scholarly journals Effect of Poly(vinyl alcohol) on Nanoencapsulation of Budesonide in Chitosan Nanoparticles via Ionic Gelation and Its Improved Bioavailability

Polymers ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 1101 ◽  
Author(s):  
Georgia Michailidou ◽  
Nina Maria Ainali ◽  
Eleftheria Xanthopoulou ◽  
Stavroula Nanaki ◽  
Margaritis Kostoglou ◽  
...  

Chitosan (CS) is a polymer extensively used in drug delivery formulations mainly due to its biocompatibility and low toxicity. In the present study, chitosan was used for nanoencapsulation of a budesonide (BUD) drug via the well-established ionic gelation technique and a slight modification of it, using also poly(vinyl alcohol) (PVA) as a surfactant. Scanning electron microscopy (SEM) micrographs revealed that spherical nanoparticles were successfully prepared with average sizes range between 363 and 543 nm, as were measured by dynamic light scattering (DLS), while zeta potential verified their positive charged surface. X-ray diffraction (XRD) patterns revealed that BUD was encapsulated in crystalline state in nanoparticles but with a lower degree of crystallinity than the neat drug, which was also proven by differential scanning calorimetry (DSC) and melting peak measurements. This could be attributed to interactions that take place between BUD and CS, which were revealed by FTIR and by an extended computational study. An in vitro release study of budesonide showed a slight enhancement in the BUD dissolution profile, compared to the neat drug. However, drug release was substantially increased by introducing PVA during the nanoencapsulation procedure, which is attributed to the higher amorphization of BUD on these nanoparticles. The release curves were analyzed using a diffusion model that allows estimation of BUD diffusivity in the nanoparticles.

2018 ◽  
Vol 10 (1) ◽  
pp. 115 ◽  
Author(s):  
Napaphak Jaipakdee ◽  
Thaned Pongjanyakul ◽  
Ekapol Limpongsa

Objective: The objectives of this study were to prepare and characterize a buccal mucoadhesive patch using poly (vinyl alcohol) (PVA), poly (vinyl pyrrolidone) (PVP) as a mucoadhesive matrix, Eudragit S100 as a backing layer, and lidocaine HCl as a model drug.Methods: Lidocaine HCl buccal patches were prepared using double casting technique. Molecular interactions in the polymer matrices were studied using attenuated total reflectance-fourier transform infrared spectroscopy (ATR-FTIR), differential scanning calorimetry (DSC) and X-ray diffractometry. Mechanical and mucoadhesive properties were measured using texture analyzer. In vitro permeation of lidocaine HCl from the patch was conducted using Franz diffusion cell.Results: Both of the free and lidocaine HCl patches were smooth and transparent, with good flexibility and strength. ATR-FTIR, DSC and X-ray diffractometry studies confirmed the interaction of PVA and PVP. Mechanical properties of matrices containing 60% PVP were significantly lower than those containing 20% PVP (*P<0.05). Mucoadhesive properties had a tendency to decrease with the concentration of PVP in the patch. The patch containing 60% PVP had significantly lower muco-adhesiveness than those containing 20% PVP (*P<0.05). In vitro permeation revealed that the pattern of lidocaine HCl permeation started with an initial fast permeation, followed by a slower permeation rate. The initial permeation fluxes follow the zero-order model of which rate was not affected by the PVP concentrations in the PVA/PVP matrix.Conclusion: Mucoadhesive buccal patches fabricated with PVA/PVP were successfully prepared. Incorporation of PVP in PVA/PVP matrix affected the strength of polymeric matrix and mucoadhesive property of patches.


Author(s):  
MONTUKUMAR PATEL ◽  
NIRAV V. PATEL ◽  
TEJAS B. PATEL

Objective: The primary objective of the current research was to prepare rilpivirine loaded Nanoparticles containing Chitosan using the ionic gelation method for HIV infections. Methods: The nanoparticles of rilpivirine were prepared using the ionic gelation technique. Further, nanoparticles were characterized by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and in vitro drug release. Results: The optimized nanoparticles were found with a particle size of 130.30±5.29 nm (mean±SD) and entrapment efficiency (% EE) of 77.10±0.50%. Scanning electron microscopy technique exposed spherical particles with uniform size. It was observed that the nanoparticles created showed the absence of the crystalline nature of the drug and its switch to the amorphous state. Results showed that more than 45% of the pure drug is released in 50 min and after 90 min almost about 95% of the drug is released. Conclusion: The research study concluded that the in vitro release profile of nanoparticles was found to be sustained up to 24 hr. Sustained release of the rilpivirine could improve patient obedience to drug regimens, growing action effectiveness. 


1993 ◽  
Vol 331 ◽  
Author(s):  
Becky J. Ficek ◽  
Nicholas A. Peppas

AbstractPoly(vinyl alcohol) microparticles were prepared by a novel freezing-thawing process in the absence of a crosslinking agent. An aqueous PVA solution to which 1.25 wt% sodium lauryl sulfate was added was dispersed in corn oil. The system was agitated and the ensuing suspended droplets of PVA solution were solidified by a cyclic freezing-thawing process. Key parameters of the process were the PVA to corn oil ratio, the amount of surfactant added, agitation speed, number of freeze cycles, temperatures of freezing and thawing, and presence of additional components.Crystallization was observed during the freezing-thawing process. The degree of crystallinity was measured with differential scanning calorimetry. Bovine serum albumin was incorporated into the particles by an absorption technique. Studies of BSA release from the microparticles in vitro showed that the release could be prolonged for up to 7 days. BSA diffusion coefficients were calculated from these data and the release mechanism was identified.


2020 ◽  
Vol 26 (6) ◽  
pp. 1155-1164
Author(s):  
Camila Fernandes Higa ◽  
Thatyanne Gradowski ◽  
Selene Elifio-Esposito ◽  
Marcelo Fernandes de Oliveira ◽  
Paulo Inforçatti ◽  
...  

Purpose This study aims to investigate the production of scaffolds by selective laser sintering (SLS) using poly(vinyl alcohol) (PVA) polymer, for in vitro studies, a relatively new and growing area in which scaffolds could be used in the design of three-dimensional models for in vitro disease model or tissue equivalent for safety and effectiveness tests. Design/methodology/approach The influence of the SLS process parameters laser power, 26 W and 32 W, and number of laser scans, 1, 2, 4 and 6, on the surface microstructure of the samples and on the degree of crystallinity and chemical stability of PVA material, was investigated using powder with particle size of 20-320 µm. Laser sintered PVA samples were subjected to cell culture tests using osteoblastic cells derived from human osteosarcoma (SaOs-2). Findings The laser power has no significant influence on the microstructure of the laser-sintered samples, however the number of scans has a considerable influence on the sintering degree; the SLS process causes a decrease in the degree of crystallinity and changes the chemical structure of the as-received PVA, especially when using higher laser power and more number of scans. Preliminary in vitro cell culture tests show that the laser-sintered PVA material is biocompatible with SaOs-2 cells. Originality/value SLS offers good potential for the fabrication of scaffolds and thus, may be applied as an alternative to conventional scaffold fabrication processes to overcome their limitations.


2013 ◽  
Vol 709 ◽  
pp. 215-220 ◽  
Author(s):  
Dou Dou Zhang ◽  
Li Xing Dai

A series of poly(vinyl alcohol)/silk fibroin nanofibers loaded with 10 wt.% vanillin were successfully prepared from aqueous solutions via electrospinning. The morphology, weight loss and swelling ability of the nanofibers were characterized. The controlled release characteristics of vanillin in the nanofiber mats were evaluated by in vitro release test. Vanillin-loaded nanofibers had smooth surfaces like drug-free nanofibers, and showed thinner diameter than the latter. The release rate of vanillin in the nanofiber mats decreased with the increment of silk fibroin content, so by regulating the content the drug release could be controlled. Moreover, after treated with ethanol the nanofiber mats showed better stability against disintegration in water and sustained release rate of vanillin than untreated mats.


2018 ◽  
Vol 83 (11) ◽  
pp. 1243-1259
Author(s):  
Oum Larbi ◽  
Haouaria Merine ◽  
Youssef Ramli ◽  
Fawzia Toumi ◽  
Kaddour Guemra ◽  
...  

Hydrochlorothiazide (HCTZ), which was developed and introduced in the late 1950s, is still one of the most frequently employed drugs in antihypertensive treatments. Its poor aqueous solubility is one of the reasons for its limited bioavailability after oral administration. The present paper provides details of the preparation of HCTZ-loaded microspheres by the solvent evaporation technique. A total of seven formulations were prepared using ethyl cellulose, poly(?-caprolactone) (PCL), ?-cyclodextrin (?-CD) and synthesized poly-(methyl methacrylate) (PMMA) of different molecular weights in different drug-to-carrier ratios in order to investigate their effect on the encapsulation efficiency and drug release kinetics. The prepared formulations were characterized by Fourier transform-infrared (FTIR) spectroscopy, powder X-ray diffractometry, differential scanning calorimetry, yield, drug loading, optical microscopy, surface morphology by scanning electron microscopy (SEM), and in vitro release studies in simulated gastrointestinal tract fluid. The loading efficiency was found in the range from 18?0.34 to 39?0.95 %. The microspheres were spherical, and the mean Sauter diameter (d32) of the obtained microparticles ranged from 26?0.16 to 107?0.58 ?m. The presence of the drug and polymer carriers in the microparticles was confirmed by FTIR spectroscopy and XRD analysis. In vitro dissolution studies showed that the release rate was largely affected by the characteristics of the microparticles, namely the particle size and the nature of the matrix. The release data are best fitted to the Higuchi model with high correlation coefficients (r?).


2011 ◽  
Vol 68 (7) ◽  
pp. 1905-1919 ◽  
Author(s):  
K. Madhusudana Rao ◽  
B. Mallikarjuna ◽  
K. S. V. Krishna Rao ◽  
M. N. Prabhakar ◽  
K. Chowdoji Rao ◽  
...  

Author(s):  
Gayatri Patel ◽  
Rutu Patel ◽  
Balaram Gajra ◽  
R. Parikh

ABSTRACTObjective: The objective of this work was to formulate, optimize, and characterize ganciclovir (GCV) loaded dry chitosan nanoparticles (CSNPs).Methods: The GCV loaded CSNPs was prepared by ionic gelation method. Box–Behnken design was employed to optimize the influence of independentprocess and formulation variables like drug to polymer ratio, concentration of sodium tripolyphosphate, and stirring time (min) on the dependentvariables such as particle size (PS) and drug encapsulation efficiency (% EE). The optimum conditions were determined by regression analysis of theoutput data.Results: The independent variables had interactive effects and they affected both the responses. The optimum formulation had PS within the range of100-120 nm and % EE between 85% and 86%. The prepared GCV loaded CSNPs were dried by fluidized bed drying method. Fourier transform infraredspectra showed there was no physicochemical interaction between GCV and CS. Powder X-ray diffraction study showed less intense crystalline peaksindicated that GCV may exist in the formulation as amorphous nanodispersion or molecular dispersion form. Differential scanning calorimetry studywas performed which indicated that the drug was molecularly dispersed inside the matrix of CS. Higuchi model was the best to fit the in vitro releasedata for the GCV loaded CSNPs.Conclusion: From the results, it can be concluded that the GCV loaded dry CSNPs were formulated, optimized, and characterized using desiredpharmacotechnical properties.Keywords: Chitosan nanoparticles, Box–Behnken design, Sodium tripolyphosphate, Ionic gelation.


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