Realization of polyaspartamide-based nanoparticles and in vivo lung biodistribution evaluation of a loaded glucocorticoid after aerosolization in mice.

Gaetano Giammona, Gennara Cavallaro, Emanuela Fabiola Craparo, Belgiovine, Di Gioia, Conese, Cellamare, Giammona, Trapani, Mandracchia

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Abstract

In this study, novel polymeric nanoparticles (NPs) were developed and their potential as carriers forbeclomethasone dipropionate (BDP) into the lung after aerosolization was demonstrated by in vivostudies in mice. In particular, these NPs were obtained starting from two polyaspartamide-basedcopolymers which were synthesized by chemical reaction of a,b-poly(N-2-hydroxyethyl)-DL-aspartamide(PHEA) and its pegylated derivative (PHEA-PEG2000) with poly(lactic acid) (PLA). To obtainnanosized particles, the high pressure homogenization (HPH)—solvent evaporation method wasfollowed by using an organic phase containing both PHEA-PLA and PHEA-PEG2000-PLA (at a weight ratioequal to 1:1), lactose as cryoprotectant and no surfactant was adopted. PHEA-PLA/PHEA-PEG2000-PLA NPswere characterized by a quite spherical shape, z potential slightly negative, and size lower than 50 and200 nm, respectively, for empty and BDP-loaded NPs. In vivo biodistribution of BDP and its metabolites invarious lung compartments, i.e. bronchoalveolar lavagefluid (BALF), alveolar macrophages (MPG)obtained from BALF, and lung tissue, was carried out at 3 h post-administration in mice by aerosolizationof BDP-loaded NPs or free BDP (commercial formulation, Clenil1) at the dose of 0.5 mg/kg BDP. Resultsdemonstrated that BDP entrapped into NPs reached all analyzed lung compartments and wereinternalized by both alveolar MPG and respiratory epithelial cells, and detected amounts werecomparable to those of Clenil-treated mice. Moreover, the entrapment into NPs protects the drug fromthe enzymatic hydrolysis, allowing a significant lower amount of beclomethasone (BOH) into the lungtissue and BALF than that obtained after Clenil administratio
Lingua originaleEnglish
pagine (da-a)263-270
Numero di pagine8
RivistaInternational Journal of Pharmaceutics
Volume510
Stato di pubblicazionePublished - 2016

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

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