INVITRO AND INVIVO ANTITUMORAL ACTIVITY OF FREE, AND ENCAPSULATED TAXOL

被引：64

作者：

BARTOLI, MH

BOITARD, M

FESSI, H

BERIEL, H

DEVISSAGUET, JP

PICOT, F

PUISIEUX, F

机构：

[1] UFR de Pharmacie, Domaine de la Merci, 38700, La Tranche

[2] UA CNRS 1218, Centre d'Etudes Pharmaceutiques, 92296, Chatenay-Malabry Cédex, 5, Rue J. B. Clément

[3] CNRS, Institut de Chimie des Substances Naturelles

来源：

JOURNAL OF MICROENCAPSULATION | 1990年 / 7卷 / 02期

关键词：

D O I：

10.3109/02652049009021832

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

The anti-tumoral activity of taxol encapsulated either in liposomes or in nanocapsules was compared with that of free taxol, using the P388 and L1210 leukaemia test systems. The in vitro inhibition of cell growth was measured after 48 h and 96 h exposure to various concentrations of taxol. With P388 cells, the inhibitory activities of the three forms of the drug were similar. With the L1210 cells, however, the concentrations required for a 50 per cent inhibition of cell growth (IC50) after 48 h exposure to the drug were greater for nanocapsules than for liposomes or free taxol, the values being 0·060, 0·043 and 0·035 μg ml-1, respectively. However, a greater efficiency of nanocapsules was observed after 96 h exposure. Using cytomorphometric analysis, no difference was found between L1210 cells treated either with free or encapsulated taxol. In vivo, mice bearing P388 leukaemia, and treated either with taxol solubilized with 5 per cent DMSO+5 per cent cremophor in saline solution, or with taxol encapsulated in liposomes (IP daily dose of 12·5 mg Kg-1 body weight · 4 days) showed ILS values of 65·8% and 67·9% respectively. Nanocapsules proved to be toxic, apparently due to their composition: this problem is currently under investigation. © 1990 Informa UK Ltd All rights reserved: reproduction in whole or part not permitted.

引用

页码：191 / 197

页数：7

共 10 条

[1] Brugal G., Chassery J.M., Un nouveau système d'analyse densitométrique et morphologique des préparations microscopiques. Application à la reconnaissance et au comptage automatique des cellules dans les différentes phases du cycle mitotique, Histochemistry, 52, pp. 241-248, (1977)
[2] Chauviere G., Guenard D., Picot F., Senilh V., Potier P., Analyse structurale et étude biochimique de produits isolés de l'If Taxus baccata L. (Taxacées), Comptes Rendus de l'Academie des Sciences, I, 293, pp. 501-503, (1981)
[3] Fessi H., Devissaguet J.P., Puisieux F., French patent, (1988)
[4] Jacrot M., Riondel J., Picot F., Leroux D., Mouriquand C., Beriel H., Potier P., Action du taxol vis à vis de tumeurs humaines transplantées sur souris athymiques, Comptes Rendus de l'Académie des Sciences, III, 297, pp. 597-600, (1983)
[5] Laham A., Clapeton N., Dubussel J.J., Fattal E., Delattre J., Puisieux F., Couvreur P., Rossignol P., Liposomally entrapped A.T.P. improved efficiency against experimental brain ischemia in rat, Life Sciences, 40, pp. 2011-2016, (1987)
[6] Riondel J., Jacrot M., Picot F., Beriel H., Mouriquand C., Potier P., Therapeutic response to taxol of six human xenografted into nude mice, Cancer Chemotherapy and Pharmacology, 17, pp. 137-142, (1986)
[7] Riondel J., Jacrot M., Nissou M.F., Picot F., Beriel H., Mouriquand C., Potier P., Antineoplastic activity of two taxol derivatives on an ovarian tumor xenografted into nude mice, Anticancer Research, 8, pp. 387-390, (1988)
[8] Seigneurin D., Cytologie quantitative de la maturation granulocytaire dans la moelle normale et au cours des syndromes myélodysplasiques, (1987)
[9] Senilh V., Blechert S., Colin M., Guenard D., Picot F., Potier P., Varenne P., Mise en évidence de nouveaux analogues du taxol extraits de Taxus baccata, Journal of Natural Products, 47, pp. 134-137, (1984)
[10] Wiernick P.H., Schwartz E.L., Straiman J.J., Dutcher J.P., Lipton R.B., Paietta E., Phase I clinical and pharmacokinetic study of taxol, Cancer Research, 47, pp. 2486-2493, (1987)

← 1 →