scholarly journals Coaxial Electrospinning with Mixed Solvents: From Flat to Round Eudragit L100 Nanofibers for Better Colon-Targeted Sustained Drug Release Profiles

2014 ◽  
Vol 2014 ◽  
pp. 1-8 ◽  
Author(s):  
Deng-Guang Yu ◽  
Ying Xu ◽  
Zan Li ◽  
Lin-Ping Du ◽  
Ben-Guo Zhao ◽  
...  
Keyword(s):  
Drug Release ◽  
Diclofenac Sodium ◽  
Mixed Solvents ◽  
Amorphous State ◽  
Electrospinning Process ◽  
Release Time ◽  
Coaxial Electrospinning ◽  
Sustained Drug Release ◽  
Eudragit L100 ◽  
Physical Form

A modified coaxial electrospinning process was developed for creating drug-loaded composite nanofibers. Using a mixed solvent of ethanol and N,N-dimethylacetamide as a sheath fluid, the electrospinning of a codissolving solution of diclofenac sodium (DS) and Eudragit L100 (EL100) could run smoothly and continuously without any clogging. A series of analyses were undertaken to characterize the resultant nanofibers from both the modified coaxial process and a one-fluid electrospinning in terms of their morphology, physical form of the components, and their functional performance. Compared with those from the one-fluid electrospinning, the DS-loaded EL100 fibers from the modified coaxial process were rounder and smoother and possessed higher quality in terms of diameter and distribution with the DS existing in the EL100 matrix in an amorphous state; they also provided a better colon-targeted sustained drug release profile with a longer release time period. The modified coaxial process not only can smooth the electrospinning process to prevent clogging of spinneret, but also is a useful tool to tailor the shape of electrospun nanofibers and thus endow them improved functions.

scholarly journals Mucoadhesive Particles: A Novel, Prolonged-Release Nanocarrier of Sitagliptin for the Treatment of Diabetics

2019 ◽  
Vol 2019 ◽  
pp. 1-9 ◽  
Author(s):  
Nagaraja SreeHarsha ◽  
Chandramouli Ramnarayanan ◽  
Bandar E. Al-Dhubiab ◽  
Anroop B. Nair ◽  
Jagadeesh G. Hiremath ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Oral Delivery ◽  
Amorphous State ◽  
Release Time ◽  
Prolonged Release ◽  
Delivery Method ◽  
Sustained Drug Release ◽  
Scanning Calorimetry ◽  
Percentage Yield

Sitagliptin (MK–0431) is a widely and commonly used oral hypoglycemic drug in the treatment of type 2 diabetes mellitus; patients typically take higher doses of this drug (50 mg, twice daily). One drawback is that only 38% of the drug is bound reversibly to plasma proteins and 79% is excreted in urine without being metabolized. To overcome this issue, there is a need for a better drug-delivery method to improve its efficacy in patients. It has been found that in existing formulations, the drug content is 72.5% ± 5% and the percentage yield is 84.9% ± 3%. In this study, sitagliptin nanoparticles (sizes ranging from 210 to 618 nm) were developed. The bioadhesion properties of the nanoparticles, as well as the swelling of the nanoparticles on the mucus membrane aided in sustained drug release. The pattern of drug release was in accordance with the Peppas model. Fourier-transform infrared (FTIR) spectroscopy demonstrated that there were no significant interactions between sitagliptin and chitosan. Differential scanning calorimetry (DSC) results showed an absence of drug peaks due to the fact that the drug was present in an amorphous state. Mucoadhesive nanoparticles were formulated using sitagliptin and were effective for about 12 hours in the gastrointestinal tract. When compared to conventional sitagliptin administration, use of a nanoparticle delivery system demonstrated greater benefits for use in oral delivery applications. This is the first time that a drug-delivery method based on the mucoadhesive properties of nanoparticles could prolong the drug-release time of sitagliptin.

Ferulic Acid-Loaded Shellac Microparticles Prepared Using Electrohydrodynamic Atomization

2013 ◽  
Vol 675 ◽  
pp. 326-330 ◽  
Author(s):  
Deng Guang Yu ◽  
Wei Qian ◽  
Xia Wang ◽  
Ying Li ◽  
Wei Jun Lu ◽  
...  
Keyword(s):  
Drug Release ◽  
Ferulic Acid ◽  
Diffusion Mechanism ◽  
Amorphous State ◽  
Fickian Diffusion ◽  
In Vitro Dissolution ◽  
Release Time ◽  
Infrared Analysis ◽  
Sustained Drug Release ◽  
Electrohydrodynamic Atomization

An Electrohydrodynamic atomization (EHDA) process was exploited to prepare ferulic acid (FA)-loaded shellac microparticles. SEM observations showed that all the particles were round and solid with their sizes gradually increased from 0.68 ± 0.21 to 2.75 ± 0.64 μm as the concentrations of shellac and FA in ethanol raised from 20% to 50% (w/v). Wide-angle X-ray diffraction analyses demonstrated that FA had been totally converted into an amorphous state in the shellac matrix microparticles. Attenuated total reflectance Fourier transform infrared analysis disclosed that the hydrogen bonding presented between FA and shellac molecules. In vitro dissolution tests verified that all the microparticles were able to provide a fine sustained drug release profile. The release time periods had a close relationship with the diameters of microparticles. All the microparticles released the loaded FA via a typical Fickian diffusion mechanism. The present study provides an easy way to develop novel drug delivery microparticles for providing sustained drug release profiles.

Drug Sustained Release Multiple-Component Polymeric Microparticles Fabricated Using an Electrospray Process

2014 ◽  
Vol 937 ◽  
pp. 269-275 ◽  
Author(s):  
Xiao Yan Li ◽  
Deng Guang Yu ◽  
Fa Ping Jiang ◽  
Kong Jing Deng ◽  
Zhi Du ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Amorphous State ◽  
Release Time ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
Electron Microscopic ◽  
Polymeric Microparticles ◽  
Multiple Component ◽  
Release Profiles

The present study investigates the preparation of ferulic acid (FA) sustained-release cellulose acetate (CA) microparticles, in which a third component, polyvinylpyrrolidone (PVP), was included into the microcomposites for an improved sustained drug release profile. An electrospraying process was exploited for the fabrication of multiple-component microparticles. Under an applied voltage of 18 kV, FA/PVP/CA composite microparticles were successfully generated. Field emission scanning electron microscopic observations demonstrated that these microparticles had an indented surface morphology with an average diameter of 1.71 ± 0.56 μm. The drug presented in the polymeric microparticles in an amorphous state due to the favorable secondary interactions among the components, as verified by the X-ray diffraction (XRD) patterns and attenuated total reflectance Fourier transform spectra. The triple-component microparticles could provide a fine sustained release profiles with full release completeness and small tailing-off release time period. The electrospraying process is a useful tool for developing sustained release microparticles and multiple-component co-existence in the microparticles can be taken to adjust the sustained drug release profiles.

Borneol-Shellac Nanofiber Membranes Fabricated Using a Modified Coaxial Electrospinning

2014 ◽  
Vol 1058 ◽  
pp. 78-82 ◽  
Author(s):  
Deng Guang Yu ◽  
Ying Xu ◽  
Song Liu ◽  
Yu Hai Wang ◽  
Xiao Duan ◽  
...  
Keyword(s):  
Physical Stability ◽  
Amorphous State ◽  
Average Diameter ◽  
Electrospinning Process ◽  
Flow Rate Ratio ◽  
Coaxial Electrospinning ◽  
High Quality ◽  
Pure Ethanol ◽  
Sheath Fluid ◽  
Nanofiber Membranes

A modified coaxial electrospinning process is developed for producing medicated nanofiber membranes of shellac. With pure ethanol as a sheath fluid, high quality borneol-loaded shellac nanofibers have been successfully fabricated using the modified coaxial process. Electron scanning microscopic observations demonstrated that the nanofibers had better quality than those fabricated using a single fluid electrospinning in terms of nanofiber diameters and their distributions. The former had an average diameter of 570 ± 80 nm under a sheath-to-core flow rate ratio of 0.25, whereas the later was 940 ± 230 nm. X-ray diffraction results verified that borneol existed in the shellac matrix in an amorphous state. The medicated nanofiber membranes could significantly improved the physical stability of borneol due to the favorable hydrogen bonding between the drug and the polymer matrix, as demonstrated by the weight loss experiments. The modified coaxial electrospinning process described here expands the capability of electrospinning process in generating high quality functional membranes.

scholarly journals Triple-Component Drug-Loaded Nanocomposites Prepared Using a Modified Coaxial Electrospinning

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Wei Qian ◽  
Deng-Guang Yu ◽  
Ying Li ◽  
Xiao-Yan Li ◽  
Yao-Zu Liao ◽  
...  
Keyword(s):  
Flow Rate ◽  
Average Diameter ◽  
Electrospinning Process ◽  
Flow Rate Ratio ◽  
Uniform Structure ◽  
Coaxial Electrospinning ◽  
Sustained Drug Release ◽  
Sheath Fluid ◽  
Transdermal Drug Delivery Systems

Triple-component nanocomposites for improved sustained drug release profiles are successfully fabricated through a modified coaxial electrospinning process, in which only organic solvent N,N-dimethylacetamide was used as sheath fluid. Using polyacrylonitrile (PAN) as filament-forming matrix, ibuprofen (IBU) as functional ingredient, and polyvinylpyrrolidone (PVP) as the additional component, the IBU/PVP/PAN triple-component nanocomposites had uniform structure and an average diameter of620±120 nm and650±120 nm when the contents of PVP in the nanofibers were 10.5% and 22.7%, respectively. The optimal sheath-to-core flow rate ratio was 0.11 under a total sheath and core fluid flow rate of 1.0 mL/h. Compared with the IBU/PAN composite nanofibers, the triple-component composites could release 92.1% and 97.8% of the contained IBU, significantly larger than a value of 73.4% from the former. The inclusion of PVP in the IBU/PAN could effectively avoid the entrapment of IBU in the insoluble PAN molecules, facilitating thein vitrorelease of IBU. The modified coaxial process and the resulted multiple component nanocomposites would provide new way for developing novel drug sustained materials and transdermal drug delivery systems.

The immobilization of antibiotic-loaded polymeric coatings on osteoarticular Ti implants for the prevention of bone infections

2017 ◽  
Vol 5 (11) ◽  
pp. 2337-2346 ◽  
Author(s):  
Dan Li ◽  
Pengfei Lv ◽  
Linfeng Fan ◽  
Yaoyi Huang ◽  
Fei Yang ◽  
...  
Keyword(s):  
Drug Release ◽  
Release Time ◽  
Burst Release ◽  
Polymeric Coatings ◽  
Sustained Drug Release ◽  
Initial Burst ◽  
Initial Burst Release ◽  
Bone Infections

Polymeric multilayers covalently fixed to Ti surfaces could offer a sustained drug release with no initial burst release and extend the drug release time.

Linear drug release membrane prepared by a modified coaxial electrospinning process

2013 ◽  
Vol 428 ◽  
pp. 150-156 ◽  
Author(s):  
Deng-Guang Yu ◽  
Wei Chian ◽  
Xia Wang ◽  
Xiao-Yan Li ◽  
Ying Li ◽  
...  
Keyword(s):  
Drug Release ◽  
Electrospinning Process ◽  
Coaxial Electrospinning

scholarly journals Formation of Drug-Participating Catanionic Aggregates for Extended Delivery of Non-Steroidal Anti-Inflammatory Drugs from Contact Lenses

Biomolecules ◽  
2019 ◽  
Vol 9 (10) ◽  
pp. 593 ◽  
Author(s):  
Cesar Torres-Luna ◽  
Abdollah Koolivand ◽  
Xin Fan ◽  
Niti R. Agrawal ◽  
Naiping Hu ◽  
...  
Keyword(s):  
Drug Release ◽  
Cationic Surfactant ◽  
Naproxen Sodium ◽  
Contact Lenses ◽  
Release Kinetics ◽  
Diclofenac Sodium ◽  
In Vitro Release ◽  
Release Time ◽  
Hydrophobic Drugs ◽  
Anti Inflammatory

This paper focuses on extending drug release duration from contact lenses by incorporating catanionic aggregates. The aggregates consist of a long-chain cationic surfactant, i.e., cetalkonium chloride (CKC), and an oppositely charged anti-inflammatory amphiphilic drug. We studied three non-steroidal anti-inflammatory (NSAID) drugs with different octanol–water partition coefficients; diclofenac sodium (DFNa), flurbiprofen sodium (FBNa), and naproxen sodium (NPNa). Confirmation of catanionic aggregate formation in solution was determined by steady and dynamic shear rheology measurements. We observed the increased viscosity, shear thinning, and viscoelastic behavior characteristic of wormlike micelles; the rheological data are reasonably well described using a Maxwellian fluid model with a single relaxation time. In vitro release experiments demonstrated that the extension in the drug release time is dependent on the ability of a drug to form viscoelastic catanionic aggregates. Such aggregates retard the diffusive transport of drug molecules from the contact lenses. Our study revealed that the release kinetics depends on the CKC concentration and the alkyl chain length of the cationic surfactant. We demonstrated that more hydrophobic drugs such as diclofenac sodium show a more extended release than less hydrophobic drugs such as naproxen sodium.

Electrospun amorphous medicated nanocomposites fabricated using a Teflon-based concentric spinneret

e-Polymers ◽  
2018 ◽  
Vol 18 (1) ◽  
pp. 3-11 ◽  
Author(s):  
Qing Wang ◽  
Deng-Guang Yu ◽  
Sun-Yi Zhou ◽  
Chen Li ◽  
Min Zhao
Keyword(s):  
Drug Carrier ◽  
Hydroxypropyl Methylcellulose ◽  
Amorphous State ◽  
Electrospinning Process ◽  
Water Soluble ◽  
Coaxial Electrospinning ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Model Drug

AbstractFacile methods to improve the dissolution rate of poorly water-soluble drugs are highly sought after. In this study, a modified coaxial electrospinning process was exploited to create medicated amorphous nanocomposites, an approach characterized by the application of a Teflon-coated coaxial spinneret. The hydrophilic polymer hydroxypropyl methylcellulose and the active ingredient tamoxifen citrate (TAM) were selected as the drug carrier and model drug, respectively. Their electrospun nanocomposites showed linear morphology with the drug presented in an amorphous state. The loaded cargoes could be released from the nanocomposites simultaneously when they were placed in the dissolution media, showing faster dissolution rates than their counterparts (physical mixtures). Based on the reasonable application of the polymeric carrier, the reported protocols not only provided an approach to enhance the dissolution of poorly water-soluble drugs, but also exhibited a method to facilitate the implementation of coaxial electrospinning.

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