Formulation Development of Self-Micro Emulsifying Drug Delivery System (SMEDDS) for Oral Bioavailability enhancement of a low soluble Anti-Diabetic Drug: Gliclazide (original) (raw)
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Self Micro Emulsifying Drug Delivery System (Smedds): An Approach to Enhance an Oral Bioavailability
2017
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. The oral bioavailability of poorly water soluble drugs may be enhanced when co administered with meal rich in fat has led to increasing recent interest in the formulation of poorly water soluble drugs in lipids. One of the most new way for such a mentioned problem is the Self microemulsifying drug delivery system (SMEDDS). Self micro emulsifying drug delivery systems are isotropic mixtures of oil, surfactant, co-surfactant and drug with a unique ability to form fine oil in water microemulsion upon mild agitation following dilution with aqueous phase. The hypothesis behind dissolution rate enhancement with SMEDDS is the spontaneous formation of the emulsion in the gastrointestinal tract which presents the drug in solubilized form and the small size of the formed droplet provides a large interfacial surface area fo...
Review of formulation and evaluation of self-micro emulsifying drug delivery system (SMEDDS)
ScienceRise: Pharmaceutical Science
Approximately half of the new drug applicants that reach formulation have poor water solubility. Oral delivery has been the main route of drug administration for the chronic treatment of numerous diseases. In different cases, in oral conveyance, 50 % of the medication compound is hampered because of the high lipid soluble or fat soluble of the medication itself. Around 40 % of new drug applicants show low solubility in water, which prompts poor oral bioavailability, high Intra and Intersubject changeability, and deficiency of dose proportionality Aim of review. The main aim of this review article is to gather the information related to design and evaluation of SMEDDS. These information can be utilized to enhance the bioavailability of the poorly aqueous soluble drug for various types of orally administered drugs. In this review article, various literature are reviewed and summerised in single paper to serve as reference guide to various research scholars and researchers working on self-micro-emulsifying drug delivery systems. Materials and Methods. To prepare this manuscript various keywords were searched in different search engine such as Google, Yahoo and Bing etc. This review article reviews the recent work done in the field of SMEDDS. It comprises review of literatures available in public domain and formulation of SMEDDS and its characterization is summarized in this article. Result. The various strategies to developed poor aqueous soluble drug for improvement of bioavailability for example, salt development and molecular size reduction of the compound might be one technique to enhance the dissolution rate of the drug. In any case, these methods have their limitations. SMEDDS is one of the novel applications for the delivery of low water soluble and low bioavailability of drug. SMEDDS is a method to improve the aqueous solubility of the medication; SMEDDS are described as isotropic blenders of oils, surfactants, and co-surfactant. Upon slightly stir followed by dilution with distilled water, for example, gastrointestinal liquids, these techniques can define clear o/w micro emulsion. SMEDDS is first choice and key technology for developing the lipophilic drug and other different factors that chance to affect the oral bioavailability. Conclusions. This review paper attempts to describe the preparation of SMEDDS and furthermore discusses the development of pseudo ternary phase diagram for SMEDDS. It describes the mechanism and method of preparation involved in SMEDDS. The capability of oral absorption of drug compound from the SMEDDS relies upon numerous formulation−related parameters, for example, surfactant concentration, oil/surfactant ratio, and hydrophobicity of emulsion, globule size and charge, in vitro, in vivo all of which basically characterized the ability of self-emulsification. SMEDDS are administered as unit dosage form and it also protect the degradation of drug.
2016
Poorly water soluble drug candidates are becoming more prevalent and it has been estimated that 40-50% of drug molecules are poorly soluble in aqueous media or have a low permeability which does not allow for their adequate absorption from gastrointestinal tract following by oral administration. Formulation scientists have to adopt different strategies to enhance their absorption. Lipidic formulations are seen to be a promising approach to combat the challenges and especially self-microemulsifying drug delivery(SMEDDS) system approach are used to increase the absorption of poorly absorbed drug which ultimately increased there bioavailability. The attempts of various scientist to convert the liquid SMEDDS to solid-SMEDDS by adsorption, spray drying, lyophilisation, melt granulation and extrusion techniques. Formulation of SMEDDS is a potential strategy to deliver poorly soluble drug and low absorption drug with enhanced dissolution rate and bioavailability.
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.
Self Micro-emulsifying Drug Delivery System: Approach to Improve Solubility and Permeability
INTERNATIONAL JOURNAL OF INSTITUTIONAL PHARMACY AND LIFE SCIENCES, 2015
Self Micro-emulsifying drug delivery systems (SMEDDS) are usually used to improve the bioavailability of hydrophobic drugs. Approximately 60-70% of new chemical entities exhibit poor aqueous solubility and present a major challenge to modern drug delivery system, because of their low bioavailability. SMEDDS is isotropic (one phase system) mixture of oil or modified oils, surfactants and co-surfactants, which form the fine oil-in-water microemulsion when introduced into aqueous phase under condition of gentle agitation. The digestive motility of the stomach and intestine provide the agitation necessary for self-microemulsion in-vivo. Triglyceride is the one of the component of SMEDDS, which helps in the absorption of drugs from the GI tract. SMEDDS enhance the bioavailability enabling reduction in dose of the drug. SMEDDS is evaluated by various methods like visual assessment, droplet polarity and droplet size, size of emulsion droplet, dissolution test, charge of oil droplets, viscosity determination, in-vitro diffusion study. This article gives an overview of improvement in the rate and extent of oral absorption of drugs by SMEDDS approach. The characterization of SMEDDS and application of SMEDDS is also introduced, with particular emphasis being placed on the developments of Solid self micro-emulsifying delivery system and dosage form of SMEDDS.
2016
SELF-MICRO EMULSIFYING DRUG DELIVERY SYSTEM (SMEDDS): A PROMISING DRUG DELIVERY SYSTEM FOR ENHANCEMENT OF BIOAVAILABILITY Shraddha D. Pawar*, Nayan A.Gujarathi, Bhushan R.Rane, Sunil P. Pawar P.S.G.V.P. Mandal’s, Department of Pharmaceutics, College of Pharmacy, Shahada-425409, Maharashtra, India. *For Correspondence: P.S.G.V.P. Mandal’s, Department of Pharmaceutics, College of Pharmacy, Shahada-425409, Maharashtra, India ABSTRACT In modern drug discovery techniques, there has been a consistent increase in the number of new pharmacologically active lipophilic compounds that are poorly water-soluble. Approximately 40% of new drug candidates are lipophilic and exhibit poor water solubility. Various techniques are used to improve the bioavailability of such drugs, like salt formation, pH change, β-cyclodextrin complex, Micro emulsions etc. Self-micro emulsifying drug delivery system (SMEDDS) is the one of the method for improvement of oral bioavailability. Self-micro emulsifying drug d...
Self micro-emulsifying drug delivery system (SMEDDS) : Review
2015
Oral route has always been preferred route for formulators and has dominated over other routes of administrations. However this preferred route is limited to those drugs molecule that are permeable across the gastric mucosa and are at least sparingly soluble. 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. Realization that the oral bioavailability of poor water soluble drugs may be enhanced when co-administered with meal rich in fat has led to increasing recent interest in the formulation of poorly water soluble drugs in lipids. Also Lipid-based drug delivery systems have gained considerable interest after the commercial success of Sandimmune NeoralTM (Cyclosporine A), Novartis Pvt. Ltd. and Fortovase (Saquinavir), Roche Laboratories Inc. with much attention focused on self micro-emulsifying drug delivery systems (SMEDDS). SMEDDS are isotropic mixtures of oi...
Journal of Drug Delivery and Therapeutics
Nearly 40% of new drug candidates exhibit low solubility in water, which is a challenge in development of optimum oral solid dosage form in terms of formulation design and bioavailability of new pharmaceutical products. Many strategies have been used to overcome these problems either by means of modifying the solubility or maintaining the drug in dissolved form throughout gastric transit time. Much attention has focused on lipid solutions, emulsions and emulsion pre-concentrates, which can be prepared as physically stable formulations suitable for encapsulation of such poorly soluble drugs. Recently, self-micro emulsifying drug delivery systems (SMEDDS) especially have attracted increasing interest primarily because these are physically stable, easy to manufacture, can be filled in soft gelatin capsules and then will generate a drug containing micro-emulsion with a large surface area upon dispersion in the gastrointestinal tract. The emulsions will further facilitate the absorption of the drug due via intestinal lymphatic pathway and by partitioning of drug into the aqueous phase of intestinal fluids. In the present review, an overview of SMEDDS as a key technology for formulating lipophilic drugs and various factors that potentially affect the oral bioavailability of such drugs are presented.
International Journal of Applied Pharmaceutics, 2019
Currently a marked interest in developing lipid-based formulations to deliver lipophilic compounds. Self-emulsifying system has emerged as a dynamic strategy for delivering poorly water-soluble compounds. These systems can embrace a wide variety of oils, surfactants, and co-solvents. An immediate fine emulsion is obtained on exposure to water/gastro-intestinal fluids. The principal interest is to develop a robust formula for biopharmaceutical challenging drug molecules. Starting with a brief classification system, this review signifies diverse mechanisms concerning lipidbased excipients besides their role in influencing bioavailability, furthermore pertaining to their structured formulation aspects. Consecutive steps are vital in developing lipid-based systems for biopharmaceutical challenging actives. Such a crucial structured development is critical for achieving an optimum formula. Hence lipid excipients are initially scrutinized for their solubility and phase behavior, along with biological effects. Blends are screened by means of simple dilution test and are consequently studied with more advanced biopharmaceutical tests. After discerning of the principle formula, diverse technologies are offered to incorporate the fill-mass either in soft/hard gelatin capsules. There is also feasibility to formulated lipid-system as a solid dosage form. Although such solid technologies are desirable but such should not undermine the biopharmaceutical potential of lipid-formulations.
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 ...