Development and characterisation study of liposomes-encapsulated piroxicam.

Abstract

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.

Evaluation of antinociceptive activity of nanoliposome-encapsulated and free-form diclofenac in rats and mice

“…Further evaluation via the formalin test suggested that liposome-encapsulated diclofenac is more effective in suppressing inflammatory pain and that stronger peripheralmediated antinociceptive activity could be attained using the present liposomal formulations. Indeed, encapsulation with liposomes 29 or other materials [30][31][32] will significantly improve a drug's efficacy, and thus reduce its side effects by using lower doses. 33 Similarly to other NSAIDs, the usage of diclofenac is often associated with gastric mucosal erosion, ulceration, hemorrhage, epigastric pain, and platelet dysfunction owing to the inhibition of prostaglandin synthesis by cyclooxygenase enzyme (COX).…”

Liposomal Encapsulated Rhodomyrtone: A Novel Antiacne Drug

“…There are several reports indicating the advantages of the use of liposomal substance as carriers. Liposomes are composed of lipids similar to those present in biological membranes; therefore, they are expected to be biocompatible, biodegradable, practically nonimmunogenic, and nontoxic [19, 20]. In addition, liposomes are well suited for delivery of therapeutic agents because they usually provide a sustained drug releasing their content slowly, gradually, and increase overall drug efficacy.…”

Cytoprotective and enhanced anti-inflammatory activities of liposomal piroxicam formulation in lipopolysaccharide-stimulated RAW 264.7 macrophages

“…20 Briefly, stock piroxicam solution (60 mg/mL DMSO) was added into Pro-lipo Duo and stirred moderately (125 ± 25 rpm) for 1 hour. Concentrated piroxicam-loaded liposomal suspension was formed by the dropwise addition of distilled water (dH 2 O).…”

“…20,21 Duplicate samples for analysis were prepared from each of the three individual batches of liposomal samples (n = 6). The morphological observation of blank liposomes and liposome-encapsulated piroxicam was done using a Philips CM12 transmission electron microscope (Amsterdam, The Netherlands).…”