Polymeric delivery systems for dexamethasone

Urbańska, Justyna; Karewicz, Anna; Nowakowska, Maria

doi:10.1016/j.lfs.2013.12.020

Cited by 30 publications

(26 citation statements)

References 49 publications

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“…Due to the hydrophobicity and short half-life of the drug, high doses are required to maintain its therapeutic level in the blood plasma which has undesirable side effects [4]. Long-term systemic exposure to Dex causes adverse side effects.…”

Section: Introductionmentioning

confidence: 99%

Effect of Formulation and Processing Variables on Dexamethasone Entrapment and Release of Niosomes

2015

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Multilamellar niosomes entrapping Dexamethasone (Dex) were prepared by thin film hydration, sonication, respectively. The influence of different processing variables (sonication time, temperature) and formulation variable (cholesterol content) on Dex entrapment efficiency % (EE) was demonstrated. Also, the Dex release from the prepared niosomes in phosphate buffer (pH 7.4) was illustrated. Results indicated that cholesterol increased or decreased the noisome size and EE % depending on its concentration within the formulae. The maximum loading efficiency was 29.2 % when the span 60:cholesterol molar ratio was 100:50 and the hydrating step was conducted by 30 min sonication. Increasing sonication time also increased and then decreased the EE % of Dex into niosomes. Finally, results indicated that in vitro release profiles of Dex from all niosome formulations is an apparently biphasic release process and 5-15 % of drug released from niosomes after 8 h incubation in buffer, depending on the type of niosome.

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Section: Introductionmentioning

confidence: 99%

Effect of Formulation and Processing Variables on Dexamethasone Entrapment and Release of Niosomes

2015

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“…Oral or inhaled corticosteroids and steroids are the first choices for preventative and reliefproviding asthma treatments. However, these drugs, in addition to potential resistance (Barnes 2013) and undesired systemic and local side effects, such as osteoporosis (Hurson, et al 2007), hypertension (Goodwin et al 2011), fluid retention (Rhen and Cidlowski 2005;Urbańska et al 2014) and hypersensitivity (Shakouri and Bahna 2013), are not curative (Apter 2014). Thus, the development of efficient alternative agents and therapeutics for asthma is urgently needed.…”

Section: Introductionmentioning

confidence: 99%

AcCystatin, an immunoregulatory molecule from Angiostrongylus cantonensis, ameliorates the asthmatic response in an aluminium hydroxide/ovalbumin-induced rat model of asthma

Yang

et al. 2014

Parasitol Res

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Epidemiological surveys have demonstrated that helminth infections are negatively related to atopic diseases, including asthma. Defining and characterising specific helminth molecules that have excellent immunomodulatory capacities as potential therapeutics for the treatment or prophylaxis of allergic manifestations are of great interest. AcCystatin, a cystatin protease inhibitor of Angiostrongylus cantonensis, is a homologue of other nematode cystatins with immunoregulatory properties. Here, we aim to determine the effects of AcCystatin on an ovalbumin/aluminium hydroxide (OVA/Al[OH]3)-induced rat model of asthma. Wistar rats were randomly divided into four groups, including a control group, an OVA/Al[OH]3-induced asthma group, a group receiving AcCystatin immunisation prior to OVA/Al[OH]3-induced asthma and a group receiving AcCystatin treatment after OVA/Al[OH]3-induced asthma. The numbers of eosinophils, basophils, neutrophils, lymphocytes and monocytes in the peripheral blood and of eosinophils in the bronchoalveolar lavage fluid (BALF) were counted for each animal. The expression levels of the cytokines interferon-γ, interleukin (IL) 4, IL-5, IL-6, IL-10, IL17A and tumour necrosis factor receptor-α in BALF, of OVA-specific immunoglobulin E in BALF and serum and of the chemokines eotaxin-1, eotaxin-2, eotaxin-3, MCP-1 and MCP-3 in lung tissue were measured. In addition, the degree of peribronchial and perivascular inflammation and the intensity of goblet cell metaplasia were qualitatively evaluated. The sensitised/challenged rats developed an extensive cell inflammatory response of the airways. AcCystatin administration significantly reduced the cellular infiltrate in the perivascular and peribronchial lung tissues and reduced both goblet mucous production and eosinophil infiltration. The rats that were treated with AcCystatin before or after sensitisation with OVA showed significant decreases in eotaxin-1, eotaxin-3 and MCP-1 expression in the lung tissue. The production of IL-4, IL-5, IL-6 and IL-17A and of OVA-specific IgE antibodies was also significantly reduced in AcCystatin-treated rats compared with untreated asthmatic rats. The AcCystatin treatment was associated with a significant increase in IL-10 levels. Our present findings provide the first demonstration that AcCystatin is an effective agent in the prevention and treatment of the airway inflammation associated with asthma.

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“…Despite many published studies about nanoparticles containing DEX in the last decade [15][16][17][18], there are few reports about in vitro skin penetration/permeation after cutaneous administration of these formulations.…”

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confidence: 99%

Submicron polymeric particles prepared by vibrational spray-drying: Semisolid formulation and skin penetration/permeation studies

Beber¹,

Andrade²,

Kann³

et al. 2014

European Journal of Pharmaceutics and Biopharmaceutics

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Topical glucocorticoids (TG) such as dexamethasone (DEX) have been used for decades for the treatment of skin diseases. However, TG present welldocumented side effects and their delivery to the skin is often insufficient.Therefore, many efforts have been undergone to improve the amount of drug delivered to the skin and to reduce side effects at the same time. In this work, the feasibility of DEX-submicron polymeric particles (SP) prepared by vibrational spray-drying as an approach to overcome the challenges associated with the topical administration of this drug class was evaluated. DEX was homogeneously dispersed in the SP matrix, according to confocal Raman microscopy analysis. Drug-loaded SP were incorporated into the oil phase of oil-in-water emulsions (creams). The formulation containing polymeric submicron particles (C-SP) showed controlled drug release kinetics and a significant drug accumulation in skin compared to formulations containing nonpolymeric particles or free drug. DEX accumulation in the stratum corneum was evaluated by tape stripping and a depot effect over time was observed for C-SP, while the formulation containing the free drug showed a decrease over time.Similarly, C-SP presented higher drug retention in epidermis and dermis in skin penetration studies performed on pig skin in Franz diffusion cells, while drug permeation into the receptor compartment was negligible. It was demonstrated, for the first time, the advantageous application of submicron polymeric particles obtained by vibrational spray-drying in semisolid formulations for cutaneous administration to overcome challenges related to the therapy with TG such as DEX.

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Polymeric delivery systems for dexamethasone

Cited by 30 publications

References 49 publications

Effect of Formulation and Processing Variables on Dexamethasone Entrapment and Release of Niosomes

Effect of Formulation and Processing Variables on Dexamethasone Entrapment and Release of Niosomes

AcCystatin, an immunoregulatory molecule from Angiostrongylus cantonensis, ameliorates the asthmatic response in an aluminium hydroxide/ovalbumin-induced rat model of asthma

Submicron polymeric particles prepared by vibrational spray-drying: Semisolid formulation and skin penetration/permeation studies

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