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

IF 4 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Lord Sam Liston, Suranate Phanapithakkun, Nuttakul Pimsarn, Nuttapon Dangkaokhia, Thanat Nakasan, Attawadee Sae Yoon, Hiroaki Todo, Teerapol Srichana, Somchai Sawatdee, Gerard Lee See, Florencio Arce, Pajaree Sakdiset
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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.

局部皮肤给药用含姜黄素Bigels的配方开发与表征。
姜黄素是一种多效分子,由于其抗炎、伤口愈合、抗菌和抗衰老的作用,已被报道可以调节皮肤健康和功能。姜黄素是一种亲脂分子,皮肤渗透性差,导致治疗皮肤病的功效下降。在这项研究中,配制了一种含有姜黄素的bigel,以促进姜黄素的皮肤沉积。一般来说,凝胶由水凝胶(HG)和有机凝胶(OG)组成,并具有这两种体系的理想特性。HG含有2% w/v的HPMC, OG含有Span®60、杏仁油和姜黄素(0.25%),以不同的HG:OG比例在90:10 ~ 10:90之间混合。HG:OG、BG50(50:50)、BG40(60:40)、BG30(70:30)三种配比均可形成淡黄色浑浊光滑凝胶。微滴尺寸为7.10 ~ 30.60µm,微滴结构为0 /w体系。所有bigel配方均表现出假塑性行为,油浸出率低。皮肤渗透实验表明,BG30在角质层、活表皮和真皮层的姜黄素积累量最高,分别是对照OG的1.61±0.17倍和3.63±0.89倍。姜黄素在62.5 ~ 1000 μg/mL浓度下对小鼠成纤维细胞株L929均无毒性。根据L929划痕实验,B30提供了最高的伤口愈合效果。在24 h时,迁移率增加到70.11±1.11,在48 h时增加到100%。这些发现表明,BG30可以潜在地用于局部应用的姜黄素输送。
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来源期刊
AAPS PharmSciTech
AAPS PharmSciTech 医学-药学
CiteScore
6.80
自引率
3.00%
发文量
264
审稿时长
2.4 months
期刊介绍: AAPS PharmSciTech is a peer-reviewed, online-only journal committed to serving those pharmaceutical scientists and engineers interested in the research, development, and evaluation of pharmaceutical dosage forms and delivery systems, including drugs derived from biotechnology and the manufacturing science pertaining to the commercialization of such dosage forms. Because of its electronic nature, AAPS PharmSciTech aspires to utilize evolving electronic technology to enable faster and diverse mechanisms of information delivery to its readership. Submission of uninvited expert reviews and research articles are welcomed.
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