scholarly journals Self-Microemulsifying Drug Delivery Systems: An Attractive Strategy for Enhanced Therapeutic Profile

2014 ◽  
Vol 2014 ◽  
pp. 1-11 ◽  
Author(s):  
Samatha Akula ◽  
Aravind Kumar Gurram ◽  
Srinivas Reddy Devireddy

Ease of administration and painless approach made oral route the most preferred. Poor oral bioavailability is pronounced with the majority of recent active ingredients because of dissolution rate limited absorption. Failure to attain intended therapeutic effect of the poor water soluble drugs by this route led to development of novel drug delivery systems which will fulfill therapeutic needs with minimum dose. Although many formulation approaches like solid dispersions, complexation, pH modification, and cocrystals exist, lipid based delivery systems finding increased appliance with the apparent increase in absorption of drug. Among lipid based formulations, self-microemulsifying formulations (droplet size < 100 nm) are evident to improve the oral bioavailability of hydrophobic drugs primarily due to their efficiency in facilitating solubilization and in presenting the hydrophobic drug in solubilized form whereby dissolution process can be circumvented. Various components that are used to formulate these dosage forms like surfactants and lipids contribute to the overall improvement in oral bioavailability via promoting the lymphatic transport; thereby hepatic first pass metabolism can be surmounted. The present paper gives exhaustive information on the formulation design and characterization of SMEDDS along with the probable mechanisms by which the bioavailability can be improved with SMEDDS.

2013 ◽  
Vol 63 (4) ◽  
pp. 427-445 ◽  
Author(s):  
Katja Čerpnjak ◽  
Alenka Zvonar ◽  
Mirjana Gašperlin ◽  
Franc Vrečer

Abstract Low oral bioavailability as a consequence of low water solubility of drugs is a growing challenge to the development of new pharmaceutical products. One of the most popular approaches of oral bioavailability and solubility enhancement is the utilization of lipid-based drug delivery systems. Their use in product development is growing due to the versatility of pharmaceutical lipid excipients and drug formulations, and their compatibility with liquid, semi-solid, and solid dosage forms. Lipid formulations, such as self-emulsifying (SEDDS), self-microemulsifying SMEDDS) and self- -nanoemulsifying drug delivery systems (SNEDDS) were explored in many studies as an efficient approach for improving the bioavailability and dissolution rate of poorly water-soluble drugs. One of the greatest advantages of incorporating poorly soluble drugs into such formulations is their spontaneous emulsification and formation of an emulsion, microemulsion or nanoemulsion in aqueous media. This review article focuses on the following topics. First, it presents a classification overview of lipid-based drug delivery systems and mechanisms involved in improving the solubility and bioavailability of poorly water-soluble drugs. Second, the article reviews components of lipid-based drug delivery systems for oral use with their characteristics. Third, it brings a detailed description of SEDDS, SMEDDS and SNEDDS, which are very often misused in literature, with special emphasis on the comparison between microemulsions and nanoemulsions.


Author(s):  
Navneet Sharma ◽  
Sabna Kotta ◽  
Mohd Aleem ◽  
Shubham Singh ◽  
Rakesh Kumar Sharma

In the last decade, there has been a mounting concern in lipid-based formulations to deliver water-soluble drugs. Lipid-based drug delivery systems are one of the budding and promising technologies designed to tackle the poor bioavailability problems. This chapter stresses the different mechanisms of lipophilic drug absorption along with its advantages and limitations. It points out the different mechanisms of how lipid-based excipients and the different formulations interact with the absorption process. This review provides a comprehensive summary about the lipid formulation classification scheme (LFCS), a guide for the selection of appropriate formulation and commonly used excipients for lipid-based formulations, along with the important factors to be considered in formulation design and excipient selection. This review also focuses on the formulation of solid lipid-based formulations, important evaluation aspects, and commercial formulations available for the purpose.


Author(s):  
Srikanth Reddy Sokkula ◽  
Suresh Gande

Lipid-based drug delivery systems are extensively reported in literature for enhancing the drug solubility, permeability and bioavailability. These systems include   simple oil solutions, coarse, multiple and dry emulsions, complex self-emulsifying, microemulsifying or nanoemulsifying drug delivery systems. Self-emulsifying systems are further classified as self-microemulsifying drug delivery systems (SMEDDS) and self-nanoemulsifying drug delivery systems (SNEDDS) are most prevailing and commercially viable oil based approach for drugs that exhibit low dissolution rate and inadequate absorption. Ever since the progress of SNEDDS, they drew the interest of researchers in order to deal with the challenges of poorly water-soluble drugs. SNEDDS is a proven method for enhancing solubility and bioavailability of lipophilic compounds. Considering the ease of large-scale production and the robustness of SNEDDS, several formulations techniques are commercially available. The stability of SNEDDS can be further enhanced by solidifying liquid SNEDDS. Controlled release and supersaturated SNEDDS received patient compliance with larger drug loading. Presence of biodegradable ingredients and ‘drug-targeting opportunities’ facilitate SNEDDS a clear merit and distinction amongst available solubility enhancement techniques. In this article attempt was made to present an overview of SNEDDS, their mechanism, formulation excipients and potentials of SNEDDS, recent advancements, advantages and disadvantages of SNEDDS formulations. The article also focuses on reviewing the application of SNEDDS in enhancing bioavailability of antihypertensive drugs.


Author(s):  
Bhikshapathi D. V. R. N. ◽  
Priya Keerthi

Development of self-emulsifying drug delivery systems (SEDDS) are becoming more popular to improve the oral bioavailability of poorly water-soluble drugs. Rosuvastatin is a lipid-lowering agent used in patients suffering from dyslipidemia. It is a competitive inhibitor of 3-hydroxy 3-methyl glutaryl coenzyme A, which converts mevalonate to cholesterol. Rosuvastatin is a BCS class II (poor solubility) drug; hence, SNEDDS are being formulated to enhance oral bioavailability of the drug. In the present study, rosuvastatin SNEDDS were formulated using different oils, surfactant and co-surfactant. The optimized formulation F9 has composition of Las (PEG-8-Caprylic glycerides), Maisine 35-1 and Tween 20 as oil phase, surfactant and co-surfactant respectively. Composition of SNEDDS was optimized using Pseudo-ternary phase diagram, where the formulations showed increased self-emulsification with increased concentration of surfactants. Formulation F9 was found to be best formulation based on evaluation parameters. The particle size of the optimized SNEDDS formulation was found to be 10.9 nm & Z-Average of 55.6 nm indicating all the particles were in the nanometer range. The zeta potential of the optimized SNEDDS formulation was found to be -11.2 mV, which comply with the requirement of the zeta potential for stability. The developed rosuvastatin SNEDDS have the potential to minimize the variability in absorption and provide rapid onset of action of the drug.   


Molecules ◽  
2015 ◽  
Vol 20 (11) ◽  
pp. 20397-20408 ◽  
Author(s):  
Matthew McKenzie ◽  
David Betts ◽  
Amy Suh ◽  
Kathryn Bui ◽  
London Kim ◽  
...  

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