Preparation and characterization of propranolol hydrochloride nanoparticles: a comparative study

被引:83
作者
Ubrich, N
Bouillot, P
Pellerin, C
Hoffman, M
Maincent, P
机构
[1] Fac Pharm Nancy, Pharm Galen Lab, F-54001 Nancy, France
[2] Pfizer Ltd, Sandwich CT13 9NJ, Kent, England
[3] Fac Pharm Nancy, Lab Hematol & Physiol, F-54001 Nancy, France
关键词
nanoparticle; w/o/w emulsion; hydrophilic drug; low molecular weight drug; propranolol hydrochloride;
D O I
10.1016/j.jconrel.2004.03.023
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
The water-in-oil-in-water (w/o/w) emulsification process is the method of choice for the encapsulation inside polymeric particles of hydrophilic drugs such as proteins and peptides which are high molecular weight macromolecules. Our objective was to apply this technique in order to formulate nanoparticles loaded with both a hydrophilic and a low molecular weight drug such as propranolol-HCl. Nanoparticles were prepared using a pressure homogenization device with various polymers (poly-epsilon-caprolactone, poly(lactide-co-glycolide), ethylcellulose) and different amounts of drug and were compared in terns of particle size, encapsulation efficiency and drag release. Higher encapsulation efficiencies were obtained with both PCL (77.3%) and PLGA (83.3%) compared to ethylcellulose (66.8%). The in vitro drug release was characterized by an initial burst and an incomplete dissolution of the drug. When decreasing the polymer/drug ratio, the release appeared more controlled and prolonged up to 8 h. It can be concluded that nanoparticles prepared by w/o/w emulsification followed by solvent evaporation might be potential drug carriers for low molecular weight and hydrophilic drugs. (C) 2004 Elsevier B.V. All rights reserved.
引用
收藏
页码:291 / 300
页数:10
相关论文
共 31 条
[1]   THE MOLECULAR-BASIS OF MOISTURE EFFECTS ON THE PHYSICAL AND CHEMICAL-STABILITY OF DRUGS IN THE SOLID-STATE [J].
AHLNECK, C ;
ZOGRAFI, G .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1990, 62 (2-3) :87-95
[2]   ENCAPSULATION OF WATER-SOLUBLE DRUGS BY A MODIFIED SOLVENT EVAPORATION METHOD .1. EFFECT OF PROCESS AND FORMULATION VARIABLES ON DRUG ENTRAPMENT [J].
ALEX, R ;
BODMEIER, R .
JOURNAL OF MICROENCAPSULATION, 1990, 7 (03) :347-355
[3]   DISTRIBUTION, KINETICS AND ELIMINATION OF RADIOACTIVITY AFTER INTRAVENOUS AND INTRAMUSCULAR INJECTION OF C-14 SAVOXEPINE LOADED POLY(D,L-LACTIC ACID) NANOSPHERES TO RATS [J].
ALLEMANN, E ;
GURNY, R ;
DOELKER, E ;
SKINNER, FS ;
SCHUTZ, H .
JOURNAL OF CONTROLLED RELEASE, 1994, 29 (1-2) :97-104
[4]   Development and characterization of protein-loaded poly(lactide-co-glycolide) nanospheres [J].
Blanco, MD ;
Alonso, MJ .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 1997, 43 (03) :287-294
[5]   PREPARATION AND CHARACTERIZATION OF MICROOSPHERES CONTAINING THE ANTI-INFLAMMATORY AGENTS, INDOMETHACIN, IBUPROFEN, AND KETOPROFEN [J].
BODMEIER, R ;
CHEN, H .
JOURNAL OF CONTROLLED RELEASE, 1989, 10 (02) :167-175
[6]   A poly(D,L-lactide-co-glycolide) microsphere depot system for delivery of haloperidol [J].
Cheng, YH ;
Illum, L ;
Davis, SS .
JOURNAL OF CONTROLLED RELEASE, 1998, 55 (2-3) :203-212
[7]   Effect of the type of hydrophobic polymers on the size of nanoparticles obtained by emulsification-solvent evaporation [J].
Chernysheva, YV ;
Babak, VG ;
Kildeeva, NR ;
Boury, F ;
Benoit, JP ;
Ubrich, N ;
Maincent, P .
MENDELEEV COMMUNICATIONS, 2003, (02) :65-68
[8]   NEW APPROACH FOR ORAL-ADMINISTRATION OF INSULIN WITH POLYALKYLCYANOACRYLATE NANOCAPSULES AS DRUG CARRIER [J].
DAMGE, C ;
MICHEL, C ;
APRAHAMIAN, M ;
COUVREUR, P .
DIABETES, 1988, 37 (02) :246-251
[9]   Specific interaction of lectins with liposomes and monolayers bearing neoglycolipids [J].
Faivre, V ;
Costa, MDL ;
Boullanger, P ;
Baszkin, A ;
Rosilio, V .
CHEMISTRY AND PHYSICS OF LIPIDS, 2003, 125 (02) :147-159
[10]   NANOCAPSULE FORMATION BY INTERFACIAL POLYMER DEPOSITION FOLLOWING SOLVENT DISPLACEMENT [J].
FESSI, H ;
PUISIEUX, F ;
DEVISSAGUET, JP ;
AMMOURY, N ;
BENITA, S .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1989, 55 (01) :R1-R4