scholarly journals Optimization of Chitosan Microspheres Spray Drying via 32 Full Factorial Design

Folia Medica ◽  
2017 ◽  
Vol 59 (3) ◽  
pp. 310-317 ◽  
Author(s):  
Plamen D. Katsarov ◽  
Bissera A. Pilicheva ◽  
Hristo M. Manev ◽  
Paolina K. Lukova ◽  
Margarita I. Kassarova
Keyword(s):  
Particle Size ◽  
Factorial Design ◽  
Size Distribution ◽  
Spray Drying ◽  
Process Parameters ◽  
Polymer Concentration ◽  
Production Yield ◽  
Nasal Administration ◽  
Chitosan Microspheres ◽  
Pump Rate

AbstractBackground:Generally, the preparation of spray-dried microspheres is strongly affected by the process parameters. Particle size and production yield are mainly influenced by the spraying solution concentration and the pump rate of the spray dryer.Aim:The aim of this study was to assess optimum spray drying parameters - polymer concentration and pump rate required for the production of chitosan microspheres with high production yield and targeted for nasal administration particle size.Materials and methods:Full 32factorial design was used to study the investigated parameters. Three different concentrations of the chitosan solution were selected: a low concentration of 1%, average concentration of 1.5% and high concentration of 2%. The rate of the peristaltic pump was also varied at three levels: low rate of 10%, medium rate of 14% and high rate of 18%.Results:Nine models of chitosan microspheres were formulated and characterized in terms of shape, surface morphology, size, particle size distribution and production yield. The particles obtained from 2% chitosan solutions, sprayed at 10% pump rate were of the highest yield (64.33%) and appropriate for nasal administration median diameter (3,434 μm).Conclusion:The two investigated spray-drying parameters interact with each other and their influence on the production yield and the size of the chitosan microspheres should be evaluated together, instead of one at a time. The assessed process parameters allow the production of chitosan microparticles with high yield and desirable characteristics (size, size distribution and shape) for intranasal delivery.

Formulation and Evaluation of Atenolol Nanocrystals Using 3(2) Full Factorial Design

2020 ◽  
Vol 10 (3) ◽  
pp. 306-315
Author(s):  
Rupa Mazumder ◽  
Swarnali Das Paul
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Organic Solvent ◽  
Factorial Design ◽  
Goodness Of Fit ◽  
Production Yield ◽  
Pharmacokinetic Property ◽  
Potential Yield ◽  
Simple Method ◽  
Pure Drug

Background: Atenolol is a commonly used antihypertensive drug of class III BCS category. It suffers from the problem of poor intestinal absorption or permeability thus low bioavailability. The objective of the present study was to enhance the permeability of atenolol by using a suitable technique, which is economical and devoid of using any organic solvent. Methods: The nanocrystal technology by high-pressure homogenization was chosen for this purpose, which is a less expensive and simple method. In this technique, no organic solvent was used. The study was further aimed to characterize prepared nanocrystals in the solid state by Fourier Transform Infrared Spectroscopy (FTIR), Powder X-Ray Diffraction (PXRD) patterns, particle size, zeta potential, %yield and drug permeation study through isolated goat’s intestine. An in-vivo study was carried out to determine the pharmacokinetic property in comparison to pure drug powder using rats as experimental animals. The formulation design was optimized by a 3(2) factorial design. In these designs, two factors namely surfactant amount (X1) and speed of homogenizer (X2) were evaluated on three dependent variables namely particle size (y1), zeta potential (y2) and production yield (y3). Results: PXRD study indicated the presence of high crystal content in the prepared formulation. These nanocrystal formulations were found with a narrow size range from 125 nm to 652 nm and positive zeta potential of 16-18 mV. Optimized formulations showed almost 90% production yield. Permeability study revealed 90.88% drug release for optimized formulation in comparison to the pure drug (31.22%). The FTIR study also exposed that there was no disturbance in the principal peaks of the pure drug atenolol. This confirmed the integrity of the pure drug and its compatibility with the excipients used. A significant increase in the area under the concentration-time curve Cpmax and MRT for nanocrystals was observed in comparison to the pure drug. The higher values of the determination coefficient (R2) of all three parameters indicated the goodness of fit of the 3(2) factorial model. The factorial analysis also revealed that speed of homogenizer had a bigger effect on particle size (-0.2812), zeta potential (-0.0004) and production yield (0.0192) whereas amount of surfactant had a lesser effect on production yield (-370.4401), zeta potential (-43.3651) as well as particle size (-6169.2601). Conclusion: It is concluded that the selected method of nanocrystal formation and its further optimization by factorial design was effective to increase the solubility, as well as permeability of atenolol. Further, the systematic approach of factorial design provides rational evaluation and prediction of nanocrystals formulation on the selected limited number of smart experimentation.

scholarly journals Physico-Chemical and In Vitro Characterization of Chitosan-Based Microspheres Intended for Nasal Administration

Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 608
Author(s):  
Csilla Bartos ◽  
Patrícia Varga ◽  
Piroska Szabó-Révész ◽  
Rita Ambrus
Keyword(s):  
Drug Delivery ◽  
Spray Drying ◽  
Process Parameters ◽  
Sodium Tripolyphosphate ◽  
Structural Characteristics ◽  
Nasal Administration ◽  
Drug Bioavailability ◽  
Intranasal Application ◽  
Spray Dried

The absorption of non-steroidal anti-inflammatory drugs (NSAIDs) through the nasal epithelium offers an innovative opportunity in the field of pain therapy. Thanks to the bonding of chitosan to the nasal mucosa and its permeability-enhancing effect, it is an excellent choice to formulate microspheres for the increase of drug bioavailability. The aim of our work includes the preparation of spray-dried cross-linked and non-cross-linked chitosan-based drug delivery systems for intranasal application, the optimization of spray-drying process parameters (inlet air temperature, pump rate), and the composition of samples. Cross-linked products were prepared by using different amounts of sodium tripolyphosphate. On top of these, the micrometric properties, the structural characteristics, the in vitro drug release, and the in vitro permeability of the products were studied. Spray-drying resulted in micronized chitosan particles (2–4 μm) regardless of the process parameters. The meloxicam (MEL)-containing microspheres showed nearly spherical habit, while MEL was present in a molecularly dispersed state. The highest dissolved (>90%) and permeated (~45 µg/cm2) MEL amount was detected from the non-cross-linked sample. Our results indicate that spray-dried MEL-containing chitosan microparticles may be recommended for the development of a novel drug delivery system to decrease acute pain or enhance analgesia by intranasal application.

Synthesis of Nd2Fe14B powders by spray-drying and reduction–diffusion processes

2001 ◽  
Vol 16 (4) ◽  
pp. 1083-1089 ◽  
Author(s):  
X. L. Dong ◽  
B. K. Kim ◽  
C. J. Choi ◽  
K. S. Park ◽  
Z. D. Zhang
Keyword(s):  
Particle Size ◽  
Thermal Properties ◽  
Spray Drying ◽  
Process Parameters ◽  
Diffusion Processes ◽  
Liquid Solution ◽  
Metal Salts ◽  
Mechanochemical Method ◽  
Precursor Powders ◽  
Spray Dried

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.

Formulation of Dry Powder Inhaler of Anti-tuberculous Drugs Using Spray Drying Technique and Optimization Using 23 Level Factorial Design Approach

2019 ◽  
Vol 14 (3) ◽  
pp. 239-260
Author(s):  
Vaishali Thakkar ◽  
Ekta Pandey ◽  
Tosha Pandya ◽  
Purvi Shah ◽  
Asha Patel ◽  
...  
Keyword(s):  
Particle Size ◽  
Factorial Design ◽  
Spray Drying ◽  
Dry Powder Inhaler ◽  
Entrapment Efficiency ◽  
Inlet Temperature ◽  
Compatibility Study ◽  
Dry Powder ◽  
Residual Solvent ◽  
Critical Process

Background: Targeting anti-tubercular therapeutics to alveolar macrophages using microparticles technology mainly focuses on increasing local concentrations of therapeutics and potentially reducing the frequency of dosing requirements. Rifampicin (RIF), Ofloxacin (OFX) and Ethambutol (ETH) combination show synergism. Objective: In light of the above facts, the focus of the present study was to develop and characterize novel Dry powder Inhaler formulation incorporating novel drug combination as a pulmonary delivery for the effective eradication of Tuberculosis. Method: Biodegradable microparticles containing RIF, OFX and ETH were prepared by a spray drying technique using PLGA polymer through the critical process as well as polymer attributes were screened and optimized using 23 factorial design. The identified critical process parameters (CPP’s) viz. Inlet temperature, Aspiration rate, and feed rate were selected as independent variables while percentage yield, percentage entrapment efficiency, and particle size were selected as a response. The formulated microparticles were evaluated for particle size, drug-polymer compatibility study, aerodynamic behavior, morphology, particle size distribution, crystallinity, residual solvent content, in-vitro drug release study, and stability study. Results: By choosing the optimum spray drying conditions maximum yield of 73%, entrapment efficiency of 86% and particle size of 1.4 μm was attained of the optimized batch. Thus the results revealed that spherical microparticles are suitable for inhalation and sustained release for 12 h. Conclusion: The successful formulation and evaluation of dry powder could be used as an enhanced therapeutic alternative of the standard oral anti-tubercular regimen, rescuing oral dosing, shortening drug regimen and limiting toxicity. This will ultimately improve patient compliance and diminish the prevalence of MDR resistance.

Process Factors Using Centrifugal Spray Drying to Prepare Bauxite Microspheres

2011 ◽  
Vol 399-401 ◽  
pp. 828-833
Author(s):  
Xiao Su Cheng ◽  
Meng Qi Peng ◽  
Yu Fa Zhong
Keyword(s):  
Particle Size ◽  
Particle Size Distribution ◽  
Size Distribution ◽  
Spray Drying ◽  
Average Diameter ◽  
Optimal Operation ◽  
Solid Content ◽  
Diameter Distribution ◽  
Drying Process ◽  
Process Factors

The centrifugal spray drying process of bauxite slurry was studied to investigate the influence of slurry solid content on the particle size distribution and the sphericity of the microspheres, and so was operation technology on average diameter and the sphericity of the microspheres. The optimal operation parameters are obtained to prepare high spherical microspheres bauxite with the diameter distribution of 100 μm and whose particle size distribution is narrow: the slurry solid content is 70 wt%, the dry air temperature is 250 °C, the rotation rate of spray head is 6000 rpm and the feed flow rate is 1 L/h in the experiments.

scholarly journals An Orthogonal Model to Study the Effect of Electrospraying Parameters on the Morphology of poly (d,l)-lactide-co-glycolide (PLGA) Particles

2019 ◽  
Vol 9 (6) ◽  
pp. 1077 ◽  
Author(s):  
Ming-Yi Hsu ◽  
Chu-Han Feng ◽  
Yen-Wei Liu ◽  
Shih-Jung Liu
Keyword(s):  
Particle Size ◽  
Size Distribution ◽  
Orthogonal Design ◽  
Polymer Concentration ◽  
Spherical Geometry ◽  
Volumetric Flow Rate ◽  
Travel Distance ◽  
Plga Microspheres ◽  
Polymeric Microparticles ◽  
Processing Factors

Electrospraying has been recognized as an important technique for the production of microparticles for pharmaceutical applications. Nevertheless, the produce of poly (d,l)-lactide-co-glycolide (PLGA) microspheres with a desired size distribution remains a challenge. We conducted an empirical study, based on a fractional orthogonal design, to optimize the size distribution of electrosprayed particles. The influence of different processing factors, including PLGA concentration in the solution, volumetric flow rate of the solution, travel distance between the needle tip and the collection, voltage applied to the polymer solution, size of the needle, and type of solvent on the electrospraying of polymeric microparticles was investigated. After electrospraying, the size distribution of the PLGA particles was characterized and analyzed. Among the selected factors, the type of solvent used was the principal factor affecting the particle size of electrosprayed microspheres. Hexafluoro-2-propanol (HFIP) electrosprayed microparticles with the smallest diameter. However, hollowed particles could be seen among these microspheres. Dichloromethane (DCM) was found to electrospray microspheres with a fairly spherical geometry, while trichloromethane (TCM) electrosprayed particles with relatively rougher surfaces. Finally, the particle size of sprayed microspheres decreases somewhat with the polymer concentration and travel distance.

Formulation and Process Optimization of Solid Dispersion of Meloxicam and PEG8000 Prepared by Spray Drying

2009 ◽  
Vol 2 (3) ◽  
pp. 647-653
Author(s):  
Patel R.P. ◽  
Patel M. P. ◽  
Suthar A. M. ◽  
Baria A.H.
Keyword(s):  
Particle Size ◽  
Spray Drying ◽  
Solid Dispersion ◽  
Feed Rate ◽  
Polymer Concentration ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Inlet Temperature ◽  
Drying Method ◽  
Melting Method

The poor solubility and wettability of meloxicam leads to poor dissolution and hence shows poor bioavailability. The present study is aimed at increasing solubility of drug using solid dispersion technique. The solid binary systems were prepared using different drug: polymer ratio (1:1, 1:5 and 1:10) with polyethylene glycol 8000 by different techniques like physical mixing, melting method and spray drying method. The formulations were characterized by differential scanning colorimetry, scanning electron microscopy and in vitro dissolution rate studies. The solubility of drug increased linearly with the increase in polymer concentration. The solid dispersion of drug prepared by spray drying method demonstrated higher drug dissolution rates in comparison to solid dispersion prepared by physical mixtures, melting method and pure meloxicam. Moreover, spray drying process parameters inlet air temperature and feed rate were also optimized to obtain maximum powder yield and satisfactory particle size and compressibility. The outcome indicated that with the increase in feed rate, the powder yield and Carr’s index decreases but particle size increases. On the other hand, as the inlet temperature increases, powder yield and Carr’s index increases.

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