DESIGN AND DEVELOPMENT OF SELF-MICROEMULSIFYING DRUG DELIVERY SYSTEMS (SMEDDS) OF TELMISARTAN FOR ENHANCEMENT OF IN VITRO DISSOLUTION AND ORAL BIOAVAILABILITY IN RABBIT (original) (raw)
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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.
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
The biopharmaceutical classification system (BCS) has become an increasingly important tool for world-wide regulation of drug products. Regarding improvement of bioavailability BCS class II, III, and IV; formulation approaches can be taken into considerations, though present researches are focussed mainly on BCS II (drugs with low solubility, high permeability), but talking about BCS III they too suffer poor oral bioavailability due to their low permeability through lipid membranes and are mostly subjected to parenteral route for administration. Here we have discussed about some formulation strategies to enhance oral bioavailability of BCS class III drugs which have shown promising abilities in enhancing permeability of drug through gastrointestinal tract.
International journal of Applied Pharmaceutics, 2024
Objective: Develop and optimize a novel self-micro emulsifying drug delivery system (SMEDDS) for enhancing the water solubility of Azilsartan (AZL) by employing the Box-Behnken design and the desirability function. Methods: The formulation of AZL-SMEDDS consists of clove oil (oil component), Tween 20 (surfactant), propylene glycol (co-surfactant) as the independent variables and the active drug. Using a 3-level Design, the impact of independent variables on the formulation was examined. These variables' specified ranges are 20-40 mg, 50-80 mg, and 5-30 mg for X1, X2 and X3 respectively. Particle size (Y1), PDI (Y2), and dissolution % (Y3) were the response variables investigated in this study. Results: The results indicated that the optimal values for Clove oil (X1), Tween 20 (X2), and Propylene glycol (X3) were determined to be 28.69, 76.45, and 24.93 (mg), respectively. Based on these optimized conditions, the predicted data points for the response variable s Particle Size (Y1), Polydispersity (Y2), and dissolution % (Y3) were determined to be 59.85 nm, 0.729 and 55.406%, respectively. Conclusion: The empirical results obtained from the optimized formulation exhibited a strong correlation with the predicted values. The optimized AZL-SMEDDS formulation demonstrated a rapid rate of drug solubility and greater bioavailability than AZL powder.
FORMULATION APPROACHES TO ENHANCE DRUG SOLUBILITY-BRIEF OVERVIEW
The solubility of drugs molecules remains one of the most challenging aspects in formulation development. With the advent of combinatorial chemistry and high throughput screening, the number of poorly water soluble compounds has increased solubility. A success of formulation depends on how efficiently it makes the drug available at the site of action. Therapeutic effectiveness of a drug depends upon the bioavailability and ultimately upon the solubility of drug molecules. Solubility is one of the important parameter to achieve desired concentration of drug in systemic circulation for pharmacological response to be shown. Solubility enhancement of various poorly soluble compounds is a challenging task for researchers and pharmaceutical scientists. On the basis of solubility, drugs are classified into four classes of the BCS classification. Solubility challenges are faced in the Class II and Class IV of the BCS system. To improve solubility and bioavailability of poorly soluble drug we use various technologies and formulation approaches. This review presents highlight information about the solubility significance, factors affecting solubility, and different formulation approaches used for the enhancement of the solubility of poorly soluble drugs including; pH-adjustment, co-solvents, surfactants, complex formation, lipidbased formulations, nano-suspensions and solid solution/dispersion technologies.
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 ...
ISRN pharmaceutics, 2013
Poorly water-soluble drug candidates are becoming more prevalent. It has been estimated that approximately 60-70% of the drug molecules are insufficiently soluble in aqueous media and/or have very low permeability to allow for their adequate and reproducible absorption from the gastrointestinal tract (GIT) following oral administration. Formulation scientists have to adopt various strategies to enhance their absorption. Lipidic formulations are found to be a promising approach to combat the challenges. In this review article, potential advantages and drawbacks of various conventional techniques and the newer approaches specifically the self-emulsifying systems are discussed. Various components of the self-emulsifying systems and their selection criteria are critically reviewed. The attempts of various scientists to transform the liquid self-emulsifying drug delivery systems (SEDDS) to solid-SEDDS by adsorption, spray drying, lyophilization, melt granulation, extrusion, and so forth ...
International Journal of Pharmaceutical Investigation, 2011
Background and Aim: Telmisartan (TEL) is an angiotensin II receptor blocker (ARB) antihypertensive agent. The aim of the present investigation was to develop a self-nanoemulsifying drug delivery system (SNEDDS) to enhance the oral bioavailability of poorly water soluble TEL. Materials and Methods: The solubility of TEL in various oils was determined to identify the oil phase of a SNEDDS. Various surfactants and co-surfactants were screened for their ability to emulsify the selected oil. Pseudoternary phase diagrams were constructed to identify the efficient self-emulsifying region. A SNEDDS was further evaluated for its percentage transmittance, emulsification time, drug content, phase separation, dilution, droplet size, zeta potential, pH, refractive index, and viscosity. Results: The developed SNEDDS formulation contained TEL (20 mg), Tween ® 20 (43.33%w/w), Carbitol ® (21.67%w/w), and Acrysol ® EL 135 (32%w/w). The optimized formulation of the TEL-loaded SNEDDS exhibited a complete in vitro drug release in 15 min as compared with the plain drug, which had a limited dissolution rate. It was also compared with the pure drug suspension by oral administration in male Wister rats. The in vivo study exhibited a 7.5-fold increase in the oral bioavailability of TEL from the SNEDDS compared with the pure drug suspension. Conclusions: These results suggest the potential use of the SNEDDS to improve the dissolution and oral bioavailability of poorly water soluble TEL.