Delivery of ofloxacin to the lung and alveolar macrophages via hyaluronan microspheres for the treatment of tuberculosis

Hwang, Sang Mee; Kim, D.D.; Chung, Suk‐Jae; Shim, Chang-Su

doi:10.1016/j.jconrel.2008.04.009

Cited by 96 publications

(45 citation statements)

References 35 publications

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“…Hyaluronate has also been proposed as carrier for drug delivery to the lung, either as a scaffold for modified release formulations or for particle/drug targeting to alveolar macrophages, e.g. for treatment of tuberculosis (Hwang et al, 2008).…”

Section: Introductionmentioning

confidence: 99%

Engineered sodium hyaluronate respirable dry powders for pulmonary drug delivery

Martinelli

Balducci

Kumar

et al. 2017

International Journal of Pharmaceutics

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Engineered sodium hyaluronate respirable dry powders for pulmonary drug delivery.International Journal of Pharmaceutics http://dx.doi.org/10. 1016/j.ijpharm.2016.12.002 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. Abstract:Sodium hyaluronate (HYA) warrants attention as a material for inhalation due to its (i) therapeutic potential, (ii) utility as a formulation excipient or drug carrier, and (iii) ability to target lung inflammation and cancer. This study aimed to overcome formulation and manufacturing impediments to engineer biocompatible spray-dried HYA powders for inhalation. Novel methodology was developed to produce HYA microparticles by spray drying. Different types of surfactant were included in the formulation to improve powder respirability, which was evaluated in vitro using cascade impactors. The individual formulation components and formulated products were evaluated for their biocompatibility with A549 respiratory epithelial cells. The inclusion of stearyl surfactants, 5% w/v, produced the most respirable HYA-powders; FPF 59.0-66.3%. A trend to marginally higher respirability was observed for powders containing stearylamine > stearyl alcohol > cetostearyl alcohol. Pure HYA was biocompatible with A549 cells at all concentrations measured, but the biocompatibility of the stearyl surfactants (based on lethal concentration 50%; LC50) in the MTT assay ranked stearyl alcohol > cetostearyl alcohol > stearylamine with LC50 of 24.7, 13.2 and 1.8 µg/mL, respectively. We report the first respirable HYA powders produced by spray-drying. A lead formulation containing 5% stearyl alcohol was identified for further studies aimed at translating the proposed benefits of inhaled HYA into safe and clinically effective HYA products.

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Section: Introductionmentioning

confidence: 99%

Engineered sodium hyaluronate respirable dry powders for pulmonary drug delivery

Martinelli

Balducci

Kumar

et al. 2017

International Journal of Pharmaceutics

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“…However, the concentration of the drug in the lung was 10-times higher following direct delivery to the lung, demonstrating the great potential of the formulation in the therapy of lung tuberculosis. This effect was also much more pronounced for ofloxacin-loaded hyaluronic acid microparticles as compared to the unformulated powder of the drug (Hwang et al, 2008), evidencing a positive effect of the hyaluronic acid that is justified by its mucoadhesive character (Grabovac et al, 2005). Encapsulation in presence of the polymer was also reported to enhance the in vitro uptake of ofloxacin by macrophages (cell line RAW 264.7), as compared to control ofloxacin microparticles spray-dried in the absence of polymer (Hwang et al, 2008).…”

Section: Natural Drug Carriers Designed For Tuberculosis Treatmentmentioning

confidence: 88%

“…This effect was also much more pronounced for ofloxacin-loaded hyaluronic acid microparticles as compared to the unformulated powder of the drug (Hwang et al, 2008), evidencing a positive effect of the hyaluronic acid that is justified by its mucoadhesive character (Grabovac et al, 2005). Encapsulation in presence of the polymer was also reported to enhance the in vitro uptake of ofloxacin by macrophages (cell line RAW 264.7), as compared to control ofloxacin microparticles spray-dried in the absence of polymer (Hwang et al, 2008). Apart from the recognition of hyaluronan evidenced by CD44 receptors of macrophages, as the authors mentioned, this effect might be additionally attributed to a Among all the described formulations of polymeric microparticles, only those composed by alginate were tested in animal models of the disease.…”

Section: Natural Drug Carriers Designed For Tuberculosis Treatmentmentioning

confidence: 94%

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Natural carriers for application in tuberculosis treatment

Costa

Grenha

2012

Journal of Microencapsulation

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“…For example, it has been shown that spray-dried HA microspheres allow favourable ofloxacin delivery to the lung via inhalation, determining a superior pharmacological effect compared to free ofloxacin and to other routes of ofloxacin administration [199]. Similarly, inhaled HA microparticles have displayed prolonged pulmonary retention of salbutamol sulphate and reduced systemic exposure and side effects in a rat model [200].…”

Section: Drug Delivery Systemsmentioning

confidence: 99%

Hyaluronic Acid in the 3<sup>rd</sup> Millennium

Fallacara¹,

Baldini²,

Manfredini³

et al. 2018

Preprint

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Since its first isolation in 1934, hyaluronic acid (HA) has been studied across a variety of research areas. This unbranched glycosaminoglycan consisting of repeating disaccharide units of N-acetyl-D-glucosamine and D-glucuronic acid is almost ubiquitary in humans and in other vertebrates. HA is involved in many key processes -including cell signaling, wound reparation, tissue regeneration, morphogenesis, matrix organization and pathobiology-, and has unique physico-chemical properties -such as biocompatibility, biodegradability, mucoadhesivity, hygroscopicity and viscoelasticity. For these reasons, exogenous HA has been investigated as drug delivery system and treatment in cancer, ophthalmology, arthrology, pneumology, rhinology, urology, aesthetic medicine and cosmetic. To improve and customize its properties and applications, HA can be subjected to chemical modifications: conjugation and crosslinking. The present review gives an overview regarding HA, describing its history, physico-chemical, structural and hydrodynamic properties, and biology -occurrence, biosynthesis (by hyaluronan synthases), degradation (by hyaluronidases and oxidative stress), roles, mechanisms of action and receptors. Furthermore, both conventional and recently emerging methods developed for the industrial production of HA and its chemical derivatization are presented. Finally, the medical, pharmaceutical and cosmetic applications of HA and its derivatives are reviewed, reporting examples of HA-based products which currently are on the market or are undergoing further investigations.

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Delivery of ofloxacin to the lung and alveolar macrophages via hyaluronan microspheres for the treatment of tuberculosis

Cited by 96 publications

References 35 publications

Engineered sodium hyaluronate respirable dry powders for pulmonary drug delivery

Engineered sodium hyaluronate respirable dry powders for pulmonary drug delivery

Natural carriers for application in tuberculosis treatment

Hyaluronic Acid in the 3<sup>rd</sup> Millennium

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