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过氧化苯甲酰和维甲酸的单独溶胶-凝胶微囊化能够实现对皮肤的控释。

Individual sol-gel microencapsulation of benzoyl peroxide and tretinoin enables controlled release onto the skin.

作者信息

Hakak Hila, Neimann Karine, Toledano Ofer, Erlich Maya

机构信息

Sol-Gel Technologies, Ltd., Golda Meir 7, Ness Ziona, Israel.

出版信息

Heliyon. 2024 Jun 1;10(11):e32275. doi: 10.1016/j.heliyon.2024.e32275. eCollection 2024 Jun 15.

Abstract

A combination of benzoyl peroxide (BPO) and tretinoin is recommended for treating acne; however, concurrent administration can be irritating, and coformulation is prevented by BPO-mediated oxidation of tretinoin. In rosacea, benzoyl peroxide has been shown to be efficacious; however, its use has been limited by poor tolerability. To overcome these limitations, the active ingredients can be encapsulated within silica microcapsules. The US Food and Drug Administration has approved 2 products using this technology, a combination of encapsulated benzoyl peroxide and encapsulated tretinoin product for acne vulgaris and encapsulated benzoyl peroxide to treat inflammatory lesions in rosacea. The active ingredients are released through small channels in the silica shell, gradually releasing the active ingredients to the skin. This study describes the stability and release profiles of encapsulated tretinoin and encapsulated benzoyl peroxide from the silica shell in physiologically relevant conditions and provides differentiation from traditional formulations.

摘要

推荐使用过氧化苯甲酰(BPO)和维甲酸联合治疗痤疮;然而,同时给药可能会有刺激性,并且由于BPO介导的维甲酸氧化作用,二者无法制成复方制剂。在酒渣鼻治疗中,已证明过氧化苯甲酰有效;然而,其应用因耐受性差而受到限制。为克服这些局限性,可将活性成分封装在二氧化硅微胶囊中。美国食品药品监督管理局已批准了2种使用该技术的产品,一种是用于寻常痤疮的封装过氧化苯甲酰和封装维甲酸的复方产品,另一种是用于治疗酒渣鼻炎症性皮损的封装过氧化苯甲酰产品。活性成分通过二氧化硅外壳中的小通道释放,将活性成分逐渐释放到皮肤中。本研究描述了在生理相关条件下,封装维甲酸和封装过氧化苯甲酰从二氧化硅外壳中的稳定性和释放曲线,并与传统制剂进行了区分。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0303/11214359/92681ee7bd9c/ga1.jpg

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