Abstract
Budesonide is a corticosteroid used by inhalation in the prophylactic management of asthma. However, frequent dosing and adverse effects (local and systemic) remain a major concern in the use of budesonide. Liposomal systems for sustained pulmonary drug delivery have been particularly attractive because of their compatibility with lung surfactant components. In the present investigation, pulmonary liposomal delivery system of budesonide was prepared by film hydration method and evaluated for sustained release. Various parameters were optimized with respect to entrapment efficiency as well as particle size of budesonide liposomes. For better shelf life of budesonide liposomes, they were freeze dried using trehalose as cryoprotectant. The liposomes were characterized for entrapment efficiency, particle size, and surface topography; in vitro drug release was evaluated out in simulated lung fluid at 37° at pH 7.4. The respirable or fine particle fraction was determined by using twin stage impinger. The stability study of freeze dried as well as aqueous liposomal systems was carried out at 2-8° and at ambient temperature (28±40). The freeze dried liposomes showed better fine particle fraction and drug content over the period of six months at ambient as well as at 2-8° storage condition compared to aqueous dispersion of liposomes.
Highlights
Budesonide is a corticosteroid used by inhalation in the prophylactic management of asthma
Inhalation delivery of medications in the treatment of lung diseases like asthma, lung cancer and COPD is advantageous over the conventional systemic therapy as it is a non-invasive mode of administration that avoids first pass metabolism along with reduction in systemic side effect
Liposomes offer several attractive features for pulmonary drug delivery. They can serve as a solubilization matrix for poorly soluble agents, act as a pulmonary sustained release reservoir, facilitate intracellular delivery of drugs, to alveolar macrophages, show good compatibility with lung surfactant components, low order of local irritation to lung tissue and reduced pulmonary toxicity[3,8,9]
Summary
Liposomes offer several attractive features for pulmonary drug delivery. Sustained release formulation of BDS in the lung can offer prolonged retention time as well as minimized biodistribution throughout the systemic circulation. It will be the ideal treatment effective in preventing bronchospasm for 6-8 h during which the patients are asleep[11]. There is a need to develop sustained release budesonide formulations that can prolong the drug release and the antiinflammatory action[12,13]. The objective of the present work was to develop an effective sustained action BDS liposomal aerosol formulation for lung delivery, and thereby achieve improved therapy in asthma
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