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Development and evaluation of a tampering resistant transdermal fentanyl patch
Uppsala University, Disciplinary Domain of Science and Technology, Technology, Department of Engineering Sciences, Applied Materials Sciences. (Material in Medicine)
Uppsala University, Disciplinary Domain of Science and Technology, Technology, Department of Engineering Sciences, Applied Materials Sciences. (Material in Medicine)
Uppsala University, Disciplinary Domain of Science and Technology, Technology, Department of Engineering Sciences, Applied Materials Sciences. (Material in Medicine)
2015 (English)In: International Journal of Pharmaceutics, ISSN 0378-5173, E-ISSN 1873-3476, Vol. 488, no 1-2, 102-107 p.Article in journal (Refereed) Published
Place, publisher, year, edition, pages
2015. Vol. 488, no 1-2, 102-107 p.
Keyword [en]
Transdermal patch, Tamper-resistance, Geopolymer, Fentanyl, Abuse, Drug delivery
National Category
Ceramics Substance Abuse
Identifiers
URN: urn:nbn:se:uu:diva-245029DOI: 10.1016/j.ijpharm.2015.04.061ISI: 000355887100013PubMedID: 25913120OAI: oai:DiVA.org:uu-245029DiVA: diva2:790287
Available from: 2015-02-24 Created: 2015-02-24 Last updated: 2017-12-04Bibliographically approved
In thesis
1. Ceramic Materials for Administration of Potent Drugs
Open this publication in new window or tab >>Ceramic Materials for Administration of Potent Drugs
2015 (English)Doctoral thesis, comprehensive summary (Other academic)
Abstract [en]

This thesis aimed to investigate and document the potential of applying ceramics in two specific drug delivery applications: tamper-resistant opioid formulations and transdermal enhancement protrusions.

Geopolymers were developed into the matrix for a tamper-resistant formulation, aiming to protect drug substances from non-medical abuse. The synthesis conditions and excipients composition of the geopolymer-based formulation were modified in this work to facilitate a stable and extended drug delivery. Results showed that 37ºC 100% humidity for 48 hours were applicable conditions to obtain geopolymer with suitable mechanical strength and porosity. Moreover, it was found that the integration of poly(methyl acrylate) into the geopolymer-based formulation could reduce the drug release at low pH and, meanwhile, maintain the mechanical strength. Therefore, the geopolymer-based drug formulations concluded from these studies were applied in oral and transdermal delivery systems. Evidence of the tamper-resistance of geopolymer-based oral and transdermal formulations was documented and compared to the corresponding commercial opioid formulations. The results provided experimental support for the positive effects of geopolymers as drug carriers for the tamper-resistance of oral and transdermal delivery systems.

Self-setting bioceramics, calcium phosphate and calcium sulfate were fabricated into transdermal enhancement protrusions in this work for the first time. Results showed that, under mild conditions, both bioceramics could form pyramid-shaped needles in the micron size. The drug release from these needles could be controlled by the bulk surface area, porosity and degradation of the bioceramics. An in vitro insertion test showed that the bioceramic microneedles had enough mechanical strength to insert into skin. Further optimization on the geometry of needles and the substrate material was also performed. The higher aspect-ratio needles with a flexible and self-swellable substrate could release most of the drug content within 4 hours and could penetrate through the stratum corneum by manual insertion. This study explored the potential application of bioceramics in transdermal enhancement protrusions and showed promising indication of their future developments.

Place, publisher, year, edition, pages
Uppsala: Acta Universitatis Upsaliensis, 2015. 65 p.
Series
Digital Comprehensive Summaries of Uppsala Dissertations from the Faculty of Science and Technology, ISSN 1651-6214 ; 1235
Keyword
Tamper-resistance, Oral formulation, Transdermal formulation, Biomaterials, Microneedles
National Category
Biomaterials Science Ceramics
Identifiers
urn:nbn:se:uu:diva-245031 (URN)978-91-554-9188-8 (ISBN)
Public defence
2015-04-28, Polhemssalen, Lägerhyddsvägen 2, Uppsala, 10:00 (English)
Opponent
Supervisors
Available from: 2015-04-07 Created: 2015-02-24 Last updated: 2015-04-17

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Cai, BingBredenberg, SusanneEngqvist, Håkan

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