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

Author(s):  
Saurabh Singh ◽  
Sachin Kumar Singh ◽  
Malti G. Chauhan ◽  
Bimlesh Kumar ◽  
Narendra Kumar Pandey ◽  
...  

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.

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Chetan Borkhataria ◽  
Dhavalkumar Patel ◽  
Swati Bhagora ◽  
Nilesh Patel ◽  
Kalpesh Patel ◽  
...  

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.


Author(s):  
Kranti Singh ◽  
Surajpal Verma ◽  
Shyam Prasad ◽  
Indu Bala

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.


Author(s):  
Gülsel Yurtdaş Kırımlıoğlu ◽  
Sinan Özer ◽  
Gülay Büyükköroğlu ◽  
Yasemin Yazan

Background: Considering the low ocular bioavailability of conventional formulations used for ocular bacterial infection treatment, there’s a need for designing efficient novel drug delivery systems that may enhance of precorneal retention time and corneal permeability. Aim and Objective: The current research focuses on developing nanosized and non-toxic Eudragit® RL 100 and Kollidon® SR nanoparticles loaded with moxifloxacin hydrochloride (MOX) for its prolonged release to be promising for effective ocular delivery. Methods: In this study, MOX was incorporation was carried out by spray drying method aiming ocular delivery. In vitro characteristics were evaluated in detail with different methods. Results: MOX was successfully incorporated into Eudragit® RL 100 and Kollidon® SR polymeric nanoparticles by spray-drying process. Particle size, zeta potential, entrapment efficiency, particle morphology, thermal, FTIR, XRD and NMR analyses and MOX quantification using HPLC method were carried out to evaluate the nanoparticles prepared. MOX loaded nanoparticles demonstrated nanosized and spherical shape while in vitro release studies demonstrated modified release pattern which followed Korsmeyer-Peppas kinetic model. Following successful incorporation of MOX into the nanoparticles, the formulation (MOX: Eudragit® RL 100, 1:5) (ERL-MOX 2) was selected for further studies by the reason of its better characteristics like cationic zeta potential, smaller particle size, narrow size distribution and more uniform prolonged release pattern. Moreover, ERL-MOX 2 formulation remained stable for 3 months and demonstrated higher cell viability values for MOX. Conclusion: In vitro characterization analyses showed that non-toxic, nano-sized and cationic ERLMOX 2 formulation has the potential of enhancing ocular bioavailability.


Author(s):  
MAGFIRAH ◽  
INDAH KURNIA UTAMI

Objective: Parang romang (Boehmeria virgata) is one of the traditional medicines that are used empirically by Makassar tribal healers, South Sulawesi, as an antitumor drug. This traditional medicine contains secondary metabolites such as alkaloids, flavonoids, tannins, and saponins. However, secondary metabolites of those leaves extract have low solubility in water. Hence, to be formula, self-nanoemulsifying drug delivery system (SNEDDS) is one of the solutions to increase the extract solubility. Methods: The optimization of two formula optimum SNEDDS parang romang leaves (T80PGMZ and T20PGMZ) was using the simple lattice design (SLD) method which will give 28 SNEDDS formula parang romang leaves each of which the formula is tested for its characteristics as a critical point include emulsification time, % transmittance, drug loading, particle size, zeta potential, polydispersity index, and morphology particle. Results: The results of SNEDDS characterization obtained the optimum formula T80PGMZ with emulsification time 12.6 s, % transmittance 92.21%, drug loading 68.21 ppm, particle size 370.26 nm, zeta potential −31.4 mV, polydispersity index of 0.615, and regular particle morphology with spherical chunks at a magnification of 10,000 times with a particle size of 10 μm. Conclusion: SNEDDS of parang romang leaves extracts that used olive oil as oil phase, Tween 80 as a surfactant, and propylene glycol as the cosurfactant provided nanoemulsion with good characteristics.


Author(s):  
RAMA RAO NADENDLA ◽  
LAKSHMI SWAPNA SAI ◽  
NIHITHA SANKA ◽  
SANTHI PRIYA NAGAM

Objective: The present study was focused to design an herbal formulation for the treatment of Alzheimer’s disease (AD) to develop the formulation using various techniques such as spray drying, centrifugation, and lyophilization and to conduct behavioral studies to evaluate the activity of the herbal formulation. Methods: Formulation contains herbal extracts such as curcumin, guggul, and ashwagandha. To develop this formulation, various techniques such as spray drying, centrifugation, and lyophilization were employed along with a natural polymer chitosan in various combinations of excipient. Preformulation studies such as solubility of herbal extracts and Fourier transmission infrared spectroscopy (FT-IR) studies for compatibility of the natural polymer with herbal extracts were studied. The formulation was characterized by tests such as particle size determination using optical microscopy, surface morphological evaluation using scanning electron microscopy (SEM), and behavioral testing by Morris water maze test using diazepam-induced amnesia method. Results: The particle size varied from 12.27 μ for normal chitosan to 3.59 μ for spray-dried chitosan. In the same way, the particle of normal formulation (12.9 μ) was about 4–5 times larger than that of spray-dried formulation (2.7 μ). The SEM images showed no proper morphology for chitosan, round surface with wrinkles for spray-dried chitosan, improper structures for normal formulation, and rounded smooth surface for spray-dried formulation. Significant p value was shown when the spray-dried test formulation was tested using diazepam-induced amnesia method. The transfer latency was noted on the 8th day and after 24 h of intraperitoneal administration of diazepam for the test group. Conclusion: In the present research study, an attempt was made to design and develop a novel drug delivery system using herbal medicine to treat AD. FT-IR compatibility study was carried out using the selected polymer and the herbal extracts using novel spray-drying techniques; behavioral studies were also done.


2001 ◽  
Vol 16 (4) ◽  
pp. 1083-1089 ◽  
Author(s):  
X. L. Dong ◽  
B. K. Kim ◽  
C. J. Choi ◽  
K. S. Park ◽  
Z. D. Zhang

The magnetic Nd–Fe–B powders were prepared by a mechanochemical method, including the processes of spray drying, debinding, milling, H2 reduction, Ca reduction, and washing. The liquid solution dissolved with various metal salts was first spray-dried to prepare the precursor powders having uniformly dispersed Nd, Fe, and B components. The precursor powders in turn were subjected to the subsequent processes. The particle size of the resultant Nd–Fe–B powders was about 1 μm. Effects of the process parameters on phases, morphologies, microstructures, compositions, and thermal properties of the powders were investigated.


2018 ◽  
Vol 10 (5) ◽  
pp. 125 ◽  
Author(s):  
Ali Nasr ◽  
Mona Qushawy ◽  
Shady Swidan

Objective: In the present investigation efforts were considered to optimize the different conditions for the preparation of spray dried lactose based proniosomes. The aim of this research was to investigate the feasibility of proniosomes as stable precursors for the development of niosomes as oral drug delivery system for poorly water-soluble drugs.Methods: A total of twenty-eight plain proniosomal formulae were prepared with various surfactant-cholesterol loading ratios in each formula using spray dried lactose as a carrier. Span 20, 40, 60 and 80 were used in various molar ratios with cholesterol. Different evaluation techniques were performed to study the performance of the prepared proniosomes. The micromeritic properties of the prepared proniosomes were analyzed. The reconstituted niosomes were further evaluated for morphological characterization using transmission electron microscope (TEM), particle size analysis, zeta potential, and polydispersity index (PDI). Finally, selected proniosomal formulae were tested for stability study.Results: The proniosomal formulae prepared using span 40 and span 60 exhibited excellent flowability while those prepared with span 20 and span 80 showed poor flow properties. TEM photographs revealed that the vesicles were discrete, spherical without aggregation. The mean vesicle size of reconstituted niosomes was found to be in the range between (252.9±0.43–624.3±0.23 nm) with perfect PDI values (0.387±0.05–0.835±0.03). The negative values of zeta potential indicated that all prepared formulae were stabilized by electrostatic repulsion forces. Stability studies confirmed that proniosomes give a more stable system that could overcome the problems of standard niosomes. Formulae with the smallest particle size, higher surface charge values and best flow properties were selected to be loaded with poorly soluble drugs for further study.Conclusion: The obtained results offered evidence that spray-dried lactose based proniosomes are promising stable drug delivery carriers and ready to incorporate various poorly water-soluble drugs in order to improve their limited oral bioavailability.


Author(s):  
MONOWAR HUSSAIN ◽  
ANUPAM SARMA ◽  
SHEIKH SOFIUR RAHMAN ◽  
ABDUL MATIN SIDDIQUE ◽  
TANUKU PAVANI EESWARI

Objective: Tuberculosis (TB) is an infectious bacterial disease caused by Mycobacterium tuberculosis which most commonly affects the lungs. TB has the highest mortality rate than any other infectious disease occurs worldwide. The main objective of the present investigation was to develop polymeric nanoparticles based drug delivery system to sustain the ethambutol (ETB) release by reducing the dose frequency. Methods: The Preformulation studies of drug ETB were done by physical characterization, melting point determination, and UV spectrophotometric analysis. The ETB loaded nanoparticles were prepared by double-emulsion (W/O/W) solvent evaporation/diffusion technique. The prepared polymeric nanoparticles were evaluated for particle size, polydispersity index, zeta potential, drug entrapment efficiency, drug loading, drug-polymer compatibility study, surface morphology, in vitro drug release, and release kinetics. Results: Based on the result obtained from the prepared formulations, F11 showed the best result and was selected as the optimized formulation. Optimized batch (F11) showed better entrapment efficiency (73.3%), good drug loading capacity (13.21%), optimum particle size (136.1 nm), and zeta potential (25.2 mV) with % cumulative drug release of 79.08% at the end of 24 h. Conclusion: These results attributed that developed polymeric nanoparticles could be effective in sustaining the ETB release over 24 h. Moreover, the developed nanoparticles could be an alternate method for ETB delivery with a prolonged drug release profile and a better therapeutic effect can be achieved for the treatment of tuberculosis.


Author(s):  
Sneha Dekate Shreeram Hirlekar ◽  
Srinivas Bhairy ◽  
Srinivas Bhairy ◽  
Rajashree Hirlekar ◽  
Rajashree Hirlekar

Objective: The principle objective of the present research work was to improve the bioavailability of curcumin (CUR) by decreasing its particle size. Nanosuspension (NS) of CUR was prepared using poloxamer-188 (P188) as a surfactant. The prepared NSs were characterized for particle size, polydispersity index (PDI), zeta potential, drug loading, saturation solubility, and drug release kinetic studies.Methods: Components required for NS preparation, such as solvent, anti-solvent and surfactant were screened. Precipitation high-speed homogenization (HSH) method was used for the preparation of NS using selected components. Evaluation of NS for particle size, PDI, drug loading, saturation solubility and in vitro drug release was done. Pharmacokinetic studies of the NS in sprague dawley (SD) rats were performed.Results: The particle size, PDI and zeta potential of the optimized formulation was 596.5±5 nm, 0.233±0.010 and-23±2 mV respectively. The pH of all the formulations was in the range of 5-6 which is acceptable when related to drug stability. The optimized formulation showed an increase in saturation solubility in water and phosphate buffer pH 6.8 when compared to plain CUR suspension (S). Results of pharmacokinetic studies indicated that Cmax and AUC0-6 were increased 8 and 10 times respectively from plain CUR S to CUR NS.Conclusion: CUR NS was prepared using P188 as the stabilizer. Amongst various stabilizers screened P188 rendered a stable NS with the particle size in nano range. Pharmacokinetic studies revealed the better performance of CUR NS as compared to plain CUR S.


Author(s):  
Yuchuan Wang ◽  
Ying Cui ◽  
Bo Wang ◽  
Min Zhang

Skimmed milk powders (SMP) were produced by ultrasonic atomizing-assisted spray drying (UASD). It was found that UASD can produce high quality SMP (with < 5% moisture content and < 2% insolubility) at lower inlet temperatures (~130℃). The particle size of the UASD-SMP was 10 times smaller (decreased from ~20 µm to 4 µm) than the tranditionally spray-dried SMP and the color appeal of UASD-SMP was also better (L* value increased by > 6 %). Overall, this research shown that UASD can be used to produce small particle size and high quality SMP. Keywords: Skimmed milk powder; ultrasonic atomization; spray dryer; particle size distribution; color  


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