Evaluating the effect of sodium alginate and sodium carboxymethylcellulose on pulmonary delivery of levofloxacin spray-dried microparticles.

Background: Patients with cystic fibrosis commonly suffer from lung infections caused by Pseudomonas aeruginosa. Recently, the Levofloxacin (LVF) nebulizing solution (Quinsair®) has been prescribed for the antimicrobial management. The sustained-release (SR) dry powder formulation of LVF is a convenient alternative to Quinsair®.

Preparation, Optimization and Characterization of Fluticasoneloaded Mixed Micelles Based on Stearic Acid-g-chitosan as a Pulmonary Delivery System.

Purpose: The primary objective of this study was to optimize formulation variables and investigate the characteristics of fluticasone propionate (FP)-loaded mixed polymeric micelles, which were composed of depolymerized chitosan-stearic acid copolymer (DC-SA) in combination with either tocopheryl polyethylene glycol succinate or dipalmitoylphosphatidylcholine for pulmonary drug delivery.

Methods: A D-optimal design was employed for the optimization procedure, considering lipid/ polymer ratio, polymer concentration, drug/ polymer ratio, and lipid type as independent variables. Dependent variables included particle size, polydispersion index, zeta potential, drug encapsulation efficiency, and loading efficiency of the polymeric micelles.

Engineering of levodopa inhalable microparticles in combination with leucine and dipalmitoylphosphatidylcholine by spray drying technique.

The aim of this work was to study the effect of concomitant use of leucine and dipalmitoylphosphatidylcholine, in different ratios, on aerosolization performance of levodopa. Three-component formulations were selected based on a central composite design using percentages of leucine and dipalmitoylphosphatidylcholine as the independent variables. Particle size, surface roughness index, surface phosphorus and fine particle fraction were considered as dependent variables in the model.

Preparation and evaluation of vancomycin spray-dried powders for pulmonary delivery.

The aim of the current study was to achieve a dry powder formulation of vancomycin by spray drying whilst evaluating the effect of pH and excipient type and percentage used in formulation on particle characteristics and aerosolization performance. A D-optimal design was applied to optimize the formulation comprising vancomycin and two main excipient groups; a carbohydrate bulking agent (lactose, mannitol or trehalose) and a second excipient (hydroxypropyl beta-cyclodextrin or L-leucine) at pH 4 and 7. The physicochemical properties of particles (size, morphology, crystallinity state, residual moisture content), stability, and aerosolization characteristics were investigated.

The effect of metal salts on aerosol performance of spray dried carrier-free formulations of levofloxacin.

Purpose: Metal salts are used in formulation of dry powder inhalers (DPIs) for different purposes. Recently the role of these salts in production of small, dense but highly dispersible particles has emerged. In this study the effect of some such salts on dispersibility and respirability of spray dried levofloxacin formulations was evaluated in normal and reduced inhalation air flow or by increasing powder filling in capsules.

Effect of pH and leucine concentration on aerosolization properties of carrier-free formulations of levofloxacin.

The aim of this study was to evaluate the effect of leucine at different pH values preferred for inhalation on particle characteristics and aerosolization performance of spray dried carrier-free formulations of levofloxacin. A full factorial design was applied to optimize the formulation containing levofloxacin with or without leucine in different pH values and the optimum condition was determined. Particle size and morphology, crystallinity state, electrostatic charge and surface composition of the particles were determined.

Radiofrequency electric field hyperthermia with gold nanostructures: role of particle shape and surface chemistry.

Hyperthermia treatment of cancerous cells has been recently developed drastically with the help of nanostructures. Heating of gold nanoparticles in non-invasive radiofrequency electric field (RF-EF) is a promising and unique technique for cancer hyperthermia. However, because of differences between particles (i.

Effect of molecular weight and ratio of poly ethylene glycols' derivatives in combination with trehalose on stability of freeze-dried IgG.

The influence of poly ethylene glycol (PEG) at different molecular weights (MWs) and ratios was studied on the stability of freeze-dried immune globulin G (IgG). PEGs (600-4000 Dalton) at concentrations of 0.5 and 5% W/V were applied in the presence of 40 and 60% W/W of trehalose to prepare freeze-dried IgG formulations.

In-vitro cytotoxicity and combination effects of the docetaxel-conjugated and doxorubicin-conjugated poly(lactic acid)-poly(ethylene glycol)-folate-based polymeric micelles in human ovarian cancer cells.

Objectives: The pH-sensitive doxorubicin (DOX)-conjugated and docetaxel (DTX)-conjugated poly(lactic acid)-poly(ethylene glycol)-folate (PLA-PEG-FOL)-based polymeric micelles were developed and characterized in this study.

Key Findings: The drugs were released from the micelles (particle size, ~185 nm) in a pH-dependent manner. The drug-conjugated PLA-PEG-FOL micelles showed higher cellular uptake than nontargeting ones.

Nanoliposome containing cyclosporine A reduced neuroinflammation responses and improved neurological activities in cerebral ischemia/reperfusion in rat.

Cyclosporine A (CsA) is known as a neuroprotective agent against cerebral ischemia/reperfusion (I/R) in animal models. However, the significant therapeutic effects of CsA have been observed in high systemic doses or manipulating the blood-brain barrier, resulting in systemic side effects and toxicity. As the liposome nanocarriers have been developed for efficient delivery of peptide and proteins, liposomal CsA (Lipo-CsA) could improve cerebral (I/R) injuries.

The effect of excipients on the stability and aerosol performance of salmon calcitonin dry powder inhalers prepared via the spray freeze drying process.

Spray freeze drying was developed to produce dry powders suitable for applications such as inhalation delivery. In the current study, the spray freeze drying technique was employed to produce inhalable salmon calcitonin microparticles. Effects of the carrier type, concentration of hydroxyl propyl-β-cyclodextrin and the presence of Tween 80 on the chemical and structural stability, as well as on the aerosol performance of the particles were investigated.

Systemic delivery of parathyroid hormone (1-34) using spray freeze-dried inhalable particles.

Pulmonary delivery of peptides remains an important, noninvasive route of administration that is attractive because it offers high bioavailability and patient compliance. Optimization of particle characteristics for deposition in the deep regions of the lung after inhalation and retention of peptide stability are key challenges to their delivery to the lungs. The present study investigated the use of spray freeze-drying to produce porous inhalable parathyroid hormone (1-34)-loaded microparticles suitable for pulmonary delivery.

Inhaled sildenafil nanocomposites: lung accumulation and pulmonary pharmacokinetics.

Context: Administration of sildenafil citrate (SC) is considered as a strategy in the treatment of pulmonary hypertension.

Objective: This study reports production of the inhalable microparticles containing SC-loaded poly(lactide-co-glycolic acid)-nanoparticles.

Methods: SC-nanoparticles were prepared by the double emulsion solvent evaporation method.

Polymeric Micelles of PEG-PLA Copolymer as a Carrier for Salinomycin Against Gemcitabine-Resistant Pancreatic Cancer.

Purpose: Resistance to gemcitabine in pancreatic cancer (PC) may account for the failure of conventional treatments. Recently, salinomycin (SAL) has been identified as selective inhibitor of cancer stem cells (CSCs). In our study, we aimed to deliver SAL to gemcitabine-resistant PC by the aid of poly ethylene glycol-b-poly lactic acid (PEG-b-PLA) polymeric micelles (PMs).

Preparation and In-vitro Evaluation of Rifampin-loaded Mesoporous Silica Nanoaggregates by an Experimental Design.

The goal of this research is preparation, optimization and in-vitro evaluation of rifampin-loaded silica nanoparticles in order to use in the pulmonary drug delivery. Nanoparticles are exhaled because of their small size. Preparation of nanoaggregates in a micron-size scale and re-dispersion of them after deposition in the lung is an approach to overcome this problem.

Factors affecting viability of Bifidobacterium bifidum during spray drying.

Background: There is substantial clinical data supporting the role of Bifidobacterium bifidum in human health particularly in benefiting the immune system and suppressing intestinal infections. Compared to the traditional lyophilization, spray-drying is an economical process for preparing large quantities of viable microorganisms. The technique offers high production rates and low operating costs but is not usually used for drying of substances prone to high temperature.

Preparation and characterization of rifampin loaded mesoporous silica nanoparticles as a potential system for pulmonary drug delivery.

The goal of this research is to determine the feasibility of loading rifampin into mesoporous silica nanoparticles. Rifampin was selected as a model lipophilic molecule since it is a well-documented and much used anti tuberculosis drug. The mesoporous silica nanoparticles were prepared by using tetraethyl ortho silicate and cetyltrimethyl ammonium bromide (as surfactant).

Development and optimization of N-Acetylcysteine-loaded poly (lactic-co-glycolic acid) nanoparticles by electrospray.

N-Acetylcysteine (NAC) loaded PLGA nanoparticles were prepared by electrospray method. The influence of independent parameters such as concentration, flow rate and nozzle to collector distance was studied on particle size and size distribution of generated nanoparticles using a Box-Behnken experimental design. Smallest size was found to be obtained at minimum value for both flow rate and concentration of polymer, regardless of collecting distance value in the ranges studied.

Stabilization of canthaxanthin produced by Dietzia natronolimnaea HS-1 with spray drying microencapsulation.

The strain bacterium Dietzia natronolimnaea has propounded as a source for biological production of canthaxanthin. Because of sensitivity of this pigment, examine on its stability is important. In this study, stability of encapsulated canthaxanthin from D.

Formulation of inhalable lipid-based salbutamol sulfate microparticles by spray drying technique.

Background: The aim of this work was to develop dry powder inhaler (DPI) formulations of salbutamol sulfate (SS) by the aid of solid lipid microparticles (SLmPs), composed of biocompatible phospholipids or cholesterol.

Methods: The SLmPs were prepared by using two different solvent systems (ethanol and water-ethanol) and lipid carriers (dipalmitoylphosphatidylcholine (DPPC) and cholesterol) with/without L-leucine in the spray drying process. The spray-dried microparticles were physically-mixed with coarse lactose monohydrate in order to make our final DPI formulations and were investigated in terms of physical characteristics as well as in vitro drug release profile and aerosolization behavior.

Preparation, optimization and in vitro characterization of stearoyl-gemcitabine polymeric micelles: a comparison with its self-assembled nanoparticles.

Although gemcitabine (Gem) constitutes first-line therapy for pancreatic cancer, its clinical outcome suffers from rapid metabolism and acquired drug resistance. To overcome its limitations, several lipophilic prodrugs including 4-(N)-stearoyl Gem (GemC18) have been studied for their efficacy over Gem. Herein, we aimed to prepare and characterize the GemC18-loaded poly(ethylene glycol)-poly(d,l-lactide) (PEG-PLA) polymeric micelles (PMs) as well as its self-assembled nanoparticles (NPs).

Production, characterisation, and in vitro nebulisation performance of budesonide-loaded PLA nanoparticles.

The aim of this study is to prepare a nanosuspension of budesonide for respiratory delivery using nebuliser by optimising its particle size and characterising its in vitro deposition behaviour. PLA (poly lactic acid)-budesonide nanosuspension (BNS) was prepared using high-pressure emulsification/solvent evaporation method. To optimise particle size, different parameters such as PLA concentration, sonication time, and amplitude were investigated.

The use of amino acids to prepare physically and conformationally stable spray-dried IgG with enhanced aerosol performance.

This study investigated the effect of various amino acids on the molecular and thermodynamic stability of IgG (immune globulin G) as well as its aerosol performance. The antibody was spray-dried in the presence of different amino acids (leucine, phenylalanine, cysteine, glycine, lysine and arginine) using 20% and 50% (w/w) amino acid. SEC-HPLC, SDS-PAGE and IR-spectroscopy were performed to evaluate the stability of spray-dried IgG.

Doxorubicin-conjugated PLA-PEG-Folate based polymeric micelle for tumor-targeted delivery: synthesis and in vitro evaluation.

Background: Selective delivery of anticancer agents to target areas in the body is desirable to minimize the side effects while maximizing the therapeutic efficacy. Anthracycline antibiotics such as doxorubicin (DOX) are widely used for treatment of a wide variety of solid tumors.This study evaluated the potential of a polymeric micellar formulation of doxorubicin as a nanocarrier system for targeted therapy of a folate-receptor positive human ovarian cancer cell in line.