Nanoemulsions as a formulation approach for topicals

11. February 2025

Penetrating the skin barrier and ensuring the bioavailability of active ingredients, as well as their protective capacity, are considered to be major challenges in the development of topical dosage forms.¹

Nanoemulsions offer a promising method for dissolving and delivering active ingredients, especially BCS classes II and IV, in relevant quantities. IMWITOR® 375 opens up new possibilities to meet these current efficacy requirements. Several case studies have shown how our product can be used in nanoemulsions and what concrete advantages result from this.

A partner of IOI Oleo GmbH has developed and tested two nanoemulsion systems (W/O/W and O/W) with IMWITOR® 375. In Franz cell tests, both systems showed reproducible results in terms of good bioavailability as well as optimized penetration depth and speed compared to existing topical formulations under development.

Case study I: Hydrocortisone from W/O/W nanoemulsion

  • 0.5 % 3H-hydrocortisone

  • Application: 10 µl/cm² over 24 h

  • Franz diffusion cell, 3 benchmarks (commercial gel, aqueous solution, liposome) vs. IMWITOR® 375 based nanoemulsion

    • IMWITOR® 375 based nanoemulsion delivers 3-4x as much active ingredient into the subcutis as the benchmarks
    • IMWITOR® 375 based nanoemulsion delivers 2-3x as much active ingredient into the acceptor fluid of the Franz diffusion cell as the benchmarks

Case study II: Ibuprofen from O/W nanoemulsion

  • 0.5 % 3H-ibuprofen

  • Application: 10 µl/cm² over 24 h

  • Franz diffusion cell, 2 benchmarks (commercial gel, non-commercialized gel) vs. IMWITOR® 375 based nanoemulsion

    • IMWITOR® 375-based nanoemulsion delivers the highest amount of active ingredients to the skin
    • IMWITOR® 375 based nanoemulsion delivers 3-4x as much active ingredient into the acceptor fluid of the Franz diffusion cell as both benchmarks

With these study results, IMWITOR® 375-based nanoemulsions promise far better bioavailability with constant active ingredient use on the one hand or, on the other hand, enable reduced quantities of active ingredients to be used while maintaining the same bioavailability. This can have advantages for the cost structure, formulation economy and expected side effects or incompatibilities.

We are happy to share specific study details and further studies on other active ingredients with you on request!

Key features of the nanoemulsions based on IMWITOR® 375:

  • High loadings of up to 12 % active ingredient

  • Significant improvement in solubility compared to non-encapsulated active ingredient presentation, e.g. tocopherol @ 100 mg/ml

  • PSD: 120-250 nm and smaller

  • PDI: <0.2

  • Green chemistry based on plant-based raw materials such as sunflower, sugar beet, sugar cane and rapeseed

  • Confirmed uses in semi-solid and liquid dosage forms

  • Patentable

IMWITOR® 375-based nanoemulsions offer a modern, technologically interesting and sustainable alternative to other solubilization and encapsulation technologies. They open up unique opportunities for product innovations and product range extensions.

For sample requests and detailed information on how these systems can support your projects, please get in touch with your known contacts. IOI Oleo GmbH offers comprehensive R&D support for new product developments, the expansion of existing product lines and relaunch projects.

If you are interested in individual formulations or further information, we look forward to hearing from you.

¹Wen-Kai Hsiao et.al, Opportunities of topical drug products in a changing dermatological landscape, European Journal of Pharmaceutical Sciences, Volume 203, 2024, 106913, https://doi.org/10.1016/j.ejps.2024.106913

Share this article!

Robert Radsziwill

Robert is the Business Development Manager for Functional Excipients in the Pharma Division of IOI Oleo GmbH. Prior to this role he held technical and commercial roles focusing raw materials used in the pharmaceutical and medical device industry for 13 years. In each position he leveraged his diploma degree in Business Chemistry earned at Westfälische Wilhelms-University to drive interdisciplinary projects and work as interface between commercial and technical decision makers. Understanding technical, commercial and regulatory drivers from ideation to successful project-completion is key for him. In his free time he enjoys guitar heavy music as well as cooking for and with family and friends.