scholarly journals Antimicrobial and antioxidant therapy with bioactive plant molecules on Fe3O4 phytohybrid nanoplatforms

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Janesline Fernandes ◽  
Teotone Vaz ◽  
Tushar S. Anvekar
Keyword(s):  
Essential Oils ◽  
Entrapment Efficiency ◽  
Antioxidant Therapy ◽  
Biomedical Sciences ◽  
Drug Molecules ◽  
Antimicrobial Studies ◽  
Transmission Electron ◽  
Developed Surface ◽  
Secondary Layer ◽  
Reduced Toxicity

Abstract Background Nanobiomedicines have gained increasing attention for their potential to improve efficacy and are emerging as a promising therapeutic paradigm. Magnetic nanoconjugates loaded with bioactive drugs have the advantage of sustained circulation in the bloodstream and significantly reduced toxicity of therapeutic agents in a precise manner. The well-developed surface chemistry of Fe3O4 has led to the development better tools, promoting them as nanoplatforms with potential technological applications in biomedical sciences. Results Fe3O4 phytohybrids with Laxmitaru extract as the primary coating and loaded with Eugenol and Ylang-Ylang essential oils were successfully synthesized. The X-ray diffraction technique has revealed the high purity nanoparticle materials, as no additional impurity peaks were observed. Fourier transform infra-red spectra have confirmed the presence of a primary coating of Laxmitaru extract and a secondary layer of essential oil, as additional peaks and broadening are observed in drug-loaded Fe3O4 nanoparticles. Magnetic susceptibility values indicate the material's superparamagnetic nature. Transmission electron microscopy images have ensured that the particles were spherical, monodispersed, and in the range of 4.30 nm to 13.98 nm. Antimicrobial studies show inhibition zones on the microorganisms S. Aureus and E. Coli with enhanced activity. Drug entrapment efficiency studies revealed the encapsulation of drug molecules onto Fe3O4-Laxmitaru composite. Dynamic light scattering studies confirm the increase in hydrodynamic size, indicating the loading of essential oils and the decrease in polydispersity index ensures monodispersed nanoparticles. The antioxidant study showed the essential oils retained their antioxidant activity even after they were conjugated on Fe3O4-Lax composites. Conclusions Laxmitaru phytochemical-coated Fe3O4 nanoparticles were successfully conjugated with Eugenol and Ylang-Ylang essential oils. Our results provide a model therapeutic approach for the development of new alternative strategies for enhancing antimicrobial and antioxidant therapy, with potential advantages in the field of nanobiomedicine.

IN VITRO EVALUATION OF LECTINIZED CISPLATIN BEARING LIPOSOMES SYSTEM

2020 ◽  
pp. 60-64
Author(s):  
RAHUL TIWARI ◽  
KALIYAPERUMAL VISWANATHAN ◽  
SURESH PRASAD VYAS ◽  
VANDANA SONI
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Wheat Germ Agglutinin ◽  
Wheat Germ ◽  
Entrapment Efficiency ◽  
Cancer Drug ◽  
Drug Molecules ◽  
Transmission Electron ◽  
Surface Modified

Objective: The purpose of this study was to evaluate the extent and mechanism anti-cancer drug-loaded liposomes using wheat germ agglutinin as a guiding molecule. Methods: For the drug-loaded liposome synthesis, the thin film hydration method was used and the drug cisplatin was loaded during the synthesis and followed by the surface modification using wheat germ agglutinin (WGA) lectin. The developed system was confirmed based on transmission electron microscopy (TEM), atomic force microscopy (AFM), particle size (PS) analyzer, polydispersity index and Zeta Potential analyzer. Results: The results showed the surface modified by liposomes had the particle size 200±5 nm. The wheat germ agglutinin coated on the surface to liposome led to a reduction in zeta potential and drug entrapment efficiency while particle size increased. Plain liposomes containing cisplatin had less effect than WGA modified liposome on MCF-7 cell lines. Conclusion: The MTT studies indicated that the drug molecules were initially get delivered to the inside the cell. This formulation offered new simple approach and effectively kill the cells via targeting the nucleus.

Lead Molecule Prediction and Characterization for Designing MERS-CoV 3C-like Protease Inhibitors: An In silico Approach

2018 ◽  
Vol 15 (1) ◽  
pp. 82-88 ◽  
Author(s):  
Md. Mostafijur Rahman ◽  
Md. Bayejid Hosen ◽  
M. Zakir Hossain Howlader ◽  
Yearul Kabir
Keyword(s):  
Binding Energy ◽  
Middle East ◽  
Virtual Screening ◽  
In Silico ◽  
Screening Method ◽  
Middle East Respiratory Syndrome ◽  
Cytochrome P450 Enzymes ◽  
Drug Molecules ◽  
Essential Enzyme ◽  
Reduced Toxicity

Background: 3C-like protease also called the main protease is an essential enzyme for the completion of the life cycle of Middle East Respiratory Syndrome Coronavirus. In our study we predicted compounds which are capable of inhibiting 3C-like protease, and thus inhibit the lifecycle of Middle East Respiratory Syndrome Coronavirus using in silico methods. </P><P> Methods: Lead like compounds and drug molecules which are capable of inhibiting 3C-like protease was identified by structure-based virtual screening and ligand-based virtual screening method. Further, the compounds were validated through absorption, distribution, metabolism and excretion filtering. Results: Based on binding energy, ADME properties, and toxicology analysis, we finally selected 3 compounds from structure-based virtual screening (ZINC ID: 75121653, 41131653, and 67266079) having binding energy -7.12, -7.1 and -7.08 Kcal/mol, respectively and 5 compounds from ligandbased virtual screening (ZINC ID: 05576502, 47654332, 04829153, 86434515 and 25626324) having binding energy -49.8, -54.9, -65.6, -61.1 and -66.7 Kcal/mol respectively. All these compounds have good ADME profile and reduced toxicity. Among eight compounds, one is soluble in water and remaining 7 compounds are highly soluble in water. All compounds have bioavailability 0.55 on the scale of 0 to 1. Among the 5 compounds from structure-based virtual screening, 2 compounds showed leadlikeness. All the compounds showed no inhibition of cytochrome P450 enzymes, no blood-brain barrier permeability and no toxic structure in medicinal chemistry profile. All the compounds are not a substrate of P-glycoprotein. Our predicted compounds may be capable of inhibiting 3C-like protease but need some further validation in wet lab.

Development of intravaginal rod insert bearing liposomal raloxifene hydrochloride and Leuprolide acetate as a potential carrier for uterine targeting

2021 ◽  
Author(s):  
Arpita Patel ◽  
Rahul Dhande ◽  
Hetal Thakkar
Keyword(s):  
Entrapment Efficiency ◽  
Leuprolide Acetate ◽  
Liposomal Formulation ◽  
Molar Ratio ◽  
White Female ◽  
Transmission Electron ◽  
Freeze Dried ◽  
Intravaginal Administration ◽  
Raloxifene Hydrochloride ◽  
Dual Drug

Abstract Objectives This project aimed at the formulation of dual drug entrapped liposomes held as freeze-dried intravaginal rod insert (IVR), to be administered by vaginal route for uterine targeting. Methods Liposomes were formulated by dehydration–rehydration method using 3 : 1 molar ratio of1,2-distearoyl-sn-glycero-3-phosphocholine : Cholesterol. Characterization was done for vesicle size, zeta potential, entrapment efficiency, surface morphology and % loading. Key findings Spherical and discrete vesicles of size 354 nm were observed in transmission electron microscopy (TEM) image. The entrapment efficiency of 90.91% and 74.3% w/w was obtained for Raloxifene Hydrochloride (RLX) and Leuprolide acetate (LA) respectively. Drug release was sustained for 6 days. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay results showed that dual drug entrapped liposomal formulation show significant cytotoxicity, as also confirmed by higher apoptosis in cell cycle analysis and apoptosis studies (FACS) analysis. Pharmacodynamic studies in New Zealand white female rabbits revealed that intravaginal administration of RLX-LA entrapped liposomal formulation shows considerable fibroid regression. Conclusions Uterine targeting of liposomal RLX-LA suggests its potential to solve the limitations of the presently available therapeutic options.

scholarly journals Preparation, characterization and scale-up of sesamol loaded solid lipid nanoparticles

2012 ◽  
Vol 2 (1) ◽  
pp. 8 ◽  
Author(s):  
Vandita Kakkar ◽  
Indu Pal Kaur
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Scale Up ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Solid Lipid ◽  
Transmission Electron ◽  
The Brain

Sesamol loaded solid lipid nanoparticles (SSLNs) were prepared with the aim of minimizing its distribution to tissues and achieving its targeting to the brain. Three scale-up batches (100x1 L) of S-SLNs were prepared using a microemulsification technique and all parameters were statistically compared with the small batch (1x;10 mL). S-SLNs with a particle size of less than 106 nm with a spherical shape (transmission electron microscopy) were successfully prepared with a total drug content and entrapment efficiency of 94.26±2.71% and 72.57±5.20%, respectively. Differential scanning calorimetry and infrared spectroscopy confirmed the formation of lipidic nanoparticles while powder X-ray diffraction revealed their amorphous profile. S-SLNs were found to be stable for three months at 5±3°C in accordance with International Conference on Harmonisation guidelines. The SLN preparation process was successfully scaled-up to a 100x batch on a laboratory scale. The procedure was easy to perform and allowed reproducible SLN dispersions to be obtained.

CURRENTLY USED ANTI-TUBERCULAR AGENTS, THEIR ANALOGUES AND RECENTLY DEVELOPED DRUGS

INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (07) ◽  
pp. 5-19
Author(s):  
A Mohammad ◽  
Keyword(s):  
Antimicrobial Activity ◽  
Side Effects ◽  
Multidrug Resistant ◽  
Drug Resistant ◽  
Duration Of Treatment ◽  
Duration Of Therapy ◽  
Drug Molecules ◽  
Prolonged Duration ◽  
Resistant Strains ◽  
Reduced Toxicity

Tuberculosis (TB) is one of most prevailing diseases, responsible for the morbidity and mortality of a large number of populations worldwide. Traditionally, it has relied on a limited number of drugs such as isoniazid, rifampicin, ethambutol, streptomycin, ethionamide and pyrazinamide. However, many of these drugs have different disadvantages such as prolonged duration of treatment, host toxicity and ineffectiveness against resistant strains. This has motivated the search of newer drug molecules, capable of rapid mycobactericidal action with shortened duration of therapy, reduced toxicity and enhanced activity against multidrug resistant strains. These observations have been guiding for the currently used and newly developed anti-tubercular agents that possess potent antimicrobial activity and their side effects, activity against multi drug resistant Mycobacterium, and also in patients co-infected with HIV/AIDS.

scholarly journals Prodrugs of NSAIDs: A Review

2017 ◽  
Vol 11 (1) ◽  
pp. 146-195 ◽  
Author(s):  
Kamal Shah ◽  
Jeetendra K. Gupta ◽  
Nagendra S. Chauhan ◽  
Neeraj Upmanyu ◽  
Sushant K. Shrivastava ◽  
...  
Keyword(s):  
Active Drug ◽  
Pharmacological Action ◽  
Patient Acceptance ◽  
Synergistic Activity ◽  
Bioavailability Enhancement ◽  
Drug Molecules ◽  
Presystemic Metabolism ◽  
Pass Through ◽  
Reduced Toxicity ◽  
Mutual Prodrug

Intoroduction:Prodrug approach deals with chemical biotransformation or enzymatic conversion or involves inactive or less active bio-reversible derivatives of active drug molecules. They have to pass through enzymatic or chemical biotransformation before eliciting their pharmacological action.Methods & Materials:The two different pharmacophores combine to give synergistic activity or may help in targeting the active drug to its target. Prodrug super seeds the problems of prodrug designing, for example solubility enhancement, bioavailability enhancement, chemical stability improvement, presystemic metabolism, site specific delivery, toxicity masking, improving patient acceptance, or eradicating undesirable adverse effects.Results:As an outcome the search for a prodrug or mutual prodrug with reduced toxicity has continued during recent years. This present review emphasizes the common help to revamp physiochemical, pharmaceutical and therapeutic effectiveness of drugs.Conclusion:This gives the researcher a common platform where they can find prodrugs of commonly used NSAIDs to overcome the gastrointestinal toxicity (irritation, ulcergenocity and bleeding).

scholarly journals Development of NIPAAm-PEG acrylate polymeric nanoparticles for co-delivery of paclitaxel with ellagic acid for the treatment of breast cancer

2019 ◽  
Vol 39 (3) ◽  
pp. 271-278 ◽  
Author(s):  
Suruchi Suri ◽  
Mohd. Aamir Mirza ◽  
Md. Khalid Anwer ◽  
Abdullah S. Alshetaili ◽  
Saad M. Alshahrani ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Particle Size ◽  
Ellagic Acid ◽  
Oral Delivery ◽  
Polymeric Nanoparticles ◽  
Entrapment Efficiency ◽  
Shell Nanoparticles ◽  
Transmission Electron ◽  
Core Shell Nanoparticles

Abstract The aim of the current study was to develop a dual-loaded core shell nanoparticles encapsulating paclitaxel (PTX) and ellagic acid (EA) by membrane dialysis method. Based on particle size, polydispersity index (PDI), and entrapment efficiency, the dual drug-loaded nanoparticles (F2) was optimized. The optimized nanoparticles (F2) showed a particle size of 140±2 nm and a PDI of 0.23±3. The size and the morphology were confirmed by transmission electron microscopy (TEM) and found agreement with the results of dynamic light scattering. The entrapment efficiencies of total drug (PTX and EA), PTX, and EA in the nanoparticles (F2) were measured as 80%, 62.3%, and 37.7%, respectively. The in vitro release profile showed a controlled release pattern for 48 h. A higher cytotoxicity was observed with nanoparticles (F2) in comparison to free PTX. The results revealed that co-delivery of PTX and EA could be used for its oral delivery for the effective treatment of breast cancer.

The Ultrastructure of Brachiopod Shells - A Mechanically Optimized Material with Hierarchical Architecture

2005 ◽  
Vol 898 ◽  
Author(s):  
Erika Griesshaber ◽  
Klemens Kelm ◽  
Angelika Sehrbrock ◽  
Reinhart Job ◽  
Wolfgang W. Schmahl ◽  
...  
Keyword(s):  
Electron Microscopy ◽  
Distribution Pattern ◽  
Vickers Microhardness ◽  
Hierarchical Architecture ◽  
Low Magnesium ◽  
Primary Layer ◽  
Transmission Electron ◽  
Secondary Layer ◽  
Magnesium Calcite ◽  
Oceanographic Conditions

AbstractBrachiopod shells consist of low-magnesium calcite and belong to one of the most intriguing species for studies of marine paleoenvironments, variations in oceanographic conditions and ocean chemistry [6, 7, 11 – 13]. We have investigated the ultrastructure together with nano- and microhardness properties of modern brachiopod shells with transmission electron microscopy (TEM), scanning electron microscopy (SEM), nanoindentation and Vickers microhardness analyses. Brachiopod shells are structured into several layers, a thin, outer, hard, protective primary layer composed of randomly oriented nanocrystalline calcite, which is followed inward towards the soft tissue of the animal by a much softer shell segment (secondary layer) built of long calcite fibres, stacked parallely into blocks. The hardness distribution pattern within the shells is non-uniform and varies on scales as small as a few tens of microns. Our results show that the hardness of this biomaterial is controlled by two predominant features: (1.) The morphological orientation of the calcite fibres (not by the crystallographic orientation of the fibres), and (2.) the amount and distribution pattern of organic material between and within the calcite crystals.

scholarly journals Ufasomes Mediated Cutaneous Delivery of Dexamethasone: Formulation and Evaluation of Anti-Inflammatory Activity by Carrageenin-Induced Rat Paw Edema Model

2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Rajkamal Mittal ◽  
Arvind Sharma ◽  
Sandeep Arora
Keyword(s):  
Oleic Acid ◽  
Entrapment Efficiency ◽  
Inflammatory Activity ◽  
Molar Ratio ◽  
Paw Edema ◽  
Rat Paw Edema ◽  
Transmission Electron ◽  
Edema Model ◽  
Anti Inflammatory ◽  
Rat Paw

The purpose of study is to formulate and evaluate ufasomal gel of dexamethasone. Ufasomal suspension was made by sonication method using different concentrations of Span 80, Span 20 and cholesterol along with 25 mg of drug. Ufasomal gel was formulated by hydration method using carbopol 940. Ufasomal vesicles appeared as spherical and multilamellar under Transmission Electron Microscope. Ufasomal formulation prepared with drug to oleic acid molar ratio 8:2 (UF-2) produced greater number of vesicles and greater entrapment efficiency. UF-2 was optimized for further evaluation. The transdermal permeation and skin partitioning of from optimized formulation was significantly higher () as compared to plain drug and plain gel formulation which is due to presence of surfactant acting as permeation enhancer. Permeation of optimized formulation was found to be about 4.7 times higher than plain drug gel. Anti-inflammatory activity evaluated by inhibition Carrageenan induced rat paw edema model. Significant reduction of edema () was observed in comparison to the commercial product. Hence oleic acid based vesicles can be used as alternate carrier for topical delivery.

Chemical and Antimicrobial Studies ofJuniperus SabinaL. andJuniperus foetidissimaWilld. Essential Oils

2010 ◽  
Vol 13 (1) ◽  
pp. 25-36 ◽  
Author(s):  
J. Asili ◽  
S.A. Emami ◽  
M. Rahimizadeh ◽  
B.S. Fazly-Bazzaz ◽  
M.K. Hassanzadeh
Keyword(s):  
Essential Oils ◽  
Antimicrobial Studies
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