Solid dispersions containing ursolic acid in Poloxamer 407 and PEG 6000: A comparative study of fusion and solvent methods

Eloy, Josimar O.; Marchetti, Juliana Maldonado

doi:10.1016/j.powtec.2013.11.017

Cited by 104 publications

(85 citation statements)

References 43 publications

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“…Solid dispersion was prepared following a solvent evaporation method previously described by our group (Eloy et al, 2012a;Eloy, Marchetti, 2014). Briefly, the drug, poloxamer 407 and sodium caprate (0.2:1:1), w/w/w) were solubilized in methanol (10% w/v), followed by evaporation of the solvent at room temperature with magnetic stirring.…”

Section: Physical Mixture and Solid Dispersion Preparationmentioning

confidence: 99%

“…Dissolution studies were performed using an SR8 Plus Hanson Corporation instrument (Chatsworth, CA, USA) by incubating a known amount of sample (equivalent to 7.5 mg drug) in 900 mL of pH 6.8 phosphate buffer (37 °C ± 0.2 °C) with mechanical stirring at 75 rpm with a paddle (Eloy et al, 2012a;Eloy, Marchetti, 2014). At designated time intervals, 1-mL aliquots were withdrawn and filtered (0.45 um), and then the drug was analyzed by HPLC, following the method already described.…”

Section: In Vitro Drug Dissolutionmentioning

confidence: 99%

“…To overcome this disadvantage, some alternatives have been proposed, including complexation with cyclodextrines (Li, 2009) and encapsulation in liposomes (Both et al, 2002); however none of these approaches have been evaluated for the enhancement of the trypanocidal activity. In previous studies, our group incorporated ursolic acid in solid dispersion formulations, which are mixtures of lipophilic drugs and hydrophilic carriers, resulting in improvement of drug solubility and dissolution profile as a consequence of decreased particle size, improved wettability and presence of drug in the more soluble molecular or amorphous state (Eloy et al, 2012a;Eloy, Marchetti, 2014;Vasconcelos, Sarmento, Costa, 2007). In those studies, we employed the lipid mixture Gelucire 50/13 and the polymer poloxamer 407 as carriers and investigated the physicochemical aspects of the solid dispersion formation and we established the best method for the formulation preparation.…”

Section: Introductionmentioning

confidence: 99%

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Preparation, characterization and evaluation of the in vivo trypanocidal activity of ursolic acid-loaded solid dispersion with poloxamer 407 and sodium caprate

Eloy

Saraiva

Albuquerque

et al. 2015

Braz. J. Pharm. Sci.

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Ursolic acid is a promising candidate for treatment of Chagas disease; however it has low aqueous solubility and intestinal absorption, which are both limiting factors for bioavailability. Among the strategies to enhance the solubility and dissolution of lipophilic drugs, solid dispersions are growing in popularity. In this study, we employed a mixture of the surfactants poloxamer 407 with sodium caprate to produce a solid dispersion containing ursolic acid aimed at enhancing both drug dissolution and in vivo trypanocidal activity. Compared to the physical mixture, the solid dispersion presented higher bulk density and smaller particle size. Fourier Transform Infrared Spectroscopy results showed hydrogen bonding intermolecular interactions between drug and poloxamer 407. X-ray diffractometry experiments revealed the conversion of the drug from its crystalline form to a more soluble amorphous structure. Consequently, the solubility of ursolic acid in the solid dispersion was increased and the drug dissolved in a fast and complete manner. Taken together with the oral absorption-enhancing property of sodium caprate, these results explained the increase of the in vivo trypanocidal activity of ursolic acid in solid dispersion, which also proved to be safe by cytotoxicity evaluation using the LLC-MK2 cell line. O ácido ursólico é um candidato promissor para o tratamento da doença de Chagas, contudo este fármaco possui baixa solubilidade aquosa e limitada absorção intestinal, ambos os fatores limitantes da biodisponibilidade. Entre as estratégias para potencializar a solubilidade e a dissolução de fármacos lipofílicos, as dispersões sólidas estão crescendo em popularidade. Neste estudo, empregamos mistura dos tensoativos, poloxamer 407 e caprato de sódio, para produzir dispersão sólida contendo ácido ursólico, com o objetivo de aumentar tanto a dissolução do fármaco quanto a atividade tripanocida in vivo. Comparada à mistura física, a dispersão sólida apresentou maior densidade e menor tamanho de partícula. Os resultados da análise de espectroscopia no infravermelho com transformada de Fourier mostraram interações intermoleculares do tipo ligações de hidrogênio entre o fármaco e o poloxamer 407. Os experimentos de difratometria de raio-X revelaram a conversão do fármaco de sua forma cristalina para a forma amorfa, mais solúvel. Consequentemente, a solubilidade do ácido ursólico em dispersão sólida foi aumentada e o fármaco dissolveu-se de maneira mais rápida e completa. Em conjunto com as propriedades promotoras de absorção oral do caprato de sódio, estes resultados explicaram o aumento da atividade tripanocida in vivo do ácido ursólico em dispersão sólida, que também se provou segura após avaliação de citotoxicidade empregando a linhagem celular LLC-MK2.Unitermos: Ácido ursólico/atividade tripanocida. Doença de Chagas/tratamento. Tensoativos. Dispersões sólidas/dissolução. Poloxamer 407. Caproato de sódio.

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Section: Physical Mixture and Solid Dispersion Preparationmentioning

confidence: 99%

Section: In Vitro Drug Dissolutionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Preparation, characterization and evaluation of the in vivo trypanocidal activity of ursolic acid-loaded solid dispersion with poloxamer 407 and sodium caprate

Eloy

Saraiva

Albuquerque

et al. 2015

Braz. J. Pharm. Sci.

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“…[21,22] This method involves cosolubilization of copolymer with the porphyrin, which is then followed by rotative evaporation as follows:…”

Section: Incorporation Of Porphyrins Into Pluronic F127mentioning

confidence: 99%

“…The incorporation of all porphyrins into micelles was carried out using the solid dispersion method which has been described in literature [21,22] as stated above. The porphyrins become water soluble after incorporation into Pluronic dissolved in organic solvents and when they are embedded in micelles since different solvents are used.…”

Section: Characterization Of Porphyrins When Embedded In Pluronic F127mentioning

confidence: 99%

Porphyrins Encapsulated into Pluronic F127 Micelles: Evaluating the Effect of the Central Metal and Substituents on the Photophysicochemical Properties in Water

Managa¹,

Nyokong²

2017

MHC

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Ursolic acid: Pharmacokinetics process in vitro and in vivo, a mini review

Wen

2019

Archiv der Pharmazie

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Ursolic acid (UA) is a natural triterpene compound found in various fruits and vegetables. UA has a widespread pharmacologic effect, including antitumor, anti‐inflammatory, anti‐oxidant, anti‐apoptotic, anti‐allergy, and anti‐carcinogenic effects. UA can be used as an alternative medicine for the treatment and prevention of many diseases. However, the bioavailability of UA by oral administration is low since it is absorbed by the intestine through passive diffusion. Therefore, some novel technologies are used to produce UA preparations that can change the pharmacokinetics process and increase its solubility and bioavailability. At present, pharmacokinetic studies on UA are few. In this paper, we will review the pharmacokinetics features of free UA and some novel UA preparations in vitro and in vivo, in order to provide a reference for rational utilization and drug design of UA.

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Solid dispersions containing ursolic acid in Poloxamer 407 and PEG 6000: A comparative study of fusion and solvent methods

Cited by 104 publications

References 43 publications

Preparation, characterization and evaluation of the in vivo trypanocidal activity of ursolic acid-loaded solid dispersion with poloxamer 407 and sodium caprate

Preparation, characterization and evaluation of the in vivo trypanocidal activity of ursolic acid-loaded solid dispersion with poloxamer 407 and sodium caprate

Porphyrins Encapsulated into Pluronic F127 Micelles: Evaluating the Effect of the Central Metal and Substituents on the Photophysicochemical Properties in Water

Ursolic acid: Pharmacokinetics process in vitro and in vivo, a mini review

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