scholarly journals Study of homogenization on media milling time in preparation of irbesartan nanosuspension and optimization using design of experiments (DoE)

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Chetan Borkhataria ◽  
Dhavalkumar Patel ◽  
Swati Bhagora ◽  
Nilesh Patel ◽  
Kalpesh Patel ◽  
...  
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Zirconium Dioxide ◽  
Milling Time ◽  
Stability Study ◽  
Combination Method ◽  
Poloxamer 407 ◽  
Potential Value ◽  
Media Milling ◽  
Accelerated Stability

Abstract Background The present investigation aimed at preparing nanosuspension of irbesartan to improve its dissolution. Dissolution enhancement of irbesartan can improve the oral bioavailability. Here, it was also studied how media milling time can be reduced by subjecting irbesartan to prior homogenization and then media milling. Results First, homogenization of irbesartan was carried out in the presence of poloxamer 407 at 6000 rpm for 2 h. Final nanosuspension preparation was done by media milling with zirconium dioxide beads. Here, the amount of poloxamer 407 and zirconium dioxide beads was studied as statistical independent variables. Response surface plot analysis and desirability function were applied to the selected optimized batch. The prepared batches were subjected to evaluation for zeta potential value, mean particle size, PDI, dissolution study, and stability study. Target particle size was less than 500 nm, and in vitro dissolution in 10 min was more than 80%. Zeta potential value was ~ 27 mV for optimized nanosuspension. Desirability of 0.941 was achieved. Checkpoint batch was prepared and evaluated to confirm the validity of mathematical model. Accelerated stability study was performed on the optimized batch at 40 ± 2 °C/75 ± 5% RH for 6 months. Conclusion The results confirmed the stability of formulation at accelerated stability conditions. Using presuspension prepared by homogenization, media milling time primarily reduced from 24–28 h to 18 h. Future perspective is to study other factors in combination method in discrete.

Quality by Design-based Optimization of Formulation and Process Variables for Controlling Particle Size and Zeta Potential of Spray Dried Incinerated Copper Nanosuspension

2019 ◽  
Vol 12 (3) ◽  
pp. 248-260
Author(s):  
Saurabh Singh ◽  
Sachin Kumar Singh ◽  
Malti G. Chauhan ◽  
Bimlesh Kumar ◽  
Narendra Kumar Pandey ◽  
...  
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Spray Drying ◽  
Milling Time ◽  
Drug Loading ◽  
Optimization Procedure ◽  
Process Variables ◽  
Media Milling ◽  
Predicted Values ◽  
Spray Dried

Background: In the present study copper nanosuspension was prepared from Incinerated Copper Powder (ICP) by top down media milling. Glycyrrhiza glabra (GG) and Gum Acacia (GA) were used as stabilizers in the formulation. Methods: Box Behnken Design was used to investigate the effect of formulation and process variables on particle size and zeta potential and optimize their ratio to get target product profile. The ratio of GA and GG to ICP was varied along with milling time and its speed. Further the prepared nanosuspensions were solidified using spray drying. Results: The particle size was found to be decreased with the increase in GG to ICP ratio, milling time and milling speed, whereas, reverse effect on particle size was observed with an increase in GA to ICP ratio. The zeta potential was found to be increased with the increase in GG to CB ratio and milling speed and it decreased with the increase in GA to ICP ratio and milling time. The obtained value for particle size was 117.9 nm and zeta potential were -9.46 mV which was in close agreement with the predicted values by the design which was, 121.86 nm for particle size and -8.07 mV for zeta potential respectively. This indicated the reliability of optimization procedure. The percentage drug loading of copper in the nanosuspension was 88.26%. The micromeritic evaluation of obtained spray dried nanoparticles revealed that the particles were having good flow and compactibility. Conclusion: It can be concluded that application of media milling, design of experiment and spray drying have offered very good copper nanosuspension that has the potential to be scaled up on industrial scale.

Novel Formulation Development and Evaluation of Nanoparticles Based in Situ Gelling System for The Ophthalmic Delivery of Ciprofloxacin Hydrochloride

2015 ◽  
Vol 5 (4) ◽  
Author(s):  
Kranti Singh ◽  
Surajpal Verma ◽  
Shyam Prasad ◽  
Indu Bala
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Drug Loading ◽  
In Vitro Release ◽  
Formulation Development ◽  
Ciprofloxacin Hydrochloride ◽  
Potential Value ◽  
The Mean ◽  
In Situ Gelling

Ciprofloxacin hydrochloride loaded Eudragit RS100 nanoparticles were prepared by using w/o/w emulsification (multiple emulsification) solvent evaporation followed by drying of nanoparticles at 50°C. The nanoparticles were further incorporated into the pH-triggered in situ gel forming system which was prepared using Carbopol 940 in combination with HPMC as viscosifying agent. The developed nanoparticles was evaluated for particle size, zeta potential value and loading efficiency; nanoparticle incorporated in situ gelling system was evaluated for pH, clarity, gelling strength, rheological studies, in-vitro release studies and ex-vivo precorneal permeation studies. The nanopaticle showed the mean particle size varying between 263.5nm - 325.9 nm with the mean zeta potential value of -5.91 mV to -8.13 mV and drug loading capacity varied individually between 72.50% to 98.70% w/w. The formulation was clear with no suspended particles, showed good gelling properties. The gelling was quick and remained for longer time period. The developed formulation was therapeutically efficacious, stable and non-irritant. It provided the sustained release of drug over a period of 8-10 hours.

scholarly journals Enhanced Oral Bioavailability of Celecoxib Nanocrystalline Solid Dispersion based on Wet Media Milling Technique: Formulation, Optimization and In Vitro/In Vivo Evaluation

Pharmaceutics ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 328 ◽  
Author(s):  
Zhuang Ding ◽  
Lili Wang ◽  
Yangyang Xing ◽  
Yanna Zhao ◽  
Zhengping Wang ◽  
...  
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Solid Dispersion ◽  
Oral Bioavailability ◽  
Stability Study ◽  
Sprague Dawley ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation

Celecoxib (CLX), a selective COX-2 inhibitor, is a biopharmaceutics classification system (BCS) class II drug with its bioavailability being limited by thepoor aqueoussolubility. The purpose of this study was to develop and optimize CLX nanocrystalline(CLX-NC) solid dispersion prepared by the wet medium millingtechnique combined with lyophilizationto enhance oral bioavailability. In formulation screening, the resulting CLX-NC usingpolyvinylpyrrolidone (PVP) VA64 and sodiumdodecyl sulfate (SDS) as combined stabilizers showed the minimum particle size and a satisfactory stability. The formulation and preparation processwere further optimized by central composite experimentaldesign with PVP VA64 concentration (X1), SDS concentration (X2) and milling times (X3) as independent factors and particle size (Y1), polydispersity index (PDI, Y2) and zeta potential (Y3) as response variables. The optimal condition was determined as a combination of 0.75% PVP VA64, 0.11% SDS with milling for 90 min.The particle size, PDI and zeta potential of optimized CLX-NC were found to be 152.4 ± 1.4 nm, 0.191 ± 0.012 and −34.4 ± 0.6 mV, respectively. The optimized formulation showed homogeneous rod-like morphology as observed by scanning electron microscopy and was in a crystalline state as determined by differential scanning calorimetry and powder X-ray diffraction. In a storage stability study, optimized CLX-NC exhibited an excellent physical stability during six months’ storage at both the refrigeration and room conditions. In vivo pharmacokinetic research in Sprague-Dawley ratsdisplayed that Cmax and AUC0–∞ of CLX-NC were increased by 2.9 and 3.1 fold, compared with physical mixture. In this study, the screening and optimizing strategy of CLX-NC formulation represents a commercially viable approach forenhancing the oral bioavailability of CLX.

scholarly journals Formulation, Optimization, and Characterization of Repaglinide Loaded Nanocrystal for Diabetes Therapy

2015 ◽  
Vol 2015 ◽  
pp. 1-7 ◽  
Author(s):  
Gajanan Shinde ◽  
Mitesh Patel ◽  
Manan Mehta ◽  
Rajesh Kesarla ◽  
Ganesh Bangale
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Polymer Concentration ◽  
Study Data ◽  
Stability Study ◽  
Diabetes Therapy ◽  
Peg 4000 ◽  
Number Of Cycles

The aim of the present investigation was to formulate and characterize nanocrystal formulation of Repaglinide for diabetes therapy. Formulation was done by high pressure homogenization. HPH pressure and cycles range were screened by preliminary batches (T1 and T2). 5, 8, and 10 cycles and 500 to 1500 bar pressure range had kept for further investigation. Taguchi design was used to optimize type of polymer, % polymer concentration, number of cycles, and HPH pressure for nanocrystal formulation. Formulations were characterized for particle size, zeta potential, and in vitro drug release. Optimized formulation (NC 3) showed particle size of 187 nm, zeta potential of −29.4 mv, and % drug release of 80.58% and it was used for further study. Data analysis proved significant effects of factors on responses. Polydispersity index (PDI) Analysis of optimized formulation were found to be 0.248. SEM showed nanocrystal aggregation of drug, may be due to water removal process. DSC showed slight change in crystallinity, may be due to the presence of PEG 4000. Stability study was carried out for 3 months. It indicated no significant change in particle size and zeta potential. However, further studies in higher animals and human being need to be performed before this formulation can be commercially exploited.

Anaerobic vs. aerobic preparation of silicon nanoparticles by stirred media milling. The effects of dioxygen, milling solvent, and milling time on particle size, surface area, crystallinity, surface/near-surface composition, and reactivity

RSC Advances ◽  
2016 ◽  
Vol 6 (113) ◽  
pp. 112370-112380
Author(s):  
Eric V. Bukovsky ◽  
Karlee P. Castro ◽  
Brent M. Wyatt ◽  
Olga V. Boltalina ◽  
Steven H. Strauss
Keyword(s):  
Particle Size ◽  
Surface Area ◽  
Silicon Nanoparticles ◽  
Milling Time ◽  
Surface Composition ◽  
Near Surface ◽  
Media Milling ◽  
Attritor Milling

Silicon nanoparticles milled anaerobically in heptane or mesitylene are smaller and much more reactive than SiNPs milled aerobically in the same solvents for equal attritor milling times.

FORMULATION AND EVALUATION OF CURCUMIN LOADED NANOCRYSTAL FOR DIABETES THERAPY

INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (12) ◽  
pp. 5-11
Author(s):  
G Shinde ◽  
◽  
C Jaiswal ◽  
G Bangale ◽  
K.S. Rajesh
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Pressure Range ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
High Pressure Homogenization ◽  
Diabetes Therapy ◽  
In Vitro Drug Release ◽  
Polymer Ratio

The aim of the present investigation was to design and characterize nanocrystal formulation of curcumin for diabetes therapy. Formulation was prepared by High Pressure Homogenization. HPH cycles and pressure range were screened by preliminary batches (T1 & T2). 15 cycles were optimized and the pressure range was kept at 500-2000 bar. A Taguchi design was used to optimize type of polymers, Drug: polymer ratio, amount of SLS and HPH pressure. Formulations were characterized for particle size, % entrapment efficiency and in vitro drug release. Optimized formulation (NC 4) showed a particle size of 147.8nm, % EE of 85.35%, % DR of 77.46% and was used for further study. Zeta potential and PDI was found to be -39.63 and 0.252 respectively. Stability study was carried out for 3 weeks. It indicated no significant change in particle size, Zeta Potential, PDI and settling.

scholarly journals OPTIMIZATION AND IN VITRO EVALUATION OF THE RELEASE OF CLASS II DRUG FROM ITS NANOCUBOSOMAL DISPERSION

2019 ◽  
pp. 86-90
Author(s):  
Sadeq Jaafar Al-sakini ◽  
Nidhal Khazaal Maraie
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Entrapment Efficiency ◽  
Class Ii ◽  
Poloxamer 407 ◽  
In Vitro Test ◽  
Surfactant Mixtures ◽  
Onset Of Action

Objective: This work involves investigation and evaluation of the factors that affect the preparation and the release of the model class II drug (erythromycin) to optimize the efficiency of its prepared nanocubosomal dispersion to give very fast initial burst effect within the first hour that can continue for further two hours. Methods: The work involved preparation of ten formulas of cubosomal dispersion by emulsifying different concentrations of glyceryl monooleate (GMO) (lipid content)/surfactant mixtures which were nano-sized and characterized morphologically by Transmission electronic microscopic (TEM), zeta potential, particle size, polydispersity index (pdI), pH, entrapment efficiency, conductivity test, dilution test and in vitro drug release. Results: The selected nanocubosomal formula (F1) showed pH (7.41), particle size (315.05 nm), pdI (0.194), zeta potential (-30.852), entrapment efficiency (91%) and gave a 70% drug release within the first hour of the in vitro test and continued until it gave 96.3% drug release with further 2 h. Conclusion: this work succeeded in preparing optimized cubosomal dispersion for erythromycin using different GMO/poloxamer 407 percent. The optimum formula gave an immediate release of the model drug (erythromycin) and it was ready to be incorporated in any suitable dosage form to give fast onset of action.

scholarly journals Formulation and Characterization of Moxifloxacin Nanoparticles with Ion Exchange Resin

2020 ◽  
Vol 10 (1-s) ◽  
pp. 51-61 ◽  
Author(s):  
Jigar Vyas ◽  
Kapil Daxini ◽  
Jitendra Patel
Keyword(s):  
Particle Size ◽  
Ion Exchange ◽  
Zeta Potential ◽  
Exchange Resin ◽  
Diffusion Mechanism ◽  
In Vitro Release ◽  
Ion Exchange Resin ◽  
Fickian Diffusion ◽  
Stoichiometric Ratio ◽  
Media Milling

Moxifloxacin (MOX) is a fluoroquinolone anti-infective drug, indicated for the treatment of bacterial conjunctivitis. The drug is soluble in water but still produces low ocular bioavailability due to biological barriers and so it requires dosing for two/three times a day. The present study was designed to formulate, optimize and characterize polymeric Nanoparticles MOX for ocular administration using Ion Exchange Resin (IER). IER-nanoparticles were prepared by media milling method, formulation/process parameters were optimized based on evaluation parameters such as color of nanosuspension, sedimentation behaviour, particle size and zeta potential. MOX-IER nanosuspensions were prepared at different stoichiometric ratio of MOX and IER and characterized by entrapment efficiency, pH, particle size and zeta potential of nanosuspension. In vitro release study of optimized batch MNIER3 exhibited sustained release pattern which follows Korsmeyer-Peppas model with Fickian diffusion mechanism for drug release. Based on these results optimized batch of MOX-IER nanosuspension formulated in the laboratory was found suitable for ocular delivery. Keywords: Moxifloxacin; nanoparticles, nanosuspension; media milling; stoichiometric ratio; sedimentation behaviour.

Preparation of La0.7Sr0.3Co0.2Fe0.8O3-δ (LSCF 7328) by Combination of Mechanochemical and Solid State Reaction

2017 ◽  
Vol 744 ◽  
pp. 399-403 ◽  
Author(s):  
Silvana Dwi Nurherdiana ◽  
Nikmatin Sholichah ◽  
Rendy Muhamad Iqbal ◽  
Mutya Sandei Sahasrikirana ◽  
Wahyu Prasetyo Utomo ◽  
...  
Keyword(s):  
Particle Size ◽  
Solid State ◽  
Milling Time ◽  
High Energy ◽  
Milling Process ◽  
Perovskite Oxide ◽  
Combination Method ◽  
Structure Evolution ◽  
Preparation Methods ◽  
Grinding Method

Structure evolution and morphology of La0.7Sr0.3Co0.8Fe0.2O3-δ (LSCF 7328) were investigated during two different preparation methods namely mechanochemical and combination of mechanochemical-solid state. The result shows that no characteristic peak of perovskite oxide was found on the diffractogram of the product of sole mechanochemical method at 600 rpm and up to 12 h of high energy milling process. On the other hand, the manual grinding method that was followed by solid state calcination produces irregular particle size. Due to the result, the combination of both methods was proposed to obtain the fine structure formation and particle size distribution. Rietveld refinement was used to investigate the lattice distortion. It was found that unit cell remains unchanged at increasing milling time. Moreover, the combination method produces regular particle size at milling time of 0.5 h. At longer milling time, the more regular particle size is formed which comes from highly energy transfer of milling.

scholarly journals PREPARATION OF SOLID LIPID NANOPARTICLES CONTAINING MANGOSTEEN PERICARP EXTRACT

2018 ◽  
Vol 11 (15) ◽  
pp. 80
Author(s):  
Siti Nur Diniyanti
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Physical Characteristics ◽  
Protection Factor ◽  
Potential Value ◽  
Solid Lipid ◽  
Sun Protection Factor ◽  
Viscous Substance

Objectives: The aim of this study was to develop solid lipid nanoparticles (SLNs) containing mangosteen pericarp extract (MPE) to achieve enhanced photoprotection and to provide an alternative to synthetic sunscreens in the market.Materials and Methods: The MPE was prepared using the maceration method, and evaluated for sun protection factor (SPF) value using an ultraviolet (UV)-Vis spectrophotometer. SLNs were prepared through ultrasonication method. Blank-SLNs were formulated using stearic acid (SA) or palmitic acid (PA) as solid lipids at a concentration of 3%. Tween® 80 or polyvinyl alcohol (PVA) was employed as a surfactant with a concentration ranging from 1 to 2%. The obtained blank-SLNs were investigated for their physical characteristics, (i.e., morphology, particle size, polydispersity index [PDI], and zeta potential values). The blank-SLNs with suitable physical characteristics were selected to encapsulate MPE and evaluated for the physical characteristics.Results: The MPE was a brownish viscous substance with an SPF value that ranged from 3.09±0.005 to 27.20±0.05 at a concentration ranging from 0.02 to 0.1 mg/ml. Based on the physical characteristics, the blank-SLNs employing PA or SA with 1% of PVA were selected. The MPE-SLNs were spherical, with a particle size that ranged from 443.51±6.50 to 533.52±16.15 nm; PDI ranged from 0.35±0.008 to 0.459±0.02, and zeta potential value ranged from 18.32±1.37 to −19.03±0.64. The entrapment efficiencies of MPE-PA-SLNs and MPE-SA-SLNs were 83.24±1.37% and 84.17±0.411%, respectively.Conclusion: The results indicated the promising potential of MPE as a UVB photoprotector. The MPE-SLNs were also successfully formulated, but, further study is needed to confirm the potential of MPE-SLNs to be used as a sunscreen, and their stability during storage.

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