Alkyl glucopyranoside-based niosomes containing methotrexate for pharmaceutical applications: evaluation of physico-chemical and biological properties.
We designed novel niosomes based on alkyl glucopyranoside surfactants and containing methotrexate as anticancer drug, to be used in the pharmaceutical field. The effects of surfactants with chains of different length on niosome size and their distribution, drug entrapment efficiencies and in vitro drug release were determined. Systems made of alkyl glucopyranosides and cholesterol form vesicles whose average size scales with the alkyl chains length of such surfactants. Vesicles size ranges between 300 and 500 nm, with low polydispersity index. In addition, the hemolytic activity of alkyl glucopyranosides as surfactant solutions or vesicular formulations was studied and compared, to identify possible structure-activity relationships. High methotrexate entrapment efficiency was obtained, confirming significant interactions between the drug and the niosomal matrices. After 24h the amount of methotrexate released from niosomal formulations is effectively delayed, compared to the free drug in solution. Hemolytic tests show that sugar-based surfactants are more hemolytic the longer is their alkyl chain. When the surfactants are in vesicular form, the reverse behavior holds. It was also inferred that vesicle formation reduces the surfactant toxicity. These niosomal formulations can be used as methotrexate delivery systems in anticancer therapy.
Dipartimento di Farmacia e Scienze della Salute e della Nutrizione, Università della Calabria, Edificio Polifunzionale, 87036 Arcavacata di Rende, Cosenza, Italy. Electronic address: rita.muzzalupo@unical.it.
Rita
R
Muzzalupo
Lorena
L
Tavano
Camillo
C
La Mesa
D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D002784:Cholesterol / Q000008:administration & dosage / Q000737:chemistry; D008081:Liposomes / Q000008:administration & dosage* / Q000737:chemistry*; D008727:Methotrexate / Q000008:administration & dosage* / Q000737:chemistry*; D010316:Particle Size; D012996:Solutions / Q000737:chemistry; D013329:Structure-Activity Relationship; D013501:Surface-Active Agents / Q000008:administration & dosage / Q000737:chemistry
D000970:Antineoplastic Agents; D008081:Liposomes; D012996:Solutions; D013501:Surface-Active Agents; D002784:Cholesterol; D008727:Methotrexate
Alkyl glucopyranoside surfactants; Hemolysis; Methotrexate; Niosomes; Parenteral release