Comparative study of sustained-release lipid microparticles and solid dispersions containing ibuprofen

Almeida, Hugo; Amaral, Maria Helena; Lobão, Paulo

doi:10.1590/s1984-82502012000300020

Cited by 12 publications

(12 citation statements)

References 10 publications

(5 reference statements)

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“…Stearic acid was melted on a water bath with a temperature limit of 72°C. The drug particles grounded to the fine size was dispersed with molten stearic acid aqueous phase consisting of water and tween 80 at 72°C was the molten phase was slowly added to the aqueous phase by steering and the emulsification was assisted by homogenizer for 15 minutes 8 . The dispersion rapidly cools down at 20°C by immersing the solution in ice bath.…”

Section: Issn 2321-547xmentioning

confidence: 99%

Formulation And Evaluation Of Acyclovir Sodium Solid Lipid Microparticles

Nagappa¹,

Agarwal²,

Chikkamath³

et al. 2016

Am J Drug Deliv

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Acyclovir sodium is an antiviral drug used to treat herpes, chicken pox and herpes skin infections. Acyclovir sodium potential as an antiviral drug is limited by its low oral bioavailability (20-30%) with short half-life (2-3 hours) with poor plasma protein binding. There is an opportunity to utilize Acyclovir sodium as an antiviral drug by enhancing the bioavailability by formulation technology. In this paper solid microparticle (o/w) of Acyclovir was prepared by melt dispersion technique. The characterization of drug using scanning electron microscopy, FT-IR, particle size, percentage yield, drug loading capacity, hausner's ratio and carr's index, bulk density and tapped density. In vitro drug release studies using phosphate buffer has shown as formulation F5 sustained release for 17 hrs.

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Section: Issn 2321-547xmentioning

confidence: 99%

Formulation And Evaluation Of Acyclovir Sodium Solid Lipid Microparticles

Nagappa¹,

Agarwal²,

Chikkamath³

et al. 2016

Am J Drug Deliv

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“…Lipid microparticles of 1:2 ibuprofen/hydrogenated castor oil (Cutina ® HR) ratio were prepared using the emulsion/chilling method [17]. The lipophilic excipient was melted on a hot plate (85-88°C) under stirring at 600 rpm and ibuprofen was added [17].…”

Section: Preparation Of Lipid Microparticlesmentioning

confidence: 99%

“…The lipophilic excipient was melted on a hot plate (85-88°C) under stirring at 600 rpm and ibuprofen was added [17]. The oil phase was slowly added to a Tween ® 80 solution (1.5%, w/w) at the same temperature, followed by the quick addition of a mixture of water:propylene glycol (75:25) at 0°C, maintaining the agitation at 600 rpm [17]. The obtained lipid microparticles were filtered and washed with water [17].…”

Section: Preparation Of Lipid Microparticlesmentioning

confidence: 99%

“…Microparticles can have numerous advantages, as a good biocompatibility, low toxicity, high stability, and can improve efficacy, absorption, and bioavailability [16,17]. Some of the methods for production of lipid microparticles include: doubleemulsion solvent evaporation, emulsion/chilling, fluid supercritical, atomization and extrusion [17][18][19][20][21][22][23][24][25].…”

Section: Introductionmentioning

confidence: 99%

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Development and Characterization of Buccal Bilayer Tablets containing Microparticles with Ibuprofen

Conceição

Estanqueiro²,

Amaral³

et al. 2014

AJMSM

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The aim of this study was to develop and characterize buccal bilayer tablets containing ibuprofen microparticles, prepared through emulsion/chilling method, to obtain a sustained release. In this way, three formulations of bilayer tablets containing three bioadhesive polymers, namely Noveon ® AA-1 Polycarbophil USP, Carbopol ® 974 and Carbopol ® 980 were prepared. Weight uniformity, friability, hardness and in vitro drug release studies, by two different methods, were evaluated in the manufactured tablets. The calculation of similarity factor (f 2 ) was also carried out. In addition, three gels (0.5%, w/w) with the same polymers were prepared and textural analysis (firmness and adhesiveness) were assessed in comparison with the bioadhesive layer of tablets. Buccal bilayer tablets with suitable physical properties (weight uniformity, hardness and friability) were produced. In vitro dissolution tests, performed during 8 hours, have demonstrated a sustained release of ibuprofen (maximum drug released: 30.0 -45.1%). According to f 2 , both dissolution methods and the three studied polymers showed similar dissolution profiles (f 2 > 50). Tablets containing Carbopol ® 974 showed higher values of firmness and adhesiveness after 6 h of hydration in phosphate buffer pH 7.4. On the other hand, it was not possible to verify a relationship between the textural parameters of the gels and the bioadhesive layer of tablets containing the same polymers.

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“…This technique allows for reducing particle size to a nearly molecular level (Krishnamoorthy, Suchandrasen, Prasad, 2012). Several advantages of SD include the uniform and homogeneous distribution of small quantities of drug in the solid state, the stabilization of unstable drugs, the dispersion of liquid or gaseous compounds and the production of prolonged release systems (Almeida, Amaral, Lobão, 2012). The present study aims to develop solid lipid dispersions with dithranol and evaluates drug stability, through color evaluation.…”

Section: Introductionmentioning

confidence: 99%

Use of solid dispersions to increase stability of dithranol in topical formulations

Estanqueiro

Conceição

Amaral

et al. 2014

Braz. J. Pharm. Sci.

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The present study was planned to improve the stability of dithranol using solid dispersions (SD). Two different SD at a 1:9 ratio of dithranol/excipient were prepared: one of them using glyceryl behenate as excipient and the other using a mixture of argan oil with stearic acid (1:8 ratio) as excipient. Pure dithranol and SD of dithranol were incorporated in an oil-in-water cream and in a hydrophobic ointment in a drug/ dermatological base ratio of 1:10. The physical and mechanical properties of semisolid formulations incorporating the pure drug and the developed SD were evaluated through rheological and textural analysis. To evaluate the stability, L*a*b* color space parameters of SD and semisolid formulations, and pH of hydrophilic formulations were determined at defined times, during one month. Each sample was stored at different conditions namely, light exposure (room temperature), high temperature exposition (37 °C) (protected from light) and protected from light (room temperature). Despite higher values of firmness and adhesiveness, hydrophobic ointment exhibited the best rheological features compared to the oil-in-water cream, namely a shear-thinning behavior and high thixotropy. These formulations have also presented more stability, with minor changes in L*a*b* color space parameters. The results of this study indicate that is possible to conclude that the developed SD contributed to the increased stability of dithranol.Uniterms: Dithranol/stability. Topical formulations/development. Solid dispersions/preparation. Stearic acid. Glyceryl behenate. Argan oil.Este trabalho teve como objetivo aumentar a estabalidade do ditranol através da preparação de dispersões sólidas (DS). Prepararam-se duas DS diferentes em proporção de 1:9 de ditranol/excipiente: em uma das DS utilizou-se beenato de glicerila como excipiente e na outra se utilizou mistura de óleo de argan com ácido esteárico (razão 1:8). Posteriormente, efetuou-se a incorporação de ditranol puro e das DS contendo este fármaco num creme hidrófilo ou óleo-água (O/A) e em pomada hidrófoba, na proporção 1:10 (fármaco ou respetivas DS/base dermatológica). As propriedades físicas e mecânicas das formulações semissólidas incorporando fármaco ou as respetivas DS previamente desenvolvidas, foram avaliadas através da análise do comportamento reológico e das propriedades de textura. Para avaliar a estabilidade, os parâmetros do espaço de cor L*a*b* das DS e das formulações semissólidas e o pH das preparações hidrófilas foram determinados em períodos de tempo definidos, durante um mês para cada amostra armazenada sob diferentes condições, especificamente, exposição à luz (à temperatura ambiente), protegidas da luz à temperatura elevada (37 °C) e protegidas da luz (temperatura ambiente). Embora tenham apresentado valores de firmeza e de adesividade mais elevados, as pomadas hidrófobas apresentaram melhores características reológicas do que os cremes óleo-água. Além disso, as pomadas hidrófobas também apresentaram melhor estabilidade, com pequenas alterações nos parâ...

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Comparative study of sustained-release lipid microparticles and solid dispersions containing ibuprofen

Cited by 12 publications

References 10 publications

Formulation And Evaluation Of Acyclovir Sodium Solid Lipid Microparticles

Formulation And Evaluation Of Acyclovir Sodium Solid Lipid Microparticles

Development and Characterization of Buccal Bilayer Tablets containing Microparticles with Ibuprofen

Use of solid dispersions to increase stability of dithranol in topical formulations

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