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Liposomal tacrolimus is a novel formulation of the immunosuppressant tacrolimus, encapsulated within liposomes to enhance site-specific delivery, prolong tissue residence time, and reduce systemic toxicity. Liposomal encapsulation enables controlled and sustained release, improved tissue penetration, and local retention, which is particularly advantageous for conditions where localized immunosuppression or anti-inflammatory action is desired. The mechanism of action is based on inhibition of T-cell activation through FKBP-12 binding and subsequent inhibition of calcineurin, which decreases IL-2 transcription and cytokine production. Major indications under development include treatment of hemorrhagic cystitis (via intravesical delivery) and immune-mediated skin diseases (via topical delivery). Lipella Pharmaceuticals is developing liposomal tacrolimus (LP-10 and related codes) for urologic and dermatologic diseases, including lichen planus and graft-versus-host disease. Liposomal tacrolimus inhalation powder formulations for pulmonary delivery have been investigated as potential rescue therapy for lung transplant rejection[1][3][4][9].
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