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SEDDS technologies & nano-emulsions for the oral administration of active ingredients rethought
SEDDS technologies & nano-emulsions for the oral administration of active ingredients rethought
Lipid-based excipients from IOI Oleo help to improve the bioavailability of poorly soluble active ingredients.
The majority of new active ingredient candidates in clinical development show low solubility, poor absorption capacity or a combination of both. This means that formulation developers are faced with growing challenges, while, at the same time, interest in orally available therapies for complex molecules is growing. One example is the intensive research on GLP-1 analogues, which additionally draws attention to formulation technologies that should enable or support the oral delivery of sophisticated active ingredients. This includes established self-emulsifying carriers for active ingredients (SEDDS, SMEDDS and SNEDDS), which continue to gain importance in the course of these developments.
Against this backdrop, lipid-based excipients are also increasingly in focus. With decades of experience in lipid chemistry, GMP-compliant production and application development, IOI Oleo supports formulators in the development of drug delivery systems for oral, topical and parenteral applications.
IMWITOR® 742: An amphiphilic excipient for lipophilic active ingredients
IMWITOR® 742 is often used in SEDDS formulations to improve the solubility of lipophilic active ingredients. Thanks to its amphiphilic properties, the excipient supports the faster formation of fine emulsions in gastrointestinal fluids. Scientific studies on SEDDS technologies show that IMWITOR® 742 can be an effective tool for addressing formulation challenges posed by poorly soluble active ingredients in the BCS classes II and IV.
Why SEDDS? Solutions for current challenges in bioavailability
SEDDS (self-emulsifying drug delivery systems) are based on a combination of lipids, surfactants and co-solvents. Following contact with gastrointestinal fluids, they spontaneously form fine emulsions or nano-emulsions, which significantly enlarge the surface available for active ingredient distribution. Thus, the active ingredient can be present in soluble form for longer and absorbed more efficiently.
This mechanism offers several advantages:
- improved solubilisation of poorly soluble active ingredients
- increased absorption and bioavailability
- lower effect of food on the absorption of active ingredients
- quicker and better reproducible onset of action
Functional excipients as key high-performance SEDDS formulations
Today, different classes of lipid-based excipients are available for the development of SEDDS. Diverse lipids, emulsifiers and solubilisers are used, depending on active ingredient and formulation goal. IOI Oleo offers a portfolio for various areas of application:
- Medium-chained triglycerides (MCTs) of the MIGLYOL® series serve as a polar, low-viscosity oil phase that dissolves and solubilises active ingredients
- Partial glycerides of the IMWITOR® product family are multifunctional as active ingredient carriers, surfactants and solubilisers
- SOFTIGEN® 767 as a co-surfactant and solubiliser
Here, the individual components fulfil a variety of functions. They can support the solubilisation of the active ingredient, influence emulsion formation or contribute to the stability of the formulation. It is their coordinated interaction that determines the performance of the system.1,2
IMWITOR® 375: Support for nano-emulsions
Internal analyses and studies with development partners show that IMWITOR® 375 can promote the formation of nano-emulsions and improve the encapsulation of active ingredients. These properties make the excipient an interesting option for formulations in which the aim is to achieve high active ingredient loading capacity and efficient release.
What must be taken into account for an SEDDS formulation?
The selection of suitable excipients is an important component of formulation development. In addition, various physiochemical parameters must be considered:
- the hydrophilic-lipophilic balance (HLB value)
- droplet size distribution of the resulting emulsion (in the case of SNEDDS, typically below 100 nm)
- the thermodynamic stability of the formulation
- the compatibility between active ingredient and excipients
- the achievable loading capacity of the active ingredient
The weighting of these parameters depends on the properties of the respective active ingredient and the desired formulation goal.
Oral GLP-1 formulations as a field of research for self-emulsifying active ingredient carrier systems
The development of orally available peptide therapies has significantly increased the interest in lipid-based carrier systems for active ingredients in recent years. Studies on self-emulsifying formulations for GLP-1 active ingredients show the central role the selection of suitable excipients plays for solubilisation, stability and active ingredient absorption. Several of the excipient types applied in these studies are also found in IOI Oleo’s portfolio. Moreover, comparable lipid-based excipients have already been tested in similar formulation concepts.3
Read the original article here
Source: IOI Oleo, website SEDDS Technologies & Lipid-based Active Ingredients | IOI Oleo
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