scholarly journals Fabrication of Supercritical Antisolvent (SAS) Process-Assisted Fisetin-Encapsulated Poly (Vinyl Pyrrolidone) (PVP) Nanocomposites for Improved Anticancer Therapy

Nanomaterials ◽  
2020 ◽  
Vol 10 (2) ◽  
pp. 322 ◽  
Author(s):  
Lin-Fei Chen ◽  
Pei-Yao Xu ◽  
Chao-Ping Fu ◽  
Ranjith Kumar Kankala ◽  
Ai-Zheng Chen ◽  
...  

Due to its hydrophobicity, fisetin (FIS) often suffers from several limitations in terms of its applicability during the fabrication of pharmaceutical formulations. To overcome this intrinsic limitation of hydrophobicity, we demonstrate here the generation of poly (vinyl pyrrolidone) (PVP)-encapsulated FIS nanoparticles (FIS-PVP NPs) utilizing a supercritical antisolvent (SAS) method to enhance its aqueous solubility and substantial therapeutic effects. In this context, the effects of various processing and formulation parameters, including the solvent/antisolvent ratio, drug/polymer (FIS/PVP) mass ratio, and solution flow rate, on the eventual particle size as well as on distribution were investigated using a 23 factorial experimental design. Notably, the FIS/PVP mass ratio significantly affected the morphological attributes of the resultant particles. Initially, the designed constructs were characterized systematically using various techniques (e.g., chemical functionalities were examined with Fourier-transform infrared (FTIR) spectroscopy, and physical states were examined with X-ray diffraction analysis (XRD) and differential scanning calorimetry (DSC) techniques). In addition, drug release as well as cytotoxicity evaluations in vitro indicated that the nanosized polymer-coated particles showed augmented performance efficiency compared to the free drug, which was attributable to the improvement in the dissolution rate of the FIS-PVP NPs due to their small size, facilitating a higher surface area over the raw form of FIS. Our findings show that the designed SAS process-assisted nanoconstructs with augmented bioavailability, have great potential for applications in pharmaceutics.

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.


2015 ◽  
Vol 2015 ◽  
pp. 1-12 ◽  
Author(s):  
Ying Zhang ◽  
Xiuhua Zhao ◽  
Wengang Li ◽  
Yuangang Zu ◽  
Yong Li ◽  
...  

TotalPanaxnotoginsenosides nanoparticles, typical multicomponent extracts from traditional Chinese medicine, were prepared with a supercritical antisolvent (SAS) process using ethanol as solvent and carbon dioxide as antisolvent. The optimum conditions were determined to be as follows: TPNS solution concentration of 2.5 mg/mL, TPNS solution flow rate of 6.6 mL/min, precipitation temperature of 40°C, and precipitation pressure of 20 MPa. Under the optimum conditions, TPNS nanoparticles with a MPS of 141.5 ± 18.2 nm and total saponins amounts (TSA) of 78.9% were obtained. The TPNS nanoparticles obtained were characterized by scanning electron microscopy (SEM), dynamic light scattering (DLS), Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimeters (DSC), and high performance liquid chromatography (HPLC). The results showed that the chemical and crystal structure of the obtained TPNS nanoparticles has not changed. Dissolutionin vitrostudies showed that the solubility and dissolution rate of notoginsenosides R1 and ginsenoside Rb1 in TPNS nanoparticles are higher than these in raw TPNS, with no obvious difference in Rg1. These results suggest that TPNS nanoparticles can be helpful to the improvement of its bioavailability for the treatment of cardiovascular diseases.


Materials ◽  
2020 ◽  
Vol 13 (14) ◽  
pp. 3087
Author(s):  
Rana Smaida ◽  
Luc Pijnenburg ◽  
Silvia Irusta ◽  
Erico Himawan ◽  
Gracia Mendoza ◽  
...  

The treatment of osteochondral defects remains a challenge. Four scaffolds were produced using Food and Drug Administration (FDA)-approved polymers to investigate their therapeutic potential for the regeneration of the osteochondral unit. Polycaprolactone (PCL) and poly(vinyl-pyrrolidone) (PVP) scaffolds were made by electrohydrodynamic techniques. Hydroxyapatite (HAp) and/or sodium hyaluronate (HA) can be then loaded to PCL nanofibers and/or PVP particles. The purpose of adding hydroxyapatite and sodium hyaluronate into PCL/PVP scaffolds is to increase the regenerative ability for subchondral bone and joint cartilage, respectively. Human bone marrow-derived mesenchymal stem cells (hBM-MSCs) were seeded on these biomaterials. The biocompatibility of these biomaterials in vitro and in vivo, as well as their potential to support MSC differentiation under specific chondrogenic or osteogenic conditions, were evaluated. We show here that hBM-MSCs could proliferate and differentiate both in vitro and in vivo on these biomaterials. In addition, the PCL-HAp could effectively increase the mineralization and induce the differentiation of MSCs into osteoblasts in an osteogenic condition. These results indicate that PCL-HAp biomaterials combined with MSCs could be a beneficial candidate for subchondral bone regeneration.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 556
Author(s):  
Luca Éva Uhljar ◽  
Sheng Yuan Kan ◽  
Norbert Radacsi ◽  
Vasileios Koutsos ◽  
Piroska Szabó-Révész ◽  
...  

Nanofibers of the poorly water-soluble antibiotic ciprofloxacin (CIP) were fabricated in the form of an amorphous solid dispersion by using poly(vinyl pyrrolidone) as a polymer matrix, by the low-cost electrospinning method. The solubility of the nanofibers as well as their in vitro diffusion were remarkably higher than those of the CIP powder or the physical mixture of the two components. The fiber size and morphology were optimized, and it was found that the addition of the CIP to the electrospinning solution decreased the nanofiber diameter, leading to an increased specific surface area. Structural characterization confirmed the interactions between the drug and the polymer and the amorphous state of CIP inside the nanofibers. Since the solubility of CIP is pH-dependent, the in vitro solubility and dissolution studies were executed at different pH levels. The nanofiber sample with the finest morphology demonstrated a significant increase in solubility both in water and pH 7.4 buffer. Single medium and two-stage biorelevant dissolution studies were performed, and the release mechanism was described by mathematical models. Besides, in vitro diffusion from pH 6.8 to pH 7.4 notably increased when compared with the pure drug and physical mixture. Ciprofloxacin-loaded poly(vinyl pyrrolidone) (PVP) nanofibers can be considered as fast-dissolving formulations with improved physicochemical properties.


Pharmaceutics ◽  
2019 ◽  
Vol 11 (8) ◽  
pp. 417 ◽  
Author(s):  
Emese Sipos ◽  
Nóra Kósa ◽  
Adrienn Kazsoki ◽  
Zoltán-István Szabó ◽  
Romána Zelkó

Aceclofenac-loaded poly(vinyl-pyrrolidone)-based nanofiber formulations were prepared by electrospinning to obtain drug-loaded orally disintegrating webs to enhance the solubility and dissolution rate of the poorly soluble anti-inflammatory active that belongs to the BCS Class-II. Triethanolamine-containing ternary composite of aceclofenac-poly(vinyl-pyrrolidone) nanofibers were formulated to exert the synergistic effect on the drug-dissolution improvement. The composition and the electrospinning parameters were changed to select the fibrous sample of optimum fiber characteristics. To determine the morphology of the nanofibers, scanning electron microscopy was used. Fourier transform infrared spectroscopy (FT-IR), and differential scanning calorimetry (DSC) were applied for the solid-state characterization of the samples, while the drug release profile was followed by the in vitro dissolution test. The nanofibrous formulations had diameters in the range of few hundred nanometers. FT-IR spectra and DSC thermograms indicated the amorphization of aceclofenac, which resulted in a rapid release of the active substance. The characteristics of the selected ternary fiber composition (10 mg/g aceclofenac, 1% w/w triethanolamine, 15% w/w PVPK90) were found to be suitable for obtaining orally dissolving webs of fast dissolution and potential oral absorption.


2011 ◽  
Vol 217-218 ◽  
pp. 1497-1503
Author(s):  
Jie Liang Wang ◽  
Ai Juan Gu ◽  
Guo Zheng Liang

Poly vinyl pyrrolidone (PVP(K30)) / Bisphenol A Dicyanate ester (BADCy) blends were fabricated to increase the toughness of BADCy by blending processing in this paper. Curing parameters were determined by gelation time curves and differential scanning calorimetry (DSC) of the systems. Fourier transform infrared spectrometry (FTIR) and DSC data were employed to show the curing behavior and kinetics of the systems. Mechanical properties of the cured resin had been improved rapidly with the increasing of PVP(K30) at low mass fraction, but would decrease when mass fractions of PVP(K30) were higher than 15%. Scanning electron micrograph (SEM) was applied to show the microstructures of the cured matrixes. Based on the thermogravimetric analysis (TGA) curves, water absorption curves, SEM images and dielectric properties of the blends, it can be concluded that the addition of PVP(K30) can improve the toughness of BADCy greatly with little loss of other properties.


2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Toshihiro Inami ◽  
Yasuhiro Tanimoto ◽  
Masayuki Ueda ◽  
Yo Shibata ◽  
Satoshi Hirayama ◽  
...  

This work describes the fabrication, optimization, and characterization of electrospun fibrous poly(D,L-lactic acid) (PDLLA) for biomedical applications. The influences of the polymer concentration of the electrospinning solution (5, 10, or 15 wt%) and the solution flow rate (0.1, 0.5, 1.0, or 2.0 mL/h) on the morphology of the obtained fibrous PDLLA were evaluated. Thein vitrobiocompatibility of two types of PDLLA, ester terminated PDLLA (PDLLA-R) and carboxyl terminated PDLLA (PDLLA-COOH), was evaluated by monitoring apatite formation on samples immersed in Hanks’ balanced salt (HBS) solution. 15 wt% polymer solution was the most beneficial for preparing a fibrous PDLLA structure. Meanwhile, no differences in morphology were observed for PDLLA prepared at various flow rates. Apatite precipitate is formed on both types of PDLLA only 1 day after immersion in HBS solution. After 7 days of immersion, PDLLA-COOH showed greater apatite formation ability compared with that of PDLLA-R, as measured by thin-film X-ray diffraction. The results indicated that the carboxyl group is effective for apatite precipitation in the body environment.


Author(s):  
Abdul Ahad Hindustan ◽  
U Anand Babu ◽  
K Nagesh ◽  
D Sai Kiran ◽  
K Bindu Madhavi

The main purpose of the present work was to develop matrix tablets of Glimepiride with Datura stramonium leaves mucilage and Poly Vinyl Pyrrolidone and to study its functionality as a matrix forming agent for sustained release tablet formulations. Mucilage from Datura stramonium leaves was extracted, isolated, purified and characterized. Physicochemical properties of the dried powdered mucilage of Datura stramonium leaves were studied. Various formulations of Glimepiride Datura stramonium leave mucilage and Poly Vinyl Pyrrolidone were prepared. The formulated tablets were tested for mechanical properties, friability, swelling behavior, in vitro drug release pattern and the dissolution data was treated with mathematical modeling and the optimized formulation was tested for accelerated stability studies. The formulated tablets were found to have good mechanical properties, good swelling properties. The in vitro dissolution data was perfectly fitting to zero order and the release of drug from the formulation followed Higuchi’s release. The accelerated stability studies revealed that the tablets retain their characteristics even after stressed storage conditions. From this study it was concluded that the dried Datura stramonium leaves mucilage and Poly Vinyl Pyrrolidone combination can be used as a matrix forming material for making sustained release matrix tablets. DOI: http://dx.doi.org/10.3126/kuset.v8i1.6044 KUSET 2012; 8(1): 63-72


Sign in / Sign up

Export Citation Format

Share Document