High encapsulation efficiency of sodium alendronate in eudragit S100/HPMC blend microparticles

Cruz, Letícia; Assumpção, Evelise Rodrigues; Guterres, Sı́lvia Stanisçuaski; Pohlmann, Adriana Raffin

doi:10.1590/s0100-40422009000500016

Cited by 11 publications

(7 citation statements)

References 23 publications

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“…Results show that microencapsulation efficiency ranged from 85 to 89% among MD formulations and 98 to 99% for Hi‐cap100 formulations (Table ). This indicates acceptable encapsulation of flaxseed oil (Cruz, Assumpção, Guterres, & Pohlmann, ). The SEM images of MD and Hi‐cap100 formulations demonstrated that the spray‐dried particles possessed a combination of compact smooth, rough, and dented surface morphologies, whereas freeze‐dried formulations were less spherical and had many surface pores (Figure ).…”

Section: Resultsmentioning

confidence: 99%

A Fluorescence‐based Method for Estimation of Oxygen Barrier Properties of Microspheres

Kak

Bajaj

Bhunia

et al. 2019

Journal of Food Science

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In this study, we developed a fluorescence method to quantify oxygen barrier properties for wall materials used in microencapsulation of oxygen‐sensitive compounds. We used a reversible, oxygen quenching dye, tris (4,7‐diphenyl‐1, 10‐phenanthroline) ruthenium(II) dichloride complex, as a marker to monitor oxygen transport across spray‐dried and freeze‐dried Hi‐cap100 and maltodextrin microspheres. We fit the rate of oxygen transport to Fick's second law and extrapolated an effective oxygen diffusion coefficient Deff. Results show that the Deff for spray‐dried maltodextrin and Hi‐cap100 formulations were in the range of 6.46 × 10−15 to 7.45 × 10−15 m2/s and 16.0 × 10−15 to 22.4 × 10−15 m2/s, respectively. Results also show an increasing trend in thiobarbituric acid reactive substances reaction rate constants, with an increasing Deff for each formulation. Additionally, freeze‐dried maltodextrin formulations had significantly higher Deff (31.1 × 10−15 to 36.0 × 10−15 m2/s) compared to spray‐dried matrices due to a more porous morphology. This new method provides a framework for the in situ estimation of Deff for wall materials in microspheres. Potential applications include the design and selection of wall materials for maximum oxidative stability of encapsulated ingredients. Practical Application Currently, the selection of wall materials used in microencapsulation of lipids takes a trial‐and‐error approach, which can be time consuming and prone to error. In this study, we developed a new methodology to directly assess the oxygen barrier properties of wall materials in microspheres. This method can be used by food scientists to screen wall materials in order to optimize the oxidative stability of encapsulated lipids.

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Section: Resultsmentioning

confidence: 99%

A Fluorescence‐based Method for Estimation of Oxygen Barrier Properties of Microspheres

Kak

Bajaj

Bhunia

et al. 2019

Journal of Food Science

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“…Concerning the encapsulation efficiency, a spectrophotometric method based on the derivatization of sodium alendronate with o-phthalaldehyde was used (Al Deeb et al, 2004;Cruz et al, 2009). A portion of microparticles equivalent to 10 mg of sodium alendronate was dissolved in 50 mL of 0.2 M NaOH and filtered using a filter paper (Whatman n° 40).…”

Section: Determination Of Yield and Encapsulation Efficiencymentioning

confidence: 99%

“…The experiments were carried out as described in our previous work (Cruz et al, 2009), in order to evaluate the gastroresistance at pH 1.2 and the sodium alendronate release profiles at pH 6.8.…”

Section: In Vitro Drug Release Studiesmentioning

confidence: 99%

Microencapsulation of sodium alendronate reduces drug mucosal damage in rats

et al. 2010

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“…The yield was calculated by the ratio of the experimental weight and the sum of the weights of all components, disregarding the water content. Encapsulation efficiency was determined spectrophotometrically at 333 nm using OPA as derivatizing agent (Cruz et al, 2009). Size and size distributions of microparticles were analyzed by laser diffractometry (Malvern Mastersizer, 2000 Inserir referência na parte reference, Malvern Instruments, UK).…”

Section: Preparation and Characterization Of Microparticlesmentioning

confidence: 99%

Formulation of gastroresistant tablets containing sodium alendronate-loaded blend microparticles

Ferreira

Velasquez

Schaffazick

et al. 2015

Braz. J. Pharm. Sci.

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Sodium alendronate is an antiresorptive drug used for the treatment of postmenopausal osteoporosis. However, its oral administration is associated with low bioavailability and gastroesophageal irritation. This work aimed at developing tablets containing sodium alendronate-loaded microparticles by direct compression to achieve a safe and effective form. The parameters evaluated were average weight, hardness, thickness and drug content. In vitro release tests were carried out using simulated gastric and intestinal fluids, and the profiles were analyzed through the Korsmeyer-Peppas mono-or biexponential dependent approaches. Tablets presented adequate average weight, thickness, good mechanical properties and drug content close to 100%. Moreover, the formulation released less than 11% of sodium alendronate in gastric fluid, exhibiting a good gastroresistance. At pH 6.8, almost 100% of the drug was released in 12h, showing a prolonged profile. The mathematical modeling indicated that the experimental data was better fitted to the biexponential equation. Furthermore, a good correlation coefficient was obtained for the Korsmeyer-Peppas model and the release exponent suggested that the drug dissolution was driven by anomalous transport. In conclusion, the microparticulated tablets can be considered a promising alternative for oral delivery of sodium alendronate.Uniterms: Microparticulated tablets/release profile. Sodium alendronate/oral administration. Sodium alendronate/controlled release/in vitro study.O alendronato de sódio é um fármaco da classe dos bisfosfonatos, comumente utilizado no tratamento da osteoporose pós-menopausa. Entretanto, sua administração oral está associada à baixa biodisponibilidade e irritação gastroesofágica. Este trabalho objetivou o desenvolvimento de comprimidos contendo micropartículas de alendronato de sódio por compressão direta, a fim de obter uma forma segura e eficaz. Os parâmetros avaliados foram peso médio, dureza, espessura e teor de fármaco. Estudos de liberação in vitro foram realizados utilizando fluído gástrico e intestinal simulado e o perfil de liberação foi analisado pelos modelos matemáticos de Korsmeyer-Peppas, mono-e biexponencial. Os comprimidos apresentaram peso médio adequado, espessura, dureza e teor próximo a 100%. Além disso, a formulação liberou menos de 11% do fármaco em fluído gástrico, mostrando uma boa gastrorresistência. Em pH 6,8, em torno de 100% do fármaco foram liberados em 12 h, apresentando liberação prolongada. A modelagem matemática indica que os resultados seguem a equação biexponencial. Pela análise do expoente de liberação obtido no modelo de Korsmeyer-Peppas sugere-se que a dissolução do fármaco ocorre por transporte anômalo. Concluindo, a preparação dos comprimidos microparticulados pode ser considerada uma alternativa promissora para a liberação oral do alendronato de sódio. Unitermos:Comprimidos microparticulados/perfil de liberação. Alendronato de sódio/administração oral. Alendronato de sódio/liberação controlada/estudos in vitro.

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High encapsulation efficiency of sodium alendronate in eudragit S100/HPMC blend microparticles

Cited by 11 publications

References 23 publications

A Fluorescence‐based Method for Estimation of Oxygen Barrier Properties of Microspheres

A Fluorescence‐based Method for Estimation of Oxygen Barrier Properties of Microspheres

Microencapsulation of sodium alendronate reduces drug mucosal damage in rats

Formulation of gastroresistant tablets containing sodium alendronate-loaded blend microparticles

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