"2nd Conference on

Innovation in Drug Delivery: From Preformulation to Development through Innovative

Evaluation Process"

3-6 October, 2010

Palais des Congrès, Aix-en-Provence - France

Abstract Reproduction Form

Deadline: 1 May, 2010

(To aid completion of the Abstract Form please refer to the instructions)

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INSTRUCTIONS FOR SUBMISSION
Format of Abstract: One page, Font: Times New Roman, size 14, margin: Top= 3.2 cm, Bottom= 4.3 cm, Left=
3.5 cm, Right= 3.5 cm
a. The Abstract should be limited to the following sections:
 Purpose
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 Results
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TYPING INSTRUCTIONS
a. The abstract must be clearly typed in ENGLISH
b. The abstract form, when completed, should be sent by email or disk to the address
APGI 5 Rue Jean Baptiste Clément, FR-92296 Châtenay-Malabry Cedex ,
France
E-mail: apgi.asso@u-psud.fr Return completed abstract form by 1 May, 2010
COMBINED POLY (ALKYL CYANOACRYLATE)/
CYCLODEXTRIN NANOPARTICLES

Dominique Duchêne, Gilles Ponchel

UMR CNRS 8612, Faculty of Pharmacy, Paris-Sud University,
Châtenay Malabry, France
E-mail: dominique.duchene@cep.u-psud.fr

Purpose: To investigate the effect of cyclodextrins on the feasibility,

in aqueous medium, of biodegradable poly(alkyl cyanoacrylate)
nanoparticles loaded with water insoluble or poorly soluble drugs,
intended for oral or parenteral administration.
Methods: Nanoparticles are prepared by anionic emulsion
polymerisation of alkyl cyanoacrylate in the presence of poloxamer
188 and a cyclodextrin (α, β, γ-cyclodextrin, their hydroxypropyl
derivatives, or β-cyclodextrin sulfobutyl ether) or an inclusion
compound of a drug in a cyclodextrin (steroids or saquinavir).
Results: The smallest and best monodispersed blank nanoparticules
are obtained with hydroxypropyl β or γ-cyclodextrin. The loading
capacity of the steroids undergoes a 5 to 130-fold increase in the
presence of a cyclodextrin. The drug is either molecularly dispersed or
in amorphous state in the nanoparticules. Its release is very fast up to a
plateau depending on the particle size and the nature of the medium.
The presence of esterases in the medium allows a complete release of
the drug. The cytotoxicity of polyalkyl cyanoacrylate nanoparticules
on Caco-2 cells is decreased in the presence of cyclodextrins.
Conclusions: The role of hydroxypropyl cyclodextrins in the
formulation of poly(alkyl cyanoacrylate) nanoparticules is favourable
on the drug loading, and its prolonged release, furthermore, they
decrease and the polymer toxicity. By their hydroxyl groups and
possible slight ionisation, they could contribute to the polymerisation
process. Their high concentration at the nanoparticle surface suggests
their role in the steric stabilisation of particles. The drug loading
increase could be the consequence of adsorption of free or included
drug at the particle surface and of the encapsulation of either the
drug/cyclodextrin inclusion compound or drug molecules provided by
dissociation of the inclusion compound and entrapment of the drug as
a function of its partition coefficient between the preparation medium
and the polymer.