GSH-PEGylated liposomal methylprednisolone in comparison to free methylprednisolone: slow release characteristics and prolonged lymphocyte depression in a first-in-human study.

Kanhai KMS, Zuiker RGJA, Stavrakaki I, Gladdines W, Gaillard PJ, Klaassen ES, Groeneveld GJ

Intravenous high-dose free methylprednisolone hemisuccinate (MP) is the primary treatment for an acute relapse in relapsing-remitting (RR) multiple sclerosis (MS). However, it is inconvenient and its side effects are undesirable. Both dose and dosing frequency can be reduced by incorporating free MP in glutathione (GSH) PEGylated liposomes, creating a slow-release formulation with reduced toxicity and prolonged peripheral efficacy. This first-in-human study was designed to assess the safety, pharmacokinetics (PK) and pharmacodynamics (PD) of GSH-PEGylated liposomes containing MP (2B3-201).