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Pharmaceutics
Special Issues
Advanced Transdermal Drug Delivery
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Advanced Transdermal Drug Delivery

A special issue of Pharmaceutics (ISSN 1999-4923).

Deadline for manuscript submissions: closed (30 December 2013) | Viewed by 43059

Special Issue Editor

Prof. Dr. Bozena B. Michniak-Kohn

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Guest Editor
Pharmaceutics, Ernest Mario School of Pharmacy, Center for Dermal Research (CDR) & Laboratory for Drug Delivery (LDD), NJ Center for Biomaterials, Life Sciences Building, Rutgers-The State University of New Jersey, 145, Bevier Road, Piscataway, NJ 08854, USA
Interests: topical; transdermal; percutaneous drug delivery; skin transport pathways; skin carrier systems; skin formulations; skin drug delivery; human skin equivalents; skin models
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleague,

Transdermal delivery (TDD) systems offering a number of advantages over oral delivery have been available since 1979, when the first passive patch containing scopolamine was approved by the FDA. The future success of this dosage form is limited by the inability to deliver most drugs through the skin in therapeutically effective amounts. However, through novel designs of devices, new materials and active drug delivery approaches, we have the potential to significantly impact the future of TDD especially for those dosage forms containing macromolecules. Examples include microneedles, laser, ultrasound, iontophoresis and electroporation as well as thermal poration. In this “Advanced Transdermal Drug Delivery” Special Issue we will discuss the transdermal technologies of the future: the potential and the challenges.

Prof. Dr. Bozena B. Michniak-Kohn
Guest Editor


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Keywords

  • transdermal
  • microneedles
  • transdermal delivery of macromolecules
  • acoustical methods
  • electric methods
  • iontophoresis
  • electroporation
  • sonophoresis
  • thermal poration
  • drugs

Published Papers (5 papers)

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Research

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720 KiB  
Article
Human Growth Hormone Delivery with a Microneedle Transdermal System: Preclinical Formulation, Stability, Delivery and PK of Therapeutically Relevant Doses
by Mahmoud Ameri, Miryam Kadkhodayan, Joe Nguyen, Joseph A. Bravo, Rebeca Su, Kenneth Chan, Ahmad Samiee and Peter E. Daddona
Pharmaceutics 2014, 6(2), 220-234; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics6020220 - 15 May 2014
Cited by 43 | Viewed by 12002
Abstract
This study evaluated the feasibility of coating formulated recombinant human growth hormone (rhGH) on a titanium microneedle transdermal delivery system, Zosano Pharma (ZP)-hGH, and assessed preclinical patch delivery performance. Formulation rheology and surface activity were assessed by viscometry and contact angle measurement. rhGH [...] Read more.
This study evaluated the feasibility of coating formulated recombinant human growth hormone (rhGH) on a titanium microneedle transdermal delivery system, Zosano Pharma (ZP)-hGH, and assessed preclinical patch delivery performance. Formulation rheology and surface activity were assessed by viscometry and contact angle measurement. rhGH liquid formulation was coated onto titanium microneedles by dip-coating and drying. The stability of coated rhGH was determined by size exclusion chromatography-high performance liquid chromatography (SEC-HPLC). Preclinical delivery and pharmacokinetic studies were conducted in female hairless guinea pigs (HGP) using rhGH coated microneedle patches at 0.5 and 1 mg doses and compared to Norditropin® a commercially approved rhGH subcutaneous injection. Studies demonstrated successful rhGH formulation development and coating on microneedle arrays. The ZP-hGH patches remained stable at 40 °C for six months with no significant change in % aggregates. Pharmacokinetic studies showed that the rhGH-coated microneedle patches, delivered with high efficiency and the doses delivered indicated linearity with average Tmax of 30 min. The absolute bioavailability of the microneedle rhGH patches was similar to subcutaneous Norditropin® injections. These results suggest that ZP-transdermal microneedle patch delivery of rhGH is feasible and may offer an effective and patient-friendly alternative to currently marketed rhGH injectables. Full article
(This article belongs to the Special Issue Advanced Transdermal Drug Delivery)
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340 KiB  
Article
The Flux of Phenolic Compounds through Silicone Membranes
by John Prybylski and Kenneth B. Sloan
Pharmaceutics 2013, 5(3), 434-444; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics5030434 - 21 Aug 2013
Cited by 5 | Viewed by 5191
Abstract
Phenols as a class of molecules have been reported to exhibit higher log maximum fluxes through human stratum corneum, SC, from water, log JMHAQ, than other classes of molecules. This suggests that their corresponding log maximum fluxes through silicone from water, [...] Read more.
Phenols as a class of molecules have been reported to exhibit higher log maximum fluxes through human stratum corneum, SC, from water, log JMHAQ, than other classes of molecules. This suggests that their corresponding log maximum fluxes through silicone from water, log JMPAQ, may be useful to extend the existing n = 63 log JMPAQ database to include more log JMPAQ values greater than 0.0. The log JMPAQ values for n = 7 phenols predicted to give log JMPAQ values greater than 0.0 based on their log JMHAQ values have been experimentally determined. These n = 7 new log JMPAQ values have been added to the existing n = 63 log JMPAQ database to give a new n = 70 database and the n = 7 literature log JMHAQ values have been added to the existing n = 48 log JMHAQ database (matched to the n = 63 log JMPAQ database) to give a new n = 55 database. The addition of the n = 7 phenols improved the correlations of these flux databases when fitted to the Roberts-Sloan equation, RS, as well as the correlation between the matched experimental (Exp.) log JMPAQ with the Exp. log JMHAQ. Full article
(This article belongs to the Special Issue Advanced Transdermal Drug Delivery)
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4025 KiB  
Article
Transdermal Delivery of Adriamycin to Transplanted Ehrlich Ascites Tumor in Mice
by Masataka Shiozuka, Yoshiaki Nonomura and Ryoichi Matsuda
Pharmaceutics 2013, 5(3), 385-391; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics5030385 - 11 Jul 2013
Cited by 2 | Viewed by 6578
Abstract
There is considerable interest in the skin as a site of anti-cancer drug application. Nevertheless, the skin poses a formidable barrier to drug penetration, thereby limiting topical and transdermal bioavailability. However, we previously showed that a thioglycolate-based depilatory agent increases the drug permeability [...] Read more.
There is considerable interest in the skin as a site of anti-cancer drug application. Nevertheless, the skin poses a formidable barrier to drug penetration, thereby limiting topical and transdermal bioavailability. However, we previously showed that a thioglycolate-based depilatory agent increases the drug permeability of mouse skin. In the present report, we investigated the skin permeability and efficacy of the anti-cancer drug adriamycin increased when administered transdermally to mice in combination with a thioglycolate-based depilatory agent. Adriamycin in combination with depilatory treatment reduced Ehrlich tumor growth in hairless mice about the weight and size of harvested tumors. In addition, our delivery method for adriamycin increased the therapeutic effectiveness of this agent by decreasing toxicity. Moreover, measurement of adriamycin autofluorescence revealed that topically applied adriamycin penetrate the dermis after depilatory agent treatment. These results indicate that the transdermal delivery of anti-cancer drugs is feasible by handy pretreatment of the skin with a thioglycolate-based depilatory agent. Full article
(This article belongs to the Special Issue Advanced Transdermal Drug Delivery)
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Review

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327 KiB  
Review
Overcoming the Cutaneous Barrier with Microemulsions
by Luciana B. Lopes
Pharmaceutics 2014, 6(1), 52-77; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics6010052 - 28 Feb 2014
Cited by 138 | Viewed by 9888
Abstract
Microemulsions are fluid and isotropic formulations that have been widely studied as delivery systems for a variety of routes, including the skin. In spite of what the name suggests, microemulsions are nanocarriers, and their use as topical delivery systems derives from their multiple [...] Read more.
Microemulsions are fluid and isotropic formulations that have been widely studied as delivery systems for a variety of routes, including the skin. In spite of what the name suggests, microemulsions are nanocarriers, and their use as topical delivery systems derives from their multiple advantages compared to other dermatological formulations, such as ease of preparation, thermodynamic stability and penetration-enhancing properties. Composition, charge and internal structure have been reported as determinant factors for the modulation of drug release and cutaneous and transdermal transport. This manuscript aims at reviewing how these and other characteristics affect delivery and make microemulsions appealing for topical and transdermal administration, as well as how they can be modulated during the formulation design to improve the potential and efficacy of the final system. Full article
(This article belongs to the Special Issue Advanced Transdermal Drug Delivery)
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405 KiB  
Review
Mathematical Model to Predict Skin Concentration after Topical Application of Drugs
by Hiroaki Todo, Takeshi Oshizaka, Wesam R. Kadhum and Kenji Sugibayashi
Pharmaceutics 2013, 5(4), 634-651; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics5040634 - 16 Dec 2013
Cited by 21 | Viewed by 8656
Abstract
Skin permeation experiments have been broadly done since 1970s to 1980s as an evaluation method for transdermal drug delivery systems. In topically applied drug and cosmetic formulations, skin concentration of chemical compounds is more important than their skin permeations, because primary target site [...] Read more.
Skin permeation experiments have been broadly done since 1970s to 1980s as an evaluation method for transdermal drug delivery systems. In topically applied drug and cosmetic formulations, skin concentration of chemical compounds is more important than their skin permeations, because primary target site of the chemical compounds is skin surface or skin tissues. Furthermore, the direct pharmacological reaction of a metabolically stable drug that binds with specific receptors of known expression levels in an organ can be determined by Hill’s equation. Nevertheless, little investigation was carried out on the test method of skin concentration after topically application of chemical compounds. Recently we investigated an estimating method of skin concentration of the chemical compounds from their skin permeation profiles. In the study, we took care of “3Rs” issues for animal experiments. We have proposed an equation which was capable to estimate animal skin concentration from permeation profile through the artificial membrane (silicone membrane) and animal skin. This new approach may allow the skin concentration of a drug to be predicted using Fick’s second law of diffusion. The silicone membrane was found to be useful as an alternative membrane to animal skin for predicting skin concentration of chemical compounds, because an extremely excellent extrapolation to animal skin concentration was attained by calculation using the silicone membrane permeation data. In this chapter, we aimed to establish an accurate and convenient method for predicting the concentration profiles of drugs in the skin based on the skin permeation parameters of topically active drugs derived from steady-state skin permeation experiments. Full article
(This article belongs to the Special Issue Advanced Transdermal Drug Delivery)
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