Chitosan-based spray-dried respirable powders for sustained delivery of terbutaline sulfate

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

doi:10.1016/j.ejpb.2007.04.017

Cited by 109 publications

(60 citation statements)

References 53 publications

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“…Positive features of potential use of microparticles as drug carrier systems include the possibility of controlled drug release and drug targeting, providing protection of incorporated active compounds against degradation, lack of toxicity as its solid matrix is composed of physiological and welltolerated polymers, e.g., chitosan and gelatin, and they allow hydrophilic and/or hydrophobic drugs to be incorporated (5,8). The drug solubility, chemical and physical structure of polymers, and their polymorphic state determine the loading capacity of drug in microparticles.…”

Section: Introductionmentioning

confidence: 99%

“…BUD decreases airway hyper-responsiveness and reduces the number of inflammatory cells and mediators present in airways of patients with asthma. There are many advantages for developing sustained-release formulations for pulmonary drug delivery, which include reduced dosing frequency, improved patient compliance, and reduction of side effects (5)(6)(7).…”

Section: Introductionmentioning

confidence: 99%

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Development of Budesonide Microparticles Using Spray-Drying Technology for Pulmonary Administration: Design, Characterization, In Vitro Evaluation, and In Vivo Efficacy Study

et al. 2009

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Abstract. The purpose of this research was to generate, characterize, and investigate the in vivo efficacy of budesonide (BUD) microparticles prepared by spray-drying technology with a potential application as carriers for pulmonary administration with sustained-release profile and improved respirable fraction. Microspheres and porous particles of chitosan (drug/chitosan, 1:2) were prepared by spray drying using optimized process parameters and were characterized for different physicochemical parameters. Mass median aerodynamic diameter and geometric standard deviation for conventional, microspheres, and porous particles formulations were 2.75, 4.60, and 4.30 µm and 2.56, 1.75, and 2.54, respectively. Pharmacokinetic study was performed in rats by intratracheal administration of either placebo or developed dry powder inhalation (DPI) formulation. Pharmacokinetic parameters were calculated (Ka, Ke, T max , C max , AUC, and Vd) and these results indicated that developed formulations extended half life compared to conventional formulation with onefold to fourfold improved local and systemic bioavailability. Estimates of relative bioavailability suggested that developed formulations have excellent lung deposition characteristics with extended T 1/2 from 9.4 to 14 h compared to conventional formulation. Anti-inflammatory activity of BUD and developed formulations was compared and found to be similar. Cytotoxicity was determined in A549 alveolar epithelial cell line and found to be not toxic. In vivo pulmonary deposition of developed conventional formulation was studied using gamma scintigraphy and results indicated potential in vitro-in vivo correlation in performance of conventional BUD DPI formulation. From the DPI formulation prepared with porous particles, the concentration of BUD increased fourfold in the lungs, indicating pulmonary targeting potential of developed formulations.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Development of Budesonide Microparticles Using Spray-Drying Technology for Pulmonary Administration: Design, Characterization, In Vitro Evaluation, and In Vivo Efficacy Study

et al. 2009

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“…However, the spray drying process variables must be controlled to avoid low yields, sticking and high moisture content. Spray dried particulates can be designed by inclusion of polymers such as, hyaluronan, 7) polylactic acid, 8) chitosan, 9) and poly(lacticco-glycolic acid). 10) Among the cellulose based poly-mers, hydroxypropyl cellulose 11) and hydroxypropyl methyl cellulose 12) have been studied for inhalation delivery.…”

Section: Introductionmentioning

confidence: 99%

Formulation Optimization and Characterization of Spray Dried Microparticles for Inhalation Delivery of Doxycycline Hyclate

Mishra

2011

YAKUGAKU ZASSHI

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The local delivery of antibiotics in the treatment of infectious respiratory diseases is an attractive alternative to deliver high concentration of antimicrobials directly to the lungs and minimize systemic side eŠects. In this study, inhalable microparticles containing doxycycline hyclate, sodium carboxymethylcellulose, leucine and lactose were prepared by spray drying of aqueous ethanol formulations. Box-Behnken design was used to study the in‰uence of various independent variables such as polymer concentration, leucine concentration, ethanol concentration and inlet temperature of the spray dryer on microparticle characteristics. The microparticles were characterized in terms of particle morphology, drug excipient interaction, yield, entrapment e‹ciency, Carr's index, moisture content, thermal properties, X-ray powder diŠraction, aerosolization performance and in vitro drug release. The eŠect of independent variables on spray dryer outlet temperature was also studied. The overall shape of the particles was found to be spherical like doughnuts in the size range of 1.16 5.2 mm. The optimized formulation (sodium carboxymethylcellulose concentration 14％ w/v, leucine concentration 33％ w/v, ethanol concentration 36％ v/v, inlet temperature of 140°C) exhibited the following properties: yield 56.69％, moisture content 3.86％, encapsulation e‹ciency 61.74％, theoretical aerodynamic diameter 3.11 mm and Carr's index 23.5％ at an outlet temperature 77°C. The powders generated were of a suitable mass median aerodynamic diameter (4.89 mm) with 49.3％ˆne particle fraction and exhibited a sustained drug release proˆle in vitro.

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“…Because of its bioadhesive properties, chitosan has received substantial attention as carrier in novel bioadhesive drug delivery systems which prolong the residence time of the drugs at the site of absorption and increase the drug bioavailability (Varum et al, 2008). Thus, some drugs administered via nasal (Learoyd et al, 2008) or gastrointestinal routes have improved their treatment efficacy when they are included into chitosan-based systems (Guerrero et al, 2010).…”

Section: Chitosanmentioning

confidence: 99%

Polysaccharide-Based Nanoparticles for Controlled Release Formulations

Martı́nez¹,

Fernandez²,

Pérez³

et al. 2012

The Delivery of Nanoparticles

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Chitosan-based spray-dried respirable powders for sustained delivery of terbutaline sulfate

Cited by 109 publications

References 53 publications

Development of Budesonide Microparticles Using Spray-Drying Technology for Pulmonary Administration: Design, Characterization, In Vitro Evaluation, and In Vivo Efficacy Study

Development of Budesonide Microparticles Using Spray-Drying Technology for Pulmonary Administration: Design, Characterization, In Vitro Evaluation, and In Vivo Efficacy Study

Formulation Optimization and Characterization of Spray Dried Microparticles for Inhalation Delivery of Doxycycline Hyclate

Polysaccharide-Based Nanoparticles for Controlled Release Formulations

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