Exploration of a transdermal nanoemulgel as an alternative therapy for postmenopausal osteoporosis

Abstract

The study investigated the ability of a transdermal nanoemulgel formulation to enhance the bioavailability and anti-osteoporotic efficacy of raloxifene hydrochloride (RH) using recent techniques such as micro-CT, SEM-EDX analysis. The ex-vivo permeation, histopathology, SEM, DSC and CLSM studies were carried out to determine the mechanistics of permeation. The in-vivo pharmacokinetic and pharmacodynamic studies were performed after establishing osteoporosis model using ovariectomy surgery. The biocompatibility of the developed nanoemulgel was tested as per OECD TG 439 protocol. The permeation of RH enhanced by 13 fold compared to plain drug gel. DSC and SEM examination showed change in microstructure of the skin which is the foundation for improved permeation. The pharmacokinetic study suggested 26 fold improved bioavailability of RH compared to per-oral marketed treatment. The micro-CT study demonstrated 202% enhanced bone mineral density. Improved pharmacokinetic and pharmacodynamic performance supported our claim of a successful delivery system. Our formulation is proposed to be safe, patient compliant and therapeutically effective alternative to the available marketed product.