Proposome for transdermal delivery of tofacitinib

• Published in: International journal of pharmaceutics Vol. 585; p. 119558
• Main Authors: Kathuria, Himanshu, Nguyen, Diep T.P., Handral, Harish K., Cai, Junyu, Cao, Tong, Kang, Lifeng
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 30-07-2020
• Subjects: Administration, Cutaneous; Cadaver; Chemistry, Pharmaceutical - methods; Drug Delivery Systems - methods; Drug Stability; Follicular transport; Humans; Liposomes - chemistry; Male; Middle Aged; Nanovesicle; Particle Size; Piperidines - administration & dosage; Piperidines - pharmacokinetics; Proposome; Propylene Glycol - chemistry; Protein Kinase Inhibitors - administration & dosage; Protein Kinase Inhibitors - pharmacokinetics; Pyrimidines - administration & dosage; Pyrimidines - pharmacokinetics; Skin Absorption - physiology; Skin deposition; Tofacitinib; Transdermal; Nanovesicle; Transdermal; Tofacitinib; Follicular transport; Proposome; Skin deposition
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2020.119558

[Display omitted]
Tofacitinib citrate (TC) has recently gained interest in treating skin disorders such as psoriasis, atopic dermatitis and baldness. Unfortunately, the oral administration shows side effects, such as decreased neutrophil counts. To this end, the topical delivery of TC can be used to reduce the risk associated with systemic exposure. However, TC shows minimal absorption via skin. Hence, the objective of this study is to enhance the skin delivery of TC using a non-invasive approach. The liposomes based on propylene glycol, named as proposomes, carrying TC, were studied. The vesicle characteristics and in vitro skin permeation were assessed. The proposomes enhanced the skin permeability of TC by 4–11 folds. The composition of proposomes was found to affect the skin permeation and deposition of TC. The proposomes were stable for at least 6 months. Overall, proposomes were effective for targeted topical drug delivery.