APPLICATION AND EVALUATION THE EFFECT OF METALIC NANOPARTICLES ON METRONIDAZOLE PERFORMANCE AS A NOVEL TECHNOLOGY

Author(s):  
Mustafa R. Abdulbaqi ◽  
Furqan M. Abdulelah

Objective: The scope of this study is to evaluate the influence of metal nanoparticles application on pharmaceutical properties and biologic activity of antifungal drug, metronidazole (MTZ). Method: Metal nanoparticles used in the study, bismuth sulfide (Bi2S3) used as the nanocarriers for metronidazole (MTZ) and they were synthesized by chemical co-precipitation method. Drug loading on Bi2S3 nanoparticles, lattice property alteration and average particles sizes were evaluated using fourier transform infra-red (FTIR) spectroscopy, atomic force microscopy(AFM), and powder x-ray diffraction(PXRD). The evaluation of the release of MTZ from Bi2S3 nanoparticles was carried out using USP type II rotating puddle apparatus. The antimicrobial activity of MTZ before and after loading was carried out by disc diffusion method against two aerobic gram +ve and one aerobic gram –ve bacteria, in addition to two fungi. Result: This study showed successful loading process as well as particles size reduction of MTZ after loading on Bi2S3 nanoparticles. In vitro release study showed significant* increase in solubility and dissolution of MTZ after loading on Bi2S3 nanoparticles. MTZ showed significant* increase in antibacterial (against gram +ve aerobic staphylococcus aureus and bacillus subtilis) and antifungal (Candida glabrata and Candida tropicalis) activities after loading process. Conclusion: Nanotechnology was applied successfully to improve both, solubility and biologic activity of the model drug used, metronidazole (MTZ).

Author(s):  
Mustafa R. Abdulbaqi

Objective: This study aimed to evaluate the application of nanotechnology in improving the solubility and biologic activity as the antibacterial and antifungal drug of metronidazole (MTZ).Methods: Nanoparticles of bismuth sulfide (Bi2S3) were used as the nanocarriers for metronidazole (MTZ) and they were synthesized by chemical co-precipitation method. Drug loading on Bi2S3 nanoparticles, lattice property alteration and average particles sizes were evaluated using fourier transform infrared (FTIR) spectroscopy, atomic force microscopy (AFM), and powder X-ray diffraction (PXRD). The evaluation of the release of MTZ from Bi2S3 nanoparticles was carried out using USP type II rotating paddle apparatus. The antimicrobial activity of MTZ before and after loading was carried out by disc diffusion method against two aerobic gram+ve and one aerobic gram–ve bacteria, in addition to two fungi.Results: This study showed successful loading process as well as particles size reduction of MTZ after loading on Bi2S3 nanoparticles. In vitro release study showed a significant* increase in solubility and dissolution of MTZ after loading on Bi2S3 nanoparticles. MTZ showed a significant* increase in antibacterial (against gram+ve aerobic staphylococcus aureus and bacillus subtilis) and antifungal (Candida glabrata and Candida tropicalis) activities after loading process.Conclusion: Nanotechnology was applied successfully to improve both, solubility and biologic activity of the model drug used, metronidazole (MTZ). 


Pharmacia ◽  
2020 ◽  
Vol 67 (4) ◽  
pp. 351-356
Author(s):  
Teodora Popova ◽  
Christina Voycheva ◽  
Borislav Tzankov

The present study explored solvent impregnation drug loading process of the poorly soluble non-steroid anti-inflammatory drug indomethacin on MCM-41 type mesoporous silica carrier. Different technological factors that can influence drug-loading process as time of reaction, temperature, use of non-solvent as well as different ratios between drug and MCM-41 were studied. TEM and DLS were used to characterize physicochemical properties of obtained particles. The influence of drug-loading rate on dissolution process were studied using in-vitro release tests. Our results established that changes in explored technological factors could lead to different indomethacin loading. Moreover, the in-vitro release tests proved that drug loading rate had a direct influence on indomethacin release from MCM-41 particles. Our finding suggested that by tuning the main technological factors it would be possible different drug delivery systems with different drug loading rate to be obtained.


2021 ◽  
Vol 22 (21) ◽  
pp. 11353
Author(s):  
Mateusz Pawlaczyk ◽  
Grzegorz Schroeder

The following research aims at the synthesis of magnetite nanoparticles functionalized with triazine-based dendrons and the application of the obtained materials as effective sorptive materials dedicated to acidic bioactive compounds. The adopted synthetic approach involved: (1) the synthesis of nanosized Fe3O4 particles via classic co-precipitation method, (2) the introduction of amine groups on their surface leading to materials’ precursor, and (3) the final synthesis of branched triazine-based dendrons on the support surface by an iterative reaction between cyanuric chloride (CC) and piperazine (p) or diethylenetriamine (DETA) via nucleophilic substitution. The characterized materials were tested for their adsorptive properties towards folic acid, 18β–glycyrrhetinic acid, and vancomycin, showing high adsorption capacities varying in the ranges of 53.33–401.61, 75.82–223.71, and 68.17–132.45 mg g–1, respectively. The formed material–drug complexes were also characterized for the drug-delivery potential, performed as in vitro release studies at pH 2.0 and 7.4, which mimics the physiological conditions. The release profiles showed that the proposed materials are able to deliver up to 95.2% of the drugs within 48 h, which makes them efficient candidates for further biomedical applications.


Micro ◽  
2021 ◽  
Vol 1 (2) ◽  
pp. 250-266
Author(s):  
Eleni Kavetsou ◽  
Ioanna Pitterou ◽  
Annita Katopodi ◽  
Georgia Petridou ◽  
Abdelaziz Adjali ◽  
...  

The aim of the present study was the encapsulation of cedar (Juniperus phoenicea) essential oil (CEO) of Greek origin in β-cyclodextrin (β-CD) through the formation of inclusion complexes (ICs) using the co-precipitation method with different β-CD-to-CEO weight ratios (90:10, 85:15, 80:20, 70:30 (w/w)). The encapsulation of CEO in β-CD through host–guest interactions was confirmed by Nuclear Magnetic Resonance (NMR) spectroscopy, FT-IR spectroscopy, Differential Scanning Calorimetry (DSC) and Thermogravimetric Analysis (TGA). The obtained ICs exhibited nanoscale size (315.9 nm to 769.6 nm),Polydispersity Index from 0.326 to 0.604 and satisfactory stability in suspension (−37.0 mV to −17.0 mV). The process yield was satisfactory, ranging between 65% and 78%, while the inclusion efficiency ranged from 10% to 27%. The in vitro release study conducted for the IC with the optimal characteristics (β-CD:CEO 80:20 (w/w)) exhibited a sustained release profile, with an initial burst effect in the first 5 h. The release profile could be well expressed by the Higuchi equation: Q = 18.893 t1/2 + 9.5919, R2 = 0.8491. The cedar EO presented significant acetylcholinesterase inhibition (IC50 37 μg/mL), which was prolonged by its encapsulation into the β-CD cavity.


2019 ◽  
Vol 16 (2) ◽  
pp. 174-182
Author(s):  
M. Sathish Kumar ◽  
M. Saroja ◽  
M. Venkatachalam

The development of biomedical electronics, biosynthesis of ZnS nanoparticles(NPs) much attracted researchers, due to an eco-friendly and cost-effective routes forsynthesisZnSnanoparticles. In this present work, ZnS NPswas synthesized by using acalypha indica and curcuma longa plant extract using chemical co-precipitation method. The structural, morphological, element composition of biosynthesisZnS NPs was characterized by XRD, SEM and EDAX respectively. Optical and photoluminescence (PL) properties were evaluated by UV Visible spectroscopy. The formation of inhibition zone diameter against human pathogenic microorganisms was screened by in vitro disc diffusion method. From this investigation formation of inhibition zones clearly shows biosynthesizedZnS NPs have high antimicrobial activity against tested organisms, especially curcuma longa plant extract mediated ZnS NPs was formed maximum inhibition against all the tested microorganism.


2019 ◽  
Vol 2019 ◽  
pp. 1-14 ◽  
Author(s):  
Hui Lin ◽  
Guoyong Jia ◽  
Peng Sun ◽  
Liqiao Zhu ◽  
Jinna Chen ◽  
...  

The aim of this study was to explore the synthesis parameters of desogestrel-polylactic acid nanoparticles (DG-PLA-NPs), optimise the preparation technology, and elucidate the in vitro release characteristics. Considering encapsulation efficiency (EE) and drug loading as the main evaluation indexes, DG-PLA-NPs were prepared using the modified emulsion solvent diffusion method and single factor and orthogonal design tests were performed to investigate the influencing factors and optimise the preparation method. Morphology of the nanoparticles was observed using transmission electron microscopy (TEM), average particle diameter and distribution were determined using dynamic laser particle size analysis, and the EE and drug loading were measured using reversed-phase high-performance liquid chromatography. Among the eight factors, the drug-to-material ratio, water-to-organic phase ratio, and polyvinyl alcohol (PVA) concentration significantly affected the NP EE. In the optimised formulation, the PLA/DG ratio, PVA concentration, and oil-to-water phase ratio were 5, 0.5%, and 5, respectively. The DG-PLA-NPs prepared with the optimised formulation were round or spherical with an average diameter of 209 nm, 79.60% EE, and 6.81% drug loading capacity. The polydispersity index was 0.181, and the zeta potential was −27.37 mV. The in vitro releases of both DG and DG-PLA-NPs conformed to the Weibull equation. The DG-PLA-NPs released desogestrel rapidly in the early stages but slowly at later stages, indicating that compared to DG, the DG-PLA-NPs had obvious sustained-release effects. The DG-PLA-NPs prepared by the modified emulsion solvent diffusion method were small, simple to prepare, and had high drug loading with promising application prospects.


Author(s):  
Dilip Kumar Gupta ◽  
B K Razdan ◽  
Meenakshi Bajpai

The present study deals with the formulation and evaluation of mefloquine hydrochloride nanoparticles. Mefloquine is a blood schizonticidal quinoline compound, which is indicated for the treatment of mild-to-moderate acute malarial infections caused by mefloquine-susceptible multi-resistant strains of P. falciparum and P. vivax. The purpose of the present work is to minimize the dosing frequency, taste masking toxicity and to improve the therapeutic efficacy by formulating mefloquine HCl nanoparticles. Mefloquine nanoparticles were formulated by emulsion diffusion method using polymer poly(ε-caprolactone) with six different formulations. Nanoparticles were characterized by determining its particle size, polydispersity index, drug entrapment efficiency, drug content, particle morphological character and drug release. The particle size ranged between 100 nm to 240 nm. Drug entrapment efficacy was >95%. The in-vitro release of nanoparticles were carried out which exhibited a sustained release of mefloquine HCl from nanoparticles up to 24 hrs. The results showed that nanoparticles can be a promising drug delivery system for sustained release of mefloquine HCl.


Author(s):  
Prakash Goudanavar ◽  
Ankit Acharya ◽  
Vinay C.H

Administration of an antiviral drug, acyclovir via the oral route leads to low and variable bioavailability (15-30%). Therefore, this research work was aimed to enhance bioavailability of acyclovir by nanocrystallization technique. The drug nanocrystals were prepared by anti-solvent precipitation method in which different stabilizers were used. The formed nanocrystals are subjected to biopharmaceutical characterization including solubility, particle size and in-vitro release. SEM studies showed nano-crystals were crystalline nature with sharp peaks. The formulated drug nanocrystals were found to be in the range of 600-900nm and formulations NC7 and NC8 showed marked improvement in dissolution velocity when compared to pure drug, thus providing greater bioavailability. FT-IR and DSC studies revealed the absence of any chemical interaction between drug and polymers used. 


Author(s):  
V K Verma ◽  
Ram A

 Solid lipid nanoparticles (SLNs) of piroxicam where produced by solvent emulsification diffusion method in a solvent saturated system. The SLNs where composed of tripamitin lipid, polyvinyl alcohol (PVAL) stabilizer, and solvent ethyl acetate. All the formulation were subjected to particle size analysis, zeta potential, drug entrapment efficiency, percent drug loading determination and in-vitro release studies. The SLNs formed were nano-size range with maximum entrapment efficiency. Formulation with 435nm in particle size and 85% drug entrapment was subjected to scanning electron microscopy (SEM) and transmission electron microscopy (TEM) for surface morphology, differential scanning calorimetry (DSC) for thermal analysis and short term stability studies. SEM and TEM confirm that the SLNs are nanometric size and circular in shape. The drug release behavior from SLNs suspension exhibited biphasic pattern with an initial burst and prolong release over 24 h. 


Author(s):  
Nagda C. D. ◽  
Chotai N. P. ◽  
Patel S. B. ◽  
Soni T. J ◽  
Patel U. L

Aceclofenac (ACE) is NSAIDs of a phenyl acetic acid class. It is indicated in arthritis and osteoarthritis, rheumatoid arthritis, ankylosing spondylitis. It has short elimination half life of 4 hours. The objective of the study is to design, characterize and evaluate bioadhesive microspheres of ACE employing carbopol (CP) as bioadhesive polymer. Bioadhesive microspheres of ACE were prepared by solvent evaporation method. The prepared microspheres were free flowing and spherical in shape and characterized for drug loading, mucoadhesion test, infrared spectroscopy (IR), differential scanning colorimetry (DSC) and scanning electron microscopy (SEM). The in-vitro release studies were performed using pH 6.8 phosphate buffer. The drug loaded microspheres in a ratio of 1:5 showed 47% of drug entrapment; percentage mucoadhesion was 81% and 89% release in 10 h. The infrared spectra and DSC showed stable character of aceclofenac in the drug loaded microspheres and revealed the absence of drug-polymer interactions. SEM studies showed that the microspheres are spherical and porous in nature. The in vitro release profiles from microspheres of different polymer-drug ratios followed Higuchi model.


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