Mucoadhesive beclomethasone microspheres for powder inhalation: their pharmacokinetics and pharmacodynamics evaluation

“…However, BD is a highly hydrophobic drug, and it thus presents slow dissolution rate within airways and rapid mucociliary clearance, resulting on a relative short local duration of action following administration with a consequent reduction in its therapeutic effect (Jacobs, Müller, 2002;Sakagami et al, 2002). Following powder aerosol administration, BD is partially removed from its primary site of action, the lower airways, by mucociliary clearance prior to dissolution and absorption, and eventually, swallowed into the gastrointestinal tract (Hochhaus et al, 1997).…”

Section: Introductionmentioning

confidence: 99%

Stability-indicating RP-HPLC method for determination of beclomethasone dipropionate in nanocapsule suspensions

Chassot

Ferreira

Gomes

et al. 2015

Braz. J. Pharm. Sci.

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A simple stability-indicating RP-HPLC/UV method was validated for determination of beclomethasone dipropionate (BD) in nanocapsule suspensions. Chromatographic conditions consisted of a RP C 18 column (250 mm x 4.60 mm, 5 µm, 110 Å), using methanol and water (85:15 v/v) as mobile phase at 1.0 mL/ min with UV detection at 254 nm. The calibration curve was found to be linear in the concentration range of 5.0-25.0 µg/mL with a correlation coefficient > 0.999. Precision was demonstrated by a relative standard deviation lower than 2.0%. Accuracy was assessed by the recovery test of BD from nanocapsules (98.03% to 100.35%). Specificity showed no interference from the components of nanocapsules or from the degradation products derived from acid, basic and photolytic conditions. In conclusion, the method is suitable to be applied to assay BD in bulk drug and in nanocapsules, and it can be employed to study stability and degradation kinetics.Uniterms: High performance liquid chromatography/reverse phase/quantitative analysis. Beclomethasone dipropionate/determination. Nanocapsule/suspensions. Nanoparticles.Um método simples de CLAE-FR/UV indicativo de estabilidade foi validado para a determinação do dipropionato de beclometasona (BD) em suspensões de nanocápsulas. As condições cromatográficas foram: coluna C18 fase reversa (250 mm x 4,60 mm, 5 µm, 110 Å), usando como fase móvel metanol e água (85:15 v/v) a 1,0 mL/min, com detecção UV a 254 nm. A curva de calibração foi linear no intervalo de 5,0-25,0 µg/mL com coeficiente de correlação >0,999. A precisão foi demonstrada por um desvio padrão relativo menor que 2,0%. A exatidão foi avaliada pelo teste de recuperação do BD a partir das nanocápsulas (98,03% a 100,35%). O teste de especificidade não mostrou interferência dos componentes das nanocápsulas e nem dos produtos de degradação derivados de condições ácidas, básicas e fotolíticas. Em conclusão, o método é adequado para ser aplicado na avaliação do BD puro e em nanocápsulas e pode ser empregado para o estudo de estabilidade e degradação cinética.Unitermos: Cromatografia líquida de alta eficiência/fase reversa/análise quantitativa. Dipropionato de beclometasona/determinação. Nanocápsulas/suspensões. Nanopartículas.

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“…It is mostly achieved by using mucoadhesive polymers. Uses of mucoadhesive-based formulations include local action to treat the pathology of diseases [3][4][5] , protein and peptides delivery 6 , delivery of drug molecules intranasally [7][8][9] , delivery to the brain across the bloodbrain barrier 10 , in ophthalmic formulations to increase the contact time with the mucus lining of occular epithelium 11 , and drug delivery through inhalation 12 . Formulations of mucoadhesive polymercontaining formulations is of interest in the design of delivery systems to prolong the residence time of drugs present in dosage form at the site of absorption and facilitate intimate contact with the underlying absorptive surface to enhance the bioavailability of drugs.…”

Section: Introductionmentioning

confidence: 99%

Untitled

Nayak¹,

Hasnain²,

Beg³

et al. 2010

ScienceAsia

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Novel mucoadhesive beads were developed and evaluated for oral controlled release of the hypoglycaemic agent gliclazide. Various formulations of mucoadhesive beads were prepared using two different natural polymers, alginate and ispaghula, in various stoichiometric proportions with CaCl2 as a source of counter ions. The mucoadhesive beads were characterized for entrapment efficiency, particle size, surface morphology, and swelling index. The kinetics of drug release and their mucoadhesive nature in vitro using goat intestinal mucosa was also investigated at various physiological pH conditions. The effects of various proportions of the two polymers along with the effect of various percentages of counter ions on mucoadhesion property, size, entrapment efficiency, and drug release behaviour were studied. The effective mucoadhesion property with sustained release profile was observed from optimized mucoadhesive beads consisting of alginate and ispaghula husk (1:1) and polymer (2:1) with 5-10% w/v counter ions (CaCl2). These formulations showed optimum mucoadhesion behaviour having more than 70% w/v of drug entrapment and particle sizes of 896.7 ± 0.8 and 920.6 ± 1.2 µm, respectively.

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Mucoadhesive beclomethasone microspheres for powder inhalation: their pharmacokinetics and pharmacodynamics evaluation

Cited by 69 publications

References 18 publications

In vivo animal models for drug delivery across the lung mucosal barrier☆

In vivo animal models for drug delivery across the lung mucosal barrier☆

Stability-indicating RP-HPLC method for determination of beclomethasone dipropionate in nanocapsule suspensions

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