Transdermal Drug Delivery: Innovative Pharmaceutical Developments Based on Disruption of the Barrier Properties of the Stratum Corneum

Abstract

The skin offers an accessible and convenient site for the administration of medications. To this end, the field of transdermal drug delivery, aimed at developing safe and efficacious means of delivering medications across the skin, has in the past and continues to garner much time and investment with the continuous advancement of new and innovative approaches. This review details the progress and current status of the transdermal drug delivery field and describes numerous pharmaceutical developments which have been employed to overcome limitations associated with skin delivery systems. Advantages and disadvantages of the various approaches are detailed, commercially marketed products are highlighted and particular attention is paid to the emerging field of microneedle technologies.

Improving the Membrane Permeability of 5-Fluorouracil via Cocrystallization

“…All of these methods have respective weaknesses, for instance, the complexity design of prodrugs, irritation or toxicity of chemical enhancers, pain and damage of tissue caused by iontophoresis or noncavitational ultrasound and complex device design of electroporation, etc. [3][4][5][6] Pharmaceutical cocrystals can be defined as a stoichiometric multiple component supramolecular structure combined by an active pharmaceutical ingredient (API) and one or more unique cocrystal formers with non-covalent bonds. 7 Formation of pharmaceutical cocrystals can dramatically ameliorate the physicochemical properties of the API without any disruption of covalent bonds, including melting point, solubility, dissolution rate, stability 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 4 and mechanical behavior, etc.…”

Pharmacological Targeting of the Epidermal Barrier

“…Methods modifying the barrier properties can be passive or active. Passive methods include the influencing of drug and vehicle interactions and optimization of formulation to modify SC structure [104]. A widely used passive method is the application of chemical penetration enhancers that facilitate drug permeation across the skin.…”

The Influence of Solid Microneedles on the Transdermal Delivery of Selected Antiepileptic Drugs

“…The use of MNs is preferred because these devices are inexpensive and offer more reliable mode of administration by improving the pharmacokinetic and pharmacodynamics profiles of drugs [21]. MNs induce faster healing at administration site compared to hypodermic needles while allowing for a controlled rate of drug delivery [22]. Passive approaches, such as penetration enhancers, result in skin irritation and are limited to only small molecules [6,21].…”