Abstract

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.

Highlights

  • Advances in in vitro screening methods like combinatorial chemistry are leading to the emergence of many potential chemical components with marked therapeutic activity

  • (v) Along with the lipids, surfactants that are commonly used in the formulation of SMEDDS like Tween 80, Spans, Cremophors (EL and RH40), and Pluronics are reported to have inhibitory action on efflux transporters which help in improving bioavailability of the drugs which are substrates to the efflux pumps [11, 13,14,15]

  • In a study performed by Jantratid et al, comparison is made between the drug release profile using paddle type apparatus and that of reciprocating cylinder and it was found that the use of USP apparatus 3 for the evaluation of drug release from the liquid lipid dosage forms like SMEDDS is more suitable than the paddle method and produced reproducible results compared to the paddle method and concluded that this type of behavior is attributed to the uniform break-up of oil layer by the movement of inner cylinder with mesh inserts compared to the paddle method [67]

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Summary

Introduction

Advances in in vitro screening methods like combinatorial chemistry are leading to the emergence of many potential chemical components with marked therapeutic activity. The inherent properties of chemical moieties can be modified by various means like particle size reduction and by salt formation of the drug to improve the bioavailability without any formulation approach. It is not always possible with all drug molecules. Stimulation of lymphatic transport: the highly lipophilic drug (log P > 5) which has high solubility in triglycerides (>50 mg/mL) can undergo lymphatic transport when coadministered with esters of unsaturated long chain fatty acids; thereby bioavailability can be improved [7,8,9] This restricted lymphatic transport is mainly due to low lymph-to-blood flow ratio. SMEDDS usually produce microemulsions of droplet size below 100 nm upon dilution [3]

Importance of SMEDDS
Composition of SMEDDS
Mechanism of Self-Emulsification
Effect of Drug Addition on SMEDDS
Screening of Excipients
Characterization of SMEDDS
Findings
Conclusion
Full Text
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