Physicochemical stability and aerosolization performance of dry powder inhalation system containing ciprofloxacin hydrochloride

Karimi, Keyhaneh; Katona, Gábor; Csóka, Ildikó; Ambrus, Rita

doi:10.1016/j.jpba.2017.09.019

Cited by 22 publications

(15 citation statements)

References 29 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…However, they have around 50-60% FPF results due to the apparent high cohesive properties between the active ingredient's particles [26,27]. Many publications deal with the development of DPI containing ciprofloxacin or ciprofloxacin hydrochloride [12,[28][29][30][31][32][33]. A serious challenge of our previous work was using the benefits of these two formulations (applying 1:10 ratio and current inhaled antibiotics are $100 mg), the novel combined formulation (a co-spray-dried drug blended with surface modified lactose) produced by us resulted in a higher FPF value than the carrier-based and carrier-free DPI formulations [18].…”

Section: Introductionmentioning

confidence: 99%

Stability test of novel combined formulated dry powder inhalation system containing antibiotic: physical characterization andin vitro–in silicolung deposition results

Benke

Farkas

Balásházy

et al. 2019

Drug Development and Industrial Pharmacy

Self Cite

View full text Add to dashboard Cite

Objective: The aim was to study the stability of dry powder inhaler (DPI) formulations containing antibiotic with different preparation wayscarrier-based, carrier-free, and novel combined formulationand thereby to compare their physicochemical and in vitro-in silico aerodynamical properties before and after storage. Presenting a novel combined technology in the field of DPI formulation including the carrierbased and carrier-free methods, it is the most important reason to introduce this stable formulation for the further development of DPIs. Methods: The structure, the residual solvent content, the interparticle interactions, the particle size distribution and the morphology of the samples were studied. The aerodynamic values were determined based on the cascade impactor in vitro lung model. We tested the in silico behavior of the novel combined formulated samples before and during storage. Results: The physical measurements showed that the novel combined formulated sample was the most favorable. It was found that thanks to the formulation technique and the use of magnesium stearate (MgSt) has a beneficial effect on the stability compared with the carrier-based formulation without MgSt and carrier-free formulations. The results of in vitro and in silico lung models were consistent with the physical results, so the highest deposition was found for the novel combined formulated sample during the storage. Conclusions: It can be established that after the storage a novel combined formulated DPI contained amorphous drug to have around 2.5 lm mass median aerodynamic diameter and nearly 50% fine particle fraction predicted high lung deposition in silico also.

show abstract

Section: Introductionmentioning

confidence: 99%

Stability test of novel combined formulated dry powder inhalation system containing antibiotic: physical characterization andin vitro–in silicolung deposition results

Benke

Farkas

Balásházy

et al. 2019

Drug Development and Industrial Pharmacy

Self Cite

View full text Add to dashboard Cite

show abstract

“…Stability of the spray dried powder was assessed by measuring the drugs content and aerodynamic performance [38] (RS01 ® ) after storing about 100 mg of the powder in a 20 mL amber vial sealed with a clamped elastomeric stopper both for 1 month under ambient conditions and for 24 h at 50 °C.…”

Section: Methodsmentioning

confidence: 99%

Sodium Hyaluronate Nanocomposite Respirable Microparticles to Tackle Antibiotic Resistance with Potential Application in Treatment of Mycobacterial Pulmonary Infections

et al. 2019

View full text Add to dashboard Cite

Tuberculosis resistant cases have been estimated to grow every year. Besides Mycobacterium tuberculosis, other mycobacterial species are responsible for an increasing number of difficult-to-treat infections. To increase efficacy of pulmonary treatment of mycobacterial infections an inhalable antibiotic powder targeting infected alveolar macrophages (AMs) and including an efflux pump inhibitor was developed. Low molecular weight sodium hyaluronate sub-micron particles were efficiently loaded with rifampicin, isoniazid and verapamil, and transformed in highly respirable microparticles (mean volume diameter: 1 μm) by spray drying. These particles were able to regenerate their original size upon contact with aqueous environment with mechanical stirring or sonication. The in vitro drugs release profile from the powder was characterized by a slow release rate, favorable to maintain a high drug level inside AMs. In vitro antimicrobial activity and ex vivo macrophage infection assays employing susceptible and drug resistant strains were carried out. No significant differences were observed when the powder, which did not compromise the AMs viability after a five-day exposure, was compared to the same formulation without verapamil. However, both preparations achieved more than 80% reduction in bacterial viability irrespective of the drug resistance profile. This approach can be considered appropriate to treat mycobacterial respiratory infections, regardless the level of drug resistance.

show abstract

“…In accord with established technologies, the bulk material of the formulation is α-lactose monohydrate (LCS). The other components of the formulation include: polyvinyl alcohol (PVA), which is reported to enhance the morphological characteristics of particles and to improve their drug-release properties; [23][24][25] dipalmitoylphosphatidylcholine (DPPC) lung surfactant; [26][27][28][29] L-leucine (L-LC) aerolization modifier; 25,30,31 and chitosan (CS) bioadhesive. [32][33][34][35] To facilitate the selection of optimal compositions, these formulations are assessed for their production yield, morphological characteristics, and surface charge.…”

Section: Introductionmentioning

confidence: 99%

Polymer–Lipid Microparticles for Pulmonary Delivery

et al. 2018

View full text Add to dashboard Cite

Toward engineering approaches that are designed to optimize the particle size, morphology, and mucoadhesion behavior of the particulate component of inhaler formulations, this paper presents the preparation, physicochemical characterization, and preliminary in vitro evaluation of multicomponent polymer-lipid systems that are based on "spray-drying engineered" α-lactose monohydrate microparticles. The formulations combine an active (budesonide) with a lung surfactant (dipalmitoylphosphatidylcholine) and with materials that are known for their desirable effects on morphology (polyvinyl alcohol), aerosolization (l-leucine), and mucoadhesion (chitosan). The effect of the composition of formulations on the morphology, distribution, and in vitro mucoadhesion profiles is presented along with "Calu-3 cell monolayers" data that indicate good cytocompatibility and also with simulated-lung-fluid data that are consistent with the therapeutically useful release of budesonide.

show abstract

Physicochemical stability and aerosolization performance of dry powder inhalation system containing ciprofloxacin hydrochloride

Cited by 22 publications

References 29 publications

Stability test of novel combined formulated dry powder inhalation system containing antibiotic: physical characterization andin vitro–in silicolung deposition results

Stability test of novel combined formulated dry powder inhalation system containing antibiotic: physical characterization andin vitro–in silicolung deposition results

Sodium Hyaluronate Nanocomposite Respirable Microparticles to Tackle Antibiotic Resistance with Potential Application in Treatment of Mycobacterial Pulmonary Infections

Polymer–Lipid Microparticles for Pulmonary Delivery

Contact Info

Product

Resources

About