Cisplatin encapsulated in phosphatidylethanolamine liposomes enhances the in vitro cytotoxicity and in vivo intratumor drug accumulation against melanomas

Tsong Long Hwang, Woan Ruoh Lee, Shu Chiou Hua, Jia Y. Fang

Research output: Contribution to journalArticle

54 Citations (Scopus)

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 languageEnglish
Pages (from-to)11-20
Number of pages10
JournalJournal of Dermatological Science
Volume46
Issue number1
DOIs
Publication statusPublished - Apr 2007

Fingerprint

Cytotoxicity
Liposomes
Cisplatin
Melanoma
Pharmaceutical Preparations
Tumors
phosphatidylethanolamine
In Vitro Techniques
Derivatives
Neoplasms
Zeta potential
Phosphatidylcholines
Confocal Microscopy
Ovum
Microscopic examination
Cell Proliferation
Tissue
Scanning

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 journalArticle

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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.

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