Preparation and evaluation of a novel liposomal formulation of cisplatin

Xiaoju Zhou; Jiong Wang; Jianhong Wu; Xiaojuan Yang; Bryant C. Yung; L. James Lee; Robert J. Lee

doi:10.1016/j.ejps.2014.10.004

Preparation and evaluation of a novel liposomal formulation of cisplatin

Xiaoju Zhou, Jiong Wang, Jianhong Wu, Xiaojuan Yang, Bryant C. Yung, L. James Lee, Robert J. Lee^*

^*Corresponding author for this work

Institute of Biopharmaceutical Sciences

Research output: Contribution to journal › Article › peer-review

20 Scopus citations

Abstract

A novel liposomal formulation of cisplatin (L-CDDP) was synthesized and characterized. The L-CDDP was formed by conjugating CDDP to the carboxyl of oleic acid incorporated into empty liposomes. Particle size (155.4 ± 16.1 nm) and zeta potential (-50.92 ± 1.19 mV) of the L-CDDP were determined. In addition, pharmacokinetic properties and antitumor activity in vitro and in vivo were evaluated. Pharmacokinetic study demonstrated that L-CDDP had markedly prolonged circulation time relative to the free drug. Furthermore, L-CDDP showed significantly enhanced in vitro cytotoxicity in comparison to free CDDP. A549-engrafted mice treated with L-CDDP had a higher survival rate compared to those treated with free CDDP. Finally, A549-engrafted mice treated with L-CDDP showed no significant loss of body weight, whereas free CDDP treatment at the same dose caused significant loss of body weight. These results suggest further evaluation of the in vivo antitumor efficacy of the novel L-CDDP formulation is warranted.

Original language	English
Pages (from-to)	90-95
Number of pages	6
Journal	European Journal of Pharmaceutical Sciences
Volume	66
DOIs	https://doi.org/10.1016/j.ejps.2014.10.004
State	Published - 23 Jan 2015

Keywords

Antitumor activity
Cisplatin
Liposomes
Oleic acid
Pharmacokinetics

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10.1016/j.ejps.2014.10.004

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title = "Preparation and evaluation of a novel liposomal formulation of cisplatin",

abstract = "A novel liposomal formulation of cisplatin (L-CDDP) was synthesized and characterized. The L-CDDP was formed by conjugating CDDP to the carboxyl of oleic acid incorporated into empty liposomes. Particle size (155.4 ± 16.1 nm) and zeta potential (-50.92 ± 1.19 mV) of the L-CDDP were determined. In addition, pharmacokinetic properties and antitumor activity in vitro and in vivo were evaluated. Pharmacokinetic study demonstrated that L-CDDP had markedly prolonged circulation time relative to the free drug. Furthermore, L-CDDP showed significantly enhanced in vitro cytotoxicity in comparison to free CDDP. A549-engrafted mice treated with L-CDDP had a higher survival rate compared to those treated with free CDDP. Finally, A549-engrafted mice treated with L-CDDP showed no significant loss of body weight, whereas free CDDP treatment at the same dose caused significant loss of body weight. These results suggest further evaluation of the in vivo antitumor efficacy of the novel L-CDDP formulation is warranted.",

keywords = "Antitumor activity, Cisplatin, Liposomes, Oleic acid, Pharmacokinetics",

author = "Xiaoju Zhou and Jiong Wang and Jianhong Wu and Xiaojuan Yang and Yung, {Bryant C.} and Lee, {L. James} and Lee, {Robert J.}",

year = "2015",

month = jan,

day = "23",

doi = "10.1016/j.ejps.2014.10.004",

language = "English",

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pages = "90--95",

journal = "European Journal of Pharmaceutical Sciences",

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T1 - Preparation and evaluation of a novel liposomal formulation of cisplatin

AU - Zhou, Xiaoju

AU - Wang, Jiong

AU - Wu, Jianhong

AU - Yang, Xiaojuan

AU - Yung, Bryant C.

AU - Lee, L. James

AU - Lee, Robert J.

PY - 2015/1/23

Y1 - 2015/1/23

N2 - A novel liposomal formulation of cisplatin (L-CDDP) was synthesized and characterized. The L-CDDP was formed by conjugating CDDP to the carboxyl of oleic acid incorporated into empty liposomes. Particle size (155.4 ± 16.1 nm) and zeta potential (-50.92 ± 1.19 mV) of the L-CDDP were determined. In addition, pharmacokinetic properties and antitumor activity in vitro and in vivo were evaluated. Pharmacokinetic study demonstrated that L-CDDP had markedly prolonged circulation time relative to the free drug. Furthermore, L-CDDP showed significantly enhanced in vitro cytotoxicity in comparison to free CDDP. A549-engrafted mice treated with L-CDDP had a higher survival rate compared to those treated with free CDDP. Finally, A549-engrafted mice treated with L-CDDP showed no significant loss of body weight, whereas free CDDP treatment at the same dose caused significant loss of body weight. These results suggest further evaluation of the in vivo antitumor efficacy of the novel L-CDDP formulation is warranted.

AB - A novel liposomal formulation of cisplatin (L-CDDP) was synthesized and characterized. The L-CDDP was formed by conjugating CDDP to the carboxyl of oleic acid incorporated into empty liposomes. Particle size (155.4 ± 16.1 nm) and zeta potential (-50.92 ± 1.19 mV) of the L-CDDP were determined. In addition, pharmacokinetic properties and antitumor activity in vitro and in vivo were evaluated. Pharmacokinetic study demonstrated that L-CDDP had markedly prolonged circulation time relative to the free drug. Furthermore, L-CDDP showed significantly enhanced in vitro cytotoxicity in comparison to free CDDP. A549-engrafted mice treated with L-CDDP had a higher survival rate compared to those treated with free CDDP. Finally, A549-engrafted mice treated with L-CDDP showed no significant loss of body weight, whereas free CDDP treatment at the same dose caused significant loss of body weight. These results suggest further evaluation of the in vivo antitumor efficacy of the novel L-CDDP formulation is warranted.

KW - Antitumor activity

KW - Cisplatin

KW - Liposomes

KW - Oleic acid

KW - Pharmacokinetics

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DO - 10.1016/j.ejps.2014.10.004

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SN - 0928-0987

VL - 66

SP - 90

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JO - European Journal of Pharmaceutical Sciences

JF - European Journal of Pharmaceutical Sciences

ER -

Preparation and evaluation of a novel liposomal formulation of cisplatin

Abstract

Keywords

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