Active Ingredients: Ciprofloxacin
The value of inhaled delivery using the antibiotic ciprofloxacin as an example.
Reproduced from Cipolla et al. Later, specialized suspension formulations and, finally, liposomal formulations, such as amikacin and ciprofloxacin, were developed.
Formulations that are suitable for inhalation should be sterile, preservative free, and nonpyrogenic. They also should be adjusted for the lung environment with a suitable pH range 4.The development of formulations capable of for sustaining levels of ciprofloxacin in the lungs, a liposomal formulation where antibacterial activity. The present review compares two approaches sustaining ciprofloxacin concentrations in the lungs has the potential to significantly improve ciprofloxacin is encapsulated in small unilamellar vesicles, and a dry powder formulation.
More recently, dry powder formulations using PulmoSphere technology have the ability to carry a higher payload of antibiotics. The pulmonary deposition of the hollow porous particles within these powders is independent of the patient's inspiratory flow.
One possible explanation for this observation is that the free drug component of CDI is precipitating at the higher pH observed following mixing of the two formulations Fig.
Detailed information regarding the aerosol performance of CDI has not been publicly disclosed. Bruinenberg et al.
The total lung dose 16. The TLD is estimated from the product of the emitted dose and fine particle dose divided by two, to account for aerosol lost during exhalation. The reported value ca. The mass of ciprofloxacin depositing in the upper respiratory tract URT is about 17.
Deposition in the URT is 27. Pharmacokinetics Improved Lung Targeting Superior targeting of drug to the site of the infection in the airways can be achieved with inhaled sustained release formulations of ciprofloxacin, compared to current marketed oral and parenteral formulations.
For example, inhalation of 32. This is about 1000-fold higher than sputum levels achieved with oral ciprofloxacin, which range from 0. This helps to ensure that the required concentration for bactericidal action is achieved, while limiting the development of ciprofloxacin-resistant strains.
The high levels of ciprofloxacin in sputum observed for CIP are achieved without corresponding high levels of drug in the systemic circulation. Indeed, the peak plasma levels for CIP are 0. Animal Studies Demonstrating Impact of Improved Lung Targeting The pioneering work of Wong and colleagues demonstrated that encapsulation of ciprofloxacin in liposomes improves lung targeting relative to inhalation of free ciprofloxacin hydrochloride, leading to dramatic improvements in efficacy in animal models of lung infection.
At 24-h post-infection, the mice were treated with a single dose of either aerosolized free ciprofloxacin or aerosolized liposome-encapsulated ciprofloxacin.