Measuring the emulsification dynamics and stability of self-emulsifying drug delivery systems

Vasconcelos, Teófilo; Marques, Sara; Sarmento, Bruno

doi:10.1016/j.ejpb.2017.11.003

Cited by 37 publications

(15 citation statements)

References 31 publications

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“…SEDS consists of oil, surfactant, co‐surfactant, and drug . This type of system is typically self‐dispersing and consequently forms fine oil‐in‐water (O/W) emulsions or microemulsions (nanoemulsions) spontaneously . It is generally believed that the transformation from liquid SEDS to solid formulation provides better stability, lower production cost, precise dosing, easy handling and storage, and therefore, the rise of patient compliance could significantly attribute to the increase of commercialization.…”

Section: Introductionmentioning

confidence: 99%

Development of a Solid Self‐Emulsification Delivery System for the Oral Delivery of Astaxanthin

Mao

Sun

Tian

et al. 2019

Euro J Lipid Sci & Tech

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In the present study, a solid self‐emulsification delivery system (S‐SEDS) is developed to improve the bioavailability of astaxanthin (ASX). The pseudo ternary phase diagram method is used to screen the optimum composition of liquid self‐emulsification delivery system (SEDS). This liquid system is converted into solid state using the solid absorbent carrier by simple physical mixing. Through the analysis of powder flowability and adsorption capacity, silicon dioxide and anhydrous calcium hydrogen phosphate are selected as solid carriers of the liquid self‐emulsification system. Results of Fourier transform infrared spectroscopy (FTIR) and X‐ray diffraction (XRD) indicate that astaxanthin is encapsulated in these solid carriers. In the in vitro dissolution study, sustained release of astaxanthin from two different ASX‐SEDS (prepared with silicon dioxide and anhydrous calcium hydrogen phosphate) is obtained and the cumulative release is correspondingly 51.06 ± 0.98 and 49.97 ± 0.87% within 2 h. A delayed pattern of absorbed ASX‐SEDS is observed in the study with anhydrous calcium hydrogen phosphate compared to the counterpart with silicon dioxide, which is consistent with the result from the in vitro digestion study. Antioxidant study shows that astaxanthin can be encapsulated in S‐SEDS without the loss of antioxidant activity. Consequently, S‐SEDS can be a promising vehicle in food industry. Practical Applications: Traditionally, liquid‐based delivery systems are prepared using liquid components, which have some disadvantages, such as, complex production process, low active ingredient loading, narrow application range, and lacking of effective evaluation methods. The present study adopts physical adsorption, a gentle and simple process, to prepare the solid self‐emulsifying system. This system combines the advantages of liquid‐based systems and solid dosage forms, which can improve the solubility of poorly solubility active ingredient in intestinal environments, and the high solubility of active ingredient is favor to its absorption. In the present work, the active ingredients solubilization capability of solid formulations is evaluated by in vitro dissolution and digestion studies. It can be seen that over 40% of astaxanthin are released from solid self‐emulsifying systems in 120 min. After the process of digestion, the bioaccessibility reaches 10%. The results of in vitro dissolution and digestion show that after solid adsorption, astaxanthin exhibits delayed release patterns. All the studies demonstrate that solid self‐emulsifying system is an appropriate strategy to improve the bioavailability of astaxanthin. The pseudo ternary phase diagram method is used to screen the optimum composition of liquid self‐emulsification delivery system. Then, this liquid system is converted into solid state using the solid absorbent carrier by simple physical mixing.

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Section: Introductionmentioning

confidence: 99%

Development of a Solid Self‐Emulsification Delivery System for the Oral Delivery of Astaxanthin

Mao

Sun

Tian

et al. 2019

Euro J Lipid Sci & Tech

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“…Además, este grupo se puede subclasificar en tipo IIIA y IIIB según la proporción de los lípidos, tensioactivos y cosolventes, teniendo las formulaciones tipo IIIA mayor contenido de lípidos que las formulaciones tipo IIIB. Las formulaciones tipo IV son libres de lípidos y constan principalmente de mezcla de tensioactivos y cosolventes, siendo estas las de mayor carácter hidrofílico [19,32,39,40].…”

Section: Formulaciones Basadas En Lípidosunclassified

“…Los sistemas autoemulsificables se pueden definir como mezclas isotrópicas de aceites naturales o sintéticos, tensioactivos, en algunas ocasiones, cosolventes y un principio activo, que son capaces de formar emulsiones finas de aceite en agua cuando se introducen en medio acuoso bajo agitación suave [46][47][48]. La motilidad del tracto gastrointestinal proporciona la agitación necesaria para la autoemulsificación, por lo cual estos sistemas emulsionan espontáneamente al exponerse a los fluidos gastrointestinales [40,49].…”

Section: Definición De Seddsunclassified

“…De igual manera, también se observó el interés por aprovechar los beneficios de SEDDS en sustancias de las otras clases del SCB. Existen compuestos que presentan características como sensibilidad a la oxidación, termolabilidad, fotosensibilidad, susceptibilidad al metabolismo de primer paso y mecanismos de eflujo que han motivado el estudio sobre su incorporación a SEDDS debido a su baja o variable biodisponibilidad [40]. Por lo tanto, diversas investigaciones han sido desarrolladas para mejorar la biodisponibilidad de algunos fármacos y productos naturales tales como apomorfina [10,87], fenobarbital [88], vitamina D [21], resveratrol [40,89,90], coenzima Q10 [91,92] y silimarina [93], entre otros.…”

Section: Principio Activounclassified

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Sistemas de entrega de fármacos autoemulsificables: una plataforma de desarrollo alternativa para la industria farmacéutica colombiana

Cueto

Ortega

Sotomayor

2019

Rev. Colomb. Cienc. Quím. Farm.

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Los grandes avances tecnológicos en la industria farmacéutica, que involucran el uso de la química combinatoria y el cribado de alto rendimiento, han conllevado al descubrimiento de muchas entidades químicas candidatas a fármacos que presentan baja solubilidad acuosa, debido a su elevada complejidad molecular, lo que hace difícil el desarrollo de productos con estas sustancias. Los sistemas de entrega de fármacos autoemulsificables (SEDDS) han generado un interés para el desarrollo farmacéutico porque son una alternativa efectiva para mejorar la biodisponibilidad de fármacos poco solubles en agua. Para describir el estado de conocimiento sobre estos sistemas se realizó una revisión sistemática en diferentes bases de datos sobre la literatura relacionada con los SEDDS a nivel nacional e internacional, logrando así describir los aspectos más relevantes sobre los SEDDS (tipos, composición, mecanismos para aumentar biodisponibilidad, caracterización, formulaciones). A pesar de las numerosas investigaciones realizadas durante los últimos años que muestran el potencial de los SEDDS para mejorar la biodisponibilidad de los fármacos poco solubles en agua, se pudo evidenciar que solo algunas sustancias activas han sido incluidas en estos sistemas y comercializadas exitosamente, esto debido a algunas limitaciones que indican la necesidad de un mayor entendimiento sobre estos sistemas.

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“…This means fewer doses of the drug is needed to be used. In fact, these systems minimize side effects and toxicity (18)(19)(20).…”

mentioning

confidence: 99%

Preparation and Characterization of Self-Microemusifying Drug Delivery System (Smedds) of Cisplatin for Oral Use in Ovarian Cancer Treatment

Akartas¹,

Karasulu²

2020

Acta Poloniae Pharmaceutica - Drug Research

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Cancer is one of the most leading causes of death in the world. Ovarian cancer is the seventh most common cancer in women. Also, it has the highest, mortality rate among female reproductive system cancers (1). According to the American Cancer Society in 2018, 22240 new cases of ovarian cancer will be diagnosed and 14070 women will die of ovarian cancer in the United States (2). The highest incidences are related in Europe, Canada and the United States. The lowest incidences are reported in China and Africa. According to GLOBOCAN 2008 database, the incidence rates are reported as over 11 cases per 100000 in Europe, less than 3 cases per 100000 in Africa and 4-8 cases per 100000 in South American, Asian and Caribbean countries (3). The latest cancer mortality statistics of the World Health Organization (WHO) showed that mortality will increase by approximately 45% until 2030 (4). Ovarian cancer has different risk factors like family history, age, early age menarche, menopause, parity, oral contraceptive use, lactation, obesity, cigarette smoking and alcohol consumption (5-7). Epithelial ovarian cancer is the most common type of ovarian cancer. Early diagnosis increases the chances successful treatment. The pathogenesis of ovarian cancer hasnít been elucidated yet, but ovulation, hormonal factors and inflammations have an important role in it (8, 9). There are two types of ovarian tumors. Type I tumors tend to be less aggressive and slow-growing like low grade malign serous tumors, low grade malign endometrioid carcinoma and mucinous carcinoma. Type II tumors are more aggressive than Type I tumors. They are high grade malign serous carcinoma, carcinosarcoma and undifferentiated carcinoma (10, 11). Ovarian cancer is staged by using the FIGO staging system which has 4 stages. A tumor is limited to the ovary at stage I. During stage II, tumor involves one or both of the ovaries. Pelvic extension and primary peritoneal tumor occurred. At stage III,

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Measuring the emulsification dynamics and stability of self-emulsifying drug delivery systems

Cited by 37 publications

References 31 publications

Development of a Solid Self‐Emulsification Delivery System for the Oral Delivery of Astaxanthin

Development of a Solid Self‐Emulsification Delivery System for the Oral Delivery of Astaxanthin

Sistemas de entrega de fármacos autoemulsificables: una plataforma de desarrollo alternativa para la industria farmacéutica colombiana

Preparation and Characterization of Self-Microemusifying Drug Delivery System (Smedds) of Cisplatin for Oral Use in Ovarian Cancer Treatment

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