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

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.

Highlights

Transdermal nanoemulgel of raloxifene hydrochloride was prepared and evaluated for treatment of postmenopausal osteoporosis.

Nanoemulgel improved the skin permeation by 13 fold compared to plain raloxifene gel.

SEM and DSC of cadaver skin tissue samples provided mechanistic insight into transdermal delivery of raloxifene hydrochloride.

Pharmacokinetic study of nanoemulgel was compared with per-oral marketed Ralox® tablet which showed improved bioavailability by 26 fold.

Micro-CT and SEM-EDX analysis showed an enhanced bone mineral density (202%).

The formulation was biocompatible as per OECD TG 439 protocol.

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.

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Article information: Foziyah Zakir, Adil Ahmad, Mohd Amir Mirza, Kanchan Kohli, Farhan J. Ahmed, Exploration of a transdermal nanoemulgel as an alternative therapy for postmenopausal osteoporosis, Journal of Drug Delivery Science and Technology, 2021. https://doi.org/10.1016/j.jddst.2021.102745.