scholarly journals Nanoformulation Development to Improve the Biopharmaceutical Properties of Fisetin Using Design of Experiment Approach

Molecules ◽  
2021 ◽  
Vol 26 (10) ◽  
pp. 3031
Author(s):  
Wan-Yi Liu ◽  
Chia-Chen Lin ◽  
Yun-Shan Hsieh ◽  
Yu-Tse Wu
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Oral Delivery ◽  
Encapsulation Efficiency ◽  
Average Particle Size ◽  
Amorphous State ◽  
Polydispersity Index ◽  
Morphological Observation ◽  
Average Particle ◽  
Biopharmaceutical Properties

This study aimed to design an effective nanoparticle-based carrier for the oral delivery of fisetin (FST) with improved biopharmaceutical properties. FST-loaded nanoparticles were prepared with polyvinyl alcohol (PVA) and poly(lactic-co-glycolic acid) (PLGA) by the interfacial deposition method. A central composite design of two independent variables, the concentration of PVA and the amount of PLGA, was applied for the optimization of the preparative parameter. The responses, including average particle size, polydispersity index, encapsulation efficiency, and zeta potential, were assessed. The optimized formulation possessed a mean particle size of 187.9 nm, the polydispersity index of 0.121, encapsulation efficiency of 79.3%, and zeta potential of −29.2 mV. The morphological observation demonstrated a globular shape for particles. Differential scanning calorimetry and powder X-ray diffraction studies confirmed that the encapsulated FST was presented as the amorphous state. The dissolution test indicated a 3.06-fold increase for the accumulating concentrations, and the everted gut sac test showed a 4.9-fold gain for permeability at the duodenum region. In conclusion, the optimized FST-loaded nanoparticle formulation in this work can be developed as an efficient oral delivery system of FST to improve its biopharmaceutic properties.

Formulation and Evaluation of Polymeric Nanoparticles of an Antiviral Drug for Gastroretention

2012 ◽  
Vol 4 (4) ◽  
pp. 1557-1562 ◽  
Author(s):  
Ankit Anand Kharia ◽  
A K Singhai ◽  
R Verma
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Average Particle Size ◽  
Chlorinated Solvents ◽  
Entrapment Efficiency ◽  
The Body ◽  
Hydrophilic Polymers ◽  
Polydispersity Index ◽  
Average Particle ◽  
Loading Efficiency

The aim of present study was to formulate and evaluate nanoparticles of acyclovir by using different hydrophilic polymers. Acyclovir was selected as a suitable drug for gastro-retentive nanoparticles due to its short half life, low bioavailability, high frequency of administration, and narrow absorption window in stomach and upper part of GIT. The nano-precipitation method was used to prepare nanoparticles so as to avoid both chlorinated solvents and surfactants to prevent their toxic effect on the body. Nanoparticles of acyclovir were prepared by using hydrophilic polymers such as bovine serum albumin, chitosan, and gelatin. The prepared formulations were then characterized for particle size, polydispersity index, zeta potential, loading efficiency, encapsulation efficiency and drug-excipient compatibility. The prepared nanoparticulate formulations of acyclovir with different polymers in 1:1 ratio have shown particle size in the range of 250.12-743.07 nm, polydispersity index (PDI) in the range of 0.681-1.0, zeta potential in the range of -14.2 to +33.2 mV, loading efficiency in the range of 8.74-17.54%, and entrapment efficiency in the range of 55.7%-74.2%. Nanoparticulate formulation prepared with chitosan in 1:1 ratio showed satisfactory results i.e. average particle size 312.04 nm, polydispersity index 0.681, zeta potential 33.2 mV, loading efficiency 17.54%, and entrapment efficiency 73.4%. FTIR study concluded that no major interaction occurred between the drug and polymers used in the present study.  

scholarly journals Development of a novel intraarticular injection of diclofenac for the treatment of arthritis: a preclinical study in the rabbit model

2021 ◽  
Author(s):  
Xinyuan Wen ◽  
Xiaoqing Huang ◽  
Huosheng Wu
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Average Particle Size ◽  
Rabbit Model ◽  
Intraarticular Injection ◽  
Average Particle ◽  
Prepared Nanoparticles

Purpose: To develop a novel intraarticular injection of diclofenac for the treatment of arthritis. Method: Diclofenac loaded nanoparticles were prepared by a nanoprecipitation technique using Eudragit L 100 as the polymer and polyvinyl alcohol as the surfactant. The nanoparticles were evaluated for particle size, zeta potential, scanning electron microscopy, drug release, encapsulation efficiency, and loading efficiency studies. The optimized nanoparticulate formulation was developed for intra articular injection. Intraarticulate injection was evaluated for pH, appearance, viscosity, osmolarity and syringability studies. The optimized injection formulation was tested in an arthritic model consisting of 25 rabbits. Result: Nanoprecipitation method was found to be suitable for diclofenac nanoparticles. The shape of the prepared nanoparticles was found to be spherical and devoid of any cracks and crevices. The average particle size of a diclofenac nanoparticle was found to range from 87±0.47 to 103±0.26 nm. The zeta potential of the prepared nanoparticles was found to be in the range of 0.598±0.34 to 0.826±0.25 mV. The encapsulation efficiency was found to be between 73.45% to 99.03%, while the drug loading was observed between 10.34 to 35.32%. The percentage drug release at 12 hours was found to range from 73.45% to 99.03%. Conclusion: The developed intraarticular injection was found to be within the physically and chemically accepted limits. Animals treated with the intra articular injection of diclofenac showed a significant reduction in swelling as compares to the other groups.

scholarly journals Nanosized and Enhancement of Solubility Fisetin

2019 ◽  
Vol 7 (2) ◽  
pp. 6-10
Author(s):  
Muhammad Dzakwan ◽  
Eko Pramukantoro Ganet ◽  
Mauludin Rachmat ◽  
Saleh Wikarsa
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Photon Correlation Spectroscopy ◽  
Average Particle Size ◽  
Correlation Spectroscopy ◽  
Polydispersity Index ◽  
Average Particle ◽  
Polysorbate 80 ◽  
Photon Correlation ◽  
The Poor

Fisetin (3,3,4,7-tetrahydroxyflavone) is a natural antioxidant that has shown to posses anticancer, antioxidant and anti-inflammatory properties. However, the poor solubility leads to poor bioavailability and limits its development.The aim of the research is to investigate the effect of fisetin nanosuspension using a nanoprecipitation technique and additional stabilizers polysorbat 80, SLS, PVA and Eudragit on particle size average, polydispersity index and zeta potential.The suspensions of microcrystalline FIS were prepared by a nanoprecipitation technique with different proportion of stabilizers fixed. The nanosuspension produced was then characterized using Photon Correlation Spectroscopy (PCS) in  term of particle size distribution, polydispersity index, zeta potential and morphology nanosuspensiom (TEM). Result showed fisetin nanosuspension were successfully prepared by anti-solvent precipitation with additional stabilizer SLS and polysorbat 80. The nanosuspension containing polysorbat 80 showed smaller average particle size of 225.7 nm ± 1.31, a polydispersity index of 0.272 ±0.02 and zeta potential -39.3 ± 0.26 was obtained. Conclusion, FIS nanosuspension successfully prepared by nanoprecipitation tecnique with the polysorbate 80 as stabilizer and ethanol as solvent were spherical in shape..

scholarly journals Karakterisasi Nanopartikel Ekstrak Bunga Kecombrang dengan Penambahan Poloksamer

2018 ◽  
Vol 1 (3) ◽  
pp. 121-124
Author(s):  
Tresna Lestari ◽  
Tita Nofianti ◽  
Lilis Tuslinah ◽  
Ruswanto Ruswanto ◽  
Firda Adityas
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Average Particle Size ◽  
Particle Morphology ◽  
Entrapment Efficiency ◽  
Polydispersity Index ◽  
Average Particle ◽  
Flower Extract ◽  
Round Form ◽  
Nanoparticle Formulation

Bunga kecombrang diketahui memiliki aktivitas sebagai antioksidan. Teknologi formulasi nanopartikel diharapkan dapat meningkatkan aktivitas biologis dari ekstrak.Penelitian ini dilakukan untuk memperoleh nanopartikel dari ekstrak bunga kecombrang dengan karakteristik yang baik.Pembuatan nanopartikel dilakukan dengan penambahan poloksamer dengan variasi konsentrasi 1, 3 dan 5%. Formulasi selanjutnya dianalisis meliputi ukuran partikel rata-rata, indeks polidispersitas, potensial zeta, efisiensi penjeratan dan morfologi partikel menggunakan SEM.Hasil karakterisasi diperoleh ukuran partikel rata-rata ketiga formula berada dalam rentang 134,7-193,1 nm, indeks polidispersitas <0,5 untuk semua formula, nilai potensial zeta antara -41,0 - (-24,3) mV dan efisiensi penjeratan terhadap senyawa flavonoid 89,93-97,99 %. Berdasarkan hasil SEM nanopartikel diketahui berbentuk bulat dengan permukaan yang halus.Berdasarkan hasil penelitian disimpulkan bahwa nanopartikel ekstrak bunga kecombrang dengan penambahan poloksamer 1, 3 dan 5% memiliki karakteristik yang baik dan memenuhi syarat sebagai sediaan nanopartikel.   Kecombrang flowers are known to have antioxidant activity. Nanoparticle formulation technology is expected to increase the biological activity of the extract. This study was conducted to obtain the nanoparticles from kecombrang flower extract with good characteristics. The preparation of nanoparticles was carried out by adding poloxamer with various concentrations of 1, 3 and 5%.Furthermore, the formula were analyzed, including the average particle size, polydispersity index, zeta potential, entrapment efficiency and particle morphology using SEM. The results of the characterization obtained an average particle size of the three formulas in the range of 134.7-193.1 nm, polydispersity index <0 , 5 for all formulas, zeta potential values ​​in range of -41.0 - (-24.3) mV and entrapment efficiency of flavonoid compounds of 89.93-97.99%The results of SEM examination showed that nanoparticles  was in round form with a smooth surface. Based on the results of the study,  itcan be concluded that kecombrang flower extract nanoparticles with the addition of poloxamer 1, 3 and 5% had good characteristics and met the criteria of  nanoparticle

scholarly journals Sodium Alginate Nanoparticles of Isoniazid: Preparation and Evaluation

2019 ◽  
Vol 11 (06) ◽  
Author(s):  
Sumit Kumar ◽  
Dinesh Chandra Bhatt
Keyword(s):  
Particle Size ◽  
Sodium Alginate ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Average Particle Size ◽  
Average Particle ◽  
In Vitro Drug Release ◽  
Ionotropic Gelation ◽  
Preparation And Evaluation

Fabrication and evaluation of the Isoniazid loaded sodium alginate nanoparticles (NPs) was main objective of current investigation. These NPs were engineered using ionotropic gelation technique. The NPs fabricated, were evaluated for average particle size, encapsulation efficiency, drug loading, and FTIR spectroscopy along with in vitro drug release. The particle size, drug loading and encapsulation efficiency of fabricated nanoparticles were ranging from 230.7 to 532.1 nm, 5.88% to 11.37% and 30.29% to 59.70% respectively. Amongst all batches studied formulation F-8 showed the best sustained release of drug at the end of 24 hours.

scholarly journals Formulation and evaluation of polymeric nanoparticles of an antihypetensive drug for gastroretention

2018 ◽  
Vol 8 (6) ◽  
pp. 82-86 ◽  
Author(s):  
Surendranath Betala ◽  
M Mohan Varma ◽  
K Abbulu
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Chlorinated Solvents ◽  
Entrapment Efficiency ◽  
The Body ◽  
Hydrophilic Polymers ◽  
Polydispersity Index ◽  
Average Particle ◽  
Loading Efficiency ◽  
Gastro Retentive

The aim of present study was to formulate and evaluate nanoparticles of carvedilol by using different hydrophilic polymers. Carvedilol was selected as a suitable drug for gastro- retentive nanoparticles due to its short half life, low bioavailability, high frequency of administration, and narrow absorption window in stomach and upper part of GIT. The nano-precipitation method was used to prepare nanoparticles so as to avoid both chlorinated solvents and surfactants to prevent their toxic effect on the body. Nanoparticles of  carvedilol were prepared by using hydrophilic polymers such as HPMC K100M, chitosan, and gelatin. The prepared formulations were then characterized for particle size, polydispersity index, zeta potential, loading efficiency, encapsulation efficiency and drug-excipient compatibility. The prepared nanoparticulate formulations of carvedilol  with different polymers in 1:1 ratio have shown particle size in the range of 250.12-743.07 nm, polydispersity index (PDI) in the range of 0.681-1.0, zeta potential in the range of -14.2 to +33.2 mV, loading efficiency in the range of 8.74-17.54%, and entrapment efficiency in the range of 55.7%-74.2%. Nanoparticulate formulation prepared with chitosan in 1:1 ratio showed satisfactory results i.e. average particle size 312.04 nm, polydispersity index 0.681, zeta potential 33.2 mV, loading efficiency 17.54%, and entrapment efficiency 73.4%. FTIR study concluded that no major interaction occurred between  the drug and polymers used in the present study. Keywords: Nanoparticles; gastro-retentive; nano-precipitation, polydispersity index, zeta potential; entrapment efficiency.

scholarly journals Chitosan-sodium Alginate Nanoparticle as a Promising Approach for Oral Delivery of Rosuvastatin Calcium: Formulation, Optimization and In vitro Characterization

2020 ◽  
pp. 50-56 ◽  
Author(s):  
Md. Ali Mujtaba ◽  
Nawaf M. Alotaibi
Keyword(s):  
Fourier Transform ◽  
Zeta Potential ◽  
Infrared Spectra ◽  
Therapeutic Efficacy ◽  
Oral Delivery ◽  
Average Particle Size ◽  
Fourier Transform Infrared ◽  
Average Particle ◽  
Fourier Transform Infrared Spectra ◽  
Rosuvastatin Calcium

Rosuvastatin calcium is the most effective antilipidemic drug and is called "super-statin" but it exhibits low aqueous solubility and poor oral bioavailability of about 20%. The present work aimed to develop and optimize chitosan-alginate nanoparticulate formulation of rosuvastatin which can improve its solubility, dissolution and therapeutic efficacy. Chitosan-alginate nanoparticles were prepared by ionotropic pre-gelation of an alginate core followed by chitosan polyelectrolyte complexation and optimization was done in terms of two biopolymers, crosslinker concentrations. The chitosan-alginate nanoparticles were characterized by various techniques such as particle properties such as size; size distribution (polydispersity index); Zeta-potential measurements and Fourier transform infrared spectra respectively. The designed rosuvastatin loaded chitosan-alginate nanoparticle had the average particle size of 349.3 nm with the zeta potential of +29.1 mV, and had high drug loading and entrapment efficiencies. Fourier transform infrared spectra showed no chemical interaction between the rosuvastatin and chitosan-alginate nanoparticle upon the encapsulation of rosuvastatin within the nanoparticles. Nanoparticles revealed a fast release during the first two hours followed by a more gradual drug release during a 24 h period. Hence, our studies demonstrated that the new chitosan-alginate nanoparticle system of rosuvastatin is a promising strategy for improving solubility and in turn, the therapeutic efficacy of rosuvastatin. Therefore, the rosuvastatin-loaded chitosan-alginate nanoparticles are a promising approach for the oral delivery of rosuvastatin.

Preparation and characterization of natural quercetin-based Mongolia Medicine SenDeng-4 nanoemulsion (N-QUE-NE) and its antibacterial activity..

2020 ◽  
Vol 18 ◽  
Author(s):  
Yanfang Zhang ◽  
Rina Du ◽  
Pengwei Zhao ◽  
Sha Lu ◽  
Rina Wu ◽  
...  
Keyword(s):  
Particle Size ◽  
Antibacterial Activity ◽  
Zeta Potential ◽  
High Speed ◽  
Antibacterial Effect ◽  
Average Particle Size ◽  
Antagonistic Effect ◽  
Dilution Method ◽  
Average Particle

Background: Quercetin is the main active ingredient of Xanthoceras sorbifolia Bunge. Traditional compatibility theory of traditional Chinese medicine has typically reported a synergistic interaction among multiple components, while the synergistic effects of nanoemulsion have not been fully clarified. Objective: To study preparation and characterization of quercetin-based Mongolia Medicine Sendeng-4 nanoemulsion (NQUE-NE) and its antibacterial activity and mechanisms. Methods: The morphology of the nanoemulsion was observed by transmission electron microscopy (TEM), and the zeta potential, polydispersity index (PDI), and particle size distribution were determined by the nanometer particle size analyze. The stability of nanoemulsion was investigated by light test, high speed centrifugal test and storage experiment at different temperature. The combined bacteriostatic effect of N-QUE-NE was studied in vitro by double-dilution method and checkerboard dilution method. Results: The appearance of N-QUE-NE was pale yellow, clear and transparent. The nanoemulsion particles were spherical and uniformly distributed under TEM. The PDI was 0.052, the average particle size was 19.6nm, and the Zeta potential was -0.2mV. When quercetin nanoemulsion (QUE-NE) was used in combination with tannin nanoemulsion (TAN-NE) and toosendanin nanoemulsion (TOO-NE), it exhibited a synergistic antibacterial effect. However, the combination of QUE-NE and geniposide nanoemulsion (GEN-NE) exhibited an antagonistic effect. It was revealed that the antibacterial effect was in order of quercetin-tannin-toosendanin nanoemulsion (QUE-TAN-TOO-NE) ＞ quercetin-tannin nanoemulsion (QUE-TANNE) ＞ QUE-NE ＞ quercetin-tannin-toosendanin-geniposide nanoemulsion (QUE-TAN-TOO-GEN-NE). Conclusion: This study explored the preparation and efficacy of N-QUE-NE, and the results showed that quercetin, tannin and toosendanin had satisfactory synergistic antibacterial effects. The antagonistic effect of quercetin and geniposide in nanoemulsion indicated that it is not beneficial to the antibacterial effect of Sendeng-4, and further research needs to be conducted to clarify its antibacterial effect.

Effect of Poly(Vinyl Pyrrolidone) on Dispersing Carbon Black Particles

2013 ◽  
Vol 796 ◽  
pp. 432-436
Author(s):  
Xia Yuan
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Carbon Black ◽  
Ultrasonic Method ◽  
Aqueous Media ◽  
Average Particle Size ◽  
Sodium Dodecyl ◽  
Vinyl Pyrrolidone ◽  
Average Particle ◽  
Poly Vinyl Pyrrolidone

The effects of poly (vinyl pyrrolidone)(PVP) on dispersing carbon black (CB) particles were investigated by measuring Z-average particle size, Zeta potential and centrifugal stability of CB dispersions. Addition of PVP in a dispersing medium significantly reduces the size of suspended CB particles, especially in water. The dispersing efficiency of PVP was found to have been enhanced by adding an anionic surfactant, sodium methylenedinaphthalene disulphonate (NNO) in the aqueous media. The particle size of CB dispersed with PVP and NNO was 175.7 nm, significantly smaller than that dispersed with PVP and sodium dodecyl sulfate (SDS). The performance of PVP-encapsulated CB particles and that of PVP-adsorbed CB particles were also compared. The particle size and Zeta potential of PVP-encapsulated CB particles were similar to those of PVP-adsorbed CB particles using ultrasonic method, but the centrifugal stability of PVP-encapsulated CB dispersions was significantly improved. The relative absorbency of PVP/CB dispersions was increased from 42.0% to 63.7%. However, the PVP-encapsulated layer can be destroyed by prolonged ultrasonic treatment because the ultrasound over a long period of time can not only break up the flocculation bridge in the crosslinking matrix of PVP, but also flake off the PVP shells on the surface of CB particles.

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