The invention belongs to the field of pharmaceutical preparations, and discloses a
hyaluronic acid prodrug as well as a preparation method thereof and application thereof in transdermal delivery. According to the preparation method,
hyaluronic acid is used for
grafting drug molecules so as to overcome the
barrier function of
stratum corneum, and the
drug molecules are transmitted to the subcutaneous tissues by means of
intercellular space penetration and an opening of cutaneous appendages, so that
drug molecular targeting and
skin absorption efficiency are improved. As a carrier for administration,
hyaluronic acid can effectively improve the
percutaneous permeability of a drug, and helps the drug to be absorbed into the
systemic circulation, thereby enabling an effective
blood concentration of local or systemic treatment to be reached. Compared with the prior art, the hyaluronic acid
prodrug enables the
skin penetration amount of the drug molecules to be obviously increased so as to increase the
utilization rate of the drug; furthermore, the hyaluronic acid
prodrug facilitates the treatment of a doctor for a patient, can realize direct administration for certain diseases, and effectively reduces risks and side effects, thus having a broad application prospect.