":"10.1016/j.dit.2013.03.006","DOIUrl":"10.1016/j.dit.2013.03.006","url":null,"abstract":"<div><h3>Objective</h3><p>Osteomyelitis is a multibacterial bone infection which is still remains challenging and difficult to treat, despite of advances in antibiotics and new operative techniques. Present study aims at formulating Gentamicin implants in treatment of Osteomyelitis & other bone infections using glyceryl monostearate (GMS) matrices as a carrier.</p></div><div><h3>Methods</h3><p>Gentamicin implants were prepared by using combination of glyceryl monostearate and poly ethylene glycol as hydrophobic biodegradable sustained release matrices along with different percentage of Sorbitol and Tween80 as erosion enhancers. Several formulations were prepared (K1–K7) by melt granulation followed by compression to form disc shaped implants. The prepared formulations were evaluated for different <em>in vitro</em> parameters & optimized formulation was subjected to <em>in vivo</em> study.</p></div><div><h3>Results & discussion</h3><p>Formulation K4 shows excellent cumulative drug release profile and it does not completely lose its physical shape even after 28 days thus this formulation conclude to be optimum formulation among the all GMS based implant formulations. Also optimized GMS based implant does not show any severe signs of inflammation and other foreign body reactions in laboratory animals, thus it was concluded that GMS based implant have acceptable biological compatibility even after 28 days.</p></div><div><h3>Conclusion</h3><p>Therefore from this study it is proved that, the glyceryl monostearate based implants have potential to retard the drug release for more than five weeks in the treatment of osteomyelitis & bone infections.</p></div>","PeriodicalId":11284,"journal":{"name":"Drug Invention Today","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2013-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.dit.2013.03.006","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74159257","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 1

RETRACTED: Nanosuspension of vasicine from Adhatoda vasica: Isolation and characterization 撤稿:从水蛭中提取水蛭疫苗的纳米悬浮液:分离和表征

Drug Invention Today Pub Date : 2013-03-01 DOI: 10.1016/j.dit.2013.03.005

Jitender Kumar Malik , Akshat Sharma , Sanjiv Singh , Sourabh Jain

引用次数: 9

Fabrication of highly stable sonication assisted curcumin nanocrystals by nanoprecipitation method 用纳米沉淀法制备高稳定超声辅助姜黄素纳米晶体

Drug Invention Today Pub Date : 2013-03-01 DOI: 10.1016/j.dit.2013.02.003

C. Moorthi, K. Kathiresan

{"title":"Fabrication of highly stable sonication assisted curcumin nanocrystals by nanoprecipitation method","authors":"C. Moorthi, K. Kathiresan","doi":"10.1016/j.dit.2013.02.003","DOIUrl":"10.1016/j.dit.2013.02.003","url":null,"abstract":"<div><h3>Objectives</h3><p>The present study was aimed to fabricate highly stable sonication assisted curcumin nanocrystals by nanoprecipitation method to overcome the poor aqueous solubility of curcumin.</p></div><div><h3>Methods</h3><p>Sodium lauryl sulfate coated curcumin nanocrystals and poloxamer 188 coated curcumin nanocrystals were prepared using nanoprecipitation method and characterized for particle size and related parameters.</p></div><div><h3>Results</h3><p>Poloxamer 188 coating has produced a significant size reduction in the distribution width (approximately 250 times in D 90) and in the average particle size (approximately 260 times in volume weight mean) with respect to pure curcumin. Similarly, sodium lauryl sulfate coating has produced a significant size reduction in the distribution width (approximately 1000 times in D 90) and in the average particle size (approximately 750 times in volume weight mean) with respect to pure curcumin. Sodium lauryl sulfate coated curcumin nanocrystals has shown a narrow distribution even after one week than the poloxamer coated curcumin nanocrystals.</p></div><div><h3>Conclusions</h3><p>The study concludes that the anionic nature of sodium lauryl sulfate has provided higher zeta potential and offered high electrostatic force which overcomes the van der Waals force of attraction and gravitational force leading to prevention of nanocrystal aggregation resulting in narrow sized high stable curcumin nanocrystals.</p></div>","PeriodicalId":11284,"journal":{"name":"Drug Invention Today","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2013-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.dit.2013.02.003","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82571366","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 45

Preparation and evaluation of Bacopa–phospholipid complex for antiamnesic activity in rodents 假马齿苋-磷脂复合物的制备及对啮齿动物抗遗忘活性的评价

Drug Invention Today Pub Date : 2013-03-01 DOI: 10.1016/j.dit.2013.02.004

Prasanna Habbu , Smita Madagundi , Ramesh Kulkarni , Sagar Jadav , Rashmi Vanakudri , Venkatrao Kulkarni

{"title":"Preparation and evaluation of Bacopa–phospholipid complex for antiamnesic activity in rodents","authors":"Prasanna Habbu , Smita Madagundi , Ramesh Kulkarni , Sagar Jadav , Rashmi Vanakudri , Venkatrao Kulkarni","doi":"10.1016/j.dit.2013.02.004","DOIUrl":"10.1016/j.dit.2013.02.004","url":null,"abstract":"<div><h3>Objectives</h3><p><em>Bacopa</em>–phospholipid complex (BPC), a novel phytoformulation was prepared, characterized and evaluated for its possible enhancement of antiamnesic activity as compared to bacopa extract (BE) in natural aging induced amnesic mice.</p></div><div><h3>Methods</h3><p>BPC was characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and FTIR. Antiamnesic activity of BPC (40 mg/kg body weight) and BE (40 mg/kg body weight) was evaluated using elevated plus-maze (EPM), Morris water maze (MWM) and Passive shock avoidance (PSA) tests.</p></div><div><h3>Results</h3><p>SEM data showed that BPC has irregular size vesicles consisting of phoaphatidylcholine (PC) and BE was found to be intercalated in the lipid layer. BPC showed two endothermal peaks (80.90 °C and 171 °C) in DSC studies. Aged mice showed poor retention of memory in EPM, MWM and PSA models. Administration of BPC (40 mg/kg; p.o.) and BE (40 mg/kg; p.o.) significantly reversed cognitive deficits in aged mice. However, enhanced antiamnesic activity was observed with BPC as compared to BE in all the memory models tested. This is also supported by enhanced acetyl cholinesterase inhibitory activity of BPC. A higher serum concentration of bacopaside-I (12.21 μg/ml) and bacopaside-II (12.28 μg/ml) was observed for BPC in bioavailability studies as compared to BE. BPC maintained effective concentration of bacopasides for a longer period in rat serum.</p></div><div><h3>Conclusion</h3><p><em>Bacopa</em>–phospholipid complex has shown improved antiamnesic activity as compared to <em>bacopa</em> extract at the dose studied. This might be due to better absorption of bacopasides from the complex.</p></div>","PeriodicalId":11284,"journal":{"name":"Drug Invention Today","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2013-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.dit.2013.02.004","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89525264","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 50

In silico validation of human N-myc downstream-regulated gene 2 protein against Alzheimer's disease using molecular modeling, docking and dynamics studies 基于分子模型、对接和动力学研究的人类N-myc下游调控基因2蛋白抗阿尔茨海默病的计算机验证

Drug Invention Today Pub Date : 2013-03-01 DOI: 10.1016/j.dit.2013.02.002

Aathi Muthusankar, Piramanayagam Shanmughavel

{"title":"In silico validation of human N-myc downstream-regulated gene 2 protein against Alzheimer's disease using molecular modeling, docking and dynamics studies","authors":"Aathi Muthusankar, Piramanayagam Shanmughavel","doi":"10.1016/j.dit.2013.02.002","DOIUrl":"10.1016/j.dit.2013.02.002","url":null,"abstract":"<div><h3>Objectives</h3><p>The human N-myc downstream-regulated gene 2 (hNDRG2) protein is mainly responsible for Alzheimer's disease (AD). It has 371 amino acid residues in their sequence. The 3dimensional (3D) structure of the complete sequence of this protein is still unknown. The present research computationally emphases to predict the 3D structure for the complete sequence of hNDRG2 protein and efficiency of this protein against AD was evaluated with synthetic and natural compounds using docking studies. Molecular dynamics (MD) study was performed to find the stability of the best interacted molecule.</p></div><div><h3>Methods</h3><p>The hNDRG2 protein was modeled using Modeller9v10. The lead compounds were retrieved from PubChem database. Docking studies were performed using AutoDock4.2. MD study was done by Macro model.</p></div><div><h3>Results</h3><p>The modeled hNDRG2 protein was validated using Ramachandran plot and it showed the value of 90.8% in the most favored regions. From the results of docking studies, the interaction of modeled protein with synthetic tacrine showed the binding energy value of −4.44 kcal/mol and the interactions with 15 phytocompounds of <em>Rosmarinus officinalis</em>, a natural compound (+)-borneol showed the best binding energy value of −4.64 kcal/mol. The result of MD study determined that, the complex of modeled protein with (+)-borneol was stable at 2.2 ns.</p></div><div><h3>Conclusions</h3><p>In the above study, when the interaction of phytocompounds compared with synthetic tacrine, the natural compound (+)-borneol have showed good interaction with modeled protein and it is suggested to treat AD for avoiding the side effects of synthetic drugs.</p></div>","PeriodicalId":11284,"journal":{"name":"Drug Invention Today","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2013-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.dit.2013.02.002","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87280997","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 3

Review on Prosopis cineraria: A potential herb of Thar desert 塔里木沙漠潜在草本植物棘豆的研究进展

Drug Invention Today Pub Date : 2013-03-01 DOI: 10.1016/j.dit.2013.03.002

Akash Garg , Sanjeev K. Mittal

引用次数: 36