Yeo Sooho, Jung Sukkyun, Cho Heui Kyoung, Kim Young Ho, Kim Gi Hwan, Kim Dohyun, Ko Byoung Hyen, Lee Jaehwi
College of Pharmacy, Chung-Ang University, Seoul 06974, Korea.
R&D Center, Megacos, 16, Simin-daero 327 Rd, Dongan-gu, Anyang-si, Gyeonggi-do 14055, Korea.
Pharmaceutics. 2020 Dec 28;13(1):33. doi: 10.3390/pharmaceutics13010033.
Adenosine (AD), which is used for treating wrinkles, exhibits poor skin permeation. The aim of the present study was to develop a cross-linked silicone-based cellulose elastomer as an elastic artificial skin for the treatment of skin wrinkles, a biocompatible lipid-based nano-carrier for enhancing the skin permeation of AD, and a formulation consisting of the lipid-based carrier incorporated in the elastic artificial skin. AD-loaded solid lipid nanoparticles (SLNs) were prepared using a double-emulsion method. Particle characteristics and mechanical properties of SLNs and elastic artificial skin, respectively, were assessed. Skin permeation was evaluated using SkinEthic RHE tissue, a reconstructed human epidermis model. The mean particle size and zeta potential for SLNs ranged from 123.57 to 248.90 nm and -13.23 to -41.23 mV, respectively. The components of neither SLNs nor the elastic artificial skin were cytotoxic, according to cell- and tissue-viability assays and EU classification. SLNs and the elastic artificial skin exhibited sustained drug release for 48 h. The amount of AD released from SLNs and elastic artificial skin was approximately 10 times and 5 times higher, respectively, than that from AD solution. Therefore, elastic artificial skin incorporated with AD-loaded SLNs may serve as a promising topical delivery system for cosmeceutical treatment of skin wrinkles.
用于治疗皱纹的腺苷(AD)皮肤渗透性较差。本研究的目的是开发一种交联硅基纤维素弹性体作为治疗皮肤皱纹的弹性人工皮肤、一种用于增强AD皮肤渗透性的生物相容性脂质基纳米载体,以及一种由掺入弹性人工皮肤中的脂质基载体组成的制剂。采用复乳法制备了载AD固体脂质纳米粒(SLN)。分别评估了SLN和弹性人工皮肤的颗粒特性和力学性能。使用重建人表皮模型SkinEthic RHE组织评估皮肤渗透性。SLN的平均粒径和zeta电位分别为123.57至248.90 nm和-13.23至-41.23 mV。根据细胞和组织活力测定以及欧盟分类,SLN和弹性人工皮肤的成分均无细胞毒性。SLN和弹性人工皮肤表现出48小时的持续药物释放。从SLN和弹性人工皮肤释放的AD量分别比从AD溶液释放的量高约10倍和5倍。因此,掺入载AD SLN的弹性人工皮肤可能成为用于皮肤皱纹美容治疗的有前景的局部给药系统。