Physical–Chemical Aspects of the Preparation and Drug Release of Electrospun Scaffolds

Cui, Lu; Molnár, Judit Rebeka; Budai-Szűcs, Mária; Szécsényi, Mária; Burián, Katalin; Vályi, Péter; Berkó, Szilvia; Pukánszky, Béla

doi:10.3390/pharmaceutics13101645

Cited by 6 publications

(14 citation statements)

References 31 publications

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“…The miscibility of DMSO and PLA is limited; approximately 30 mass% DMSO dissolves in the polymer [33]. DCM evaporates during electrospinning and more DMSO than this 30 mass% is left behind.…”

Section: Processesmentioning

confidence: 99%

“…Plasticizers, but also solvents, accelerate the crystallization of PLA considerably [32], often more efficiently than traditional heterogeneous nucleating agents. The evaporation of the solvents results in the change of composition along the production technology, thus resulting in the partitioning of the active component between the polymer fiber and the surrounding space [33]; some of the drug is located within the fiber and a considerable amount among them [33,34]. Changing crystallinity due to the evaporation of the solvent with high boiling point results in phase separation and further in the change of composition, which influences considerably also the efficiency of the device, the amount of the released drug and the kinetics of drug release.…”

Section: Introductionmentioning

confidence: 99%

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Processes taking place during the preparation and use of electrospun PLA fibers and their effect on controlled drug release

Lan

Luo

Cui

et al. 2022

J Therm Anal Calorim

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PLA fibers containing metronidazole as the active component were produced by electrospinning from a solvent mixture of dichloromethane (DCM) and dimethyl sulfoxide (DMSO). The DMSO content of the spinning solution changed between 0 and 25 vol% in 5 vol% steps. The fibers were dried at different temperatures, and processes taking place during fiber production and drying were followed by thermogravimetric analysis and differential scanning calorimetry. The morphology and structure of the fibers were studied by microscopy and X-ray diffraction. The mechanical properties of fiber mats and the release of the drug were also determined as a function of processing and drying parameters. The results showed that several processes take place during the production and subsequent handling of the fibers including the evaporation of the solvent (DMSO), the crystallization of the polymer, the changing of composition, phase separation and the consequent partitioning of the drug. The crystalline structure of the fibers changes considerably during drying which determines their mechanical properties. The rate of evaporation and crystallization is in the same order of magnitude. The rate of both processes increases considerably with temperature, but does not depend strongly on the amount of DMSO in the spinning solution. Both the amount of the drug released and the rate of release cover a wide range depending on the parameters of the preparation technology. The large range of mechanical and functional properties obtained allows the control of the kinetics of drug release to some extent.

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Section: Processesmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Processes taking place during the preparation and use of electrospun PLA fibers and their effect on controlled drug release

Lan

Luo

Cui

et al. 2022

J Therm Anal Calorim

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“…The location of the drug within the fibers is not trivial in the case when electrospun fibers are used as carrier matrix. Depending on the mutual solubility of the components, including the polymer, the solvents used, and the drug; this latter can be located within or among the fibers [41,42]. Moreover, the drug within the fiber can be crystalline or amorphous, precipitated as a separate phase or distributed as dissolved molecules.…”

Section: Drug Morphology Locationmentioning

confidence: 99%

“…Fiber characteristics depend on several factors including the characteristics of all components like the polymer, the solvent and the drug, as well as on processing parameters as voltage, pump rate, and the distance to the collector [40]. The release of the drug from the device is influenced by all these parameter, but also by the interaction of the components which may change the form and location of the drug in the fibers and thus release kinetics [41,42]. Although many parameters influence drug release, they also offer a possibility to regulate solubility and dissolution rate at the same time.…”

Section: Introductionmentioning

confidence: 99%

Improved Release of a Drug with Poor Water Solubility by Using Electrospun Water-Soluble Polymers as Carriers

et al. 2021

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In an attempt to improve the solubility of valsartan, a BCS II drug, fibers containing the drug were prepared from three water-soluble polymers, hydroxypropyl-methyl-cellulose (HPMC), polyvinyl-pyrrolidone (PVP), and polyvinyl-alcohol (PVA). Fiber spinning technology was optimized for each polymer separately. The polymers contained 20 wt% of the active component. The drug was homogenously distributed within the fibers in the amorphous form. The presence of the drug interfered with the spinning process only slightly, the diameters of the fibers were in the same range as without the drug for the HPMC and the PVA fibers, while it doubled in PVP. The incorporation of the drug into the fibers increased its solubility in all cases compared to that of the neat drug. The solubility of the drug itself depends very much on pH and this sensitivity remained the same in the HPMC and PVP fibers; the release of the drug is dominated by the dissolution behavior of valsartan itself. On the other hand, solubility and the rate of release were practically independent of pH in the PVA fibers. The different behavior is explained by the rate of the dissolution of the respective polymer, which is larger for HPMC and PVP, and smaller for PVA than the dissolution rate of the drug. The larger extent of release compared to neat valsartan can be explained by the lack of crystallinity of the drug, its better dispersion, and the larger surface area of the fibers. Considering all facts, the preparation of electrospun devices from valsartan and water-soluble polymers is beneficial, and the use of PVA is more advantageous than that of the other two polymers.

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“…Fiber characteristics depend on a number of factors including the characteristics of the components, i.e., the polymer, the solvent and the drug, as well as on processing parameters, such as voltage, the pump rate and the distance to the collector [ 32 ]. The release of the drug from the fiber formulation is influenced by all of these parameters as well as by the interaction of the components, which may change the form and location of the drug in the fibers and thus the release kinetics [ 33 , 34 ]. Although many parameters influence drug release, they also offer a possibility of controlling solubility and the dissolution rate at the same time.…”

Section: Introductionmentioning

confidence: 99%

Levocetirizine-Loaded Electrospun Fibers from Water-Soluble Polymers: Encapsulation and Drug Release

et al. 2023

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Electrospun fibers containing levocetirizine, a BCS III drug, were prepared from three water-soluble polymers, hydroxypropyl methylcellulose (HPMC), polyvinylpyrrolidone (PVP) and polyvinyl alcohol (PVA). Fiber-spinning technology was optimized for each polymer separately. The polymers contained 10 wt% of the active component. An amorphous drug was homogeneously distributed within the fibers. The solubility of the drug in the polymers used was limited, with a maximum of 2.0 wt%, but it was very large in most of the solvents used for fiber spinning and in the dissolution media. The thickness of the fibers was uniform and the presence of the drug basically did not influence it at all. The fiber diameters were in the same range, although somewhat thinner fibers could be prepared from PVA than from the other two polymers. The results showed that the drug was amorphous in the fibers. Most of the drug was located within the fibers, probably as a separate phase; the encapsulation efficiency proved to be 80–90%. The kinetics of the drug release were evaluated quantitatively by the Noyes–Whitney model. The released drug was approximately the same for all the polymers under all conditions (pH), and it changed somewhere between 80 and 100%. The release rate depended both on the type of polymer and pH and varied between 0.1 and 0.9 min−1. Consequently, the selection of the carrier polymer allowed for the adjustment of the release rate according to the requirements, thus justifying the use of electrospun fibers as carrier materials for levocetirizine.

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Physical–Chemical Aspects of the Preparation and Drug Release of Electrospun Scaffolds

Cited by 6 publications

References 31 publications

Processes taking place during the preparation and use of electrospun PLA fibers and their effect on controlled drug release

Processes taking place during the preparation and use of electrospun PLA fibers and their effect on controlled drug release

Improved Release of a Drug with Poor Water Solubility by Using Electrospun Water-Soluble Polymers as Carriers

Levocetirizine-Loaded Electrospun Fibers from Water-Soluble Polymers: Encapsulation and Drug Release

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