How to easily provide zero order release of freely soluble drugs from coated pellets

Dekyndt, B.; Vérin, J.; Neut, Christel; Siepmann, Florence; Siepmann, Juergen

doi:10.1016/j.ijpharm.2014.10.071

Cited by 19 publications

(12 citation statements)

References 35 publications

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“…The compactness of the vehicle has increased due to the layer-by-layer crosslinking strategy which also elevated the water resistivity degree and restricted the drug molecule mobility [13][14][15]. Further to understand the mechanism of drug release, in-vitro drug release data for sample F with different drug loading and different crosslinking strategies were fitted with zero order release and R 2 values were listed.…”

Section: A C C E P T E D Mmentioning

confidence: 99%

“…Exceptional properties of such fibers, e.g. highly porous three dimensional surface, high surface-to-volume ratios, interconnected porosity with tuneable pore dimensions, found tremendous applications in different biomedical fields [9][10][11][12][13][14][15]. Various electrospinning parameters modulate the fiber diameter and thickness, which may affect sustained and controlled release profiles [16][17][18].…”

Section: Introductionmentioning

confidence: 99%

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Sustained drug release from multi-layered sequentially crosslinked electrospun gelatin nanofiber mesh

Laha

Sharma

Majumdar

2017

Materials Science and Engineering: C

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The aim of this study is to develop electrospun gelatin nanofibers based drug delivery carrier to achieve controlled and sustainable release of hydrophobic drug (piperine) for prolonged time. To accomplish this, we devised some strategies such as sandwiching the drug loaded gelatin nanofiber mesh with another gelatin nanofiber matrix without drug (acting as diffusion barrier), sequential crosslinking and finally, a combination of both. As fabricated multilayered electrospun nanofibers mesh was first characterized in terms of degradation study, morphology, drug-polymer interactions, thermal stability followed by studying their release kinetics in different physiological pH as per the gastrointestinal tract. Our results show that with optimized diffusional barrier support and sequential crosslinking together, a zero order sustained drug release up to 48 h may be achieved with a flexibility to vary the drug loading as per the therapeutic requirements. This work lays out the possibility of systematic design of multilayer nano-fiber mesh of a biopolymer as a drug delivery vehicle for hydrophobic drugs with a desired signature of zero order release for prolonged duration.

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Section: A C C E P T E D Mmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Sustained drug release from multi-layered sequentially crosslinked electrospun gelatin nanofiber mesh

Laha

Sharma

Majumdar

2017

Materials Science and Engineering: C

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“…Thus, our microparticles generated using the VOAG technology represent and advancement with a considerable advantage since the potential adverse effects that may occur due to the overwhelming burst effect would be diminished. The production of formulations with biphasic zero-order release kinetics entailed that as time elapsed, constant amounts of LTZ were released [55]. This is of high importance since these formulations were successful in modifying the release of LTZ to become linear, highly predictable, and consistent, which is one of the prime achievements of the present study.…”

Section: In Vitro Drug Release and Kinetic Modeling Investigationsmentioning

confidence: 81%

Preparation and optimization of monodisperse polymeric microparticles using modified vibrating orifice aerosol generator for controlled delivery of letrozole in breast cancer therapy

Alemrayat

Elrayess

Alany

et al. 2018

Drug Development and Industrial Pharmacy

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Letrozole (LTZ) is effective for the treatment of hormone-receptor-positive breast cancer in postmenopausal women. In this work, and for the first time, using vibrating orifice aerosol generator (VOAG) technology, monodisperse poly-ε-caprolactone (PCL), and poly (D, L-Lactide) (PDLLA) LTZ-loaded microparticles were prepared and found to elicit selective high cytotoxicity against cancerous breast cells with no apparent toxicity on healthy cells in vitro. Plackett-Burman experimental design was utilized to identify the most significant factors affecting particle size distribution to optimize the prepared particles. The generated microparticles were characterized in terms of microscopic morphology, size, zeta potential, drug entrapment efficiency, and release profile over one-month period. Long-term cytotoxicity of the microparticles was also investigated using MCF-7 human breast cancer cell lines in comparison with primary mammary epithelial cells (MEC). The prepared polymeric particles were monodispersed, spherical, and apparently smooth, regardless of the polymer used or the loaded LTZ concentration. Particle size varied from 15.6 to 91.6 µm and from 22.7 to 99.6 µm with size distribution (expressed as span values) ranging from 0.22 to 1.24 and from 0.29 to 1.48 for PCL and PDLLA based microparticles, respectively. Upon optimizing the manufacture parameters, span was reduced to 0.162-0.195. Drug entrapment reached as high as 96.8%, and drug release from PDLLA and PCL followed a biphasic zero-order release using 5 or 30% w/w drug loading in the formulations. Long-term in vitro cytotoxicity studies indicated that microparticles formulations significantly inhibited the growth of MCF-7 cell line over a prolonged period of time but did not have toxic effects on the normal breast epithelial cells.

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“…In addition, gradient systems, wherein the drug concentration increases from the outside towards the inside, have been described [11][12][13][14][15][16][17][18]. Such systems may be obtained by controlled extraction processes, coating/layering techniques or, alternatively, emerging fabrication methods, such as 3D printing and electrostatic deposition, that are still poorly exploited in the pharmaceutical field [19][20][21][22][23].…”

Section: Introductionmentioning

confidence: 99%

Novel hydrophilic matrix system with non-uniform drug distribution for zero-order release kinetics

Cerea

Maroni

Palugan

et al. 2018

Journal of Controlled Release

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A decrease in the release rate over time is typically encountered when dealing with hydrophilic matrix systems for oral prolonged release due to progressive increase of the distance the drug molecules have to cover to diffuse outwards and reduction of the area of the glassy matrix at the swelling front. In order to solve this issue, a novel formulation approach based on non-uniform distribution of the active ingredient throughout the swellable polymer matrix was proposed and evaluated. Various physical mixtures of polymer (high-viscosity hypromellose) and drug tracer (acetaminophen), having decreasing concentrations of the latter, were applied by powder-layering onto inert core seeds. The resulting gradient matrices showed to possess satisfactory physico-technological characteristics, with spherical shape and consistent thickness of the layers sequentially applied. The non-uniform matrix composition pursued was confirmed by Raman mapping analysis. As compared with a system having uniform distribution of the drug tracer, the multi-layer formulations were proved to enhance linearity of release. The simple design concept, advantageous technique, which involves no solvents nor high-impact drying operations, and the polymeric material of established use make the delivery platform hereby proposed a valuable strategy to improve the performance of hydrophilic matrix systems.

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How to easily provide zero order release of freely soluble drugs from coated pellets

Cited by 19 publications

References 35 publications

Sustained drug release from multi-layered sequentially crosslinked electrospun gelatin nanofiber mesh

Sustained drug release from multi-layered sequentially crosslinked electrospun gelatin nanofiber mesh

Preparation and optimization of monodisperse polymeric microparticles using modified vibrating orifice aerosol generator for controlled delivery of letrozole in breast cancer therapy

Novel hydrophilic matrix system with non-uniform drug distribution for zero-order release kinetics

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