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Novel cyclosporin A formulations using MPEG-hexyl-substituted polylactide micelles: a suitability study
K Mondon1, M Zeisser-Labouèbe, R Gurny
1School of Pharmaceutical Sciences, University of Geneva, University of Lausanne, Geneva, Switzerland.
Novel amphiphilic copolymers (MPEG-hexPLA) form stable micelles, significantly increasing Cyclosporin A (CsA) water solubility for transplant rejection treatment. These non-toxic micelles offer a promising injectable CsA carrier system with improved stability and reduced excipient needs.
Area of Science:
- Polymer Chemistry
- Nanotechnology
- Pharmaceutical Sciences
Background:
- Cyclosporin A (CsA) exhibits poor water solubility, necessitating non-aqueous formulations for intravenous administration in transplant rejection treatment.
- Novel amphiphilic copolymers based on methoxy-poly(ethylene glycol) (MPEG) and hexyl-substituted poly(lactides) (hexPLA) were investigated as potential drug delivery systems.
Purpose of the Study:
- To evaluate MPEG-hexPLA copolymers for CsA incorporation and formulation.
- To assess the biocompatibility and stability of CsA-loaded MPEG-hexPLA micelles.
- To determine the potential of these micelles as an injectable CsA carrier for transplant rejection treatment.
Main Methods:
- Synthesis and characterization of MPEG-hexPLA block-copolymers.
- Micelle formation above critical micellar concentration (CMC) and drug loading studies.
- In vitro and in vivo toxicity assessments (cell lines, chick embryo chorioallantoic membrane model).
- Hemolysis assays using human blood samples.
- Shelf-life stability studies at 4°C.
Main Results:
- MPEG-hexPLA copolymers self-assemble into stable, unimodal micelles (approx. 30 nm diameter) above CMC.
- Formulations demonstrated excellent shelf-life stability, with <7% drug loss after 1 year at 4°C.
- MPEG-hexPLA copolymers and their micelles exhibited no significant toxicity or hemolytic activity across tested concentrations.
- Efficient CsA incorporation into micelles (up to 6 mg/mL), achieving a 500-fold increase in water solubility.
- Required significantly less copolymer compared to conventional Cremophor®EL surfactant for clinical concentrations.
Conclusions:
- MPEG-hexPLA micelle solutions are non-toxic, biocompatible, and stable carriers for CsA.
- These novel micelles offer a substantial improvement in CsA water solubility and formulation efficiency.
- MPEG-hexPLA micelle formulations represent a promising injectable drug delivery system for managing transplant rejection.
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