Effect of Agitation Regimen on the in vitro Release of Leuprolide from Poly(Lactic-Co-Glycolic) Acid Microparticles

Schoubben, Aurelie Marie Madeleine; Blasi, Paolo; DeLuca, Patrick P.

doi:10.1002/jps.23029

Cited by 16 publications

(14 citation statements)

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“…Blank and loaded microspheres were incubated in 10 mL round bottom vials containing 0.02 M PBS added with 0.02% Tween® 80 and 0.5% sodium azide at 37±1°C in static conditions (12). The amount of microspheres (10 mg for the time points 0-20 days; 20 mg for the time points 25-40 days) and the volume of buffer were calculated to maintain sink condition during the degradation study.…”

Section: In Vitro Degradation Studiesmentioning

confidence: 99%

Accelerated Polymer Biodegradation of Risperidone Poly(d, l-Lactide-Co-Glycolide) Microspheres

2012

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Abstract. The influence of a tertiary amine, namely risperidone (pKa07.9) on the degradation of poly(D, L lactide-co-glycolide) (PLGA) microspheres was elucidated. Risperidone and blank microspheres were fabricated at two lactide/glycolide ratios, 65:35 and 85:15. The microspheres were characterized for drug loading by high-performance liquid chromatography, particle size by laser diffractometry, and surface morphology by scanning electron microscopy. Polymer degradation studies were carried out with drugloaded microspheres and blank microspheres in presence of free risperidone in 0.02 M PBS containing 0.02% Tween®80 at 37°C. Molecular weight was monitored by gel permeation chromatography. Risperidone and blank microspheres had similar size distribution and were spherical with a relatively nonporous smooth surface. The presence of risperidone within the microspheres enhanced the hydrolytic degradation in both polymeric matrices with faster degradation occurring in 65:35 PLGA. The molecular weight decreased according to pseudo-first-order kinetics for all the formulations. During the degradation study, the surface morphology of drug-loaded microspheres was affected by the presence of risperidone and resulted in shriveled microspheres in which there appeared to be an intrabatch variation with the larger microspheres being less shriveled than the smaller ones. When blank microspheres were incubated in free risperidone solutions, a concentration-dependent effect on the development of surface porosity could be observed. Risperidone accelerates the hydrolytic degradation of PLGA, presumably within the microenvironment of the drug-loaded particles, and this phenomenon must be taken into consideration in designing PLGA dosage forms of tertiary amine drugs.

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Section: In Vitro Degradation Studiesmentioning

confidence: 99%

Accelerated Polymer Biodegradation of Risperidone Poly(d, l-Lactide-Co-Glycolide) Microspheres

2012

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“…There is also a lack of suitable tools to evaluate the impact of MP features on their performances (D'Souza et al 2014b, c). That is why the FDA's Office of Generic Drug (OGD) supports research to develop in vitro-in vivo correlations and in vitro release testing methods (Schoubben et al 2012;Leblanc 2018).…”

Section: Pla and Plga Microparticles In The Pharmaceutical Marketmentioning

confidence: 99%

Meeting the unmet: from traditional to cutting-edge techniques for poly lactide and poly lactide-co-glycolide microparticle manufacturing

Schoubben

Ricci

Giovagnoli

2019

J. Pharm. Investig.

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Background Polylactides (PLA) and poly lactide-co-glycolides (PLGA) undoubtedly are among the major drivers in the pharmaceutical market. Their relevance in pharmaceutics and biomedicine is well established in light of their sustainability, safety, tunable biodegradability, and versatility. However, polymer degradability and plasticity can somehow restrain industrial developability of PLA and PLGA formulations, especially in the form of microparticles (MP). Area covered This review wants to deal with the known manufacturing issues of PLA/PLGA MP, debating the potential contribution of modern and cutting-edge manufacturing technologies to the solution of unmet production needs. Technological and regulatory aspects will be considered outlining the potential role of advanced manufacturing techniques in the advancement of PLA/PLGA MP production processes. Expert opinion The multifaceted complexity of PLA/PLGA MP manufacturing processes demands adequate standardization and updated guidelines covering the so far unmet industrialization requirements. Novel and evolving manufacturing technologies will surely support the future development of bench-to-production plant transfer for such products. Careful evaluation of production costs is demanded in order to ensure process sustainability and patient's outreach.

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“…Another critical factor is the medium used for dissolution testing, a choice which strongly depends on the purpose of the study and the compound investigated. In the development stages, using media as close as possible to the biological fluids is relevant, but for routine quality control, simple dissolution media are preferred because of their higher reproducibility, lower costs, and ease of preparation (64). A wide range of media has been tested, buffered in the pH range of 6.8-7.4 and ranging from simple compositions like phosphate buffer to simulated lung fluids (SLF) containing an array of proteins, lipids, and surfactants, like the most abundant pulmonary surfactant, DPPC (42,49,58,(64)(65)(66).…”

Section: Dissolution Mediamentioning

confidence: 99%

“…In the development stages, using media as close as possible to the biological fluids is relevant, but for routine quality control, simple dissolution media are preferred because of their higher reproducibility, lower costs, and ease of preparation (64). A wide range of media has been tested, buffered in the pH range of 6.8-7.4 and ranging from simple compositions like phosphate buffer to simulated lung fluids (SLF) containing an array of proteins, lipids, and surfactants, like the most abundant pulmonary surfactant, DPPC (42,49,58,(64)(65)(66). The most recently developed SLF is the synthetic lung fluid based on human respiratory tract lining fluid composition, proposed by Kumar et al This medium showed biocompatibility with the human A549 cell line and good correlation of the dissolution behavior of inhalable products with the API's solubility characteristics (67).…”

Section: Dissolution Mediamentioning

confidence: 99%

Towards Standardized Dissolution Techniques for In Vitro Performance Testing of Dry Powder Inhalers

Floroiu¹,

Klein²,

Krämer³

et al. 2018

Dissolution Technol.

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The pulmonary route of administration is used for both locally and systemically acting drugs. However, knowledge gaps about the fate of aerosol particles after deposition in the lung provide room for future elucidation. During pharmaceutical development as well as in quality control of oral inhalation products, in vitro performance tests are required for discriminating between formulations and to prove batch-to-batch consistency. Although the aerodynamic particle size distribution is widely recognized as the pivotal performance parameter, there is still no standardized test for in vitro dissolution testing. This review summarizes the in vitro performance testing methodologies developed for orally inhaled drug product (OIDP) evaluation, with a focus on dissolution testing of dry powders for inhalation. The dissolution setups used, together with the media, membranes, and methods employed for collecting the relevant particle fraction, are presented. With a clear focus on in vitro dissolution testing, particle size distribution is regarded as a physical reduction to the relevant moiety of the specimen to be sampled for subsequent testing.

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Effect of Agitation Regimen on the in vitro Release of Leuprolide from Poly(Lactic-Co-Glycolic) Acid Microparticles

Cited by 16 publications

References 50 publications

Accelerated Polymer Biodegradation of Risperidone Poly(d, l-Lactide-Co-Glycolide) Microspheres

Accelerated Polymer Biodegradation of Risperidone Poly(d, l-Lactide-Co-Glycolide) Microspheres

Meeting the unmet: from traditional to cutting-edge techniques for poly lactide and poly lactide-co-glycolide microparticle manufacturing

Towards Standardized Dissolution Techniques for In Vitro Performance Testing of Dry Powder Inhalers

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