Topical application of sebacoyl dinalbuphine ester-loaded nanostructured lipid carriers alleviate pruritus in scratching mouse model

研究成果: Article同行評審

2 引文 斯高帕斯(Scopus)

摘要

Sebacoyl dinalbuphine ester (SDE) is a nalbuphine (NA) prodrug capable of biotransformation in vivo and prolong the duration of NA, maximize its effect in pain and pruritus management. However, the large molecular weight, low skin penetration, and stability concerns of SDE make it difficult to be used in local skin delivery. Nanostructured lipid carrier (NLC) is a lipid-based nanoparticulate system that has the potential for formulating SDE in order to promote drug delivery through the skin. The aim of this study was to develop SDE-loaded NLC formulations (SDE-NLC) with good stability, sustained release characteristics, and sufficient antipruritic effect. SDE was successfully encapsulated into NLC and the formulation increased the stability of SDE, enhanced skin penetration through hair follicles, and sustained SDE release during pruritus management. We also demonstrated that topical application of SDE-NLCs significantly reduced the number of scratches in pruritus-induced mice. Both NA and SDE were found in the skin strata, but only NA was detectable in the plasma, indicating rapid conversion of SDE into NA. All results demonstrated that SDE-NLC formulation protected SDE from degradation in vitro, while the released prodrug was converted into NA in vivo and extended antipruritic effect. The formulation has the potential of improving the life quality of patients with chronic pruritus.

原文English
文章編號120400
期刊International Journal of Pharmaceutics
600
DOIs
出版狀態Published - 2021 五月 1

All Science Journal Classification (ASJC) codes

  • 藥學科學

指紋

深入研究「Topical application of sebacoyl dinalbuphine ester-loaded nanostructured lipid carriers alleviate pruritus in scratching mouse model」主題。共同形成了獨特的指紋。

引用此