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Journal ArticleDOI: 10.1080/17425247.2021.1856073

Orally administered self-emulsifying drug delivery system in disease management: advancement and patents.

04 Mar 2021-Expert Opinion on Drug Delivery (Taylor & Francis)-Vol. 18, Iss: 3, pp 315-332
Abstract: Introduction: Oral administration of a drug is the most common, ideal and preferred route of administration. The main problem of oral drug formulations is their low bioavailability arises from poor aqueous solubility of drug. Aqueous solubility of lipophilic drugs can be improved by various techniques like salt formation, complexation, addition of co-solvent etc. but self-emulsifying drug-delivery system (SEDDS) is getting more attention for increasing the solubility of such drugs. The SEDDS is an isotropic mixture of drug, lipids, and emulsifiers, usually with one or more hydrophilic co-solvents/co-emulsifiers. This system is having ability to generate oil-in-water (o/w) emulsions or microemulsions upon gentle agitation followed by dilution with aqueous phase. The SEDDSs are relatively newer, lipid-based technological innovations possessing unparalleled potential in improving oral bioavailability of poorly water-soluble drugs.Areas covered: This review provides updated information regarding the types of SEDDS, their preparation techniques, drug delivery and related recent patents along with marketed formulations.Expert opinion: The SEDDS has been explored for improving bioavailability, rising intra-subject heterogeneity, and increasing solubility. SEDDS offers the benefit of a protective effect against the hostile environment in the gut. The unique fabrication techniques provide specific strategy to overcome the low bioavailability and poor solubility problems.

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Topics: Bioavailability (52%), Drug delivery (51%)
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Open accessJournal ArticleDOI: 10.1016/J.APSB.2021.04.017
Haoshi Gao1, Haoyue Jia2, Jie Dong1, Xinggang Yang2  +2 moreInstitutions (2)
Abstract: The drug formulation design of self-emulsifying drug delivery systems (SEDDS) often requires numerous experiments, which are time- and money-consuming. This research aimed to rationally design the SEDDS formulation by the integrated computational and experimental approaches. 4495 SEDDS formulation datasets were collected to predict the pseudo-ternary phase diagram by the machine learning methods. Random forest (RF) showed the best prediction performance with 91.3% for accuracy, 92.0% for sensitivity and 90.7% for specificity in 5-fold cross-validation. The pseudo-ternary phase diagrams of meloxicam SEDDS were experimentally developed to validate the RF prediction model and achieved an excellent prediction accuracy (89.51%). The central composite design (CCD) was used to screen the best ratio of oil-surfactant-cosurfactant. Finally, molecular dynamic (MD) simulation was used to investigate the molecular interaction between excipients and drugs, which revealed the diffusion behavior in water and the role of cosurfactants. In conclusion, this research combined machine learning, central composite design, molecular modeling and experimental approaches for rational SEDDS formulation design. The integrated computer methodology can decrease traditional drug formulation design works and bring new ideas for future drug formulation design.

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4 Citations


Patent
16 Sep 2008-
Abstract: FIELD: medicine. SUBSTANCE: claimed invention relates to granulated from liquid pharmaceutical compositions, which contain rhein or diacerein, or their salts, and pharmaceutically acceptable carrier. Compositions contain from 20 to 45 mg of rhein or diacerein. Invention also relates to methods of producing claimed compositions. Compositions by invention are bioequivalent to preparative form of diacerein in dosage 50 mg, sold under the trade name Art 50®. Compositions do not demonstrate variability in after meal condition and on an empty stomach. EFFECT: considerable reduction of side effects, such as pulpy stool, in comparison with Art 50®. 13 cl, 37 tbl, 17 ex

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Topics: Diacerein (59%)

4 Citations


Open accessDissertation
01 Aug 2002-
Topics: Drug delivery (53%)

3 Citations


Patent
15 Jul 2004-
Abstract: Self-emulsifying and self-microemulsifying formulations for the oral administration of taxoids. The present invention relates to novel formulations of taxoids for oral administration.

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Topics: Oral administration (51%)

2 Citations


Patent
26 Aug 2005-
Abstract: The present invention relates to novel drug delivery and release systems of butylphthalide, namely self-emulsifying drug delivery systems (SEDDS), their preparation, and their use in pharmaceutical formulations. The drug delivery system comprises 1 to 65% butylphthalide and 10 to 65% emulsifier as essential ingredients with various additives required according to the desired dosage form. The present invention improves the absorbency of drugs by significantly increasing the contact area between the mucous membranes of the gastrointestinal tract and butylphthalide. Drug delivery, butylphthalide, emulsification

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Topics: Butylphthalide (59%), Drug delivery (58%), Dosage form (53%)

2 Citations


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104 results found


Journal ArticleDOI: 10.1016/J.FOODHYD.2010.09.017
Cheng Qian1, David Julian McClements1Institutions (1)
01 Jul 2011-Food Hydrocolloids
Abstract: Nanoemulsions are finding increasing utilization in the food and beverage industries for certain applications because of their unique physicochemical and functional properties: high encapsulation efficiency; low turbidity; high bioavailability; high physical stability. In this study, we examined the impact of system composition and homogenization conditions on the formation of nanoemulsions using a high-pressure homogenizer (microfluidizer). The mean particle diameter decreased with increasing homogenization pressure and number of passes, with a linear log–log relationship between mean particle diameter and homogenization pressure. The minimum droplet diameter that could be produced after 6 passes at 14 kbar depended strongly on emulsifier type and concentration: SDS

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Topics: Homogenizer (56%), Homogenization (chemistry) (51%)

651 Citations


Journal ArticleDOI: 10.1016/S0169-409X(96)00490-5
Colin W. Pouton1Institutions (1)
Abstract: Self-emulsifying drug delivery systems (SEDDS) are mixtures of oils and surfactants, ideally isotropic, sometimes including cosolvents, which emulsify under conditions of gentle agitation, similar to those which would be encountered in the gastro-intestinal tract. Hydrophobic drugs can often be dissolved in SEDDS allowing them to be encapsulated as unit dosage forms for peroral administration. When such a formulation is released into the lumen of the gut it disperses to form a fine emulsion, so that the drug remains in solution in the gut, avoiding the dissolution step which frequently limits the rate of absorption of hydrophobic drugs from the crystalline state. Generally this can lead to improved bioavailability, and/or a more consistent temporal profile of absorption from the gut. Ultra-low oil-water interfacial tension and/or substantial interfacial disruption are required to achieve self-emulsification. SEDDS are usually formulated with triglyceride oils and ethoxylated nonionic surfactants, usually at surfactant concentrations greater than 25%. In practice, disruption of the oil-water interface is caused by penetration of water into the formulation or diffusion of cosolvents away from the formulation. Both of these phenomena can be studied using equilibrium phase diagrams, which in combination with particle size measurements allow the optimisation of performance of SEDDS. The precise mechanisms of emulsification remain the subject of speculation but there is an empirical link between self-emulsification, liquid crystal formation, oil-water phase-inversion temperature and enhanced solubilization of water by oily formulations, and these phenomena are indicators of the efficiency of emulsification. This article describes strategies used for formulation of SEDDS, methods used for assessment of efficiency of emulsification and practical considerations regarding the use of SEDDS for enhancement of the bioavailability of drugs from the gastro-intestinal tract.

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Topics: Dosage form (50%)

563 Citations


Open accessJournal ArticleDOI: 10.1016/J.ULTSONCH.2009.02.008
Abstract: The efficient production of nanoemulsions, with oil droplet sizes of less than 100 nm would facilitate the inclusion of oil soluble bio-active agents into a range of water based foods. Small droplet sizes lead to transparent emulsions so that product appearance is not altered by the addition of an oil phase. In this paper, we demonstrate that it is possible to create remarkably small transparent O/W nanoemulsions with average diameters as low as 40 nm from sunflower oil. This is achieved using ultrasound or high shear homogenization and a surfactant/co-surfactant/oil system that is well optimised. The minimum droplet size of 40 nm, was only obtained when both droplet deformability (surfactant design) and the applied shear (equipment geometry) were optimal. The time required to achieve the minimum droplet size was also clearly affected by the equipment configuration. Results at atmospheric pressure fitted an expected exponential relationship with the total energy density. However, we found that this relationship changes when an overpressure of up to 400 kPa is applied to the sonication vessel, leading to more efficient emulsion production. Oil stability is unaffected by the sonication process.

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Topics: Oil droplet (54%), Sonication (50%)

480 Citations


Journal ArticleDOI: 10.1080/10942910600596464
Abstract: The efficiency of sonication and microfluidization to produce nano-emulsions were evaluated in this study. The purpose was to produce an oil-in-water nano-emulsion of d-limonene to apply it in the next step for nano-particle encapsulation. In the entrapment and retention of volatiles or for the microencapsulation efficiency, emulsion size is one of the critical factors. In this study, a bench-top sonicator and an air-driven microfluidizer were used to prepare the emulsions. Results show that, while both methods were capable of producing nano-emulsions of the size range of 150-700 nm, the microfluidizer produced emulsions with narrower size distributions and sonication was more convenient in terms of operation and cleaning. In general, the size of the emulsions decreased with increasing sonication time, or the microfluidization pressure and duration. However, for both sonication and microfluidization, optimal conditions were necessary for emulsification beyond which the emulsion sizes would either increase or have little change with further processing.

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Topics: Sonication (54%), Emulsion (51%)

413 Citations


Journal ArticleDOI: 10.1016/J.DRUDIS.2008.04.006
Bo Tang1, Gang Cheng1, Jian-Chun Gu1, Cai-Hong Xu1Institutions (1)
Abstract: Approximately 40% of new chemical entities exhibit poor aqueous solubility and present a major challenge to modern drug delivery system, because of their low bioavailability. Self-emulsifying drug delivery systems (SEDDS) are usually used to improve the bioavailability of hydrophobic drugs. Conventional SEDDS, however, are mostly prepared in a liquid form, which can produce some disadvantages. Accordingly, solid SEDDS (S-SEDDS), prepared by solidification of liquid/semisolid self-emulsifying (SE) ingredients into powders, have gained popularity. This article gives an overview of the recent advances in the study of S-SEDDS, especially the related solidification techniques and the development of solid SE dosage forms. Finally, the existing problems and the possible future research directions in this field are pointed out.

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Topics: Drug delivery (50%)

321 Citations