Abstract
Over the last few decades, biological macromolecular drugs (e.g., peptides, proteins, and nucleic acids) have become a significant therapeutic modality for the treatment of various diseases. These drugs are considered superior to small-molecule drugs because of their high specificity and favorable safety profiles. However, such drugs are limited by their low oral bioavailability and short half-lives. Biological macromolecular drugs are typically administrated via invasive methods, e.g., intravenous or subcutaneous injections, which can be painful and induce needle phobia. Noninvasive transdermal delivery is an alternative administration route for the local and systemic delivery of biological macromolecular drugs. However, a challenge with the noninvasive transdermal delivery of biological macromolecular drugs is the outermost layer of the skin, known as the stratum corneum, which is a physical barrier that restricts the entry of extraneous macromolecules. Iontophoresis (IP) relies on the application of a low level of electricity for transdermal drug delivery, in order to facilitate the skin permeation of hydrophilic and charged molecules. The IP of several biological macromolecular drugs has recently been investigated. Herein, we review the IP-mediated noninvasive transdermal delivery of biological macromolecular drugs, their routes of skin permeation, their underlying mechanisms, and their advance applications.
Highlights
Biological macromolecular drugs are large and complex molecules composed of sugars, peptides, nucleic acids, or their complex combinations [1,2]
This study found that the IP of insulin-encapsulated cationic liposomes composed of DOTAP/egg phosphatidylcholine (EPC)/cholesterol (Chol) at a molar ratio of 2:2:1 achieved a greater delivery depth via the hair follicles
The development of biological macromolecular drugs has been continuously expanding in recent years, as noninvasive routes of administration are preferable for these types of drugs
Summary
Biological macromolecular drugs ( known as biologics, biomacromolecules, biotechnology drugs) are large and complex molecules composed of sugars, peptides, nucleic acids, or their complex combinations [1,2]. The side effects are more prominent when drugs are used to treat chronic medical conditions, which may require long-term repetitive dosing [13] Considering these limitations, several noninvasive routes have been investigated, including transdermal, inhalation, buccal and sublingual routes [4,14–16]. The skin represents an attractive route for the noninvasive delivery of biological macromolecules, owing to its large surface area (1.7 m2 ), which provides a convenient and accessible administration site compared to other routes [19]. This route bypasses first-pass hepatic metabolism and avoids drug inactivation by the gastric pH and digestive enzymes in the gastrointestinal tract [20,21]. The relevant studies of this review were selected from the MEDLINE/PubMed (National Center for Biotechnology Information) and Google Scholar databases using the keywords of this article
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