Beclomethasone Dipropionate-Loaded Polymeric Nanocapsules: Development, In Vitro Cytotoxicity, and In Vivo Evaluation of Acute Lung Injury.
The aim of this work was to develop polymeric nanocapsules intended for the pulmonary delivery of beclomethasone dipropionate using ethyl cellulose or poly(ε-caprolactone). The formulations showed adequate physicochemical characteristics, namely, average diameter lower than 260 nm, low polydispersity index (< 0.2), negative zeta potential, neutral pH values, and encapsulation efficiencies close to 100%. The thermal analysis by DSC suggested that beclomethasone dipropionate encapsulated in the nanocapsules was in an amorphous state. In addition, both ethyl cellulose and poly(ε-caprolactone) nanocapsules were able to delay the drug photodegradation under UVC radiation. The in vitro drug release showed a prolonged release without burst effect using the dialysis bag diffusion technique. Moreover, ethyl cellulose and poly(ε-caprolactone) nanocapsules presented low in vitro cytotoxicity on 3T3 fibroblasts cells. In vivo, the formulations showed no acute pulmonary injury in rats. Therefore, the developed nanocapsules could be considered suitable carriers to be used for beclomethasone dipropionate pulmonary delivery.
Janaíne Micheli
JM
Chassot
Daniele
D
Ribas
Elita Ferreira
EF
Silveira
Lauren Dockhorn
LD
Grünspan
Camila Cervi
CC
Pires
Paulo Vitor
PV
Farago
Elizandra
E
Braganhol
Leandro
L
Tasso
Letícia
L
Cruz
D016475:3T3 Cells; D055371:Acute Lung Injury / Q000378:metabolism*; D000280:Administration, Inhalation; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D001507:Beclomethasone / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D001992:Bronchoalveolar Lavage Fluid / Q000737:chemistry; D002470:Cell Survival / Q000187:drug effects; D004355:Drug Stability; D008297:Male; D051379:Mice; D053769:Nanocapsules / Q000737:chemistry* / Q000633:toxicity; D011091:Polyesters / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar
D000893:Anti-Inflammatory Agents; D053769:Nanocapsules; D011091:Polyesters; C016240:polycaprolactone; D001507:Beclomethasone