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Optimization of Dihydrosphingomyelin/cholesterol Mol Ratio in Topotecan-loaded Liposomes to Enhance Drug Retention and Plasma Half-life by Understanding Physicochemical and Thermodynamic Properties of the Lipid Membrane by Noriyuki Kasagi; Issei Doi; Jun Nakabayashi; Kengo Saito; Akiko Tadakuma; Nanae Muraki; Ritsuko Hori; Toshifumi Kimura; Ken Okada; Naoki Yamada; Keiko Makita-Suzuki; Hiroki Tanisaka; Susumu Shimoyama; Mikinaga Mori is a Chemistry article available to read on EtoBox.

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Robust retention of drugs in liposomes is one of the most critical factors for liposomal drug formulation. It improves loading efficiency of the active pharmaceutical ingredient (API), stability during longterm storage, and half-life of the drug in the body. This study deductively optimized the lipid composition of topotecan-loaded liposome using dihydrosphingomyelin (DHSM), cholesterol (Chol), and 1,2distearoyl-sn-glycero-3-phosphoethanolamine-poly(ethylene glycol) (DSPE PEG) for intravenous injection by thermodynamic and fluidity analyses of the liposome membrane. High efficiency in topotecan loading was achieved in the range of the liquid-ordered phase (egg-derived DHSM/Chol molar ratio 70/25% or a higher Chol ratio with PEG constant at 5 mol%) as predicted by thermodynamic analysis. The eggderived DHSM/Chol/PEG mol ratio that minimizes topotecan leakage was estimated to be 57/38/5 via electron spin resonance (ESR) for fluidity analysis. The optimized liposome significantly prolonged the half-life of topotecan in blood compared to non-liposomal topotecan. To minimize the risk of virus contamination and ensure easier quality control for clinical application, synthetic DHSM was us

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Author

Noriyuki Kasagi; Issei Doi; Jun Nakabayashi; Kengo Saito; Akiko Tadakuma; Nanae Muraki; Ritsuko Hori; Toshifumi Kimura; Ken Okada; Naoki Yamada; Keiko Makita-Suzuki; Hiroki Tanisaka; Susumu Shimoyama; Mikinaga Mori

Publisher

Elsevier BV

Published

2023

Language

EN

Field

Chemistry (Physical Sciences)