Micellar delivery system for dequalinium - A lipophilic cationic drug with anticarcinoma activity

被引：38

作者：

Weissig, V ^{[1
]}

Lizano, C

Torchilin, VP

机构：

[1] Massachusetts Gen Hosp, Dept Radiol, Ctr Imaging Pharmaceut Res, Charlestown, MA 02129 USA

[2] Harvard Med Sch, Charlestown, MA 02129 USA

[3] Univ Alcala de Henares, Fac Med, Dept Biochem & Mol Biol, Madrid 28871, Spain

来源：

JOURNAL OF LIPOSOME RESEARCH | 1998年 / 8卷 / 03期

关键词：

micelles; liposomes; drug carriers; dequalinium; bolaamphiphiles;

D O I：

10.3109/08982109809035542

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Delocalized lipophilic cations (DLC) such as dequalinium (DQA) comprise a novel class of antitumor agents. They are more selectively toxic to carcinoma cells in comparison to non-transformed epithelial cells. In addition, DLC's have also been shown to enhance the efficacy of existing anticancer modalities such as radiation and photodynamic therapies. A severe drawback of these attractive novel anticancer agents is their limited solubility in aqueous solutions. To overcome this obstacle, we tried to incorporate DQA into liposomes and micelles. We found that incorporation in liposomes does not seem to be possible at physiological salt concentrations. However, we succeeded in preparing micelles made of polyethylene glycol derivatives of phosphatidylethanolamine (PEG-PE) which stably bind up to 30 mol % DQA.

引用

页码：391 / 400

页数：10

共 13 条

[1] WATERSOLUBLE POLYMERS IN MEDICINE [J].

BADER, H ;

RINGSDORF, H ;

SCHMIDT, B .

ANGEWANDTE MAKROMOLEKULARE CHEMIE, 1984, 123 (AUG) :457-485

[2] THE NEUROLEPTIC ACTIVITY OF HALOPERIDOL INCREASES AFTER ITS SOLUBILIZATION IN SURFACTANT MICELLES - MICELLES AS MICROCONTAINERS FOR DRUG TARGETING [J].

KABANOV, AV ;

CHEKHONIN, VP ;

ALAKHOV, VY ;

BATRAKOVA, EV ;

LEBEDEV, AS ;

MELIKNUBAROV, NS ;

ARZHAKOV, SA ;

LEVASHOV, AV ;

MOROZOV, GV ;

SEVERIN, ES ;

KABANOV, VA .

FEBS LETTERS, 1989, 258 (02) :343-345

[3] ANTIPROLIFERATIVE EFFECTS ON KERATINOCYTES OF A RANGE OF CLINICALLY USED DRUGS WITH CALMODULIN ANTAGONIST ACTIVITY [J].

MACNEIL, S ;

DAWSON, RA ;

CROCKER, G ;

TUCKER, WFG ;

BITTINER, B ;

SINGLETON, JG ;

HUNTER, T ;

TIERNEY, DF .

BRITISH JOURNAL OF DERMATOLOGY, 1993, 128 (02) :143-150

[4] INTRAMITOCHONDRIAL DYES ALLOW SELECTIVE INVITRO PHOTOLYSIS OF CARCINOMA-CELLS [J].

OSEROFF, AR ;

OHUOHA, D ;

ARA, G ;

MCAULIFFE, D ;

FOLEY, J ;

CINCOTTA, L .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1986, 83 (24) :9729-9733

[5]

RINGSDORF H, 1975, J POLYM SCI POL SYM, P135

[6]

SUN XC, 1994, CANCER RES, V54, P1465

[7] INTRACELLULAR-DISTRIBUTION OF A PLATINUM-RHODAMINE 123 COMPLEX IN CISPLATINUM SENSITIVE AND RESISTANT HUMAN SQUAMOUS CARCINOMA CELL-LINES [J].

TEICHER, BA ;

HOLDEN, SA ;

JACOBS, JL ;

ABRAMS, MJ ;

JONES, AG .

BIOCHEMICAL PHARMACOLOGY, 1986, 35 (19) :3365-3369

[8] USE OF POLYOXYETHYLENE-LIPID CONJUGATES AS LONG-CIRCULATING CARRIERS FOR DELIVERY OF THERAPEUTIC AND DIAGNOSTIC AGENTS [J].

TRUBETSKOY, VS ;

TORCHILIN, VP .

ADVANCED DRUG DELIVERY REVIEWS, 1995, 16 (2-3) :311-320

[9] DEQUALINIUM, A TOPICAL ANTIMICROBIAL AGENT, DISPLAYS ANTICARCINOMA ACTIVITY BASED ON SELECTIVE MITOCHONDRIAL ACCUMULATION [J].

WEISS, MJ ;

WONG, JR ;

HA, CS ;

BLEDAY, R ;

SALEM, RR ;

STEELE, GD ;

CHEN, LB .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1987, 84 (15) :5444-5448

[10] DQAsomes:: A novel potential drug and gene delivery system made from Dequalinium™ [J].

Weissig, V ;

Lasch, J ;

Erdos, G ;

Meyer, HW ;

Rowe, TC ;

Hughes, J .

PHARMACEUTICAL RESEARCH, 1998, 15 (02) :334-337

← 1 2 →