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含姜黄素用于皮肤局部给药的双凝胶剂的处方开发与表征

Formulation Development and Characterization of Bigels Containing Curcumin for Topical Skin Delivery.

作者信息

Liston Lord Sam, Phanapithakkun Suranate, Pimsarn Nuttakul, Dangkaokhia Nuttapon, Nakasan Thanat, Sae Yoon Attawadee, Todo Hiroaki, Srichana Teerapol, Sawatdee Somchai, See Gerard Lee, Arce Florencio, Sakdiset Pajaree

机构信息

School of Pharmacy, Walailak University, 222 Thaiburi, Nakhon Si Thammarat, 80161, Thasala, Thailand.

Drug and Cosmetics Excellence Center, Walailak University, Nakhon Si Thammarat, 80161, Thasala, Thailand.

出版信息

AAPS PharmSciTech. 2025 Jun 27;26(6):175. doi: 10.1208/s12249-025-03166-9.


DOI:10.1208/s12249-025-03166-9
PMID:40579664
Abstract

Curcumin, a pleiotropic molecule, has been reported to modulate skin health and functions owing to its anti-inflammation, wound healing, antimicrobial, and anti-aging effects. Curcumin, a lipophilic molecule, exhibits poor skin penetration that results in decreased efficacy in treating skin diseases. In this study, a bigel containing curcumin was formulated to enhance skin deposition of curcumin. Generally, bigels are composed of hydrogel (HG) and organogel (OG) and feature the ideal characteristics of both systems. The HG contained HPMC 2% w/v, and the OG contained Span® 60, almond oil, and curcumin (0.25%) mixed in different HG:OG proportions from 90:10 to 10:90. Three ratios of HG:OG, BG50 (50:50), BG40 (60:40), and BG30 (70:30) successfully formed yellowish turbid smooth bigels. The bigels were characterized as an o/w system with microdroplet size (7.10-30.60 µm) under a microscope. All bigel formulations showed pseudoplastic behavior and had low oil leaching. Skin permeation experiments revealed that BG30 provided the highest curcumin accumulation in the stratum corneum, and viable epidermis and dermis, which was higher than the control OG for 1.61 ± 0.17 and 3.63 ± 0.89-fold, respectively. All bigels were nontoxic on the murine fibroblast cell line L929 at 62.5-1,000 μg/mL of curcumin. B30 provided the highest wound healing effect as determined by the L929 scratch assay. The % migration increased to 70.11 ± 1.11 at 24 h and to 100% at 48 h. These findings suggest that BG30 could be potentially used to deliver curcumin intended for topical applications.

摘要

姜黄素是一种具有多种功能的分子,据报道,由于其抗炎、伤口愈合、抗菌和抗衰老作用,它能够调节皮肤健康和功能。姜黄素是一种亲脂性分子,皮肤渗透性较差,导致其治疗皮肤疾病的效果降低。在本研究中,制备了一种含姜黄素的双凝胶,以增强姜黄素在皮肤中的沉积。一般来说,双凝胶由水凝胶(HG)和有机凝胶(OG)组成,兼具两种体系的理想特性。水凝胶含有2% w/v的羟丙基甲基纤维素(HPMC),有机凝胶含有司盘® 60、杏仁油和姜黄素(0.25%),它们以90:10至10:90的不同HG:OG比例混合。三种HG:OG比例,即BG50(50:50)、BG40(60:40)和BG30(70:30)成功形成了淡黄色浑浊的光滑双凝胶。在显微镜下,双凝胶被表征为具有微滴尺寸(7.10 - 30.60 µm)的水包油体系。所有双凝胶制剂均表现出假塑性行为且油浸出率低。皮肤渗透实验表明,BG30在角质层、活表皮和真皮中姜黄素的积累量最高,分别比对照有机凝胶高1.61±0.17倍和3.63±0.89倍。在姜黄素浓度为62.5 - 1000 μg/mL时,所有双凝胶对小鼠成纤维细胞系L929均无毒性。通过L929划痕试验测定,BG30具有最高的伤口愈合效果。迁移率在24小时时增加到70.11±1.11%,在48小时时增加到100%。这些发现表明,BG30可能潜在地用于递送用于局部应用的姜黄素。

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本文引用的文献

[1]
The interplay of skin architecture and cellular dynamics in wound healing: Insights and innovations in care strategies.

Tissue Cell. 2024-12

[2]
Evaluation of Emulgel and Nanostructured Lipid Carrier-Based Gel Formulations for Transdermal Administration of Ibuprofen: Characterization, Mechanical Properties, and Ex-Vivo Skin Permeation.

AAPS PharmSciTech. 2024-5-31

[3]
Advancements in Dermatological Applications of Curcumin: Clinical Efficacy and Mechanistic Insights in the Management of Skin Disorders.

Clin Cosmet Investig Dermatol. 2024-5-13

[4]
Potential of Curcumin in the Management of Skin Diseases.

Int J Mol Sci. 2024-3-23

[5]
Cutaneous Pharmacokinetics of Topically Applied Novel Dermatological Formulations.

AAPS PharmSciTech. 2024-2-27

[6]
Topical drug delivery strategies for enhancing drug effectiveness by skin barriers, drug delivery systems and individualized dosing.

Front Pharmacol. 2024-1-16

[7]
Hydrogels and Wound Healing: Current and Future Prospects.

Gels. 2024-1-5

[8]
Clinical Studies on Topical Curcumin.

Skin Pharmacol Physiol. 2023

[9]
Development and Comparative Evaluation of Ciprofloxacin Nanoemulsion-Loaded Bigels Prepared Using Different Ratios of Oleogel to Hydrogels.

Gels. 2023-7-23

[10]
A biocompatible lipid-based bigel for topical applications.

Eur J Pharm Biopharm. 2023-9

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