Influence of the drug compatibility with polymer solution on the release kinetics of electrospun fiber formulation

Qiao

et al. 2011

Polym J

In this study, electrospun composite nanofibers containing nanoparticles for the programmable release of dual drugs were successfully fabricated through a one-step, single-nozzle electrospinning technique. Field-emission scanning electron microscopy and scanning electron microscopy were used to examine the morphology of the nanoparticles and electrospun nanofibers, respectively. The distribution of nanoparticles in the composite nanofibers was evaluated by fluorescence microscopy and laser scanning confocal microscopy. The results indicate that the nanoparticles were encapsulated within the composite nanofibers, forming a core-sheath structure. The different release behaviors of the drugs were ascribed to their varying distribution in the nanofibers and their interaction with carriers. A programmable release of both drugs was also achieved by adjusting the preparation process of the electrospinning solution. Composite nanofibers that can provide a platform for dual-drug loading and the programmed release of each drug may find application in drug delivery systems or in the tissue-engineering field.

Section: Resultsmentioning

confidence: 99%

Electrospun composite nanofibers containing nanoparticles for the programmable release of dual drugs

Qiao

et al. 2011

Polym J

“…The inherently high surface to volume ratio of electrospun polymer fibers can improve cell attachment, enhance drug loading, and realize sustained and controlled local drug delivery [15]. The drug release profile and the degradation rate of the electrospun membranes can be adjusted by regulating the electrospinning parameters [16]. Therefore, electrospinning was adopted to fabricate the antibacterial membranes in this study.…”

Section: Introductionmentioning

confidence: 99%

Drug loaded homogeneous electrospun PCL/gelatin hybrid nanofiber structures for anti-infective tissue regeneration membranes

Xue

Liu³

et al. 2014

Biomaterials

321

218

Email address: sharell@126.com (R. Shi). AbstractInfection is the major reason for guided tissue regeneration/guided bone regeneration (GTR/GBR) membrane failure in clinical application. In this work, we developed GTR/GBR membranes with localized drug delivery function to prevent infection by electrospinning of poly(ε-caprolactone) (PCL) and gelatin blended with metronidazole (MNA). Acetic acid (HAc) was introduced to improve the miscibility of PCL and gelatin to fabricate homogeneous hybrid nanofiber membranes. The effects of the addition of HAc and the MNA content (0,1,5,10,20,30, and 40 wt.% of polymer) on the properties of the membranes were investigated. The membranes showed good mechanical properties, appropriate biodegradation rate and barrier function. The controlled and sustained release of MNA from the membranes significantly prevented the colonization of anaerobic bacteria. Cells could adhere to and proliferate on the membranes without cytotoxicity until the MNA content reached 30%.Subcutaneous implantation in rabbits for 8 months demonstrated that MNA-loaded membranes evoked a less severe inflammatory response depending on the dose of MNA than bare membranes. The biodegradation time of the membranes was appropriate for tissue regeneration. These results indicated the potential for using MNA-loaded PCL/gelatin electrospun membranes as anti-infective GTR/GBR membranes to optimize clinical application of GTR/GBR strategies.

International Journal of Pharmaceutics

“…There are several factors that can affect the drug release from electrospun fibers: fiber construct geometry and thickness [17], fiber diameter and porosity [18], fiber composition [19], fiber crystallinity [20], fiber swelling [21], drug loading [18,21], drug state [22,23], drug molecular weight [19,24], drug solubility in the release medium [21], drug-polymer-electrospinning solvent interactions [25,26]. The release characteristics of the fiber mat are highly influenced by the state of the drug and the structure of the polymer that forms the fiber.…”

Section: Introductionmentioning

confidence: 99%

“…Drug loading is another factor that can affect the drug release: higher loadings will produce faster release ( [18,21,22]); on one hand, at high loadings, there is more surface segregated drug that dissolves fast and on the other hand, there is an increase in porosity during drug elution proportional to the initial amount of drug [18]. Drug compatibility with polymer solution was also shown to be an important factor in controlling release, as lipophilic drugs should be incorporated in lipophilic polymers and hydrophilic drugs in hydrophilic polymers in order to avoid drug deposition outside fibers and subsequent burst [26]. Moreover, the interaction between drug and the polymer can block the crystallization of the drug in the fibers, if so desired [28] and can even determine sustained release of drugs in crystalline state because of chemical interaction with the polymer [24].…”

Section: Introductionmentioning

confidence: 99%

Effects of drug solubility, state and loading on controlled release in bicomponent electrospun fibers

Natu

Sousa

Gil

2010

144

Bicomponent fibers of two semi-crystalline (co)polymers, poly(ε-caprolactone), PCL and poly(oxyethylene-b-oxypropylene-b-oxyethylene), Lu were obtained by electrospinning. Acetazolamide and timolol maleate were loaded in the fibers in different concentrations (below and above the drug solubility limit in polymer) in order to determine the effect of drug solubility in polymer, drug state, drug loading and fiber composition on fiber morphology, drug distribution and release kinetics. The high loadings fibers (with drug in crystalline form) showed higher burst and faster release than low drug content fibers, indicating the release was more sustained when the drug was encapsulated inside the fibers, in amorphous form. Moreover, timolol maleate was released faster than acetazolamide, indicating that drug solubility in polymer influences the partition of drug between polymer and elution medium, while fiber composition also controlled drug release. At low loadings, total release was not achieved (cumulative release percentages smaller than 100 %), suggesting that drug remained trapped in the fibers. The modeling of release data implied a three stage release mechanism: a dissolution stage, a desorption and subsequent diffusion through water filled pores, followed by polymer degradation control.