Nanoparticulate lipid dispersions for bromocriptine delivery: Characterization and in vivo study

被引：93

作者：

Esposito, Elisabetta ^{[1
]}

Mariani, Paolo ^{[2
]}

Ravani, Laura ^{[1
]}

Contado, Catia ^{[3
]}

Volta, Mattia ^{[4
]}

Bido, Simone ^{[4
]}

Drechsler, Markus ^{[5
]}

Mazzoni, Serena ^{[2
]}

Menegatti, Enea ^{[1
]}

Morari, Michele ^{[4
]}

Cortesi, Rita ^{[1
]}

机构：

[1] Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy

[2] Univ Politecn Marche, SAIFET Dept, Ancona, Italy

[3] Univ Ferrara, Dept Chem, I-44100 Ferrara, Italy

[4] Univ Ferrara, Dept Expt & Clin Med, I-44100 Ferrara, Italy

[5] Univ Bayreuth, Bayreuth, Germany

来源：

EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS | 2012年 / 80卷 / 02期

关键词：

Solid Lipid Nanoparticles (SLNs); Nanostructured Lipid Carrier (NLC); Bromocriptine (BC); X-ray; Drag test; Bar test; FIELD-FLOW FRACTIONATION; DRUG-DELIVERY; CUBIC PHASES; L-DOPA; PARTICLES; SYSTEMS; SLN; TRANSITIONS; SCATTERING; LIPOSOMES;

D O I：

10.1016/j.ejpb.2011.10.015

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The physico-chemical properties and in vivo efficacies of two nanoparticulate systems delivering the antiparkinsonian drug bromocriptine (BC) were compared in the present study. Monoolein Aqueous Dispersions (MADs) and Nanostructured Lipid Carriers (NLCs) were produced and characterized. Cryogenic transmission electron microscopy (cryo-TEM) and X-ray diffraction revealed the morphology of MAD and NLC. Dimensional distribution was determined by Photon Correlation Spectroscopy (PCS) and Sedimentation Field Flow Fractionation (SdFFF). In particular, BC was shown to be encapsulated with high entrapment efficiency both in MAD and in NLC, according to SdFFF combined with HPLC. Two behavioral tests specific for akinesia (bar test) or akinesia/bradykinesia (drag test) were used to compare the effects of the different BC formulations On motor disabilities in 6-hydroxydopamine hemilesioned rats in vivo, a model of Parkinson's disease. Both free BC and BC-NLC reduced the immobility time in the bar test and enhanced the number of steps in the drag test, although the effects of encapsulated BC were longer lasting (5 h). Conversely, BC-MAD was ineffective in the bar test and improved stepping activity in the drag test to a much lower degree than those achieved with the other preparations. We conclude that MAD and NLC can encapsulate BC, although only NLC provide long-lasting therapeutic effects possibly extending BC half-life in vivo. (C) 2011 Elsevier B.V. All rights reserved.

引用

页码：306 / 314

页数：9

共 51 条

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