In vitro release of Tacrolimus from Tacrolimus ointment and its speculated mechanism

Atomic force microscopy analysis of synthetic membranes applied in release studies

“…The synthetic membranes commonly used in release studies are based on cellulose products such as cellulose acetate [13,14], cellulose esters [12,15], cellulose nitrate [16] and regenerated cellulose (Cuprophan) [17,18] and they have been widely applied in quality control analyses [19,20]. Other membranes are based on synthetic polymers such as polyamide (nylon) [21,22], polyethersulfon [23,24], polyvinylidene difluoride [25,26] and polytetrafluoroethylene [10]. It is generally suggested that porous synthetic membranes do not act as rate-limiting barrier [27].…”

In Vitro Diffusion of the Immunosuppressant Tacrolimus Through Human and Rabbit Corneas

“…Studies indicate that the immunosuppressive activity of TAC is 50-100ϫ (in vitro) and 10-20ϫ (in vivo) higher than that of CsA. 1 Both TAC and CsA are calcineurin inhibitors, CsA binding to cyclophilin and TAC to FKBP12, two cytosolic proteins, respectively. The safety profile and toxicities of CsA and TAC have been found to be completely different.…”

“…It is currently employed therapeutically for the topical treatment of psoriasis, pyoderma gangrenosum, lichen planus, graft-versus-host disease, alopecia areata, allergic contact dermatitis, acnea rosacea, and pigmentary keratitis (veterinary ophthalmology), as well as ocular immunemediated diseases. 1,[8][9][10][11][12][13][14] It is also used systemically for the prophylaxis of allograft rejection in liver, kidney, corneal, lung, and heart transplant patients. 1,8,9,[15][16][17][18][19][20][21] TAC has also been used as an immunosuppressant following bone marrow transplantation and for the treatment of ocular inflammatory disorders.…”

“…1,[8][9][10][11][12][13][14] It is also used systemically for the prophylaxis of allograft rejection in liver, kidney, corneal, lung, and heart transplant patients. 1,8,9,[15][16][17][18][19][20][21] TAC has also been used as an immunosuppressant following bone marrow transplantation and for the treatment of ocular inflammatory disorders. [20][21][22] It is a macrolide (cyclic carbon backbone) antibiotic that was first discovered in 1984 and is produced by a soil organism, Streptomyces tsukubaensis.…”

“…[20][21][22] It is a macrolide (cyclic carbon backbone) antibiotic that was first discovered in 1984 and is produced by a soil organism, Streptomyces tsukubaensis. 1,8,9 The mechanism by which both TAC and CsA exert their action involves the inhibition of calcineurin activity. This enzyme plays an important role in the translocation of the pluripotent factor, nuclear factor of activated T-cell, from the cytoplasm to the nucleus.…”