Effect of particle size, polydispersity and polymer degradation on progesterone release from PLGA microparticles: Experimental and mathematical modeling

Busatto, Carlos Alberto; Pesoa, Juan Ignacio; Helbling, Ignacio Marcelo; Luna, Julio Alberto; Estenoz, Diana Alejandra

doi:10.1016/j.ijpharm.2017.12.006

Cited by 97 publications

(77 citation statements)

References 34 publications

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“…Figure presents the simulation results of polymer degradation predicted by the Degradation Module for PLGA nano‐ and microparticles. For simulations corresponding to Degradation Module, the parameters adjusted in our previous work were used . Polymer degradation occurs slowly during the release time due to the low concentration of degradation products with acid terminal groups associated with autocatalytic degradation.…”

Section: Resultsmentioning

confidence: 99%

“…Also, polymer degradation effect on drug release becomes important for microspheres with a size above 25 μm due to longer degradation time and the increased effect of autocatalytic degradation. In our previous work, it was possible to estimate a range of average molecular weights at which the mass transport mechanism changes from PLGA microparticles . The estimated ranges for

{\overset{false¯}{M}}_{n}

and

{\overset{false¯}{M}}_{w}

were 3100–3200 and 4300–4700 g mol −1 , respectively.…”

Section: Resultsmentioning

confidence: 99%

“…In our previous work, a mathematical model to describe the progesterone release from different‐sized microspheres was developed . The model considers the intraparticle dissolution and diffusion of the drug, as well as the autocatalytic polymer degradation.…”

Section: Introductionmentioning

confidence: 99%

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PLGA nano‐ and microparticles for the controlled release of florfenicol: Experimental and theoretical study

Karp

Busatto

Turino

et al. 2018

J of Applied Polymer Sci

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In this study, PLGA particle systems were studied for the controlled release of florfenicol, a broad spectrum antibiotic used in veterinary treatments. The emulsion-solvent evaporation technique was used for particle preparation. To evaluate the particle size, entrapment efficiency, and drug release behavior, factors such as solvent type, emulsification time and methods, and drug to polymer ratio were investigated. The results showed that the use of ethyl acetate and 2.5 min of ultrasonication or 30 min of homogenization can lead to sub-micron and micron-sized particles, respectively. Sizes between 200-300 nm and 2-3 μm were obtained for ultrasonication and homogenization procedures, respectively. Entrapment efficiencies were around 20% for all systems and release profiles were size dependent. In addition, a mathematical model was implemented to simulate the florfenicol transport. The model predicts the florfenicol release and takes into account the particle size, polymer molecular weight, and autocatalytic polymer degradation. Simulation results are in good agreement with experimental results.

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Section: Resultsmentioning

confidence: 99%

{\overset{false¯}{M}}_{n}

and

{\overset{false¯}{M}}_{w}

were 3100–3200 and 4300–4700 g mol −1 , respectively.…”

Section: Resultsmentioning

confidence: 99%

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PLGA nano‐ and microparticles for the controlled release of florfenicol: Experimental and theoretical study

Karp

Busatto

Turino

et al. 2018

J of Applied Polymer Sci

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“…It was difficult for such molecules to diffuse to the outside of the matrix, which caused the accumulation of acid degradation products inside the MPs, forming a local slightly acidic environment. Hydrogen ions can catalyze the hydrolysis of ester bonds, which is called the "autocatalytic effect", which also leads to the faster degradation of MPs in the later stage (Busatto et al, 2018).…”

Section: In Vitro Degradation Of Mp/dtx With Different Particle Sizesmentioning

confidence: 99%

Shear Speed-Regulated Properties of Long-Acting Docetaxel Control Release Poly (Lactic-Co-Glycolic Acid) Microspheres

et al. 2020

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Advanced drug carriers for the controlled release of chemotherapeutics in the treatment of malignant tumors have drawn significant notice in recent years. In the current study, microspheres (MPs) loaded with docetaxel (DTX) were prepared using polylactic-coglycolic acid copolymer (PLGA). The double emulsion solvent evaporation method is simple to perform, and results in high encapsulation efficiency. Electron micrographs of the MPs showed that controlling the shear rate can effectively control the size of the MPs. At present, most DTX sustained-release carriers cannot maintain stable and long-term local drug release. The 1.68 mm DTX-loaded microspheres (MP/DTX) with elastase was completely degraded in 14 d. This controlled degradation period is similar to a course of treatment for most cancers. The drug release profile of all kinds of MP/DTX demonstrated an initial rapid release, then slower and stable release to the end. The current study demonstrates that it is possible to create drug-loaded MPs with specific degradation times and drug release curves, which may be useful in achieving optimal treatment times and drug release rates for different diseases, and different drug delivery routes. The initial burst release reaches the effective concentration of the drug at the beginning of release, and then the drug concentration is maintained by stable release to reduce the number of injections and improve patient compliance.

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“…Thus, upon drug exhaust, there is no need to remove empty remnants: a major benefit for the patient. Various types of PLGA‐based controlled drug delivery systems have been described in the literature . PLGA microparticles are often more easy to administer than PLGA implants, for example, using relatively thin needles.…”

Section: Introductionmentioning

confidence: 99%

Towards a better understanding of the release mechanisms of caffeine from PLGA microparticles

Tamani

Hamoudi

Danède

et al. 2019

J of Applied Polymer Sci

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Poly(lactic‐co‐glycolic acid) (PLGA)‐based microparticles can be successfully used to control the release rate of a drug and optimize the therapeutic efficacy of a medical treatment. However, the underlying drug release mechanisms can be complex and are often not fully understood. This renders system optimization cumbersome. In this study, differently sized caffeine‐loaded PLGA microparticles were prepared and the swelling and drug release behaviors of single microparticles were monitored upon exposure to phosphate buffer pH 7.4. Ensembles of microparticles were characterized by X‐ray diffraction, differential scanning calorimetry, scanning electron microscopy, gel permeation chromatography, and optical microscopy. The observed triphasic drug release patterns could be explained as follows. The initial burst release can be attributed to the dissolution of tiny drug crystals with direct surface access. The subsequent second drug release phase (with an about constant release rate) could be attributed to the release of drug crystals in regions, which undergo local swelling. The third release phase (again rapid, leading to complete drug exhaust) could be explained by substantial polymer swelling throughout the systems. Once a critical polymer molecular weight is reached, the PLGA chains are sufficiently hydrophilic, insufficiently entangled and the osmotic pressure created by water soluble degradation products attracts high amounts of water into the system. © 2019 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2020, 137, 48710.

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Effect of particle size, polydispersity and polymer degradation on progesterone release from PLGA microparticles: Experimental and mathematical modeling

Cited by 97 publications

References 34 publications

PLGA nano‐ and microparticles for the controlled release of florfenicol: Experimental and theoretical study

PLGA nano‐ and microparticles for the controlled release of florfenicol: Experimental and theoretical study

Shear Speed-Regulated Properties of Long-Acting Docetaxel Control Release Poly (Lactic-Co-Glycolic Acid) Microspheres

Towards a better understanding of the release mechanisms of caffeine from PLGA microparticles

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