In Vitro Release Testing of PLGA Microspheres with Franz Diffusion Cells

Herrera, Laura C.; Tesoriero, María Victoria Defain; Hermida, Laura G.

doi:10.14227/dt190212p6

Cited by 22 publications

(7 citation statements)

References 27 publications

(32 reference statements)

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“…At specified time points (1-10 days and every two days thereafter), tubes were centrifuged at 8,000 rpm for 5 minutes and 1 mL supernatant was removed and then replaced with pre-warmed (37 °C) release medium. Leuprolide acetate is stable in pH 7.4 solutions for >30 days [15]. Analysis of leuprolide in release samples was performed by RP-HPLC.…”

Section: Methodsmentioning

confidence: 99%

The nature of peptide interactions with acid end-group PLGAs and facile aqueous-based microencapsulation of therapeutic peptides

Sophocleous

Desai

Mazzara

et al. 2013

Journal of Controlled Release

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An important poorly understood phenomenon in controlled-release depots involves the strong interaction between common cationic peptides and low Mw free acid end-group poly(lactic-co-glycolic acids) (PLGAs) used to achieve continuous peptide release kinetics. The kinetics of peptide sorption to PLGA was examined by incubating peptide solutions of 0.2-4 mM octreotide or leuprolide acetate salts in 0.1 M HEPES buffer, pH 7.4, with polymer particles or films at 4-37 °C for 24 h. The extent of absorption/loading of peptides in PLGA particles/films was assayed by two-phase extraction and amino acid analysis. Confocal Raman microspectroscopy and stimulated Raman scattering (SRS) and laser scanning confocal imaging techniques were used to examine peptide penetration in the polymer phase. The release of sorbed peptide from leuprolide-PLGA particles was evaluated both in vitro (PBST + 0.02% sodium azide, 37 °C) and in vivo (male Sprague-Dawley rats). We found that when the PLGA-COOH chains are sufficiently mobilized, therapeutic peptides not only bind at the surface, a common belief to date, but can also internalized and distributed throughout the polymer phase at physiological temperature forming a salt with low-molecular weight PLGA-COOH. Importantly, absorption of leuprolide into low MW PLGA-COOH particles yielded ~17 wt% leuprolide loading in the polymer (i.e., ~70% of PLGA-COOH acids occupied), and the absorbed peptide was released from the polymer for > 2 weeks in a controlled fashion in vitro and as indicated by sustained testosterone suppression in male Sprague-Dawley rats. This new approach, which bypasses the traditional encapsulation method and associated production cost, opens up the potential for facile production of low-cost controlled-release injectable depots for leuprolide and related peptides.

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Section: Methodsmentioning

confidence: 99%

The nature of peptide interactions with acid end-group PLGAs and facile aqueous-based microencapsulation of therapeutic peptides

Sophocleous

Desai

Mazzara

et al. 2013

Journal of Controlled Release

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“…MB has some inherent antibacterial activity; therefore, bacterial growth in the release media was not anticipated to be an issue for these implants [43]. However, SA was added to IS and IA release media to prevent microbial growth [23,44,45] over the course of the release experiment. The release profiles of MB from each of the five implant designs are shown in Figure 6.…”

Section: In Vitro Drug Releasementioning

confidence: 99%

Development of a Biodegradable Subcutaneous Implant for Prolonged Drug Delivery Using 3D Printing

et al. 2020

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Implantable drug delivery devices offer many advantages over other routes of drug delivery. Most significantly, the delivery of lower doses of drug, thus, potentially reducing side-effects and improving patient compliance. Three dimensional (3D) printing is a flexible technique, which has been subject to increasing interest in the past few years, especially in the area of medical devices. The present work focussed on the use of 3D printing as a tool to manufacture implantable drug delivery devices to deliver a range of model compounds (methylene blue, ibuprofen sodium and ibuprofen acid) in two in vitro models. Five implant designs were produced, and the release rate varied, depending on the implant design and the drug properties. Additionally, a rate controlling membrane was produced, which further prolonged the release from the produced implants, signalling the potential use of these devices for chronic conditions.

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“…The experimental curve relative to SLN-PRG is almost superimposable to the diffusive theoretical curve [31,33].…”

Section: In Vitro Prg Release Kineticsmentioning

confidence: 61%

Progesterone lipid nanoparticles: Scaling up and in vivo human study

Esposito

Sguizzato

Drechsler

et al. 2017

European Journal of Pharmaceutics and Biopharmaceutics

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In Vitro Release Testing of PLGA Microspheres with Franz Diffusion Cells

Cited by 22 publications

References 27 publications

The nature of peptide interactions with acid end-group PLGAs and facile aqueous-based microencapsulation of therapeutic peptides

The nature of peptide interactions with acid end-group PLGAs and facile aqueous-based microencapsulation of therapeutic peptides

Development of a Biodegradable Subcutaneous Implant for Prolonged Drug Delivery Using 3D Printing

Progesterone lipid nanoparticles: Scaling up and in vivo human study

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