Development, optimization, and evaluation of tamsulosin nanotransfersomes to enhance its permeation and bioavailability

Tamsulosin (TM) is a drug used for benign prostatic hyperplasia. This drug produces undesired side effects on oral administration due to fluctuation in the plasma level. Therefore, a transdermal delivery system is beneficial. Lipid-based systems revolutionized the transdermal route of drug delivery. Among them, nanotransfersomes, which have flexible and elastic membranes enabling them to improve skin permeation. Therefore, in the present study, we aimed to optimize nanotransfersomes by the statistical design of experiments in order to optimize the quantities of tamsulosin (drug), Lipoid S100 (lipid), and sodium deoxycholate SDC (edge activator). The responses were particle size, entrapment efficiency, and ex-vivo steady-state flux. The optimized formulation was characterized and evaluated for pharmacokinetic parameters. The results indicated that optimum nanotransfersome by the software consisted of tamsulosin (0.4664 mg), lipoid S100 (59.30 mg), and SDC (58.96 mg) showed 60 nm particle size, 42% entrapment, and 7.2 mcg/cm2.min steady state flux. Nanotransfersomes appeared spherical and uniform in TEM image. The stability index of the optimized formula was 85%. The enhancement in bioavailability was well significant when compared to the marketed tablet. Overall, the nanotransfersomes have proved as an efficient transdermal delivery system for tamsulosin. © 2020 Elsevier B.V.