Sustained delivery by leucine-modified chitosan spray-dried respirable powders

Learoyd, Tristan P.; Burrows, Jane L.; French, Eddie; Seville, Peter C.

doi:10.1016/j.ijpharm.2009.01.017

Cited by 50 publications

(36 citation statements)

References 46 publications

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“…3) because this technique is able to characterize these properties (34,36). The samples showed a spherical shape, corroborating the results of the previous works carried out with solid chitosan particles (32,37). The images showed microcapsules with smooth surfaces and without macropores, and the size of the primary particles was below 5 μm, lower than that measured using laser diffraction.…”

Section: Resultssupporting

confidence: 86%

“…The Dap-MC powder showed a light yellow color and flowed freely. These characteristics are typical of chitosan powder formulations (32). The use of highpressure homogenization before drying promoted a more homogenous formulation compared with the formulation prepared without this step, as can be observed by the span values (with homogenization, span=1.1; without homogenization, span=2.2).…”

Section: Resultsmentioning

confidence: 68%

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Development of Novel Chitosan Microcapsules for Pulmonary Delivery of Dapsone: Characterization, Aerosol Performance, and In Vivo Toxicity Evaluation

et al. 2015

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ABSTRACT. Pneumocystis carinii pneumonia (PCP) is a major opportunistic infection that affects patients with human immunodeficiency virus. Although orally administered dapsone leads to high hepatic metabolism, decreasing the therapeutic index and causing severe side effects, this drug is an effective alternative for the treatment of PCP. In this context, microencapsulation for pulmonary administration can offer an alternative to increase the bioavailability of dapsone, reducing its adverse effects. The aim of this work was to develop novel dapsone-loaded chitosan microcapsules intended for deep-lung aerosolized drug delivery. The geometric particle size (D 4,3 ) was approximately 7 μm, the calculated aerodynamic diameter (d aero ) was approximately 4.5 μm, and the mass median aerodynamic diameter from an Andersen cascade impactor was 4.7 μm. The in vitro dissolution profile showed an efficient dapsone encapsulation, demonstrating the sustained release of the drug. The in vitro deposition (measured by the Andersen cascade impactor) showed an adequate distribution and a high fine particles fraction (FPF= 50%). Scanning electron microscopy of the pulmonary tissues demonstrated an adequate deposition of these particles in the deepest part of the lung. An in vivo toxicity experiment showed the low toxicity of the drug-loaded microcapsules, indicating a protective effect of the microencapsulation process when the particles are microencapsulated. In conclusion, the pulmonary administration of the novel dapsone-loaded microcapsules could be a promising alternative for PCP treatment.

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Section: Resultssupporting

confidence: 86%

Section: Resultsmentioning

confidence: 68%

Development of Novel Chitosan Microcapsules for Pulmonary Delivery of Dapsone: Characterization, Aerosol Performance, and In Vivo Toxicity Evaluation

et al. 2015

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“…The spray-drying technique was also used to produce microspheres loaded with drugs for local effects, such as the glucocorticoid steroids betamethasone (68,69) and beclometasone dipropionate (70), and the  2 -adrenergic agonists salbutamol (71) and terbutaline sulphate (70), used in the treatment of bronchial asthma. Bethametasone-loaded chitosan microspheres (encapsulation efficiencies up to 95%) containing type-A gelatine and ethylene oxide-propylene oxide block copolymer (Pluronic F68) as modifiers, were spherical and smooth and had a size distribution of 1-5 m and a density of < 0.4 g/cm 3 (68,69).…”

Section: -71)mentioning

confidence: 99%

The potential of chitosan for pulmonary drug delivery

Grenha

Al‐Qadi

Seijo

et al. 2010

Journal of Drug Delivery Science and Technology

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A Grenha, S Al-Qadi, B Seijo, C Remuñán-López, 2010. AbstractThe administration of drugs through the pulmonary route offers great advantages, but also requires overcoming many challenges. There is a need to develop appropriate carriers for each active molecule to be delivered to the desired site in the lung, either for a local or a systemic effect. The polysaccharide chitosan is a very promising material for this purpose, given its demonstrated properties of biodegradability and biocompatibility, as well as mucoadhesivity and ability to enhance macromolecules permeation. In this review, the potential of chitosan to develop drug carriers for delivery to the lung will be discussed.The most important features that can support its selection will be explained. Besides, different approaches to increase its performance, especially concerning solubility, permeation-enhancing properties and gene transfection efficiency, will be presented.Special emphasis will be placed on information of different chitosan-based carriers, namely nanoparticles and microparticles, intended for pulmonary drug delivery.3

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“…Our results are in good correlation with the literature findings about the effect of molecular weight on drug release from the pharmaceutical formulations. 33) As the molecular weight of the chitosan is increased, the release of atorvastatin from chitosan microspheres significantly decreased. The statistical analysis of the release data with one-way ANOVA test indicated that the release profiles of the three microsphere formulations are significantly different from each other (pϽ0.05).…”

Section: Discussionmentioning

confidence: 98%

A Quadruped Study on Chitosan Microspheres Containing Atorvastatin Calcium: Preparation, Characterization, Quantification and <i>in-Vivo</i> Application

Eroğlu

Nemutlu

Türkoğlu

et al. 2010

CHEMICAL & PHARMACEUTICAL BULLETIN

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Atorvastatin is commonly used as a cholesterol lowering agent in patients. Recently, the neuroprotective effects of atorvastatin became the focus of many research studies. In this study, we have formulated chitosan microspheres containing atorvastatin calcium. In-vitro characterization of chitosan microspheres and quantification of atorvastatin calcium from formulations were also evaluated. The neuroprotective efficiency of atorvastatin calcium was investigated by an experimental spinal cord injury model. Atorvastatin calcium microspheres were implanted at the laminectomy area (1 mg/kg) immediately after trauma. Twenty-four hours after injury, motor functions of animals were scored according to modified Tarlov Scale. In spinal cord tissues tumor necrosis factor (TNF)-a, interleukin (IL)-1b, IL-6 and lipid peroxidation levels were quantified and ultrastructural changes have been investigated. The results of all parameters indicate that microspheres containing atorvastatin calcium were capable of improving functional outcome, attenuating the expression of TNF-a, IL-1b and IL-6; lowering lipid peroxidation levels and maintaining the preservation of the cellular uniformity.

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Sustained delivery by leucine-modified chitosan spray-dried respirable powders

Cited by 50 publications

References 46 publications

Development of Novel Chitosan Microcapsules for Pulmonary Delivery of Dapsone: Characterization, Aerosol Performance, and In Vivo Toxicity Evaluation

Development of Novel Chitosan Microcapsules for Pulmonary Delivery of Dapsone: Characterization, Aerosol Performance, and In Vivo Toxicity Evaluation

The potential of chitosan for pulmonary drug delivery

A Quadruped Study on Chitosan Microspheres Containing Atorvastatin Calcium: Preparation, Characterization, Quantification and <i>in-Vivo</i> Application

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