Effect of the size of biodegradable microparticles on drug release: experiment and theory

Siepmann, J.; Faisant, N.; Akiki, J; Richard, J.; Benoit, Jean‐Pierre

doi:10.1016/j.jconrel.2004.01.011

Cited by 253 publications

(175 citation statements)

References 21 publications

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“…The above-mentioned polymers, degradable hydrolytically to non-toxic bioabsorbable hydroxyacids, were used as sutures, plates and screws for bone fixation [1,2]. There are many reports on drug formulations in which poly(D,L-lactide-co-glycolide) (PLGA) nano-and microspheres were used as drug carriers [2][3][4][5][6][7][8]. Bioactive compounds in these formulations are protected by the polyester matrix from degrading enzymes and immuno-defence system.…”

Section: Introductionmentioning

confidence: 99%

Poly(L,L-lactide) and poly(L,L-lactide-co-glycolide) microparticles by dialysis

2005

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Formation of poly(L,L-lactide) (PLLA) and poly(D,L-lactide-co-glycolide) (PLGA) microparticles by dialysis from 1,4-dioxane, tetrahydrofuran (THF), acetonitrile, dimethyl sulfoxide (DMSO), and dimethylformamide (DMF) against water has been investigated. In some instances microparticles were obtained from a mixture of the above-mentioned polyesters and PLLA-block-polyglycidol-blockpoly(ethylene oxide) triblock copolymer containing a hydrophobic PLLA block as well as hydrophilic polyglycidol and poly(ethylene oxide) blocks, the former with functional -OH groups. The effects of the nature of polyester, solvent and concentration of triblock copolymer on particles morphology, size, size distribution, and degree of crystallinity have been determined. Dialysis of PLGA yielded particles in the form of microspheres regardless of the solvent. Diameters of these particles were in the range of 0.36 -1.77 µm and particles' diameter polydispersity ( D ) varied from 1.37 to 2.04, depending on the solvent. In the case of PLLA, microspheres were obtained only by dialysis from 1,4-dioxane solutions. Dialysis of PLLA solutions in THF, acetonitrile and DMF yielded particles in the form of microcrystals. In the case of dialysis of PLLA solutions in DMSO, the product was in form of crystalline flakes of c. 1 µm thickness. Microspheres composed of PLGA were amorphous. The degree of crystallinity of microparticles from PLLA was in the range of 39% -72%.

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Section: Introductionmentioning

confidence: 99%

Poly(L,L-lactide) and poly(L,L-lactide-co-glycolide) microparticles by dialysis

2005

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“…The PLGA particles may protect the drug, gene and vaccine against degradation and ensure their transport and delivery [13,14], and also can control the release rate and achieve targeting [15][16][17][18]. Among the method for preparation of PLGA particles, the emulsification-solvent evaporation is the most frequently employed one [19].…”

mentioning

confidence: 99%

Preparation and cellular uptake of PLGA particles loaded with lamivudine

et al. 2012

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Poly(D,L-lactide-co-glycolide) (PLGA) nanoparticles loaded with lamivudine and coated with bovine serum albumin (BSA) were prepared via a double emulsion method. The influences of experiments parameters such as volume of inner aqueous phase, concentration of organic phase and ultrasonication time on the particle size and drug entrapment efficiency were investigated, obtaining PLGA particles with a diameter of ~260 nm and drug entrapment efficiency of ~35%. The particles were observed by scanning electron microscopy and transmittance electron microscopy, showing a core-shell structure. BCA assay found that 58 mg BSA was present on/in 1 g LPB particles. The loaded lamivudine showed a burst release at beginning and sustained release until 24 h in physiological conditions. Low pH could accelerate the release of lamivudine from PLGA particles, making the PLGA particles potential intelligent intracellular drug carriers. The PLGA particles were readily internalized into the human liver cells within a short time and increased gradually with the prolongation of incubation time regardless of the loading of lamivudine. The particles either resided within lysosomes or transferred to cytoplasm, but could not enter into the cell nucleus. The cell viability was not significantly influenced in the presence of the particles regardless of lamivudine encapsulation, suggesting that this kind of particles may be a good candidate for the intracellular anti-hepatitis B drug delivery.PLGA, lamivudine, cell uptake, intracellular distribution, drug delivery Citation:Wang B, Chen G Q, Mao Z W, et al. Preparation and cellular uptake of PLGA particles loaded with lamivudine.

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“…Discussing only the results above the limit of 30%, it is evident that smaller particles reach total release quicker than bigger particles. This is to be expected [20,29], but it has been questioned previously [30]. The reported effects in the literature of particle size on the release are various and contrasting.…”

Section: Cumulative Drug Releasementioning

confidence: 93%

PLGA particle production for water-soluble drug encapsulation: Degradation and release behaviour

Gasparini

Holdich

Kosvintsev

2010

Colloids and Surfaces B: Biointerfaces

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Particles for subcutaneous depot use encapsulating a model water soluble drug have been produced from poly(lactic-glycolic acid) (PLGA) using a membrane emulsification -solvent evaporation technique. The release behaviour, mainly the change in size and inner morphology are reported.During release, the particles initially swelled in size, then reduced. A diffusion based model, taking in to account the change in particle size, is presented.Surface erosion is evident from the particle size and image evidence, and the diffusion model provides a fit to the data even during the surface erosion period, suggesting that the model drug diffuses before the particle degrades.

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Effect of the size of biodegradable microparticles on drug release: experiment and theory

Cited by 253 publications

References 21 publications

Poly(L,L-lactide) and poly(L,L-lactide-co-glycolide) microparticles by dialysis

Poly(L,L-lactide) and poly(L,L-lactide-co-glycolide) microparticles by dialysis

Preparation and cellular uptake of PLGA particles loaded with lamivudine

PLGA particle production for water-soluble drug encapsulation: Degradation and release behaviour

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