Journal Article•
A review on self emulsifying drug delivery system: promising approach to enhance bioavailability
TL;DR: An overview of self emulsifying drug delivery system and how SEDDS can improves the solubility and bioavailability of the poorly soluble drug are given.
Abstract: Among the approaches to improve the oral bioavailability of the molecules, the use of self-emulsifying drug delivery system has been shown to be reasonably successful in improving the oral bioavailability of poorly water soluble and lipophilic drugs. SEDDS is a novel and versatile approach for overcoming the formulation difficulties with poor aqueous solubility and low bioavailability. SEDDS are the isotropic mixture of oils and surfactants even sometimes containing cosolvents, which emulsify to produce fine oil-in-water emulsions upon gentle agitation. These systems rapidly disperse in g.i.t yielding micro or nano emulsions containing the solubilised drug with droplet size 100-300 nm. For lipophilic drugs which have dissolution rate limited absorption, SEDDS may be promising strategy to improve rate and extent of oral absorption. This review article gives an overview of self emulsifying drug delivery system and also explains how SEDDS can improves the solubility and bioavailability of the poorly soluble drug. Key words: Lipid based drug delivery system, self emulsifying drug delivery system, SEDDS, bioavailability.
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TL;DR: In vitro release study revealed that the designed solid dosage form based on the semisolid SMEDDS loaded with the therapeutic dose of 200mg, may control partitioning of the solubilized drug from in situ formed oil-in-water microemulsion carrier into the sorrounding aqueous media, and hence decrease the risk for precipitation of the drug.
18 citations
Cites background from "A review on self emulsifying drug d..."
...Generally, semisolid pharmaceutical formulations may afford higher stability of the suspended drugs, better handling in comparison with the liquids, and controled drug release (Dokania and Joshi, 2015; Pouton and Porter, 2008; Singh and Ranga, 2014)....
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TL;DR: Two piece hard gelatin liquid filling capsules are one of the most logical approaches when choosing the best dosage form to deliver these new liquid formulations for Candesartan cilexitil.
Abstract: Most of the currently available drugs are having poor water solubility and suffer from low oral bioavailability. One of the most promising approaches to deliver such insoluble drugs is by dissolving it in lipids, liquids or semi-solids to formulate new products.[1] Candesartan meets the requirement of high potency but it is poorly absorbed when administered as tablets. Therefore the prodrug Candesartan cilexitil is developed.[2] Two piece hard gelatin liquid filling capsules are one of the most logical approaches when choosing the best dosage form to deliver these new liquid formulations.[1] Liquid filled formulations were prepared by employing different cosolvents and surfactants. The formulation containing SLS-2%, PVP- 17.5%, PEG-15%, and PG-53% exhibited desire solubility, rheological property and found to be stable in hard gelatin capsules.
5 citations
TL;DR: In this article, a self-micro-emulsifying drug delivery system for modafinil was formulated and a D-optimal mixture experimental design was applied to optimize the formulation variables; oil phase X1 (Clove oil), surfactant X2 (Tween-80) and co-surfactant X3 (Polyethylene glycol-400).
5 citations
References
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01 Oct 1975
TL;DR: In this paper, the possibility that two-phase fluid systems will emulsify spontaneously, due to entropy effects, is investigated theoretically, and it is discovered that for interfacial tensions below about 2 dynes/cm, such spontaneous dispersions can occur, although with large tensions the dispersed particles are not macroscopic.
Abstract: The possibility that two-phase fluid systems will emulsify spontaneously, due to entropy effects, is investigated theoretically. It is discovered that for interfacial tensions below about 2 dynes/cm, such spontaneous dispersions can occur, although with large tensions the dispersed particles are not macroscopic. However, for interfacial tensions below 5 × 10 −4 dynes/cm, macroscopic particles are formed. Spontaneous dispersion due to entropy effects is to be distinguished from the formation of micellar solutions that form because of energetic considerations.
197 citations
TL;DR: Effect of concentrations of cosurfactant and gelling agent on emulsification process and in vitro drug diffusion was studied and showed that liquid crystal phase viscosity increased significantly with increasing amount of silicon dioxide, which in turn caused an increase in average droplet size of resultant emulsion and slower drug diffusion.
Abstract: The purpose of this study was to formulate a gelled self-emulsifying drug delivery system (SEDDS) containing ketoprofen as an intermediate in the development of sustained release solid dosage form. Captex 200 (an oil), Tween 80 (a surfactant), and Capmul MCM (a cosurfactant) were used to formulate SEDDS. Silicon dioxide was used as a gelling agent, which may aid in solidification and retardation of drug release. Effect of concentrations of cosurfactant and gelling agent on emulsification process and in vitro drug diffusion was studied using 32 factorial design. Multiple regression analysis data and response surfaces obtained showed that liquid crystal phase viscosity increased significantly with increasing amount of silicon dioxide, which in turn caused an increase in average droplet size of resultant emulsion and slower drug diffusion. Drug release from the formulation increased with increasing amount of cosurfactant.
118 citations
Journal Article•
TL;DR: Selfemulsifying drug delivery system has gained more attention due to enhanced oral bio-availability enabling reduction in dose, more consistent temporal profiles of drug absorption, selective targeting of drug(s) toward specific absorption window in GIT, and protection of drugs from the hostile environment in gut.
Abstract: Oral route still remains the favorite route of drug administration in many diseases and till today it is the first way investigated in the development of new dosage forms. The major problem in oral drug formulations is low and erratic bioavailability, which mainly results from poor aqueous solubility. This may lead to high inter- and intra subject variability, lack of dose proportionality and therapeutic failure. It is estimated that 40% of active substances are poorly soluble in water. The improvement of bio-availability of drugs with such properties presents one of the greatest challenges in drug formulations. Various technological strategies are reported in the literature including micronization, solid dispersions or cyclodextrines complex formation and different technologies of drug delivery systems. Among various approach selfemulsifying drug delivery system has gained more attention due to enhanced oral bio-availability enabling reduction in dose, more consistent temporal profiles of drug absorption, selective targeting of drug(s) toward specific absorption window in GIT, and protection of drug(s) from the hostile environment in gut.
107 citations
DOI•
20 Sep 2016
TL;DR: Self nano-emulsifying drug delivery system (SNEDDS), by mixture of oil, surfactant, and co-surfactant were prepared under gentle agitation and obtain by pseudo-ternary phase diagram and evaluate on the basis of Zeta size & potential, Conductivity measurement, Turbidity measurement and Trans mission electron microscopy analysis.
Abstract: Aim: Oral route has always been the favorite route of drug administration in many diseases and till today it is the first way investigated in the development of new dosage forms. The major problem in oral drug formulations is low and erratic bioavailability, which mainly results from poor aqueous solubility, thereby pose problems in their formulation. For the therapeutic delivery of lipophilic active moieties (BCS class II drugs), lipid based formulations are inviting increasing attention. Methods: To that aim, from the web sites of PubMed, HCAplus, Thomson, and Registry were used as the main sources to perform the search for the most significant research articles published on the subject. The information was then carefully analyzed, highlighting the most important results in the formulation and development of self-micro emulsifying drug delivery systems as well as its therapeutic activity. Results: Self-emulsifying drug delivery system (SMEDDS) has gained more attention due to enhanced oral bio-availability enabling reduction in dose, more consistent temporal profiles of drug absorption, selective targeting of drug(s) toward specific absorption window in GIT, and protection of drug(s) from the unreceptive environment in gut. Conclusions: This article gives a complete overview of SMEDDS as a promising approach to effectively deal with the problem of poorly soluble molecules.
52 citations
01 Jan 2011
TL;DR: ‘Lipid’ formulations range from pure oils, at one extreme, to blends which contain a substantial proportion of hydrophilic surfactants or co‐ solvents, which limits the bioavailability of the drug from solid dosage forms.
Abstract: Lipid formulations for oral administration of drugs generally consist of a drug dissolved in a blend of two or more excipients, which may be triglyceride oils, Partial glycerides, Surfactants or co‐surfactants. The primary mechanism of action, which leads to improved bioavailability, is usually avoidance, or partial avoidance, of the slow dissolution process, which limits the bioavailability of hydrophobic drugs from solid dosage forms. Ideally the formulation allows the drug to remain in a dissolved state throughout its transit through the gastrointestinal tract. The availability of the drug for absorption can be enhanced by presentation of the drug as a solubilizer within a colloidal dispersion. This objective can be achieved by formulation of the drug in a self‐emulsifying system or alternatively by taking advantage of the natural process of triglyceride digestion. In practice ‘Lipid’ formulations range from pure oils, at one extreme, to blends which contain a substantial proportion of hydrophilic surfactants or co‐ solvents.
50 citations