Microspheres prepared with biodegradable PHBV and PLA polymers as prolonged-release system for ibuprofen: in vitro drug release and in vivo evaluation

Bazzo, Giovana Carolina; Macedo, Aline Teixeira de; Crenca, Janine Paula; Silva, Virgínia Emiliana; Pereira, Eduardo Manoel; Zétola, Melissa; Pezzini, Bianca Ramos

doi:10.1590/s1984-82502012000400021

Cited by 17 publications

(5 citation statements)

References 19 publications

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“…On the other hand, the initial burst release is controlled by a diffusive escape of the drug, and since its release begins at the surface of the microsphere, the more regular surface porosity of the complexed TPy‐functionalized PLAs could enhance this initial release . By contrast, the smooth surface of the TPy–PLA–OH microspheres hinders penetration, and a prolonged release is observed, as also reported by Bazzo et al…”

Section: Resultsmentioning

confidence: 54%

Metallo-Polymer Chain Extension Controls the Morphology and Release Kinetics of Microparticles Composed of Terpyridine-Capped Polylactides and their Stereocomplexes

Brzeziński

Kacprzak

Calderón

et al. 2017

Macromol. Rapid Commun.

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Control over morphology and porosity of supramolecular complexed polylactide (PLA) microparticles can be achieved by manipulation of the supramolecular interactions between their constituent polymeric building blocks. It is expected that such modular systems are ideal candidates to serve as degradable delivery carriers. In view of this goal, this study reports about a modular fabrication of biodegradable microparticles from terpyridine (TPy) and bisterpyridine (bisTPy) end-functionalized PLAs that can be transiently extended by chain association through differently strong complexation to three metal cations: Ni , Co , or Fe . Further influence on the morphology of the particles can be exerted by hydrogen-bonding association of enantiomeric l- and d-PLA chains in the form of stereocomplexes. Both effects cause different stabilization of phase-separating TPy and bisTPy PLA micrograins in a process of droplet-based microfluidic particle templating, resulting in different forms of microparticle porosity. If the resulting particles are tailored such to be highly porous, they exhibit a faster release of a model drug, (S)-(+)-4-(3-amino-pyrrolidino)-7-nitrobenzo-furazan, than if they have smooth surfaces. As a result, control over the synthetic parameters, and hence, the particle porosity, can be used to tune the release profiles of drugs from the PLA microspheres.

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Section: Resultsmentioning

confidence: 54%

Metallo-Polymer Chain Extension Controls the Morphology and Release Kinetics of Microparticles Composed of Terpyridine-Capped Polylactides and their Stereocomplexes

Brzeziński

Kacprzak

Calderón

et al. 2017

Macromol. Rapid Commun.

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“…At present, most of the researches on the biomedical field of drug release are concentrated on the first and second generations, with some on the third generation, while research on the fourth generation, especially the research on drug stents, is almost absent. For example, Bazzo et al [ 7 ] prepared PHBV/PLA microspheres containing ibuprofen, to prolong the drug release and in vitro dissolution profiles, and showed that the formulation containing PHBV/PLA at the proportion of 30/70 gave the best results, in terms of prolonging the ibuprofen release. Li et al [ 8 ] prepared composite microspheres from bioactive wollastonite (W) and PHBV.…”

Section: Introductionmentioning

confidence: 99%

Drug Release Property of Poly 3-Hydroxybutyrate 4-Hydroxybutyrate (P34HB) as Drug-Eluting Coatings on Metal Coronary Stents

Jian

Zhu

2022

Polymers

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Drug-eluting stents (DES) have become the main method of interventional therapy for coronary heart disease, because their drug coating can effectively reduce the incidence of restenosis after stent implantation. Biodegradable polymers for coatings are the latest development direction for coating polymers, because they can be degraded into small molecules in the human body. In this study, the polymer P34HB(P34HB-1:4HB% = 1 mol%, Mw: 225,000; P34HB-10:4HB% = 10 mol%, Mw: 182,000), the fourth generation of biodegradable Polyhydroxy alkanoates (PHAs), was coated on stents to evaluate the drug release properties of the DES. Both P34HB-1 and P34HB-10 coatings showed increased drug release rates, as the polymer concentrations were gradually increased from 8 mg/mL to 28 mg/mL. Both P34HB-1 and P34HB-10 coatings showed increased drug release rates as the drug polymer ratios were gradually changed from 1:10 to 1:2. The drug release rates of the P34HB-1 coatings became slower than P34HB-10, thus showing sustained drug release effects. The drug release rates of the P34HB-1 coatings decreased when Rates of solution flow increased, decreased when Focusing pressures decreased, and decreased when Mandrel moving speeds increased. P34HB-1 coatings prepared with CHCl3/NPA (10:1) mixed solvents had better controlled drug release rates compared to Firebird2®. The drug release rates of P34HB-1 coatings prepared with CHCl3 solutions decreased as the outer layer weights were increased from 0 to 800 μg. When the outer layer weights reached 800 μg, the drug release rates of P34HB-1 coatings were slower than Firebird2®. P34HB-1 coatings prepared with both CHCl3/NPA (10:1) mixed solvents and double layers had more effectively controlled drug release rates than P34HB-1 coatings prepared with only mixed solvents or double layers and these effects were far greater than Firebird2@; thus, P34HB-1 represents a latent polymer for DES.

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“…The sustained slow release of IBUP from porous and hydrogel microspheres of PLGA copolymers outlined their potential use in the treatment of osteoarticular conditions [48,49]. Various biodegradable polysaccharides [50][51][52][53][54] and polyesters [55][56][57][58][59] have been evaluated as promising loading and releasing matrices for IBUP, enabling the development of unconventional and effective therapeutic systems.…”

Section: Introductionmentioning

confidence: 99%

Bioactive Ibuprofen-Loaded PLGA Coatings for Multifunctional Surface Modification of Medical Devices

et al. 2021

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To modulate the biofunctionality of implantable medical devices commonly used in clinical practice, their surface modification with bioactive polymeric coatings is an attractive and successful emerging strategy. Biodegradable coatings based on poly(lactic acid-co-glycolic acid), PLGA, represent versatile and safe candidates for surface modification of implantable biomaterials and devices, providing additional tunable ability for topical delivery of desired therapeutic agents. In the present study, Ibuprofen-loaded PLGA coatings (PLGA/IBUP) were obtained by using the dip-coating and drop-casting combined protocol. The composite materials demonstrated long-term drug release under biologically simulated dynamic conditions. Reversible swelling phenomena of polymeric coatings occurred in the first two weeks of testing, accompanied by the gradual matrix degradation and slow release of the therapeutic agent. Irreversible degradation of PLGA coatings occurred after one month, due to copolymer’s hydrolysis (evidenced by chemical and structural modifications). After 30 days of dynamic testing, the cumulative release of IBUP was ~250 µg/mL. Excellent cytocompatibility was revealed on human-derived macrophages, fibroblasts and keratinocytes. The results herein evidence the promising potential of PLGA/IBUP coatings to be used for surface modification of medical devices, such as metallic implants and wound dressings.

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Microspheres prepared with biodegradable PHBV and PLA polymers as prolonged-release system for ibuprofen: in vitro drug release and in vivo evaluation

Cited by 17 publications

References 19 publications

Metallo-Polymer Chain Extension Controls the Morphology and Release Kinetics of Microparticles Composed of Terpyridine-Capped Polylactides and their Stereocomplexes

Metallo-Polymer Chain Extension Controls the Morphology and Release Kinetics of Microparticles Composed of Terpyridine-Capped Polylactides and their Stereocomplexes

Drug Release Property of Poly 3-Hydroxybutyrate 4-Hydroxybutyrate (P34HB) as Drug-Eluting Coatings on Metal Coronary Stents

Bioactive Ibuprofen-Loaded PLGA Coatings for Multifunctional Surface Modification of Medical Devices

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