Solid Self Emulsifying Drug DeliverySystem: A Novel Approach (original) (raw)
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More than 60% of drugs have lipophilic nature and exhibit poor water-solubility. The dissolution is the rate limiting step in their absorption and oral bioavailability. To overcome this problem one approach to enhance dissolution is Self-Dispersing Lipid Formulations (SDLFs). Generally, an emulsified dosage form is rapidly absorbable; therefore, it makes sure that a poorly water-soluble drug is rapidly transported into the circulation. SDLFs consist of a mixture of oil and surfactant, in which active drug moiety is incorporated. They get emulsified under conditions of gentle agitation, similar to those which would be encountered in the gastrointestinal tract on mixing with biological fluids. In this review article introduction, advantages and uses of SDLFs to enhance the dissolution and oral bioavailability are overviewed.
Self Emulsifying Drug Delivery System: A Tool in Solubility Enhancement of Poorly Soluble Drugs
2012
Low aqueous solubility and thereby low oral bioavailability is a major concern for formulation scientist as many recent drugs are lipophillic in nature and their lower solubility and dissolution is a major drawback for their successful formulation into oral dosage forms. Aqueous solubility of drugs can be increased by different methods such as salt formation, solid dispersion, complex formation but Self Emulsifying Drug Delivery System (SEDDS) is gaining more attention for improving the solubility of lipophillic drugs. SEDDS are ideally isotropic mixtures of drug, oil, surfactant and/or co surfactant. They spontaneously form emulsion on mixing with water with little or no energy input. Generally SEDDS are prepared using triglycerides and non ionic surfactants. The present review provides an updated account of the advancements in SEDDS with regard to the selection of lipid systems for current formulations, dosage forms for SEDDS, solidification techniques, characterization and their ...
A Review on Solid Self Emulsifying Drug Delivery System
Journal of Biomedical and Pharmaceutical Research, 2013
Self-emulsifying drug delivery system (SEDDS) is one of the most popular and commercially viable formulation approaches for enhancing solubility of poorly water soluble drugs. SEDDS are isotropic mixtures of oil, surfactant and co-surfactant which are generally present in liquid or semisolid form. Solid SEDDS are solid forms of liquid SEDDS converted into solid by suitable means. These solid SEDDS are considered more stable over liquid SEDDS, also solid forms improve handling, packaging and storage. The aim of this review is to discuss various methods of preparation of solid SEDDS and different existing drug delivery systems which incorporated solid SEDDS to obtain advantage of both the systems.
Self-Emulsifying Drug Delivery Systems (SEDDS) in Pharmaceutical Development
Lipid-based formulations, such as Self-Emulsifying Drug Delivery Systems (SEDDS), are an important tool for lipophilic drugs and offer the potential for enhancing drug absorption and oral bioavailability. SEDDS are a promising approach for the formulation of drug compounds with poor aqueous solubility. These systems are easily manufactured and physically stable mixtures of oil, surfactants, co-surfactants and solubilized drug substances that are administered orally in soft or hard gelatin capsules. In the gastrointestinal tract environment, these systems spontaneously emulsify. This review focuses on SEDDS formulations, describes their different types and presents case studies in which enhanced bioavailability were demonstrated in vivo using this formulation system.
Future Journal of Pharmaceutical Sciences
Background High lipophilicity and poor aqueous solubility are the endemic problems of new drug molecules. Sixty to seventy percent of these drugs are unable to solubilize completely in aqueous media, or have very low permeability. This hampers their oral absorption and further leads to their poor bioavailability. Various researches are in progress to overcome these limitations. Novel technologies like nano-carrier systems have become popular for improving the solubility of drugs. Main body Lipid-based formulations, among nano systems, are taking pace for the enhancement of solubility, oral absorption, and hence the bioavailability of drugs. Among the lipid formulations, self-emulsification systems are gaining popularity by offering various advantages to delivery systems. Self-emulsifying drug delivery systems (SEDDS) are isotropic blends of oil and surfactant/co-surfactants. These ingredients upon gentle agitation in aqueous media results in the formation of o/w emulsion. In spite o...
Critical Reviews in Therapeutic Drug Carrier Systems, 2009
The oral delivery of hydrophobic drugs presents a major challenge because of the low aqueous solubility of such compounds. Selfemulsifying drug delivery systems (SEDDS), which are isotropic mixtures of oils, surfactants, solvents and co-solvents/surfactants, can be used for the design of formulations in order to improve the oral absorption of highly lipophilic drug compounds. SEDDS can be orally administered in soft or hard gelatin capsules and form fine relatively stable oil−in−water (o/w) emulsions upon aqueous dilution owing to the gentle agitation of the gastrointestinal fluids. The efficiency of oral absorption of the drug compound from the SEDDS depends on many formulation−related parameters, such as surfactant concentration, oil/surfactant ratio, polarity of the emulsion, droplet size and charge, all of which in essence determine the self-emulsification ability. Thus, only very specific pharmaceutical excipient combinations will lead to efficient self-emulsifying systems. Although many studies have been carried out, there are few drug products on the pharmaceutical market formulated as SEDDS confirming the difficulty of formulating hydrophobic drug compounds into such formulations. At present, there are four drug products, Sandimmune ® and Sandimmun Neoral ® (cyclosporin A), Norvir ® (ritonavir), and Fortovase ® (saquinavir) on the pharmaceutical market, the active compounds of which have been formulated into specific SEDDS. Significant improvement in the oral bioavailability of these drug compounds has been demonstrated for each case. The fact that almost 40% of the new drug compounds are hydrophobic in nature implies that studies with SEDDS will continue, and more drug compounds formulated as SEDDS will reach the pharmaceutical market in the future.
Self-Emulsifying Drug Delivery System: A Novel Approach
Oral route is the easiest and most convenient route for drug administration. Oral drug delivery systems being the most cost-effective and leads the worldwide drug delivery market. 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 water soluble (water insoluble in nature). For 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 solid dispersions, cyclodextrines complex formation, or micronization, and different technologies of drug delivery systems. Including these approaches self-emulsifying drug delivery system (SEDDS) has gained more attention for enhancement of oral bio-availability with reduction in dose. SEDDS are isotropic mixtures of oil, surfactants, solvents and co-solvents/surfactants. The principal characteristic of these systems is their ability to form fine oil-in-water (o/w) emulsions or micro-emulsions upon mild agitation following dilution by an aqueous phase. For lipophilic drugs, which have dissolution rate-limited absorption, SEDDS may be a promising strategy to improve the rate and extent of oral absorption. This review article explains how self-emulsifying drug delivery systems can increase the solubility and bioavailability of poorly soluble drug.
Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs
Biomedicine & Pharmacotherapy, 2004
The oral delivery of hydrophobic drugs presents a major challenge because of the low aqueous solubility of such compounds. Selfemulsifying drug delivery systems (SEDDS), which are isotropic mixtures of oils, surfactants, solvents and co-solvents/surfactants, can be used for the design of formulations in order to improve the oral absorption of highly lipophilic drug compounds. SEDDS can be orally administered in soft or hard gelatin capsules and form fine relatively stable oil−in−water (o/w) emulsions upon aqueous dilution owing to the gentle agitation of the gastrointestinal fluids. The efficiency of oral absorption of the drug compound from the SEDDS depends on many formulation−related parameters, such as surfactant concentration, oil/surfactant ratio, polarity of the emulsion, droplet size and charge, all of which in essence determine the self-emulsification ability. Thus, only very specific pharmaceutical excipient combinations will lead to efficient self-emulsifying systems. Although many studies have been carried out, there are few drug products on the pharmaceutical market formulated as SEDDS confirming the difficulty of formulating hydrophobic drug compounds into such formulations. At present, there are four drug products, Sandimmune ® and Sandimmun Neoral ® (cyclosporin A), Norvir ® (ritonavir), and Fortovase ® (saquinavir) on the pharmaceutical market, the active compounds of which have been formulated into specific SEDDS. Significant improvement in the oral bioavailability of these drug compounds has been demonstrated for each case. The fact that almost 40% of the new drug compounds are hydrophobic in nature implies that studies with SEDDS will continue, and more drug compounds formulated as SEDDS will reach the pharmaceutical market in the future.
Self-Emulsifying Oral Lipid Drug Delivery Systems: Advances and Challenges
AAPS PharmSciTech, 2019
The attempts to oral delivery of lipids can be challenging. Self-emulsifying drug delivery system (SEDDS) plays a vital role to tackle this problem. SEDDS is composed of an oil phase, surfactants, co-surfactants, emulsifying agents, and co-solvents. SEDDS can be categorized into self-nano-emulsifying agents (SNEDDS) and self-micro-emulsifying agents (SMEDDS). The characterization of SEDDS includes size, zeta potential analysis, and surface morphology via electron microscopy and phase separation methods. SEDDS can be well characterized through different techniques for size and morphology. Supersaturation is the phenomenon applied in case of SEDDS, in which polymers and copolymers are used for SEDDS preparation. A supersaturated SEDDS formulation kinetically and thermodynamically inhibits the precipitation of drug molecules by retarding nucleation and crystal growth in the aqueous medium. Self-emulsification approach has been successful in the delivery of anti-cancer agents, anti-viral drugs, anti-bacterial, immunosuppressant, and natural products such as antioxidants as well as alkaloids. At present, more than four SEDDS drug products are available in the market. SEDDS have tremendous capabilities which are yet to be explored which would be beneficial in oral lipid delivery.
Journal of Pharmaceutical Research
As the development of modern drug discovery techniques, there has been increase in the number of pharmaceutical compounds that are poorly water soluble. These lipophilic compounds possess low dissolution rate and therefore low bioavailability. The Formulation scientists should adopt various strategies to enhance their absorption. This paper is an insight for improving the solubility of poorly water soluble compounds. Lipidic formulations are found to be a promising approach to combat the solubility challenges. Self MicroEmulsifying Drug Delivery Systems (SMEDDS) are gaining more attention for improving the solubility of the lipophilic drugs. SMEDDS are isotropic mixtures of oil, surfactant and co surfactant and are vital tool in solving low bioavailability problems of poorly soluble drugs. Lipophilic drugs can be dissolved in these systems, enabling them to be administered per orally. When this is released into the lumen it results in w/o microemulsion with the aid of G.I fluid. This present review describes various formulation components, mechanism of emulsification, biopharm aspects, characterization methods and application of SMEDDS.