January 27, 2021
Background / Context / Abstract:
Conventional oral sirolimus and sirolimus derivatives have been associated with adverse effects due to long-term administration. In order to solve this problem, the present inventors have carefully examined
and found that the external preparations containing the constituent active ingredients of sirolimus or sirolimus derivatives and vegetable oil can transfer the active ingredients into the blood and exert an effect on the whole body. The percutaneous absorbent in the present invention has been completed.
The external drug in the present invention is a percutaneous absorbent containing vegetable oil to improve the distribution of sirolimus in blood. The formulation of this external drug can maintain a stable blood concentration for a long time, thereby providing more effective effects and reducing adverse reactions. Therefore, the external drug is suitable for sirolimus administration in the patients unable to take oral medication.
The external drug in the present invention effectively penetrates into the epidermis, does not remain in the dermis but goes through it, and transfers into the blood, thereby enabling the treatment of systemic lesions. Also, compared to conventional oral preparations, the external drug can avoid the first-pass effect, which consequently reduces the burden on the liver and lessen adverse reactions. In addition, the external drug has an AUC (area under the blood drug concentration-time curve) comparable to that of the oral formulation, which implies that sirolimus can be effectively transferred percutaneously into the blood.
Potential Applications / Potential Markets:
We will grant a license from this university to a company and aim at practical application after the conduct of clinical trials by the company.
State of Development / Opportunity / Seeking:
・Available for exclusive and non-exclusive licensing
・Exclusive/non-exclusive evaluation for defined period (set up for options)
1. Development partner
Efficiency of sirolimus delivery to the dermis and blood for liniment (SLN), gel (SG), and oral formulation (Oral S) containing sirolimus