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How wound environments trigger the release from Rifampicin-loaded liposomes
Chantal M Wallenwein1, Mukul Ashtikar1, Götz Hofhaus2
1Fraunhofer Institute for Translational Medicine and Pharmacology ITMP, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.
International Journal of Pharmaceutics
|January 12, 2023
Summary
A new liposomal rifampicin formulation offers a stable topical delivery system for chronic wounds. Oxidative stress in wound environments accelerates drug release, enhancing targeted delivery and anti-inflammatory effects.
Area of Science:
- Pharmaceutics
- Drug Delivery Systems
- Wound Healing
Background:
- Chronic wounds exhibit elevated proinflammatory cytokines, delaying healing.
- Topical rifampicin shows anti-inflammatory potential but lacks commercial topical products.
- A liposomal drug delivery system was developed to address this unmet medical need.
Purpose of the Study:
- To develop and characterize a stable liposomal topical delivery system for rifampicin.
- To investigate the in vitro release kinetics of rifampicin under simulated wound conditions.
- To identify key factors influencing rifampicin release from liposomes in a wound environment.
Main Methods:
- Liposomes prepared via thin-film hydration and freeze-dried for stability.
- In vitro rifampicin release studied using Dispersion Releaser technology in simulated wound fluid.
- Influences of oxidation, plasma proteins (albumin), and lipolysis on release were evaluated.
Main Results:
- Liposomes effectively protected rifampicin from degradation during storage.
- Plasma proteins showed minimal impact on rifampicin release (>70% albumin binding).
- Oxidative wound environment significantly accelerated rifampicin release, acting as a primary trigger.
Conclusions:
- A stable liposomal topical rifampicin formulation was successfully developed.
- Drug oxidation in simulated wound fluid accelerates rifampicin release.
- The identified oxidative trigger mechanism facilitates targeted drug delivery to inflamed tissues.
Keywords:
Chronic woundIn vitro release / dissolution / liberationLipolysisLiposomesNanocarriersRifampicinSimulated wound fluid
