Using in situ Raman spectroscopy to study the drug precipitation inhibition and supersaturation mechanism of Vitamin E TPGS from self-emulsifying drug delivery systems (SEDDS)

Raut, Shilpa; Karzuon, Basel; Atef, Eman

doi:10.1016/j.jpba.2015.02.027

Cited by 16 publications

(7 citation statements)

References 27 publications

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“…The Raman spectrum of indomethacin exhibits characteristic peaks at 632, 1089, 1397, 1580, 1621, and 1699 cm −1 , which are attributed to the γ ‐crystalline form of indomethacin . In the range of 1400–1800 cm −1 , the indomethacin band at 1580 cm −1 has been assigned to the deformation vibration of the indole ring, while the bands at 1621 and 1699 cm −1 can be attributed to aromatic CC stretching vibrations and to amide CO stretching, respectively. On the other hand, amylose and pea starch exhibit very similar spectra with characteristic Raman peaks at 479, 866, 941, and 1460 cm −1 , attributed to CCO and CCC deformations, CCH and COC deformations, α‐1,4 glycosidic linkage and CH, CH 2 , and COH stretching vibrations, respectively …”

Section: Resultsmentioning

confidence: 99%

Study of Molecular Inclusion Complex Formation of Amylose With Indomethacin

Marinopoulou¹,

Christofilos

Arvanitidis

et al. 2019

Starch Stärke

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Amylose or pea starch‐indomethacin systems are prepared using two different methods: The alkaline method, where the samples are prepared by mixing alkaline aqueous solutions of glucan and indomethacin at pH 12, and the sonication method, where the samples are prepared at pH 7 by mixing a glucan aqueous solution with indomethacin dispersed in water in the presence of cholate salts using sonication. The aim is to assess whether V‐amylose complexes can be formed with the drug indomethacin as the guest molecule. Experimental techniques, such as Raman Spectroscopy, X‐ray Diffraction, Differential Scanning Calorimetry, Optical Microscopy, and Confocal Laser Scanning Microscopy, verify the presence of the drug molecules in the examined systems. The results indicate that the sonication method is more effective for the complex preparation. However, even in this case, a very limited complexation is achieved. The bioavailability of the systems is evaluated using in vitro methods, simulating gastric, and intestinal conditions. It is shown that the systems matrix provided only limited protection to indomethacin molecules up to their release in the small intestine. Thus, it is concluded that indomethacin molecules are rather physically entrapped within the amylose or starch matrix than in the interior of the amylose helices.

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Section: Resultsmentioning

confidence: 99%

Study of Molecular Inclusion Complex Formation of Amylose With Indomethacin

Marinopoulou¹,

Christofilos

Arvanitidis

et al. 2019

Starch Stärke

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“…Vitamin E and its derivatives can also function as additives, rather than the active ingredient, in lipid nanocarriers, because vitamin E is a strong antioxidant that can stabilize oxygen-sensitive drugs or bioactive agents in lipid nanosystems [61,99]. TPGS is a non-ionic surfactant that can prevent drug precipitation and promote supersauration in lipid nanosystems [100]; it can also interact with drugs by hydrogen bonding, thereby accelerating drug dissolution [101]. Previous research reported that TPGS could inhibit presystemic drug metabolism and intestinal efflux mediated by P-pg, and increase oral drug bioavailability [62,102].…”

Section: Enhancement Of Oral Bioavailability Of Vitamins Using Lipmentioning

confidence: 99%

Use of Lipid Nanocarriers to Improve Oral Delivery of Vitamins

et al. 2019

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The chemical environment and enzymes in the gastrointestinal (GI) membrane limit the oral absorption of some vitamins. The GI epithelium also contributes to the poor permeability of numerous antioxidant agents. Thus, lipophilic vitamins do not readily dissolve in the GI tract, and therefore they have low bioavailability. Nanomedicine has the potential to improve the delivery efficiency of oral vitamins. In particular, the use of lipid nanocarriers for certain vitamins that are administered orally can provide improved solubility, chemical stability, epithelium permeability and bioavailability, half-life, nidus targeting, and fewer adverse effects. These lipid nanocarriers include self-emulsifying drug delivery systems (SEDDSs), nanoemulsions, microemulsions, solid lipid nanoparticles (SLNs), and nanostructured lipid carriers (NLCs). The use of nontoxic excipients and sophisticated material engineering of lipid nanosystems allows for control of the physicochemical properties of the nanoparticles and improved GI permeation via mucosal or lymphatic transport. In this review, we highlight recent progress in the development of lipid nanocarriers for vitamin delivery. In addition, the same lipid nanocarriers used for vitamins may also be effective as carriers of vitamin derivatives, and therefore enhance their oral bioavailability. One example is the incorporation of d-α-tocopheryl polyethylene glycol succinate (TPGS) as the emulsifier in lipid nanocarriers to increase the solubility and inhibit P-glycoprotein (P-gp) efflux. We also survey the concepts and discuss the mechanisms of nanomedical techniques that are used to develop vitamin-loaded nanocarriers.

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“…En aras de comprender el mecanismo de inhibición de precipitación de algunos excipientes, Raut et al [133] plantearon una metodología usando la espectroscopía Raman para estudiar las interacciones en diferentes SEDDS, que pueden ser responsables de dicho fenómeno. Durante esta investigación, se formularon diferentes SEDDS de indometacina y probucol variando las proporciones de sus excipientes para seleccionar las óptimas para el estudio según sus tamaños de gotas y las pruebas de solubilidad.…”

Section: Sistemas Autoemulsificables Supersaturadosunclassified

“…La dispersión y la digestión de los SEDDS en el tracto gastrointestinal son pasos críticos puesto que estos cambian el entorno al cual se expone el principio activo. Por lo tanto, la capacidad de la formulación para mantener el principio activo disuelto puede verse reducida ostensiblemente lo que incrementa en gran manera el riesgo de precipitación afectando el desempeño de la formulación [74,133].…”

Section: Solubilidadunclassified

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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Using in situ Raman spectroscopy to study the drug precipitation inhibition and supersaturation mechanism of Vitamin E TPGS from self-emulsifying drug delivery systems (SEDDS)

Cited by 16 publications

References 27 publications

Study of Molecular Inclusion Complex Formation of Amylose With Indomethacin

Study of Molecular Inclusion Complex Formation of Amylose With Indomethacin

Use of Lipid Nanocarriers to Improve Oral Delivery of Vitamins

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

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