The activity of doxorubicin niosomes against an ovarian cancer cell line and three in vivo mouse tumour models.
Demonstration of the improved doxorubicin pharmacokinetics and tumoricidal activity, after a single intravenous dose of 10mg kg-1 doxorubicin sorbitan monostearate (Span 60) based niosomes in the mouse adenocarcinoma (MAC) tumour model (Uchegbu et al., 1995) preceded the present study in which the activity of doxorubicin C16G2 (a hexadecyl diglycerol ether) based niosomes was evaluated against naive and established MAC tumour models. C16G2 niosomes were equiactive with doxorubicin solution. It is concluded that while in some tumour models, niosomal formulations demonstrate some advantages over the free drug, caution is advocated in the extrapolation of these results. The activity of doxorubicin C16G2 and Span 60 niosomes was also studied against a human ovarian cancer cell line and its doxorubicin resistant subline. There was a slight reduction in the IC50 against the resistant cell line when the drug was encapsulated in Span 60 niosomes in comparison to the drug in solution. Taking into account the in-vitro release characteristics of the various niosomal formulations, it is concluded that the use of niosomal formulations against multidrug resistance shows sufficiently encouraging results to warrant further study.
Uchegbu
I F
IF
School of Pharmacy, University of London.
Double
J A
JA
Kelland
L R
LR
Turton
J A
JA
Florence
A T
AT
D000230:Adenocarcinoma / Q000188:drug therapy / Q000473:pathology; D000704:Analysis of Variance; D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use*; D001665:Binding Sites; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy* / Q000378:metabolism; D018699:Coated Vesicles; D004317:Doxorubicin / Q000097:blood / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use*; D004339:Drug Compounding; D016503:Drug Delivery Systems; D018432:Drug Resistance, Multiple; D005260:Female; D005995:Glyceryl Ethers / Q000737:chemistry / Q000378:metabolism; D006601:Hexoses / Q000737:chemistry / Q000378:metabolism; D007275:Injections, Intravenous; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D008819:Mice, Nude; D009368:Neoplasm Transplantation; D009374:Neoplasms, Experimental / Q000188:drug therapy / Q000378:metabolism; D010051:Ovarian Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D013501:Surface-Active Agents / Q000737:chemistry / Q000378:metabolism; D014407:Tumor Cells, Cultured
D000903:Antibiotics, Antineoplastic; D005995:Glyceryl Ethers; D006601:Hexoses; D013501:Surface-Active Agents; D004317:Doxorubicin; C009298:sorbitan monostearate