scholarly journals Effects of Process and Formulation Parameters on Submicron Polymeric Particles Produced by a Rapid Emulsion-Diffusion Method

Nanomaterials ◽  
2022 ◽  
Vol 12 (2) ◽  
pp. 229
Author(s):  
Clara Luisa Domínguez-Delgado ◽  
Zubia Akhtar ◽  
Godfrey Awuah-Mensah ◽  
Braden Wu ◽  
Hugh David Charles Smyth

Emulsification-diffusion method is often used to produce polymeric nanoparticles. However, their numerous and/or lengthy steps make it difficult to use widely. Thus, a modified method using solvent blends (miscible/partially miscible in water, 25–100%) as the organic phases to overcome these disadvantages and its design space were investigated. To further simplify the process, no organic/aqueous phase saturation and no water addition after the emulsification step were performed. Biodegradable (PLGA) or pH-sensitive (Eudragit® E100) nanoparticles were robustly produced using low/medium shear stirring adding dropwise the organic phase into the aqueous phase or vice versa. Several behaviors were also obtained: lowering the partially water-miscible solvent ratio relative to the organic phase or the poloxamer-407 concentration; or increasing the organic phase polarity or the polyvinyl alcohol concentration produced smaller particle sizes/polydispersity. Nanoparticle zeta potential increased as the water-miscible solvent ratio increased. Poloxamer-407 showed better performance to decrease the particle size (~50 nm) at low concentrations (≤1%, w/v) compared with polyvinyl alcohol at 1–5% (w/v), but higher concentrations produced bigger particles/polydispersity (≥600 nm). Most important, an inverse linear correlation to predict the particle size by determining the solubility parameter was found. A rapid method to broadly prepare nanoparticles using straightforward equipment is provided.

2021 ◽  
Vol 11 (1) ◽  
pp. 10
Author(s):  
Daria Niewolik ◽  
Grzegorz Dzido ◽  
Katarzyna Jaszcz

Nanoparticles were obtained by nanoprecipitation and by emulsion solvent evaporation (ESE) method. In the ESE method, the size of the particles depended on the type and concentration of surfactant (in the water phase) and the polymer concentration (in the organic phase). The best results were obtained with ionic surfactants, however, the use of such compounds may accelerate the degradation process of polymers. In the nanoprecipitation method, the ratio of solvent (methylene chloride) to non-solvent (hexane) has a significant influence on the particle size. The smallest particles were obtained with a solvent to non-solvent ratio of 1:150.


Blood ◽  
2013 ◽  
Vol 122 (21) ◽  
pp. 4918-4918
Author(s):  
Ran Liu ◽  
Yonglu Wang ◽  
Liyao Wang ◽  
Jian Cheng ◽  
Guohua Xia ◽  
...  

Abstract A functional polymer composed of PLGA, PLL and PEG was synthesized, which was used as carrier material for fabricating drug delivery system of nanoparticles. PLGA-PLL-PEG nanoparticles simultaneously loaded with daunorubicin (DNR) and tetrandrine (Tet) were prepared in order to inhibit MDR activity and enhance the antitumor activity of DNR. A modified double-emulsion solvent evaporation/diffusion method was used to increase the incorporation of DNR (hydrophilic) and Tet (hydrophobic) into PLGA-PLL-PEG nanoparticles (NPs). The influence of various processing parameters on particle size and drug loadings were investigated systematically, such as the molecular weight, such as the molecular weight and concentration of PLGA-PLL-PEG, volume ratio of acetone to dichloromethane, PVA concentration in the external aqueous phase, the volume ratio of internal aqueous phase to external aqueous phase and the surfactants of internal aqueous phase. The particle size of the nanoparticles produced by optimized formulation and preparation was 213.0±12 nm (n = 3) with low polydispersity index (0.075 ± 0.023, n = 3). Transmission electron microscopy (TEM) examination showed that the morphology of the prepared nanoparticles was spherical in shape with a smooth surface. The drug loadings were 3.63±0.15% for DNR and 4.27±0.13% for Tet (n = 3). The entrapment efficiencies were 70.23±1.91% for DNR and 86.5±0.7% for Tet (n = 3). The release of DNR and Tet were sustained over one week. The PLGA-PLL-PEG-NPs formulation was potentially useful for hydrophilic and hydrophobic drugs that require efficient delivery to cancer cells. Disclosures: No relevant conflicts of interest to declare.


2020 ◽  
Author(s):  
Muhammad Ijaz Khan ◽  
Naveed Ahmed ◽  
Muhammad Farooq Umer ◽  
Amina Riaz ◽  
Nasir Mehmood Ahmad ◽  
...  

AbstractIntricate formulation methods and/or use of sophisticated equipment limit the prevalence of liposomal dosage-forms. Simple techniques are developed to assemble amphiphiles into globular lamellae while transiting from immiscible organic to the aqueous phase. Various parameters are optimized by injecting chloroform solution of amphiphiles into the aqueous phase and subsequent removal of the organic phase. Further simplification is achieved by reorienting amphiphiles through a spontaneous phase transition in a swirling biphasic system during evaporation of the organic phase under vacuum. Although the chloroform injection yields smaller size and PDI yet spontaneous phase transition method overrides simplicity and productivity. The size distribution of liposomes and solid/solvent ratio in both or any phases of formulation show direct relation. Surface charge dependant large unilamellar vesicles with a narrow distribution have PDI <0.4 in 10 μM saline. As small and monodisperse liposomes are prerequisites in targeted drug delivery strategies. Hence the desired size distribution <200 d.nm and PDI <0.15 is obtained through serial membrane-filtration method. Phosphatidylcholine/water 4 μmol/ml is achieved at a temperature of 10°C below the phase-transition temperature of phospholipids ensuing suitability for thermolabile entities and high entrapment efficiency. Both methods furnish the de-novo rearrangement of amphophiles into globular lamellae aiding in the larger entrapped volume. The immiscible organic phase facilitates faster and complete removable of the organic phase. High cholesterol content (55.6 mol%) imparts stability in primary hydration medium at 5+3°C for 6 months in light-protected type-1 glass vial. Collectively the reported methods are novel, scalable, time-efficient yielding high productivity in simple equipment.


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):  
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. 


1979 ◽  
Vol 44 (12) ◽  
pp. 3656-3664
Author(s):  
Oldřich Navrátil ◽  
Jiří Smola ◽  
Rostislav Kolouch

Extraction of hafnium(IV) was studied from solutions of mixtures of perchloric and nitric acids and of perchloric and hydrochloric acids for constant ionic strength, I = 2, 4, 6, or 8, and for cHf 4 . 10-4 mol l-1. The organic phase was constituted by solutions of some acidic or neutral organophosphorus reagents or of 2-thenoyltrifluoroacetone, 1-phenyl-3-methyl-4-benzoyl-5-pyrazolone, or N-benzoyl-N-phenylhydroxylamine in benzene, chloroform, or n-octane. A pronounced synergic extraction of hafnium proceeds only on applying organophosphorus reagents from an aqueous phase whose acidity is not lower than 3M-(HClO4 + HNO3) or 5M-(HClO4 + HCl). The synergic effect was not affected markedly by a variation of the initial concentration of hafnium in the range 1 . 10-8 -4 .10-4 mol l-1, it lowered with increasing initial concentration of the organophosphorus reagent and decreasing concentration of the H+ ions. It is suggested that the hafnium passes into the organic phase in the form of mixed complexes, the salting-out effect of perchloric acid playing an appreciable part.


2019 ◽  
Vol 0 (0) ◽  
Author(s):  
Ashraf Farshbaf-Sadigh ◽  
Hoda Jafarizadeh-Malmiri ◽  
Navideh Anarjan ◽  
Yahya Najian

Abstract Ginger oil in water (O/W) nanoemulsions, were produced using phase inversion composition method and Tween 80, as emulsifier. Effects of processing parameters namely, stirring rate (100 to1000 rpm) and water addition rate (1–10 mL/min) were evaluated on the physico-chemical, morphological, antioxidant and antimicrobial properties of the prepared O/W nanoemulsions using response surface methodology (RSM). Results indicated that well dispersed and spherical ginger nanodroplets were formed in the nanoemulsions with minimum particle size (8.80 nm) and polydispersity index (PDI, 0.285) and maximum zeta potential value (−9.15 mV), using stirring rate and water addition rate of 736 rpm and 8.18 mL/min, respectively. Insignificant differences between predicted and experimental values of the response variables, indicated suitability of fitted models using RSM. Mean particle size of the prepared nanoemulsion using optimum conditions were changed from 8.81 ± 1 to 9.80 ± 1 nm, during 4 weeks of storage, which revealed high stability of the resulted ginger O/W nanoemulsion. High antioxidant activity (55.4%), bactericidal (against Streptococcus mutans) and fungicidal (against Aspergillus niger) activities of the prepared nanoemulsion could be related to the presence of gingerols and shogaols, a group of phenolic alkanones, in the ginger oil, which those were detected by gas chromatography method.


2013 ◽  
Vol 813 ◽  
pp. 399-402
Author(s):  
Chimsook Thitipha ◽  
Thitiphan Chimsook

The aim of present work was to prepare floating microsphere of ketoprofen using matrix polymer of chitosan and poly (ethylene glycol) by solvent diffusion method. The floating microsphere of ketoprofen was prepared from matrix polymer of chitosan and poly (ethylene glycol) with various composition ratios and evaluated such as particle size, drug compatibility and drug release of microspheres. The scanning electron microscopy of microspheres confirmed their hollow structures with smooth surface. Formulation CPK 4 to CPK 6 exhibited the best controlled release pattern in ketoprofen. The concentration and size of poly (ethylene-glycol) affected the particle size, percentage yield and drug release of microspheres.


2015 ◽  
Vol 732 ◽  
pp. 161-164 ◽  
Author(s):  
Jan Vesely ◽  
Lukas Horny ◽  
Hynek Chlup ◽  
Milos Beran ◽  
Milan Krajicek ◽  
...  

The effects of the polyvinyl alcohol (PVA) concentration on mechanical properties of hydrogels based on blends of native or denatured collagen / PVA were examined. Blends of PVA with collagen were obtained by mixing the solutions in different ratios, using glycerol as a plasticizer. The solutions were cast on polystyrene plates and the solvent was allowed to evaporate at room temperature. Uniaxial tensile tests were performed in order to obtain the initial modulus of elasticity (up to deformation 0.1), the ultimate tensile stress and the deformation at failure of the material in the water-saturated hydrogel form. It was found that the material was elastic and the addition of PVA helped to enhance both the ultimate tensile stress and modulus of elasticity of the films. Samples prepared from denaturated collagen showed the higher ultimate tensile stress and the deformation at failure in comparison with those prepared from native collagen. The results suggest that we could expect successful application of the collagen/PVA biomaterial for tissue engineering.


2021 ◽  
Author(s):  
Dehao Fu ◽  
Yuanyuan Guo ◽  
Yongwei Liu ◽  
Chen Shi ◽  
Tingting Wu ◽  
...  

Abstract BackgroundOsteoporosis (OP) is a systemic skeletal disease marked by bone mass reduction and bone tissue destruction. Hormone replacement therapy is an effective treatment for post-menopausal OP, but estrogen has poor tissue selectivity and severe side effects.ResultsIn this study, we constructed a poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs)-based drug delivery system to co-load 17β estradiol (E2) and iron oxide (Fe3O4) together, modified with alendronate (AL) to achieve bone targeting and realize a magnetically remote-controllable drug release. The NPs were fabricated through the emulsion solvent diffusion method. The particle size was approximately 200 nm while the encapsulation efficiency of E2 was 58.34 ± 9.21%. The NPs were found to be spherical with a homogenous distribution of particle size. The NPs showed good stability, good biocompatibility, high encapsulation ability of E2 and excellent magnetic properties. The NPs could be effectively taken up by Raw 264.7 cells and were effective in enriching drugs in bone tissue. The co-loaded NPs exposed to an external magnetic field ameliorated OVX-induced bone loss through increased BV/TV, decreased Tb.N and Tb.Sp, improved bone strength, increased PINP and OC, and downregulated CTX and TRAP-5b. The haematological index and histopathological analyses displayed the NPs had less side effects on non-skeletal tissues.ConclusionsThis study presented a remote-controlled release system based on bone-targeted multifunctional NPs and a new potential approach to bone-targeted therapy of OP.


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