Physical stability and aerosol properties of liposomes delivered using an air-jet nebulizer and a novel micropump device with large mesh apertures

The objective of present work was to develop a novel liposomes-based drug delivery system for a lipophilic nonsteroidal anti-inflammatory drug, piroxicam. The system was prepared using proliposomes method and optimised for different preparation parameters including type of proliposomes, concentration of drug, duration of hydration and type of particle size reduction treatment used. All prepared liposomal samples were extensively characterized for their drug-entrapment and size profile using various in-vitro techniques. Present work showed that the most optimum formulation (Pro-lipo TM Duo; 12mg piroxicam per gram Prolipo TM ; 10 hours hydration time) produced highest amount of actual drug been entrapped in liposomes (800.4 mg/g Prolipo TM ) with a satisfactory entrapment efficiency of 15.36%. This formulation had also produced liposomal samples with a homogenous (polydispersity index = 0.45) and small particle size (359.95nm). Extrusion technique was found to cause significant reduction in drug-entrapment and size profile of drug-loaded liposomes. A 4-weeks storage study showed that drug-entrapment and size profile of liposomal samples were stable in both refrigerated and room temperature. Electron microscopy revealed that prepared liposomal samples were spherical-shaped and showed concentric lamellae. In conclusion, present work successfully demonstrated a simple, reproducible and practical method of preparation for liposomes-encapsulated piroxicam.

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“…This finding suggested the elastic deformation of the liposomes. A similar interpretation had also been suggested by Elhissi et al [26].…”

Section: Size Reduction Studysupporting

confidence: 86%

Development and characterisation study of liposomes-encapsulated piroxicam.

et al. 2011

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“…Studies using electronic nebulization have demonstrated reduced vesicle disruption of liposome formulations while also improving the rate of aerosol output. However, depending on the formulation, the observed emitted dose may be lower, and the aerodynamic diameter of the aerosol droplet produced can be larger than that obtained using jet nebulization (Wagner et al 2006, Elhissi et al 2007.…”

Section: Delivery Of Rslpi In a Liposomal Carrier For Inhalation 519mentioning

confidence: 98%

Delivery of rSLPI in a liposomal carrier for inhalation provides protection against cathepsin L degradation

Gibbons

McElvaney

Taggart

et al. 2009

Journal of Microencapsulation

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Secretory leukocyte protease inhibitor (SLPI) is an endogenous serine protease inhibitor that protects the lungs from excessive tissue damage caused by leukocyte proteases released during inflammation. Recombinant SLPI (rSLPI) has shown potential as a treatment for inflammatory lung conditions. To date, its clinical application has been limited by rapid enzymatic cleavage by cathepsins and rapid clearance from the lungs after inhalation. In this study, rSLPI was encapsulated in 1,2-Dioleoylsn-Glycero-3-[Phospho-L-Serine] : Cholesterol (DOPS : Chol) liposomes for inhalation. Incubation of rSLPI with cathepsin L leads to complete loss of activity while encapsulation of rSLPI in DOPS : Chol liposomes retained 92.6% of its activity after challenge with cathepsin L. rSLPI-loaded liposomes were aerosolized efficiently using a standard nebulizer with a minimal loss of activity and stability. This formulation was biocompatible and encapsulation did not appear to diminish access to intracellular sites of action in in vitro cell culture studies. Liposome encapsulation of rSLPI therefore improves stability and potentially reduces the level and frequency of dosing required for therapeutic effect after inhalation.

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“…27 Hence, NRE was calculated to evaluate the stability of the nanomicelles during nebulization process. As it appeared in Table 3, the retention of AmB in micellar formulations with varied drug loading did not differ significantly after nebulization ( p > 0.05).…”

Section: Nebulization Of Amb Loaded Dc-sa Micellesmentioning

confidence: 99%