Insulin-loaded PLGA/cyclodextrin large porous particles with improved aerosolization properties: In vivo deposition and hypoglycaemic activity after delivery to rat lungs

Ungaro, Francesca; Bianca, Roberta d’Emmanuele di Villa; Giovino, Concetta; Miro, Agnese; Sorrentino, Raffaella; Quaglia, Fabiana; Rotonda, Maria Immacolata La

doi:10.1016/j.jconrel.2008.12.011

Cited by 152 publications

(97 citation statements)

References 39 publications

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“…The starting volume of water should be at least 95% of the desired final volume; otherwise, a precipitate may form when some compounds are added (34). This simulated fluid was used to evaluate the in vitro release of insulin from poly(lactide-co-glycolide) (PLGA)/cyclodextrin porous particles intended for pulmonary delivery of insulin (35).…”

Section: Pulmonary Routementioning

confidence: 99%

Simulated Biological Fluids with Possible Application in Dissolution Testing

Marques¹,

Löebenberg²,

Almukainzi³

2011

Dissolution Technol.

839

514

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This literature review is a compilation of the composition and, in most cases, the preparation instructions for simulated biological fluids that may be used as dissolution media in the evaluation of dissolution profiles and amount of drug released from pharmaceutical dosage forms. The use of simulated biological fluids can give a better understanding of the release mechanisms and possible in vivo behavior of a product and enhance the predictive capability of the dissolution testing. A summary of the major characteristics of the most used routes of administration that may affect dissolution and absorption of drug substances is presented. The routes and simulated biological fluids covered by this review are:• Parenteral: simulated body fluid and simulated synovial fluid.• Oral: fasted-state simulated gastric fluid, fed-state simulated gastric fluid, fasted-state simulated intestinal fluid, fed-state simulated intestinal fluid, simulated colonic fluid, fasted-state simulated colonic fluid, and fed-state simulated colonic fluid.• Buccal and sublingual: simulated saliva.• Pulmonary: simulated lung fluid.• Vaginal: simulated vaginal fluid and simulated semen.• Ophthalmic: simulated tears.Simulated sweat is also included. Some examples of how these simulated biological fluids are used to evaluate dosage forms are included in each route of administration.

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Section: Pulmonary Routementioning

confidence: 99%

Simulated Biological Fluids with Possible Application in Dissolution Testing

Marques¹,

Löebenberg²,

Almukainzi³

2011

Dissolution Technol.

839

514

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“…8,9) Furthermore, Ungaro et al prepared gas-foamed large porous particles based on poly(lactic-co-glycolic) acid polymer (PLGA) via a double emulsion-solvent evaporation technique. [10][11][12] These reports concluded that spherical particles with hollow or porous internal structures exhibited extremely better flow and aerosolization properties than the normal mechanically micronized crystalline.We previously developed a spray freeze-drying (SFD) method, which is a combination of conventional spray-drying and freeze-drying techniques. 13,14) In this method, a solution of the drug and release-modified excipient is co-sprayed into liquid nitrogen, causing the solution to immediately freeze and form a suspension.…”

mentioning

confidence: 99%

mentioning

confidence: 99%

Spray Freeze-Dried Porous Microparticles of a Poorly Water-Soluble Drug for Respiratory Delivery

Niwa

Mizutani

Danjo

2012

CHEMICAL & PHARMACEUTICAL BULLETIN

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Particles of poorly water-soluble drugs were prepared to develop a dry powder inhaler (DPI). Spray freeze-drying (SFD) technique using a four-fluid nozzle (4N), which has been developed by authors, was applied in this research. Ciclosporin and mannitol were used as a poorly water-soluble model drug and a dissolution-enhanced carrier, respectively. The organic solution of ciclosporin and aqueous solution of mannitol were separately and simultaneously atomized through the 4N, and the two solutions were collided with each other at the tip of the nozzle edge. The spray mists were immediately frozen in liquid nitrogen to form a suspension. Then, the iced droplets were freeze-dried to prepare the composite particles of the drug and carrier. tert-Butyl alcohol (t-BuOH) was used as the organic spray solvent due to its relatively high freezing point. The resultant composite particles with varying drug content were characterized depending on their morphological and physicochemical properties. The particles contained amorphous ciclosporin and δ-crystalline mannitol. The characteristic porous structure of SFD particles potentially contributed to their good aerodynamic performance. A series of particles with a similar size distribution and different drug content revealed that the incorporation of mannitol successfully improved the cohesive behavior of ciclosporin, leading to enhanced aerosol dispersion. The dissolution test method using low-volume medium was newly established to simulate the release process from particles deposited on the surface of the bronchus and pulmonary mucosa. The composite with hydrophilic mannitol dramatically improved the in vitro dissolution behavior of ciclosporin in combination with the porous structure of SFD particles.Key words spray freeze-drying; liquid nitrogen; ciclosporin; porous particle; tert-butyl alcohol Inhalation is the most appropriate route to deliver drugs to treat respiratory disorders such as asthma, chronic obstructive pulmonary disease (COPD), and cystic fibrosis.1-3) This route directly targets the site of action and reduces the occurrence of systemic adverse effects. In addition, there is increasing interest in the use of pulmonary delivery to administer systemically-acting macromolecules, such as inhaled insulin product.4) The aerodynamic size of drug particles should be 5-6 µm or less for optimal airway deposition.5-7) However, particles in this size range have potentially cohesive property and tend to disperse poorly.One approach to achieve excellent inhalation delivery by simultaneously improving the micromeritic properties and reducing the cohesive properties of agents is to design spherical particles with relative large geometric diameters and low particle mass densities. Inter-particulate cohesion could be reduced by enlarging and spheronizing the individual particle, and aerosol performance could be improved by decreasing the weight of the particles, ultimately like soap bubbles. In particular, particle design focused on particle density has been specifically resear...

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“…Synthetic and natural degradable polymers are common and include poly(lactic-co-glycolic) acid (PLGA) (23,24), poly(ethylene glycol)-block-poly(sebacic acid) (PEG-PSA) (25), and gelatin (26), as well as liposomal delivery systems (27,28). Controlled release of insulin from PLGA microparticles in streptozotocin-induced diabetic rat lung resulted in significant reduction of blood glucose at relatively low doses (29).…”

Section: Inhalation Of Synthetic Particles For Deep Lung Depositionmentioning

confidence: 99%

Lung vascular targeting through inhalation delivery: Insight from filamentous viruses and other shapes

Mahmud

Discher

2011

IUBMB Life

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SummarySystemic delivery of therapeutic agents via inhalation of particulates remains an attractive, noninvasive means of administration due to the possibilities of high bioavailability and high patient compliance. Optimization of particle shapes and particle properties for deep lung deposition after inhalation continues to be one of the key challenges. Here, we review several aspects of nanoparticle design for deep lung deposition as well as the nature and extent of translocation through the air-blood barrier for local or systemic vascular targeting. We describe filamentous influenza virus in comparison to worm-like ''filomicelle'' polymers as one example of a nature inspired design. IUBMBIUBMB Life, 63(8): 607-612, 2011

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Insulin-loaded PLGA/cyclodextrin large porous particles with improved aerosolization properties: In vivo deposition and hypoglycaemic activity after delivery to rat lungs

Cited by 152 publications

References 39 publications

Simulated Biological Fluids with Possible Application in Dissolution Testing

Simulated Biological Fluids with Possible Application in Dissolution Testing

Spray Freeze-Dried Porous Microparticles of a Poorly Water-Soluble Drug for Respiratory Delivery

Lung vascular targeting through inhalation delivery: Insight from filamentous viruses and other shapes

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