Abstract
Background: Cisplatin is a potent anticancer drug for treating melanoma. Objective: The aim of this study was to evaluate the possibility of using liposomes, for intratumoral distribution in a melanoma, composed of phosphatidylethanolamine (PE), for its cytotoxicity. Method: The in vitro drug release, in vitro cytotoxicity against melanoma, and in vivo residence time in the tumor of liposome-encapsulated cisplatin were investigated. The liposomes were prepared and characterized in terms of their morphology, size, zeta potential, and drug loading. Result: The size of the PE liposomes attained a level of ∼100 nm. The concentration of cisplatin encapsulated in PE liposomes was 50-70% dependent on the presence or absence of polyethylene glycol (PEG) derivatives. On the other hand, no or negligible cisplatin molecules were encapsulated in egg phosphatidylcholine (EPC) liposomes. PE liposomes had higher cytotoxicity than classic liposomes or free cisplatin. Images of confocal laser scanning microscopy confirmed the great potency of PE liposomes to deliver cisplatin into cells. The incorporation of PEG derivatives completely inhibited the proliferation of melanoma cells. With in vivo intratumoral administration, the cisplatin concentration in the tumor tissue was maintained at a high level for 72 h after application of the PE liposomes. The PE liposomes delivered cisplatin into the tumor ∼3.6 times more efficiently than the free drug. Conclusion: These results demonstrate that PE liposomes represent a potentially useful strategy for targeting cisplatin delivery into melanomas.
| Original language | English |
|---|---|
| Pages (from-to) | 11-20 |
| Number of pages | 10 |
| Journal | Journal of Dermatological Science |
| Volume | 46 |
| Issue number | 1 |
| DOIs | |
| Publication status | Published - Apr 2007 |
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Keywords
- Cisplatin
- Intratumor
- Liposomes
- Melanoma
- Phosphatidylethanolamine
ASJC Scopus subject areas
- Dermatology
Cite this
Cisplatin encapsulated in phosphatidylethanolamine liposomes enhances the in vitro cytotoxicity and in vivo intratumor drug accumulation against melanomas. / Hwang, Tsong Long; Lee, Woan Ruoh; Hua, Shu Chiou; Fang, Jia Y.
In: Journal of Dermatological Science, Vol. 46, No. 1, 04.2007, p. 11-20.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Cisplatin encapsulated in phosphatidylethanolamine liposomes enhances the in vitro cytotoxicity and in vivo intratumor drug accumulation against melanomas
AU - Hwang, Tsong Long
AU - Lee, Woan Ruoh
AU - Hua, Shu Chiou
AU - Fang, Jia Y.
PY - 2007/4
Y1 - 2007/4
N2 - Background: Cisplatin is a potent anticancer drug for treating melanoma. Objective: The aim of this study was to evaluate the possibility of using liposomes, for intratumoral distribution in a melanoma, composed of phosphatidylethanolamine (PE), for its cytotoxicity. Method: The in vitro drug release, in vitro cytotoxicity against melanoma, and in vivo residence time in the tumor of liposome-encapsulated cisplatin were investigated. The liposomes were prepared and characterized in terms of their morphology, size, zeta potential, and drug loading. Result: The size of the PE liposomes attained a level of ∼100 nm. The concentration of cisplatin encapsulated in PE liposomes was 50-70% dependent on the presence or absence of polyethylene glycol (PEG) derivatives. On the other hand, no or negligible cisplatin molecules were encapsulated in egg phosphatidylcholine (EPC) liposomes. PE liposomes had higher cytotoxicity than classic liposomes or free cisplatin. Images of confocal laser scanning microscopy confirmed the great potency of PE liposomes to deliver cisplatin into cells. The incorporation of PEG derivatives completely inhibited the proliferation of melanoma cells. With in vivo intratumoral administration, the cisplatin concentration in the tumor tissue was maintained at a high level for 72 h after application of the PE liposomes. The PE liposomes delivered cisplatin into the tumor ∼3.6 times more efficiently than the free drug. Conclusion: These results demonstrate that PE liposomes represent a potentially useful strategy for targeting cisplatin delivery into melanomas.
AB - Background: Cisplatin is a potent anticancer drug for treating melanoma. Objective: The aim of this study was to evaluate the possibility of using liposomes, for intratumoral distribution in a melanoma, composed of phosphatidylethanolamine (PE), for its cytotoxicity. Method: The in vitro drug release, in vitro cytotoxicity against melanoma, and in vivo residence time in the tumor of liposome-encapsulated cisplatin were investigated. The liposomes were prepared and characterized in terms of their morphology, size, zeta potential, and drug loading. Result: The size of the PE liposomes attained a level of ∼100 nm. The concentration of cisplatin encapsulated in PE liposomes was 50-70% dependent on the presence or absence of polyethylene glycol (PEG) derivatives. On the other hand, no or negligible cisplatin molecules were encapsulated in egg phosphatidylcholine (EPC) liposomes. PE liposomes had higher cytotoxicity than classic liposomes or free cisplatin. Images of confocal laser scanning microscopy confirmed the great potency of PE liposomes to deliver cisplatin into cells. The incorporation of PEG derivatives completely inhibited the proliferation of melanoma cells. With in vivo intratumoral administration, the cisplatin concentration in the tumor tissue was maintained at a high level for 72 h after application of the PE liposomes. The PE liposomes delivered cisplatin into the tumor ∼3.6 times more efficiently than the free drug. Conclusion: These results demonstrate that PE liposomes represent a potentially useful strategy for targeting cisplatin delivery into melanomas.
KW - Cisplatin
KW - Intratumor
KW - Liposomes
KW - Melanoma
KW - Phosphatidylethanolamine
UR - http://www.scopus.com/inward/record.url?scp=33847769265&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=33847769265&partnerID=8YFLogxK
U2 - 10.1016/j.jdermsci.2006.12.011
DO - 10.1016/j.jdermsci.2006.12.011
M3 - Article
C2 - 17267180
AN - SCOPUS:33847769265
VL - 46
SP - 11
EP - 20
JO - Journal of Dermatological Science
JF - Journal of Dermatological Science
SN - 0923-1811
IS - 1
ER -