Liposomal Formulation of a Melphalan Lipophilic Prodrug: Studies of Acute Toxicity, Tolerability, and Antitumor Efficacy.
Animals
Antineoplastic Agents
/ administration & dosage
Behavior, Animal
/ drug effects
Breast Neoplasms
/ drug therapy
Cell Proliferation
/ drug effects
Diglycerides
/ chemical synthesis
Dose-Response Relationship, Drug
Drug Compounding
Drug Screening Assays, Antitumor
Female
Liposomes
/ chemical synthesis
Male
Melphalan
/ administration & dosage
Mice
Mice, Inbred C57BL
Molecular Structure
Prodrugs
/ administration & dosage
Rats
Structure-Activity Relationship
Melphalan
acute toxicity in rats
antitumor efficacy
hemopoiesis
lipophilic prodrug
lyophilized nano-sized liposomes
mouse breast cancer
natural phospholipids.
Journal
Current drug delivery
ISSN: 1875-5704
Titre abrégé: Curr Drug Deliv
Pays: United Arab Emirates
ID NLM: 101208455
Informations de publication
Date de publication:
2020
2020
Historique:
received:
01
07
2019
revised:
13
12
2019
accepted:
02
02
2020
pubmed:
15
2
2020
medline:
1
6
2021
entrez:
15
2
2020
Statut:
ppublish
Résumé
Recently we developed a scalable scheme of synthesis of melphalan ester conjugate with 1,2-dioleoyl- Herein we compared this new convenient in use formulation of MlphDG with parent drug Alkeran Liposomes of approximately 100 nm in diameter, consisting of egg phosphatidylcholine, soybean phosphatidylinositol, and MlphDG, or placebo liposomes without the drug were produced by extrusion and lyophilized. Alkeran Liposomes showed approximately two times lower acute toxicity and better tolerability than Alkeran Lower toxicity of the liposomal formulation of MlphDG promises improved quality of life for cancer patients in need of treatment with melphalan. Presumably, the list of indications for melphalan therapy could be extended.
Sections du résumé
BACKGROUND
BACKGROUND
Recently we developed a scalable scheme of synthesis of melphalan ester conjugate with 1,2-dioleoyl-
OBJECTIVE
OBJECTIVE
Herein we compared this new convenient in use formulation of MlphDG with parent drug Alkeran
METHOD
METHODS
Liposomes of approximately 100 nm in diameter, consisting of egg phosphatidylcholine, soybean phosphatidylinositol, and MlphDG, or placebo liposomes without the drug were produced by extrusion and lyophilized. Alkeran
RESULTS
RESULTS
Liposomes showed approximately two times lower acute toxicity and better tolerability than Alkeran
CONCLUSION
CONCLUSIONS
Lower toxicity of the liposomal formulation of MlphDG promises improved quality of life for cancer patients in need of treatment with melphalan. Presumably, the list of indications for melphalan therapy could be extended.
Identifiants
pubmed: 32056524
pii: CDD-EPUB-104505
doi: 10.2174/1567201817666200214105357
doi:
Substances chimiques
Antineoplastic Agents
0
Diglycerides
0
Liposomes
0
Prodrugs
0
Melphalan
Q41OR9510P
diolein
Z3MP1W91CW
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
312-323Informations de copyright
Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.