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1.
J Clin Pharmacol ; 51(7): 964-77, 2011 Jul.
Article in English | MEDLINE | ID: mdl-21148047

ABSTRACT

Transdermal drug delivery offers an attractive alternative to the conventional drug delivery methods of oral administration and injection. However, the stratum corneum acts as a barrier that limits the penetration of substances through the skin. Recently, the use of micron-scale needles in increasing skin permeability has been proposed and shown to dramatically increase transdermal delivery. Microneedles have been fabricated with a range of sizes, shapes, and materials. Most in vitro drug delivery studies have shown these needles to increase skin permeability to a broad range of drugs that differ in molecular size and weight. In vivo studies have demonstrated satisfactory release of oligonucleotides and insulin and the induction of immune responses from protein and DNA vaccines. Microneedles inserted into the skin of human subjects were reported to be painless. For all these reasons, microneedles are a promising technology to deliver drugs into the skin. This review presents the main findings concerning the use of microneedles in transdermal drug delivery. It also covers types of microneedles, their advantages and disadvantages, enhancement mechanisms, and trends in transdermal drug delivery.


Subject(s)
Drug Delivery Systems , Microtechnology , Needles , Pharmaceutical Preparations/administration & dosage , Skin/metabolism , Administration, Cutaneous , Animals , Equipment Design , Genetic Therapy/methods , Humans , Needles/adverse effects , Permeability , Pharmacokinetics , Skin/anatomy & histology , Skin/drug effects , Skin Physiological Phenomena , Vaccination/methods
2.
J Clin Pharmacol ; 49(11): 1262-83, 2009 Nov.
Article in English | MEDLINE | ID: mdl-19717723

ABSTRACT

Transdermal drug delivery offers an attractive alternative to the conventional drug delivery methods of oral administration and injection. However, the stratum corneum acts as a barrier that limits the penetration of substances through the skin. Application of high-voltage pulses to the skin increases its permeability (electroporation) and enables the delivery of various substances into and through the skin. The application of electroporation to the skin has been shown to increase transdermal drug delivery. Moreover, electroporation, used alone or in combination with other enhancement methods, expands the range of drugs (small to macromolecules, lipophilic or hydrophilic, charged or neutral molecules) that can be delivered transdermally. The efficacy of transport depends on the electrical parameters and the physicochemical properties of drugs. The in vivo application of high-voltage pulses is well tolerated, but muscle contractions are usually induced. The electrode and patch design is an important issue to reduce the discomfort of the electrical treatment in humans. This review presents the main findings in the field of electroporation-namely, transdermal drug delivery. Particular attention is paid to proposed enhancement mechanisms and trends in the field of topical and transdermal delivery.


Subject(s)
Administration, Cutaneous , Drug Delivery Systems/methods , Electroporation/methods , Skin/metabolism , Adrenergic beta-Antagonists/administration & dosage , Analgesics/administration & dosage , Animals , Anti-Inflammatory Agents/administration & dosage , Antidiuretic Agents/administration & dosage , Antineoplastic Agents/administration & dosage , Antiviral Agents/administration & dosage , Catechin/administration & dosage , Catechin/analogs & derivatives , Central Nervous System Stimulants/administration & dosage , Dextrans/administration & dosage , Folic Acid Antagonists/administration & dosage , Gene Transfer Techniques , Hormones/administration & dosage , Humans , Insulin/administration & dosage , Models, Biological , Oligonucleotides/administration & dosage , Photosensitizing Agents/administration & dosage , Wound Healing
3.
J Pharm Pharm Sci ; 12(1): 88-115, 2009.
Article in English | MEDLINE | ID: mdl-19470295

ABSTRACT

Transdermal drug delivery offers an attractive alternative to the conventional drug delivery methods of oral administration and injection. However, the stratum corneum acts as a barrier that limits the penetration of substances through the skin. Application of ultrasound to the skin increases its permeability (sonophoresis) and enables the delivery of various substances into and through the skin. Ultrasound has been used extensively for medical diagnostics and to a certain extent in medical therapy (physiotherapy, ultrasonic surgery, hyperthermia). Nevertheless, it has only recently become popular as a technique to enhance drug release from drug delivery systems. A number of studies suggest the use of ultrasound as an external mean of delivering drugs at increased rates and at desired times. This review presents the main findings in the field of sonophoresis, namely transdermal drug delivery and transdermal monitoring. Particular attention is paid to proposed enhancement mechanisms and trends in the field of topical and transdermal delivery.


Subject(s)
Chemistry, Pharmaceutical , Pharmaceutical Preparations/administration & dosage , Skin Absorption/drug effects , Skin/metabolism , Administration, Cutaneous , Drug Delivery Systems , Drug Design , Permeability/drug effects , Skin Absorption/physiology , Structure-Activity Relationship , Ultrasonography/methods
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