Delivery of theophylline as dry powder for inhalation

Theophylline(TP)is a very well established orally or intravenously delivered antiasthma drug with many beneficial effects.This study aims to improve asthma treatment by creating a dry powder inhalable(DPI)formulation of TP to be delivered directly to the lung,avoiding the side effects associated with conventional oral delivery.The DPI TP formulation was investigated for its physico-chemical characteristics using scanning electron microscopy,laser diffraction,thermal analysis and dynamic vapour sorption.Furthermore,aerosol performance was assessed using the Multi Stage Liquid Impinger(MSLI).In addition,a Calu-3 cell transport assay was conducted in vitro using a modified ACI to study the impact of the DPI formulation on lung epithelial cells.Results showed DPI TP to be physico-chemically stable and of an aerodynamic size suitable for lung delivery.The aerosolisation performance analysis showed the TP DPI formulation to have a fine particle fraction of 29.70±2.59%(P<0.05)for the TP formulation containing 1.0%(w/w)sodium stearate,the most efficient for aerosolisation.Regarding the deposition of TP DPI on Calu-3 cells using the modified ACI,results demonstrated that 56.14±7.62%of the total TP deposited(13.07±1.69μg)was transported across the Calu-3 monolayer over 180 min following deposition,while 37.05±12.62%of the deposited TP was retained in the cells.This could be due to the presence of sodium stearate in the current formulation that increased its lipophilicity.A DPI formulation of TP was developed that was shown to be suitable for inhalation.

Effects of fruit bagging on the physiochemical changes of grapefruit(Citrus paradisi)

Fruit bagging is a commonly used cultivation measure to protect citrus fruit from insects and adverse environments.The present study aimed to comprehensively investigate the effects of bagging on the physiochemical characteristics of grapefruit.The grapefruit were bagged at approximately 110–120 d after anthesis with a one-layer kraft paper bag with black coating inside(SL),a double-layer kraft paper bag with one black paper as the inner layer(DL),and a three-layer kraft paper bag with two black papers as inner layers(TL),respectively.Ultra performance liquid chromatography-high resolution mass spectrometry(UPLC-HRMS)technique was used to identify a total of 19 flavonoids,2 phenylpropanoids,9 coumarins,and 5 limonoids.By using UPLC,50 carotenoids were identified.Gas chromatography–mass spectrometry was used to identify 3 soluble sugars,3 organic acids,and 11 amino acids.In the quantitated components in the peel(albedo and flavedo),the chlorophylls and the carotenoids components(such as luteoxanthin,violaxanthin,9-cis-violaxanthin,xanthophyll,zeaxanthin andβ-carotene)were significantly downregulated by bagging,causing the surface color of bagged fruit to turn yellow earlier but paler than that of the unbagged control,particularly in the three-layer kraft bag treatment.Unlike the peel,the color and the carotenoid content of the juice sacs were less affected.The physiochem-ical compounds other than pigments,including soluble sugars,organic acids,amino acids,flavonoids,coumarins and limonoids,were minimally affected by bagging treatments.Our results indicated that bagging at approximately 110–120 d after anthesis exerted influence mainly on peel color,but less on sugars,acids,amino acids,flavonoids,limonoids and coumarins of grapefruit.