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载有百里香酚的凝胶分散纳米结构脂质载体,设计用于皮肤病理。

Gel-Dispersed Nanostructured Lipid Carriers Loading Thymol Designed for Dermal Pathologies.

机构信息

Department of Pharmacy and Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, Barcelona, Spain.

Department of Biology, Healthcare and Environment, Faculty of Pharmacy and Food Sciences, University of Barcelona, Barcelona, Spain.

出版信息

Int J Nanomedicine. 2024 Feb 7;19:1225-1248. doi: 10.2147/IJN.S433686. eCollection 2024.

Abstract

PURPOSE

is one of the most prevalent dermal disorders affecting skin health and appearance. To date, there is no effective cure for this pathology, and the majority of marketed formulations eliminate both healthy and pathological microbiota. Therefore, hereby we propose the encapsulation of an antimicrobial natural compound (thymol) loaded into lipid nanostructured systems to be topically used against acne.

METHODS

To address this issue, nanostructured lipid carriers (NLC) capable of encapsulating thymol, a natural compound used for the treatment of acne vulgaris, were developed either using ultrasonication probe or high-pressure homogenization and optimized using 2-star factorial design by analyzing the effect of NLC composition on their physicochemical parameters. These NLC were optimized using a design of experiments approach and were characterized using different physicochemical techniques. Moreover, short-term stability and cell viability using HaCat cells were assessed. Antimicrobial efficacy of the developed NLC was assessed in vitro and ex vivo.

RESULTS

NLC encapsulating thymol were developed and optimized and demonstrated a prolonged thymol release. The formulation was dispersed in gels and a screening of several gels was carried out by studying their rheological properties and their skin retention abilities. From them, carbomer demonstrated the capacity to be highly retained in skin tissues, specifically in the epidermis and dermis layers. Moreover, antimicrobial assays against healthy and pathological skin pathogens demonstrated the therapeutic efficacy of thymol-loaded NLC gelling systems since NLC are more efficient in slowly reducing viability, but they possess lower antimicrobial activity against , compared to free thymol.

CONCLUSION

Thymol was successfully loaded into NLC and dispersed in gelling systems, demonstrating that it is a suitable candidate for topical administration against acne vulgaris by eradicating pathogenic bacteria while preserving the healthy skin microbiome.

摘要

目的

是影响皮肤健康和外观的最常见皮肤疾病之一。迄今为止,这种病理还没有有效的治疗方法,大多数市售制剂都消除了健康和病态的微生物群。因此,本文提出将一种抗菌天然化合物(百里香酚)包封到脂质纳米结构系统中,以局部用于治疗痤疮。

方法

为了解决这个问题,开发了能够包封百里香酚的纳米结构脂质载体(NLC),百里香酚是一种用于治疗寻常痤疮的天然化合物,使用超声探头或高压匀质法制备,并通过分析 NLC 组成对其物理化学参数的影响,使用 2-星因子设计进行优化。使用实验设计方法对这些 NLC 进行了优化,并使用不同的物理化学技术对其进行了表征。此外,还评估了使用 HaCat 细胞的短期稳定性和细胞活力。体外和离体评估了所开发的 NLC 的抗菌功效。

结果

开发并优化了包封百里香酚的 NLC,并证明了百里香酚的释放时间延长。该制剂分散在凝胶中,并通过研究其流变性能和皮肤保留能力对几种凝胶进行了筛选。其中,卡波姆表现出高度保留在皮肤组织中的能力,特别是在表皮和真皮层。此外,针对健康和病态皮肤病原体的抗菌试验表明,负载百里香酚的 NLC 凝胶系统具有治疗功效,因为 NLC 在缓慢降低 活力方面更有效,但与游离百里香酚相比,它们对 的抗菌活性较低。

结论

百里香酚成功地负载到 NLC 中并分散在凝胶系统中,表明它是一种适合局部给药治疗寻常痤疮的候选药物,因为它可以消除致病菌,同时保留健康的皮肤微生物组。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2cfa/10859765/cd7c3b0d53f2/IJN-19-1225-g0001.jpg

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