ABSTRACT
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.
Subject(s)
Acute Lung Injury/metabolism , Anti-Inflammatory Agents/chemistry , Beclomethasone/chemistry , Nanocapsules/chemistry , 3T3 Cells , Administration, Inhalation , Animals , Anti-Inflammatory Agents/administration & dosage , Anti-Inflammatory Agents/pharmacokinetics , Anti-Inflammatory Agents/pharmacology , Beclomethasone/administration & dosage , Beclomethasone/pharmacokinetics , Beclomethasone/pharmacology , Bronchoalveolar Lavage Fluid/chemistry , Cell Survival/drug effects , Drug Stability , Male , Mice , Nanocapsules/toxicity , Polyesters/chemistry , Rats , Rats, WistarABSTRACT
The objective of this study was to evaluate the effects of the ethanolic crude extracts and fractions of the species Senecio westermanii Dusén on Lactuca sativa L. (lettuce) and Allium cepa L. (onion) seeds. We assessed the germination, growth, root respiration and photosynthesis of the target species in Petri dishes (9.0 cm diameter) containing filter paper n°6. The study was conducted using 50 seeds per plate and held in 4 replicates per concentration of each sample. In the germination there was an inhibitory effect of fractions hexane (FH) and chloroform (FCl) at concentrations of 500 and 1000 µg/mL. There was a reduction in the radicle growth of lettuce by 14 to 24% and a reduction of hypocotilum by 14 to 28%. As for the radicle of the onion was up 74% reduction to the FCl and the coleoptile was 24 and 45% reduction for FH and FCl, respectively. Inhibitory effects in the root respiration of lettuce were detected in all the samples analyzed, with results ranging from 16 to 83%. For the seeds of A. cepa, there was an encouragement for the FCl and ethyl acetate fractions (FAE), with results ranging from 94 to 142% and 76 to 150%, respectively. With regard to the photosynthesis of L. sativa, there was no significant difference between the control, and as for the A. cepa, there was a strain in inhibition concentrations of 250 and 500 µg/mL, which ranged from 27 to 68%. The samples of S. westermanii caused changes in the target species and thus can be used as a natural herbicide.