Self-emulsifying drug delivery systems (SEDDS) with polyglycolyzed glycerides for improving in vitro dissolution and oral absorption of lipophilic drugs

Shah, Nita H.; Carvajal, Micaela; Patel, Chandresh; Infeld, M. H.; Malick, A. Waseem

doi:10.1016/0378-5173(94)90271-2

Cited by 420 publications

(209 citation statements)

References 2 publications

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“…The solubiltity of hydrophobic drugs and therefore their bioavailability, is improved in such systems by selective dissolution/partitioning in the oily component [5]. Particle sizes in such systems range in the order of 100 nm or less [7,18,19]. The preparations showed high stability on copious dilution.…”

Section: Discussionmentioning

confidence: 99%

“…The behavior of such systems can be modified by the use of oil and surfactants in different ratios, and by manipulating the polarity and charge of the dispersed globules. Benefits include enhanced solubility and dissolution behaviour [7,8] and a more reproducible plasma leveltime profile [9]. The influence of such systems on the bioavailability of hydrophobic drugs has been explained in terms of drug solubilization in micellar systems [10] and ease of lymphatic absorption [11].…”

Section: Introductionmentioning

confidence: 99%

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Self-Nanoemulsifying Drug Delivery Systems Based on Melon Oil and its Admixture with a Homolipid from Bos indicus for the Delivery of Indomethacin

Obitte¹,

Ofokansi²,

Nzekwe³

et al. 2011

Trop. J. Pharm Res

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Self-Nanoemulsifying Drug Delivery Systems Based on Melon Oil and its Admixture with a Homolipid from Bos indicus for the Delivery of Indomethacin

Obitte¹,

Ofokansi²,

Nzekwe³

et al. 2011

Trop. J. Pharm Res

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“…The higher bioavailability of hydrophobic drugs incorporated in a SMEDDS has been reported elsewhere [35][36][37] . The contribution of the GRDF approach extended the length of the absorption phase in comparison with the non-gastroretentive dosage form.…”

Section: In Vivo Pharmacokinetics Study In Beagle Dogsmentioning

confidence: 99%

Novel gastroretentive sustained-release tablet of tacrolimus based on self-microemulsifying mixture: in vitro evaluation and in vivo bioavailability test

2011

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Aim: To develop a novel gastroretentive drug delivery system based on a self-microemulsifying (SME) lipid mixture for improving the oral absorption of the immunosuppressant tacrolimus. Methods: Liquid SME mixture, composed of Cremophor RH40 and monocaprylin glycerate, was blended with polyethylene oxide, chitosan, polyvinylpyrrolidone and mannitol, and then transformed into tablets via granulation, with ethanol as the wetting agent. The tablets were characterized in respect of swelling, bioadhesive and SME properties. In vitro dissolution was conducted using an HCl buffer at pH 1.2. Oral bioavailability of the tablets was examined in fasted beagle dogs. Results: The tablet could expand to 13.5 mm in diameter and 15 mm in thickness during the initial 20 min of contact with the HCl buffer at pH 1.2. The bioadhesive strength was as high as 0.98±0.06 N/cm 2 . The SME gastroretentive sustained-release tablets preserved the SME capability of the liquid SME formations under transmission electron microscope. The drug-release curve was fit to the zero-order release model, which was helpful in reducing fluctuations in blood concentration. Compared with the commercially available capsules of tacrolimus, the relative bioavailability of the SME gastroretentive sustained-release tablets was 553.4%±353.8%. Conclusion: SME gastroretentive sustained-release tablets can enhance the oral bioavailability of tacrolimus with poor solubility and a narrow absorption window.

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“…Only specific pharmaceutical excipient combinations lead to efficient self-emulsifying systems (Charman et al, 1992;Shah et al, 1994;Hauss et al, 1998;Karim et al, 1994). The components of SEFs which need considering are discussed below.…”

Section: Formulation Considerations and Potential Componentsmentioning

confidence: 99%

Self-emulsifying therapeutic system: a potential approach for delivery of lipophilic drugs

Wadhwa¹,

Nair²,

Kumria³

2011

Braz. J. Pharm. Sci.

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Self-emulsifying therapeutic system (SETs) provide an effective and intelligent solution to the various issues related to the formulation of hydrophobic drugs with limited solubility in gastrointestinal fluid. Although the potential utility of SETs is well known, only in recent years has a mechanistic understanding of the impact of these systems on drug disposition emerged. These in situ emulsion-forming systems have a high stability when incorporated in various dosage forms. SETs are being looked upon as systems which can overcome the problems associated with delivery of poorly water soluble drugs. An in-depth knowledge about lipids and surfactants that can contribute to these systems, criterion for their selection and the proportion in which they can be used, represent some crucial factors determining the in vivo performance of these systems. This article presents a comprehensive account of various types of self-emulsifying formulations with emphasis on their composition and examples of currently marketed preparations.Uniterms: Lipid based formulations. Self-emulsifying therapeutic system. Self-emulsification.O sistema terapêutico auto-emulsionante (SETs) fornece solução eficaz e inteligente para os vários problemas relativos à formulação de fármacos hidrofóbicos com solubilidade limitada no fluido gastrintestinal. Embora a utilidade potencial dos SETs seja bem conhecida, só recentemente se compreendeu, mecanisticamente,o impacto desses sistemas na disposição de fármacos. Estes sistemas de formação de emulsão in situ têm alta estabilidade, quando incorporados em várias formas de dosagem. Os SETs têm sido considerados como sistemas que podem resolver problemas associados à liberação de fármacos pouco solúveis em água. O conhecimento profundo dos lipídios e tensoativos que podem ser utilizados para estes sistemas e o critério para a sua seleção e proporção na qual eles são utilizados são alguns dos fatores cruciais que determinam o desempenho do sistema in vivo. Este artigo apresenta o relato abrangente de vários tipos de formulações auto-emulsificantes, com ênfase em sua composição e exemplos das preparações que são correntemente comercializadas.Unitermos: Formulações baseadas em lipídio. Sistema terapêutico auto-emulsificante. Autoemulsificação.

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Self-emulsifying drug delivery systems (SEDDS) with polyglycolyzed glycerides for improving in vitro dissolution and oral absorption of lipophilic drugs

Cited by 420 publications

References 2 publications

Self-Nanoemulsifying Drug Delivery Systems Based on Melon Oil and its Admixture with a Homolipid from Bos indicus for the Delivery of Indomethacin

Self-Nanoemulsifying Drug Delivery Systems Based on Melon Oil and its Admixture with a Homolipid from Bos indicus for the Delivery of Indomethacin

Novel gastroretentive sustained-release tablet of tacrolimus based on self-microemulsifying mixture: in vitro evaluation and in vivo bioavailability test

Self-emulsifying therapeutic system: a potential approach for delivery of lipophilic drugs

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