Preparation of Risedronate Nanoparticles by Solvent Evaporation Technique

Vaculíková, Eliška; Plachá, Daniela; Pisárčik, Martin; Peikertová, Pavlína; Dědková, Kateřina; Devı́nsky, Ferdinand; Jampílek, Josef

doi:10.3390/molecules191117848

Cited by 21 publications

(16 citation statements)

References 23 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Each run was carried out in triplicate to assure accuracy and reproducibility. FLC nanoparticles were prepared and coated with PEG by applying solvent antisolvent precipitation method as reported with slight modification [4,12]. The calculated amount (200 mg) of the drug and polymer was dissolved in 10 ml of ethanol (solvent) and added dropwise to 50 ml of polymer aqueous solution (antisolvent) stirred at 50 rpm for 30 min.…”

Section: Factorial Design and Preparation Of Flc-peg-npsmentioning

confidence: 99%

Hydrogel Containing PEG-Coated Fluconazole Nanoparticles with Enhanced Solubility and Antifungal Activity

et al. 2018

View full text Add to dashboard Cite

Purpose The aim of this study was to prepare fluconazole (FLC) nanoparticles coated with polyethylene glycol (PEG) in the form of FLC-PEG-NPs and optimize the size and entrapment efficiency. Methods Nine formulae were prepared by solvent antisolvent precipitation technique according to full 3 2 factorial designs. The effects of PEG molecular weight (X 1 ) and the drug polymer ratio (X 2 ) on the particle size (Y 1 ) and entrapment efficiency (Y 2 ) were explored. The prepared FLC-PEG-NPs were investigated for particle size, count rate, PDI, zeta potential, and morphology. Carbopol hydrogel was prepared, loaded with optimized FLC-PEG-NPs, and characterized for pH, FLC content, viscosity, homogeneity and spreadability, in vitro release, skin permeation, and antifungal activity. Results The formulated nanoparticles were uniform in size and spherical in shape with slightly rough surface and free from aggregations. The effect of PEG molecular was antagonistic on the particle size and was agonistic on EE %. The release of drug from hydrogel containing pure FLC was always lower than that from hydrogel containing FLC-PEG-NPs. The kinetic analysis of drug release obeys first-order release model and super case II transport mechanism. The cumulative amount of drug permeated applying hydrogel containing optimized FLC-PEG-NPs was significantly higher than the amount permeated using pure fluconazole containing hydrogel. The antifungal activity of hydrogel containing FLC in the form of optimized PEG-coated nanoparticles was better than hydrogel containing pure drug as indicated by relatively high inhibition zone using agar well-diffusion method. Conclusion Small spherical FLC nanoparticles with enhanced in vitro drug release as well as improved antifungal activity could be achieved by using PEG-coated fluconazole nanoparticles.

show abstract

Section: Factorial Design and Preparation Of Flc-peg-npsmentioning

confidence: 99%

Hydrogel Containing PEG-Coated Fluconazole Nanoparticles with Enhanced Solubility and Antifungal Activity

et al. 2018

View full text Add to dashboard Cite

show abstract

“…The majority of new drugs exhibit poor aqueous solubility, which affects their low bioavailability after oral delivery. Many strategies have been described to increase the dissolution rate of drugs by reducing their particle size and salt formation, using surfactants, cyclodextrins, liposomes or nanoparticles [1,2,3,4]. A relatively new approach for poorly soluble drugs is lipid-based formulations, particularly self-emulsifying drug delivery systems (SEDDS) [5,6].…”

Section: Introductionmentioning

confidence: 99%

Development and Evaluation of Liquid and Solid Self-Emulsifying Drug Delivery Systems for Atorvastatin

et al. 2015

View full text Add to dashboard Cite

Abstract:The objective of this work was to design and characterize liquid and solid self-emulsifying drug delivery systems (SEDDS) for poorly soluble atorvastatin. To optimize the composition of liquid atorvastatin-SEDDS, solubility tests, pseudoternary phase diagrams, emulsification studies and other in vitro examinations (thermodynamic stability, droplet size and zeta potential analysis) were performed. Due to the disadvantages of liquid SEDDS (few choices for dosage forms, low stability and portability during the manufacturing process), attempts were also made to obtain solid SEDDS. Solid SEDDS were successfully obtained using the spray drying technique from two optimized liquid formulations, CF3 and OF2. Despite liquid SEDDS formulation, CF3 was characterized by lower turbidity, higher percentage transmittance and better self-emulsifying properties, and based on the in vitro dissolution study it can be concluded that better solubilization properties were exhibited by solid formulation OF2. Overall, the studies demonstrated the possibility of formulating liquid and solid SEEDS as promising carriers of atorvastatin. SEDDS, with their unique solubilization properties, provide the opportunity to deliver lipophilic drugs to the gastrointestinal tract in a solubilized state, avoiding dissolution-a restricting factor in absorption rate of BCS Class 2 drugs, including atorvastatin.

show abstract

“… 23 In the NP preparation, the C18 chain of polysorbate 80 is partitioned into the polymer matrix via hydrophobic interactions; however, the hydrogen bonding between the polyoxyethylene group of polysorbate 80 and the carboxyl group of PLGA leads to the covering of polysorbate 80 on the surface of the NPs, 26 which prevents further aggregation among the formed particles by steric repulsion and results in stabilized NPs. 28 In addition, in a previous study, 29 the smallest NP size was achieved with the application of polysorbate 80 compared with the use of other surfactants (including sodium dodecyl sulfate, macrogol 6000, sodium carboxymethyl cellulose, and sodium carboxymethyl dextran). Furthermore, polysorbate 80 is known to be an inhibitor of P-gp, the membrane protein responsible for transporting xenobiotics back into the extracellular space.…”

Section: Resultsmentioning

confidence: 91%

Enhanced oral bioavailability of acetylpuerarin by poly(lactide-co-glycolide) nanoparticles optimized using uniform design combined with response surface methodology

Sun

Xue

Zhang

et al. 2016

DDDT

View full text Add to dashboard Cite

Acetylpuerarin (AP), an acetylated derivative of puerarin, shows brain-protective effects in animals. However, AP has low oral bioavailability because of its poor water solubility. The objective of this study was to design and develop poly(lactide-co-glycolide) (PLGA) nanoparticles (NPs) to enhance the oral bioavailability of AP. The NPs were prepared using a solvent diffusion method optimized via uniform design (UD) combined with response surface methodology (RSM) and characterized by their morphology, particle size, zeta (ζ)-potential, encapsulation efficiency (EE), drug loading (DL), and in vitro drug release. A pharmacokinetic study was conducted in Wistar rats administered a single oral dose of 30 mg/kg AP. The optimized NPs were spherical and uniform in shape, with an average particle size of 145.0 nm, a polydispersity index (PI) of 0.153, and a ζ-potential of −14.81 mV. The release of AP from the PLGA NPs showed an initial burst release followed by a sustained release, following Higuchi’s model. The EE and DL determined in the experiments were 90.51% and 17.07%, respectively. The area under the plasma concentration-time curve (AUC0−∞) of AP-PLGA-NPs was 6,175.66±350.31 h ng/mL, which was 2.75 times greater than that obtained from an AP suspension. This study showed that PLGA NPs can significantly enhance the oral bioavailability of AP.

show abstract

Preparation of Risedronate Nanoparticles by Solvent Evaporation Technique

Cited by 21 publications

References 23 publications

Hydrogel Containing PEG-Coated Fluconazole Nanoparticles with Enhanced Solubility and Antifungal Activity

Hydrogel Containing PEG-Coated Fluconazole Nanoparticles with Enhanced Solubility and Antifungal Activity

Development and Evaluation of Liquid and Solid Self-Emulsifying Drug Delivery Systems for Atorvastatin

Enhanced oral bioavailability of acetylpuerarin by poly(lactide-co-glycolide) nanoparticles optimized using uniform design combined with response surface methodology

Contact Info

Product

Resources

About