Osteoporosis is a progressive bone disease that remains unnoticed until a fracture occurs. It
is more predominant in the older age population, particularly in females due to reduced estrogen levels
and ultimately limited calcium absorption. The cost burden of treating osteoporotic fractures is too
high, therefore, primary focus should be treatment at an early stage. Most of the marketed drugs are
available as oral delivery dosage forms. The complications, as well as patient non-compliance, limit
the use of oral therapy for prolonged drug delivery. Transdermal delivery systems seem to be a promising
approach for the delivery of anti-osteoporotic active moieties. One of the confronting barriers is the
passage of drugs through the SC layers followed by penetration to deeper dermal layers. The review
focuses on how anti-osteoporotic drugs can be molded through different approaches so that they can be
exploited for the skin to systemic delivery. Insights into the various challenges in transdermal delivery
and how the novel delivery system can be used to overcome these have also been detailed.
