Lili Cui, Lichun Zha, Jiahua Mei, Rui Xue, Jie Wang, Ziwen Zhang, Yunshu Ma
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引用次数: 0
Abstract
Tetramethylpyrazine (TMP), a potent coronary vasodilator, enhances myocardial perfusion and shows promise for treating cardiovascular disorders. Its clinical utility is limited, however, by the short half-life of conventional tablets and injections, which necessitates frequent dosing. To overcome this drawback, we developed a transdermal patch that co-loadsTMP and borneol (BO-TMP). After optimization, patches containing 3% borneol as a permeation enhancer, exhibiting the highest cumulative penetration amount of TMP (6.80 mg·cm-2 over 24 h) in vitro. Pharmacokinetic profiling revealed that borneol markedly improved TMP exposure. Cmax rose from (1.96 ± 0.27) to (2.88 ± 0.72) mg/L, and AUC0-t expanded from (47.73 ± 6.93) to (73.18 ± 13.86) mg/L*h in plasma; Cmax rose from (12.99 ± 2.28) to (15.33 ± 4.24) mg/L, and AUC0-t expanded from (220.86 ± 53.88) to (374.55 ± 111.84) mg/L*h in skin, Cmax rose from (0.87 ± 0.12) to (6.20 ± 0.84) mg/L, and AUC0-t expanded from (13.08 ± 3.35) to (79.80 ± 16.31) mg/L*h in heart when BO-TMP patches were administrated compared with TMP patches. Tissue distribution studies demonstrated that borneol redirected TMP distribution, shifting the order of tissue abundance from liver > kidney > brain > spleen > heart > lung to liver > kidney > heart > brain > spleen > lung, and thus enriched the drug at its therapeutic site. By selectively heightening cardiac exposure, the BO-TMP patch transform TMP into a cardiovascular-focused therapy, offering a convenient, long-acting dosage from with the potential to enhance efficacy and improve patient outcomes.
期刊介绍：
The journal provides a unique forum for scientific publication of high-quality research that is exclusively focused on translational aspects of drug delivery. Rationally developed, effective delivery systems can potentially affect clinical outcome in different disease conditions.
Research focused on the following areas of translational drug delivery research will be considered for publication in the journal.
Designing and developing novel drug delivery systems, with a focus on their application to disease conditions;
Preclinical and clinical data related to drug delivery systems;
Drug distribution, pharmacokinetics, clearance, with drug delivery systems as compared to traditional dosing to demonstrate beneficial outcomes
Short-term and long-term biocompatibility of drug delivery systems, host response;
Biomaterials with growth factors for stem-cell differentiation in regenerative medicine and tissue engineering;
Image-guided drug therapy,
Nanomedicine;
Devices for drug delivery and drug/device combination products.
In addition to original full-length papers, communications, and reviews, the journal includes editorials, reports of future meetings, research highlights, and announcements pertaining to the activities of the Controlled Release Society.
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