Green Lawrence J, Bhatia Neal D, Toledano Ofer, Erlich Maya, Spizuoco Amy, Goodyear Benjamin C, York Jean Philippe, Jakus Jeannette
George Washington University School of Medicine, Washington, DC, USA.
Therapeutics Clinical Research, San Diego, CA, USA.
Arch Dermatol Res. 2023 Dec;315(10):2787-2793. doi: 10.1007/s00403-023-02725-z. Epub 2023 Oct 4.
Microencapsulation has received extensive attention because of its various applications. Since its inception in the 1940s, this technology has been used across several areas, including the chemical, food, and pharmaceutical industries. Over-the-counter skin products often contain ingredients that readily and unevenly degrade upon contact with the skin. Enclosing these substances within a silica shell can enhance their stability and better regulate their delivery onto and into the skin. Silica microencapsulation uses silica as the matrix material into which ingredients can be embedded to form microcapsules. The FDA recognizes amorphous silica as a safe inorganic excipient and recently approved two new topical therapies for the treatment of rosacea and acne. The first approved formulation uses a novel silica-based controlled vehicle delivery technology to improve the stability of two active ingredients that are normally not able to be used in the same formulation due to potential instability and drug degradation. The formulation contains 3.0% benzoyl peroxide (BPO) and 0.1% tretinoin topical cream to treat acne vulgaris in adults and pediatric patients. The second formulation contains silica microencapsulated 5.0% BPO topical cream to treat inflammatory rosacea lesions in adults. Both formulations use the same amorphous silica sol-gel microencapsulation technology to improve formulation stability and skin compatibility parameters.
微胶囊化因其多种应用而受到广泛关注。自20世纪40年代问世以来,这项技术已在多个领域得到应用,包括化学、食品和制药行业。非处方皮肤产品通常含有与皮肤接触后容易且不均匀降解的成分。将这些物质包裹在二氧化硅壳内可以提高它们的稳定性,并更好地控制它们在皮肤表面和进入皮肤的释放。二氧化硅微胶囊化使用二氧化硅作为基质材料,成分可以嵌入其中形成微胶囊。美国食品药品监督管理局(FDA)认可无定形二氧化硅为一种安全的无机辅料,并且最近批准了两种用于治疗酒渣鼻和痤疮的新局部疗法。首个获批的制剂使用了一种新型的基于二氧化硅的控释载体技术,以提高两种活性成分的稳定性,这两种活性成分由于潜在的不稳定性和药物降解通常不能用于同一制剂中。该制剂含有3.0%的过氧化苯甲酰(BPO)和0.1%的维甲酸局部乳膏,用于治疗成人和儿科患者的寻常痤疮。第二种制剂含有二氧化硅微胶囊化的5.0%BPO局部乳膏,用于治疗成人的炎性酒渣鼻皮损。两种制剂都使用相同的无定形二氧化硅溶胶-凝胶微胶囊化技术来提高制剂稳定性和皮肤相容性参数。