جستجوی مقالات مرتبط با کلیدواژه « statistical optimization » در نشریات گروه « پزشکی »

The present study focuses on a systemic approach to develop liposomal aztreonam as a promising dosage form for inhalation therapy in the treatment of pneumonia and explores the in-vitro antimicrobial and cell uptake efficacy.

Liposomes were prepared by ethanol injection method using the lipids - soya phosphatidylcholine (SP) and cholesterol (CH). A central composite design (CCD) was employed to optimize the lipid composition to evaluate the effect on vesicle size, zeta potential and entrapment efficiency of the formulation. A numerical and graphical optimization was carried out to predict the optimized blend. The optimized formulation was characterized for vesicle size, surface charge, encapsulation, surface morphology, differential scanning calorimetry (DSC), powder X Ray Diffraction (PXRD), thermogravimetric analysis (TGA), in vitro diffusion, accelerated stability studies, antimicrobial studies on Pseudomonas aeruginosa NCIM 2200 and in vitro cell uptake studies.

The optimized formulation was found to have a particle size of 144 nm, a surface charge of -35 mV, with satisfactory drug entrapment. The surface morphology study proved the formation of nanosized vesicles. The drug release from liposomal matrix was biphasic in nature. The solid-state study revealed the reason for good encapsulation of drug. The moisture retention capacity was found to be minimum. The anti-microbial study revealed the potential antibacterial activity of the optimized formulation over the pure drug. The formulation was found to be safe on the epithelial cells and showed a marked increase in cellular uptake of aztreonam in a lipid carrier.

It can be concluded that the optimized liposomal aztreonam could be considered as a promising approach for the delivery of aztreonam through inhalation.

Self-nanoemulsifying drug delivery systems (SNEDDS) can be used to improve the oral bioavailability of lipophilic drugs. The aim of this study was the preparation and characterization of a SNEDDS for the oral delivery of budesonide as a poorly soluble drug.

To prepare SNEDDS, budesonide (20 mg) was dissolved in the mixture of liquid paraffin, Tween 80, and propylene glycol, followed by using the Box-Behnken response surface methodology for statistical optimization. The prepared mixtures were then diluted in the simulated intestinal fluid (SIF) and their physico-chemical characteristics were studied as well. Then, SNEDDS were morphologically evaluated using transmission electron microscopy (TEM). Finally, the in vitro release profile of budesonide from nano-droplets was determined in the SIF.

Based on the results, the size, polydispersity index, zeta potential, and entrapment efficiency of statistically optimized SNEEDS were reported as 146±37 nm, 0.211±0.06, +3.6±0.84 mV, and 94.3±6.58%, respectively. In addition, TEM images revealed spherical nano-droplets. Further, the release profile of budesonide from nano-droplets exhibited 33.81±1.67% of drug release in SIF during 360 minutes of incubation at 37° C, indicating sustained drug release.

The obtained data demonstrated that SNEDDS could be regarded as a good candidate for oral delivery of budesonide as a poorly water-soluble drug representing a high first-pass metabolism.