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Master Thesis

Administration par voie intranasale d’un principe actif hydrophile d’intérêt thérapeutique potentiel pour le traitement de la maladie d’Alzheimer

Abstract : This study aimed at preparing and characterizing thermosensitive gel formulations based on a mixture of two hydrophilic polymers (Poloxamer 407 and 188) for a sustained delivery via liposomes of an active pharmaceutical ingredient (API) of potential interest for Alzheimer’s disease through nasal route. API was characterized as being a selective inhibitor of butyrylcholinesterase but presents a low permeability through brain blood barrier model. The osmolarity and the gelation temperature (T°sol-gel) of formulations, defined in a ternary diagram, were investigated by rheometry and visual determination. At the issue of assays, a mixture composed of p407/p188 (15/1 %, w/w) was selected, being compatible with intranasal administration in terms of (T°sol-gel = 34,5°c ± 0,3) and with the olfactory mucosal (280 ± 20 mOsmol, pH 6). Liposomes of API were prepared by the thin film hydration method. various parameters such as lipid ratio, concentration and lipid to drug ratio were investigated to obtain acceptable entrapment efficiency (EE). Formulations were evaluated for vesicle size granulometry, zeta potential, and EE determined after purification. Mucoadhesion studies were performed, and showed that in situ gel formulations present good natural mucoadhesive characteristics, that could be increased with liposomes. Drug release studies showed the API was successfully and completely released with a controlled rate, and slower than with API-loaded solutions or gels. The study demonstrated successful formulation of a promising API-loaded liposomes in a thermosensitive hydrogel for nasal delivery.
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Master Thesis
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https://dumas.ccsd.cnrs.fr/dumas-02433553
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  • HAL Id : dumas-02433553, version 1

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Thomas Adnet. Administration par voie intranasale d’un principe actif hydrophile d’intérêt thérapeutique potentiel pour le traitement de la maladie d’Alzheimer. Sciences pharmaceutiques. 2019. ⟨dumas-02433553⟩

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