Bergamot waste derived lipid nanosystems as novel excipients for (trans)dermal drug delivery

IF 4.5 3区医学 Q1 PHARMACOLOGY & PHARMACY

Journal of Drug Delivery Science and Technology Pub Date : 2025-05-26 DOI:10.1016/j.jddst.2025.107085

Paola Volonté , Caterina Ricci , Sebastiano Arnoldi , Gabriella Roda , Elena Del Favero , Francesco Puoci , Paola Minghetti , Silvia Franzè , Francesco Cilurzo

{"title":"Bergamot waste derived lipid nanosystems as novel excipients for (trans)dermal drug delivery","authors":"Paola Volonté , Caterina Ricci , Sebastiano Arnoldi , Gabriella Roda , Elena Del Favero , Francesco Puoci , Paola Minghetti , Silvia Franzè , Francesco Cilurzo","doi":"10.1016/j.jddst.2025.107085","DOIUrl":null,"url":null,"abstract":"<div><div>Inedible waste from the bergamot processing industry is typically used to produce essential oil, parfums, pectin etc. Nevertheless, the discarded bergamot peels can still serve as a valuable source of novel lipid ingredients. This study explores the potential of using lipid components from bergamot peels (BLCs) to create lipid-based nanosystems (LBNs) for skin application.</div><div>BLCs were extracted and characterized by GC/MS and ATR-FTIR. LBNs were prepared by hot melt homogenization, and their ultrastructure was studied by cryo-EM and SAXS. Ibuprofen (IB) was chosen as model drug. The <em>in vitro</em> skin permeation pattern of IB either loaded in LBNs (IB-LBNs) or co-administered with empty LBNs was studied using porcine skin.</div><div>The LBNs had a mean diameter of about 150 nm and a core-shell structure. LBNs increased the IB flux through porcine skin by a factor of three, both in IB-LBNs form and after co-administration with the free drug solution. This data suggests that BLCs act as skin penetration enhancers rather than drug carriers. ATR-FTIR results further indicated that BLCs perturb the structure of stratum corneum lipids, likely due to the presence of unsaturated fatty acid esters in BLCs extract.</div><div>In conclusion, BLCs could be promising novel and natural excipients for the design of cutaneous preparations.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"110 ","pages":"Article 107085"},"PeriodicalIF":4.5000,"publicationDate":"2025-05-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Drug Delivery Science and Technology","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S1773224725004885","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}

引用次数: 0

Abstract

Inedible waste from the bergamot processing industry is typically used to produce essential oil, parfums, pectin etc. Nevertheless, the discarded bergamot peels can still serve as a valuable source of novel lipid ingredients. This study explores the potential of using lipid components from bergamot peels (BLCs) to create lipid-based nanosystems (LBNs) for skin application.

BLCs were extracted and characterized by GC/MS and ATR-FTIR. LBNs were prepared by hot melt homogenization, and their ultrastructure was studied by cryo-EM and SAXS. Ibuprofen (IB) was chosen as model drug. The in vitro skin permeation pattern of IB either loaded in LBNs (IB-LBNs) or co-administered with empty LBNs was studied using porcine skin.

The LBNs had a mean diameter of about 150 nm and a core-shell structure. LBNs increased the IB flux through porcine skin by a factor of three, both in IB-LBNs form and after co-administration with the free drug solution. This data suggests that BLCs act as skin penetration enhancers rather than drug carriers. ATR-FTIR results further indicated that BLCs perturb the structure of stratum corneum lipids, likely due to the presence of unsaturated fatty acid esters in BLCs extract.

In conclusion, BLCs could be promising novel and natural excipients for the design of cutaneous preparations.

查看原文本刊更多论文

佛手柑废弃物衍生的脂质纳米系统作为经皮给药的新型赋形剂

佛手柑加工工业产生的不可食用废弃物通常用于生产精油、香水、果胶等。然而，废弃的佛手柑皮仍然可以作为一种有价值的来源，新的脂质成分。本研究探索了利用佛手柑皮脂质成分（blc）创建用于皮肤应用的脂质纳米系统（lbn）的潜力。采用GC/MS和ATR-FTIR对BLCs进行了提取和表征。采用热熔均质法制备了lbn，并用低温电镜和SAXS对其超微结构进行了研究。选择布洛芬（IB）作为模型药物。用猪皮肤研究了负载于lbn （IB- lbn）或与空lbn共给药的IB的体外皮肤渗透模式。lbn的平均直径约为150 nm，具有核壳结构。无论是以IB- lbn形式还是与游离药物溶液共同给药后，lbn通过猪皮肤的IB通量都增加了三倍。这一数据表明，blc的作用是促进皮肤渗透，而不是药物载体。ATR-FTIR结果进一步表明，blc可能由于blc提取物中存在不饱和脂肪酸酯而扰乱了角质层脂质结构。总之，blc是一种很有前途的新型天然赋形剂，可用于皮肤制剂的设计。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

求助全文

约1分钟内获得全文求助全文

来源期刊

Journal of Drug Delivery Science and Technology 医学-药学

CiteScore

8.00

自引率

8.00%

发文量

879

审稿时长

94 days

期刊介绍： The Journal of Drug Delivery Science and Technology is an international journal devoted to drug delivery and pharmaceutical technology. The journal covers all innovative aspects of all pharmaceutical dosage forms and the most advanced research on controlled release, bioavailability and drug absorption, nanomedicines, gene delivery, tissue engineering, etc. Hot topics, related to manufacturing processes and quality control, are also welcomed.