Phospholipid composition of small unilamellar liposomes containing melphalan influences drug action in mice bearing PC6 tumours

Large, Pamela; Gregoriadis, Gregory

doi:10.1016/0006-2952(83)90289-7

Cited by 10 publications

(3 citation statements)

References 21 publications

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“…Melphalan is a potent chemotherapeutic agent in MM treatment, and melphalan-based drug development and delivery optimization have been investigated since the 1980s. The studies for liposomal melphalan in past decades mainly focused on pharmacokinetics in solid tumor models, including lymph node uptake in metastasis animal models and plasma clearance. , Another research area was the efficacy of heat-sensitive liposomal melphalan combined with local hyperthermia in animal models of melanoma. , Recently, Sambamoorthy et al constituted vitamin E oil-incorporated liposomal melphalan particles and showed that the particles exhibited cytotoxicity to MM cells in vitro. Compared with previous studies of liposomal melphalan, our work is novel and valid.…”

Section: Discussionmentioning

confidence: 99%

“… 23 As early as the 1980s, researchers constituted liposomal melphalan particles and investigated their distributions in vivo in experimental animals. 24 Later, the anticancer activity of liposomal melphalan was tested in different tumor-bearing animal models, such as models of plasmacytoma, 25 melanoma, 26 retinoblastoma, 27 and breast cancer. 28 In general, liposomal melphalan exhibited potent anticancer activity with reduced systemic toxicity.…”

Section: Discussionmentioning

confidence: 99%

“…The studies for liposomal melphalan in past decades mainly focused on pharmacokinetics in solid tumor models, including lymph node uptake in metastasis animal models and plasma clearance. 24 , 25 Another research area was the efficacy of heat-sensitive liposomal melphalan combined with local hyperthermia in animal models of melanoma. 26 , 29 Recently, Sambamoorthy et al constituted vitamin E oil-incorporated liposomal melphalan particles and showed that the particles exhibited cytotoxicity to MM cells in vitro.…”

Section: Discussionmentioning

confidence: 99%

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Liposome-Encapsulated Melphalan Exhibits Potent Antimyeloma Activity and Reduced Toxicity

Zheng

Chu

et al. 2022

ACS Omega

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Multiple myeloma (MM), a plasma cell cancer in bone marrow, remains an incurable disease. Melphalan, an alkylating agent, is a conventional anticancer drug that is still widely used for MM treatment in clinics. However, melphalaninduced organ toxicity and side effects are common. In this study, we loaded melphalan into a liposomal capsule and constituted liposomal melphalan (liposomal MEL). Liposomal MEL particles were approximately 120 nm in size and stable in vitro. The liposomal particles could be effectively taken up by MM cells. In vitro cytotoxicity assays using MM cell lines and primary MM cells showed that liposomal MEL exhibited similar anti-MM activity compared to an equivalent amount of free melphalan (free MEL) compound. In animal models, liposomal particles had bone marrow enrichment and prolonged half-life in vivo. Liposomal MEL exposure resulted in less liver and colon organ toxicity than exposure to an equivalent amount of free MEL-treated mice. Importantly, liposomal MEL had potent anti-MM activity in vivo in a human MM xenograft mouse model. Overall, our findings suggested that liposome-encapsulated melphalan was an effective drug modification of the melphalan compound and showed promise in MM treatment.

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