Eficiência terapêutica das formulações lipídicas de anfotericina B

Filippin, Fabíola Branco; Souza, Liliete Canes

doi:10.1590/s1516-93322006000200003

Cited by 25 publications

(30 citation statements)

References 168 publications

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“…It is important to consider that the solution containing a compound with low solubility and high molar absorptivity may be diluted, as solution containing a compound with high solubility and low molar absorptivity may not be necessarily diluted. Thus, the dilution mainly depends on molar absorptivity of the drugs (Alves et al, 2010;Filippin, Souza, 2006;Pereira et al, 2011;Ruela, Araújo, Pereira, 2009). The cumulative quantity of dissolved drug was corrected for each sample interval according to volume collected from the each vessel.…”

Section: Intrinsic Dissolution Methodsmentioning

confidence: 99%

Equilibrium solubility versus intrinsic dissolution: characterization of lamivudine, stavudine and zidovudine for BCS classification

Dezani

Pereira

Caffaro

et al. 2013

Braz. J. Pharm. Sci.

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Solubility and dissolution rate of drugs are of major importance in pre-formulation studies of pharmaceutical dosage forms. The solubility improvement allows the drugs to be potential biowaiver candidates and may be a good way to develop more dose-efficient formulations. Solubility behaviour of lamivudine, stavudine and zidovudine in individual solvents (under pH range of 1.2 to 7.5) was studied by equilibrium solubility and intrinsic dissolution methods. In solubility study by equilibrium method (shake-flask technique), known amounts of drug were added in each media until to reach saturation and the mixture was subjected to agitation of 150 rpm for 72 hours at 37 °C. In intrinsic dissolution test, known amount of each drug was compressed in the matrix of Wood's apparatus and subjected to dissolution in each media with agitation of 50 rpm at 37 °C. In solubility by equilibrium method, lamivudine and zidovudine can be considered as highly soluble drugs. Although stavudine present high solubility in pH 4.5, 6.8, 7.5 and water, the solubility determination in pH 1.2 was not possible due stability problems. Regarding to intrinsic dissolution, lamivudine and stavudine present high speed of dissolution. Considering a boundary value presented by Yu and colleagues (2004), all drugs studied present high solubility characteristics in intrinsic dissolution method. Based on the obtained results, intrinsic dissolution seems to be superior for solubility studies as an alternative method for biopharmaceutical classification purposes.Uniterms: Drugs/solubility. Drugs/dissolution rate. Intrinsic dissolution/method/biopharmaceutical classification. Biopharmaceutical Classification System.A solubilidade e a taxa de dissolução de fármacos são de grande importância em estudos de pré-formulação de formas farmacêuticas. A melhora na solubilidade permite que os fármacos sejam candidatos potenciais à bioisenção, podendo ser uma boa maneira para desenvolver formulações dose-eficientes. O comportamento de solubilidade da lamivudina, estavudina e zidovudina em solventes individuais (sob faixa de pH 1,2 a 7,5) foi estudado pelos métodos de solubilidade em equilíbrio e dissolução intrínseca. No estudo de solubilidade pelo método do equilíbrio (método de agitação de frascos), conhecidas quantidades do fármaco foram adicionadas em cada meio até atingirem a saturação e a mistura foi submetida à agitação de 150 rpm por 72 horas a 37 °C. No ensaio de dissolução intrínseca, conhecida quantidade de cada fármaco foi comprimida na matriz do aparato de Wood e submetida à dissolução em cada meio com agitação de 50 rpm a 37 °C. No método de solubilidade em equilíbrio, a lamivudina e a zidovudina podem ser consideradas como fármacos altamente solúveis. Embora a estavudina apresente alta solubilidade nos meios pH 4,5, 6,8, 7,5 e água, a determinação da solubilidade em pH 1,2 não foi possível devido a problemas de estabilidade. Com relação à dissolução intrínseca, a lamivudina e a estavudina apresentaram alta velocidade de dissolução. Considerando o valor ...

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Section: Intrinsic Dissolution Methodsmentioning

confidence: 99%

Equilibrium solubility versus intrinsic dissolution: characterization of lamivudine, stavudine and zidovudine for BCS classification

Dezani

Pereira

Caffaro

et al. 2013

Braz. J. Pharm. Sci.

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“…The pharmacological effect may have both fungicide and fungistatic characteristics, depending on not only the blood and/or tissue concentration achieved, but also the sensitivity or resistance of the microorganism (Vartivarian et al, 1993). However, a major limitation in the use of AmB includes low drug solubility in most aqueous solvents and solubility in dimethylsulfoxide, dimethylformamide, and propylene glycol (Filippin and Souza, 2006). Moreover, because it is insoluble in water, it is presented in association with deoxycholate detergent in phosphate buffer (Filippin and Souza, 2006); this system is not homogeneous, and may have three different (polymorphic) forms: monomeric, oligomeric and aggregates of AmB mixed with deoxycholate pure micelles.…”

Section: Literature Reviewmentioning

confidence: 99%

“…However, a major limitation in the use of AmB includes low drug solubility in most aqueous solvents and solubility in dimethylsulfoxide, dimethylformamide, and propylene glycol (Filippin and Souza, 2006). Moreover, because it is insoluble in water, it is presented in association with deoxycholate detergent in phosphate buffer (Filippin and Souza, 2006); this system is not homogeneous, and may have three different (polymorphic) forms: monomeric, oligomeric and aggregates of AmB mixed with deoxycholate pure micelles. A quantitative balance is observed between the forms: the aggregate form is related to the highest toxicity (Lamy-Freund et al, 1991;Legrand et al, 1992).…”

Section: Literature Reviewmentioning

confidence: 99%

“…Among them are the development of new formulations such as liposome base encapsulation (AmBisome), the formation of lipid complexes (ABELCET®), colloidal dispersions (Amphocil®) and nanoparticles. These new formulations have demonstrated decreased toxicity and increased therapeutic efficacy; however, their high cost has limited their use (Filippin and Souza, 2006;Iman et al, 2011;Kleinberg, 2006;Hillery, 1997;.…”

Section: Challenges Of Antifungal Therapy With Amphotericin Bmentioning

confidence: 99%

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Difficulties in antifungal therapy with amphotericin B and the continuous search for new formulations: A literature review

Voncik¹,

Fermino²,

Cardoso³

et al. 2016

Afr. J. Pharm. Pharmacol.

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Despite advances in the research on new antifungal agents, Amphotericin B (AmB) is still considered as the antifungal of choice for treating most systemic mycoses due to its potency and broad-spectrum action. However, this drug has limited use because of its toxic effects on kidneys, liver and blood. The search for new and safe formulations of AmB is essential because of the emergence of antifungal resistance to other drugs and the increased number of immunosuppressed patients. Nanoparticles are a promising alternative towards achieving lower toxicity and improved pharmacokinetic properties. This study is a literature review of the use of AmB and the toxicity of formulations. Some of the current new formulations show some advantageous characteristics as compared to AmB. However, there is still need for a continued search for an effectively improved formulation.

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“…Therefore numerous attempts have been made in recent years to reduce amB toxicity. Among these new developments, formulations such as a liposomal encapsulation base, lipid complexes, colloidal dispersions and nanoparticles have been shown to cause less toxicity and increase therapeutic efficacy, but the high cost of these formulations have limited their use (Filippin and Souza, 2006;Fukui et al, 2003;Jung et al, 2009). Thus, reducing the amB dose by combining it with new antifungal products appears to be an important approach, as shown by Rosato et al (2008), who demonstrated that essential oils increased the in vitro antifungal activity of amB against Candida spp (Rosato et al, 2008).…”

Section: Introductionmentioning

confidence: 99%

Black and white teas as potential agents to combine with amphotericin B and protect red blood cells from amphotericin B-mediated toxicity

2018

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Amphotericin B is a fungicidal substance that is treatment of choice for most systemic fungal infections affecting immunocompromised patients. However, severe side effects have limited the utility of this drug. The aim of this study was to evaluate the antifungal effect of the combination of amphotericin B with black tea or white tea and protective of citotoxic effect. The present study shows that white and black teas have additive effects with amphotericin B against some species Candida. In addition, the combination of white and black tea with amphotericin B may reduce the toxicity of amphotericin B to red blood cells. Our results suggest that white and black tea is a potential agent to combine with amphotericin for antifungal efficacy and to reduce the amphotericin dose to lessen side effects.Keywords: amphotericin B, antifungal., black tea, Camellia sinensis, white tea, toxicity.Chá preto e branco de Camellia sinensis como potenciais agentes para associar com anfotericina B ResumoA anfotericina B é o tratamento de escolha para a maioria das infecções fúngicas sistémicas que afetam os doentes imunocomprometidos. No entanto, efeitos secundários graves têm limitado a utilidade desta droga. O objetivo deste estudo foi avaliar o efeito antifúngico da combinação de anfotericina B com chá preto ou chá branco, bem como o efeito citotóxico desta combinação sobre hemáceas. O presente estudo demonstra que o chá branco e preto de Camellia sinensis têm efeitos aditivos com anfotericina B contra algumas espécies de Candida sp. Além disso, a combinação de chá branco e preto com anfotericina B pode reduzir a toxicidade da anfotericina B em hemáceas. Nossos resultados sugerem que o chá branco e preto são agentes potenciais para associação com anfotericina B contribuindo para eficácia antifúngica, bem como redução de toxicidade.Palavras-chave: anfotericina B, antifúngico, chá preto, Camellia sinensis, chá branco, toxicidade.

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Eficiência terapêutica das formulações lipídicas de anfotericina B

Cited by 25 publications

References 168 publications

Equilibrium solubility versus intrinsic dissolution: characterization of lamivudine, stavudine and zidovudine for BCS classification

Equilibrium solubility versus intrinsic dissolution: characterization of lamivudine, stavudine and zidovudine for BCS classification

Difficulties in antifungal therapy with amphotericin B and the continuous search for new formulations: A literature review

Black and white teas as potential agents to combine with amphotericin B and protect red blood cells from amphotericin B-mediated toxicity

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