期刊
JOURNAL OF CONTROLLED RELEASE
卷 180, 期 -, 页码 71-80出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.jconrel.2014.02.007
关键词
Microneedles; Transdermal; Ibuprofen; Biocompatibility
资金
- BBSRC [BB/FOF/287, BB/E020534/1]
- BBSRC [BB/E020534/1] Funding Source: UKRI
- Biotechnology and Biological Sciences Research Council [BB/E020534/1] Funding Source: researchfish
We describe formulation and evaluation of novel dissolving polymeric microneedle (MN) arrays for the facilitated delivery of low molecular weight, high dose drugs. Ibuprofen sodium was used as the model here and was successfully formulated at approximately 50% w/w in the dry state using the copolymer poly(methylvinylether/maleic acid). These MNs were robust and effectively penetrated skin in vitro, dissolving rapidly to deliver the incorporated drug. The delivery of 1.5 mg ibuprofen sodium, the theoretical mass of ibuprofen sodium contained within the dry MN alone, was vastly exceeded, indicating extensive delivery of the drug loaded into the baseplates. Indeed in in vitro transdermal delivery studies, approximately 33 mg (90%) of the drug initially loaded into the arrays was delivered over 24 h. Iontophoresis produced no meaningful increase in delivery. Biocompatibility studies and in vivo rat skin tolerance experiments raised no concerns. The blood plasma ibuprofen sodium concentrations achieved in rats (263 mu g ml(-1) at the 24 h time point) were approximately 20 times greater than the human therapeutic plasma level. By simplistic extrapolation of average weights from rats to humans, a MN patch design of no greater than 10 cm(2) could cautiously be estimated to deliver therapeutically-relevant concentrations of ibuprofen sodium in humans. This work, therefore, represents a significant progression in exploitation of MN for successful transdermal delivery of a much wider range of drugs. (C) 2014 Elsevier B.V. All rights reserved.
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