Fate of different kinds of liposomes containing dexamethasone palmitate after intra-articular injection into rabbit joints

Abstract

The fate of oligolamellar and multilamellar vesicles containing dexamethasone palmitate after intra-articular injection into healthy rabbit joints was investigated to improve the liposome formulation in respect to better bioavailability of the effective substance within the arthritic joint. The defined negatively charged oligolamellar vesicles (dexamethasone) palmitate, egg phosphatidylcholine, phosphatidic acid, molar ratio 0.24:10.1) of a mean diameter of 0.75 micron gave better results than multilamellar vesicles (dexamethasone palmitate, dipalmitoylphosphatidylcholine, phosphatidic acid, molar ratio 0.24:10:1) used for the same purpose by several other authors. The positive charge carrier stearylamine does not induce any improvement.

Intra‐articular depot formulation principles: Role in the management of postoperative pain and arthritic disorders

“…Liposomal preparations containing lipophilic corticosteroid derivatives (Tab. 3) afforded sustained anti‐inflammatory activity after IA injection in the rabbit and in man 171–176. The steroids were most likely incorporated into the phosholipid bilayer.…”

Physicochemical properties of extruded and non-extruded liposomes containing the hydrophobic drug dexamethasone

“…There are a number of literature reports concerning liposome formulations of dexamethasone and other glucocorticoids (Bonanomi et al, 1987;Taniguchi et al, 1987;Tremblay et al, 1993;Benameur et al, 1995;Kulkarni and Vargha-Butler, 1995;VarghaButler and Hurst, 1995;Farshi et al, 1996;Lopes de Menezes and Vargha-Butler, 1996;Al-Muhammad et al, 1996;Al-Muhammed et al, 1996;DiMatteo and Reasor, 1997;Saarinen-Savolainen et al, 1997;Suntres and Shek, 1998;Kallinteri et al, 2002;Metselaar et al, 2002;Cevc and Blume, 2004;Chono and Morimoto, 2006;Koning et al, 2006;Tsotas et al, 2007). However, the physicochemical properties of these liposomes vary considerably.…”

“…The encapsulation of dexamethasone in carrier systems such as liposomes and microspheres can diminish the adverse effects and reduce the total amount of drug required. Liposomal and microsphere dexamethasone formulations have been investigated for hypersensitivity pneumonitis (Tremblay et al, 1993); ophthalmic anti-inflammatory action (Taniguchi et al, 1987(Taniguchi et al, , 1988Al-Muhammad et al, 1996;Al-Muhammed et al, 1996); oral ulcers (Farshi et al, 1996); arthritis (Bonanomi et al, 1987;Koning et al, 2006); atherosclerosis (Chono et al, 2005a,b;Chono and Morimoto, 2006); dermatological conditions (Cevc and Blume, 2004); pulmonary diseases (Benameur et al, 1995;Suntres and Shek, 1998); silica-induced pulmonary toxicity (DiMatteo and Reasor, 1997); localized anti-inflammatory effect for metallic stents (Kallinteri et al, 2002); brain edema (Eroglu et al, 2001); and controlling the inflammatory response to implantable devices (Hickey et al, 2002b,a).…”

Application of Liposomes in Treatment of Rheumatoid Arthritis: Quo Vadis

“…The bioavailability of drug from oligolamellar vesicles was found to be more as compared to that from multilamellar vesicles [97]. …”