scholarly journals Folic acid-containing nanofibers by simultaneous process for transdermal drug delivery:  preparation, characterization, and in vitro biocompatibility

2020 ◽  
Author(s):  
Fatma Nur Parın ◽  
Çiğdem İnci Aydemir ◽  
Gökçe Taner ◽  
Kenan Yıldırım

Abstract Nanofibers with bioactive agents are good candidates for skin-care applications due to high spesific surface area, low density and highly porous structure. In this study, hydrophilic based bioactive nanofibers were produced via an electrospinning and electrospraying simultaneous process. Polyvinyl alcohol (PVA), polyvinyl alcohol-gelatin (PVA-Gel) and polyvinyl alcohol-alginate (PVA-Alg) polymers were used as the matrix material and folic acid (FA) particles were dispersed simultaneously on the surface of these hydrophilic nanofibers. The morphology of the nanofibers (NFs) was uniform and dispersed folic acid particles incorporated into the structure of nanofibers as confirmed by scanning electron microscopy (SEM). Thermal behavior, chemical structure of the composite nanofibers were analyzed/investigated by thermogravimetric analysis (TGA) and Attenuated Total Reflectance-Fourier Transform Infrared Spectroscopy (ATR-FTIR) which showed that no chemical bonding between vitamin and polymers. A controlled release of FA-loaded electrospun fibers were carried out by UV-Vis in vitro study within the 8 hour-period in artificial sweat solutions (acidic media, pH 5,44). The obtained PVA/FA, PVA-Gel/FA and PVA-Alg/FA fibers released 49.6 %, 69.55 % and 50.88 % of the sprayed FA in 8 h, indicating the influence of polymer matrix and polymer-drug interactions, on its release from the polymer matrix. Moreover, biocompatibility of all developed novel NFs was assessed by two different cytotoxicity tests,3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and neutral red uptake (NRU) assay in L929 cell lines. In all cases, it is clearly concluded that these new electrospun fibers had fast-release of the vitamin and the hybrid process is suitable for transdermal patch applications, especially for skin-care products. Moreover, it has been proposed nanofiber with folic acid as a patch may prevent the COVID-19. The results of cytotoxicity assays on L929 cell reveal that all prepared NFs have no or slight cell toxicity. PVA and PVA-Gel with/without FA nanofibers seems more biocompatible than PVA-Alg nanofibers.

2021 ◽  
pp. 152808372199718
Author(s):  
Fatma Nur Parın ◽  
Çiğdem İnci Aydemir ◽  
Gökçe Taner ◽  
Kenan Yıldırım

In this study, hydrophilic based bioactive nanofibers were produced via an electrospinning and electrospraying simultaneous process. Poly(vinyl alcohol) (PVA), poly(vinyl alcohol)-gelatin (PVA-Gel), and poly(vinyl alcohol)-alginate (PVA-Alg) polymers were used as the matrix material and folic acid (FA) particles were dispersed simultaneously on the surface of the nanofibers. The morphology of the nanofibers (NFs) was uniform and confirmed by scanning electron microscopy. Thermal behavior, chemical structure of the composite nanofibers were investigated by thermogravimetric analysis, and Attenuated Total Reflectance-Fourier Transform Infrared Spectroscopy which showed that no chemical bonding between vitamin and polymers. A fast release of FA-loaded electrospun fibers was carried out by UV-Vis in vitro study within the 8 hour-period in artificial sweat solutions (pH 5.44). The obtained PVA/FA, PVA-Gel/FA, and PVA-Alg/FA fibers released 49.6%, 69.55%, and 50.88% of the sprayed FA in 8 h, indicating the influence of polymer matrix and polymer-drug interactions, on its release from the polymer matrix. Moreover, biocompatibility of all developed novel NFs was assessed by two different cytotoxicity tests, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and neutral red uptake (NRU) assay in L929 (mouse fibroblasts) cell lines. In all cases, it is concluded that these new electrospun fibers had fast-release of the vitamin and the hybrid process is suitable for transdermal patch applications, especially for skin-care products. The results of cytocompatibility assays on L929 reveal that all prepared NFs have no or slight cell toxicity. PVA and PVA-Gel with/without FA nanofibers seems more biocompatible than PVA-Alg nanofibers.


2021 ◽  
Vol 29 (1(145)) ◽  
pp. 17-25
Author(s):  
Fatma Nur Parın ◽  
Kenan Yıldırım

In this study, bioactive fibers were produced using polyvinyl alcohol (PVA), gelatin, polyvinyl pyrolidone (PVP) as a polymer matrix and different amounts of folic acid (FA) as an vitamin by using electrospinning method. Loading of the folic acid in the polymers was determined by the Attenuated Total Reflectance-Fourier Transform Infrared Spectroscopy (ATR-FTIR), morphologies and average diameters were analyzed by Scanning Electron Microscopy (SEM) and Thermal Gravimetric Analysis (TGA) was applied for determining thermal behaviors.The FTIR spectra TGA showed the successful incorporation of folic acid to the fibers. SEM images showed that various smooth and heterogenous electrospun fibers were produced with average diameters ranging from 125 nm to 980 nm. In vitro study was carried out by using FA dissolved in artificial sweat solution (acidic media, pH 5.44) and UV-Vis analysis of electrospun fibers were evaluated. In vitro release studies showed the FA loaded nanofibers had initial vitamin burst release behavior. The maximum vitamin release percentage of PVA/FA, gelatin/FA and PVP/FA fibers was obtained 86.88 %, 80.2 % and 76.66 %, respectively. From these results, the FA-loaded fibers are potential candidates for transdermal patches and topical applications.


2019 ◽  
Vol 9 (2) ◽  
pp. 166-172
Author(s):  
Ahmed A.G. El-Shahawy ◽  
Gamal Elghnam ◽  
Alsayed A.M. Alsherbini

Background:Gold and Iron Oxide nanoparticles NPs play as nanocarriers for a specific drug delivery and contrast agents. Intercellular uptake of these nanoparticles and targeting to individual cell and sub-cellular compartment is essential.Objective:The aim of the current study is to evaluate the intracellular uptake of these NPs to specific tumor cells in vitro conjugated with folic acid with a goal of enhancing the efficiency of specific targeting to tumor cells.Methods:We synthesized the nanoparticles by a chemical method and characterized by UV-Visible, FTIR, XRD, and TEM.Results & Conclusion:The results revealed the conjugation of Gold and Iron Oxide nanoparticles with folic acid increased the intercellular uptake with high percent compared to non- conjugated nanoparticles.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 349
Author(s):  
Anam Razzaq ◽  
Zaheer Ullah Khan ◽  
Aasim Saeed ◽  
Kiramat Ali Shah ◽  
Naveed Ullah Khan ◽  
...  

Diabetic wound infections caused by conventional antibiotic-resistant Staphylococcus aureus strains are fast emerging, leading to life-threatening situations (e.g., high costs, morbidity, and mortality) associated with delayed healing and chronic inflammation. Electrospinning is one of the most widely used techniques for the fabrication of nanofibers (NFs), induced by a high voltage applied to a drug-loaded polymer solution. Particular attention is given to electrospun NFs for pharmaceutical applications (e.g., original drug delivery systems) and tissue regeneration (e.g., as tissue scaffolds). However, there is a paucity of reports related to their application in diabetic wound infections. Therefore, we prepared eco-friendly, biodegradable, low-immunogenic, and biocompatible gelatin (GEL)/polyvinyl alcohol (PVA) electrospun NFs (BNFs), in which we loaded the broad-spectrum antibiotic cephradine (Ceph). The resulting drug-loaded NFs (LNFs) were characterized physically using ultraviolet-visible (UV-Vis) spectrophotometry (for drug loading capacity (LC), drug encapsulation efficiency (EE), and drug release kinetics determination), thermogravimetric analysis (TGA) (for thermostability evaluation), scanning electron microscopy (SEM) (for surface morphology analysis), and Fourier-transform infrared spectroscopy (FTIR) (for functional group identification). LNFs were further characterized biologically by in-vitro assessment of their potency against S. aureus clinical strains (N = 16) using the Kirby–Bauer test and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, by ex-vivo assessment to evaluate their cytotoxicity against primary human epidermal keratinocytes using MTT assay, and by in-vivo assessment to estimate their diabetic chronic wound-healing efficiency using NcZ10 diabetic/obese mice (N = 18). Thin and uniform NFs with a smooth surface and standard size (<400 nm) were observed by SEM at the optimized 5:5 (GEL:PVA) volumetric ratio. FTIR analyses confirmed the drug loading into BNFs. Compared to free Ceph, LNFs were significantly more thermostable and exhibited sustained/controlled Ceph release. LNFs also exerted a significantly stronger antibacterial activity both in-vitro and in-vivo. LNFs were significantly safer and more efficient for bacterial clearance-induced faster chronic wound healing. LNF-based therapy could be employed as a valuable dressing material to heal S. aureus-induced chronic wounds in diabetic subjects.


2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Lucy J. Newbury ◽  
Jui-Hui Wang ◽  
Gene Hung ◽  
Bruce M. Hendry ◽  
Claire C. Sharpe

Abstract Chronic Kidney Disease is a growing problem across the world and can lead to end-stage kidney disease and cardiovascular disease. Fibrosis is the underlying mechanism that leads to organ dysfunction, but as yet we have no therapeutics that can influence this process. Ras monomeric GTPases are master regulators that direct many of the cytokines known to drive fibrosis to downstream effector cascades. We have previously shown that K-Ras is a key isoform that drives fibrosis in the kidney. Here we demonstrate that K-Ras expression and activation are increased in rodent models of CKD. By knocking down expression of K-Ras using antisense oligonucleotides in a mouse model of chronic folic acid nephropathy we can reduce fibrosis by 50% and prevent the loss of renal function over 3 months. In addition, we have demonstrated in vitro and in vivo that reduction of K-Ras expression is associated with a reduction in Jag1 expression; we hypothesise this is the mechanism by which targeting K-Ras has therapeutic benefit. In conclusion, targeting K-Ras expression with antisense oligonucleotides in a mouse model of CKD prevents fibrosis and protects against renal dysfunction.


Pharmaceutics ◽  
2019 ◽  
Vol 11 (4) ◽  
pp. 158
Author(s):  
Akshaya Tatke ◽  
Narendar Dudhipala ◽  
Karthik Janga ◽  
Bhavik Soneta ◽  
Bharathi Avula ◽  
...  

Delivering an effective drug load to the posterior section of the ocular tissues, while using a non-invasive technique, has always been a challenge. In this regard, the goal of the present study was to develop sustained release triamcinolone acetonide (TA) loaded polymeric matrix films for ocular delivery. The TA-films were prepared in two different polymer matrices, with drug loadings of 10% and 20% w/w, and they were evaluated for ocular distribution in vivo in a conscious rabbit model. A 4% w/v TA suspension (TA-C) was used as a control for in vitro and in vivo studies. The TA-films, prepared with melt-cast technology, used polyethylene oxide (PEO) and Soluplus® as the polymer matrix. The films were evaluated with respect to assay, content uniformity, excipient interaction, and permeability across isolated rabbit sclera. The distribution of TA in the ocular tissues, post topical administration, was determined in New Zealand male albino rabbits as a function of dose, and was compared against TA-C. The assay of the 10% and 20% w/w film was in the range from 70–79% and 92–94% for the Soluplus® and PEO films, respectively, and content uniformity was in the range of 95–103% for both the films. The assay of the TA from Soluplus® films was less compared with the PEO films and showed an interaction with TA, as revealed by Differential Scanning Calorimetry (DSC). Hence, Soluplus® films were not selected for further studies. No interaction was observed between the drug and PEO polymer matrix. The enhancement of trans-scleral flux and permeability of TA was about 1.16 and 1.33-folds, respectively, from the 10% w/w PEO and 3.5 and 2.12-folds, respectively, from the 20% w/w PEO films, as compared with TA-C formulations. The in vivo studies demonstrate that significantly higher TA levels were observed in the anterior and posterior segments of the eye at the end of 6h with the PEO films. Therefore, the PEO based polymeric films were able to deliver TA into the back of the eye efficiently and for prolonged periods.


2006 ◽  
Vol 949 ◽  
Author(s):  
Jeffrey P. Calame

ABSTRACTResearch on the microstructure-based modeling of composite dielectrics for capacitor applications is described. Methods for predicting the composite dielectric permittivity and internal electric field distributions within the microstructure using finite difference quasi-electrostatic modeling are described, along with methods of generating realistic model spaces of particulate microstructures. An existing algorithm for generating random, monosized spheres-in-a-dielectric matrix model spaces is modified to allow the treatment of bimodal composites in which small particles are deliberately segregated into the spaces between large particles. Such composites can have substantially higher total volumetric filling fractions of particles, leading to higher composite permittivity. The variations in permittivity with the filling fractions of bimodal inclusions are studied with the new model, with cases covering three different types of polymer matrix material. The effect of the small particle additions on the electric field statistics within the polymer matrix is also explored.


2017 ◽  
Vol 751 ◽  
pp. 581-585 ◽  
Author(s):  
Piyaporn Kampeerapappun ◽  
Pornpen Siridamrong

The objective of this study was to investigate sericin-polyurethane nanofiber cover (SUC) for wound dressing materials in a rat skin. Sericin-polyurethane blended nanofibers were fabricated by using electrospinning. The composition of 3%w/v polyurethane in ethanol and 19% w/v sericin were blended and electrospun at 15 kV, 20 cm from tip to collector with a feed rate of 6.2 ml/hr. The mats, approximately 1.5 mm thick, were sterile by gamma irradiation with a radiation dose of 15 kGy. The samples of in vitro and in vivo testing were separated into three groups; gauze, polyurethane nanofiber cover (UC), and SUC. In vitro cultured L929 cell lines were investigated with inverted microscope. It was found that cells migrated to SCU. For in vivo tests, the remaining wound in rats was measured on day 2-14 after excision. Compared to original size of wound samples, the size of the wound remained 24% for SUC, 33% for gauze, and 34% for UC at day 8. The sericin, an active agent, contained in SUC mats was about 5 µl at 1.5 ×1.5 cm. It can be concluded that sericin is non-toxic to cells and can promote wound healing process in rats.


Science ◽  
1943 ◽  
Vol 98 (2538) ◽  
pp. 179-182 ◽  
Author(s):  
L. D. WRIGHT ◽  
A. D. WELCH
Keyword(s):  

Sign in / Sign up

Export Citation Format

Share Document