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Development and evaluation of inhalational liposomal system of budesonide for better management of asthma

Author(s): JJ Parmar1, DJ Singh1, Darshana D Hegde1, AA Lohade1, PS Soni2, A Samad3, Mala D Menon1
1 Bombay College of Pharmacy, Kalina, Santacruz (East), Mumbai-400 098, India 2 Board of Radiation and Isotope Technology and Medical Cyclotron Facility Parel, Mumbai-400012, India 3 Department of Medicine, Bombay Veterinary College, Parel, Mumbai-400 012, India

Correspondence Address:
Mala D Menon Bombay College of Pharmacy, Kalina, Santacruz (East), Mumbai-400 098 India E-mail: [email protected]

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.

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