Mazia Renata Sespede, de Araújo Pereira Raphaela Regina, de Francisco Lizziane Maria Belloto, Natali Maria Raquel Marçal, Dias Filho Benedito Prado, Nakamura Celso Vataru, Bruschi Marcos Luciano, Ueda-Nakamura Tânia
Programa de Pós-graduação em Ciências Farmacêuticas, Universidade Estadual de Maringá, Maringá, Paraná, Brazil.
Programa de Pós-graduação em Ciências Farmacêuticas-Faculdade de Ciências Farmacêuticas de Araraquara, Universidade Estadual Paulista "Júlio de Mesquita Filho", Araraquara, São Paulo, Brazil.
J Pharm Sci. 2016 Jan;105(1):113-21. doi: 10.1016/j.xphs.2015.11.016. Epub 2016 Jan 13.
The aim of the present work was to develop a topical delivery system that contains Brazilian green propolis extract (PE-8) to increase efficiency and convenience when applied to herpetic lesions. The cytotoxicity and antiherpetic activity was determined in vitro and in vivo. The PE-8 was added to a system that contained poloxamer 407 and carbopol 934P. The in vitro characterization of the system included rheological studies, texture profile analysis, and mucoadhesion analysis. The PE-8 inhibited the virus during the phase of viral infection, induced virion damage, and exhibited an ability to protect cells from viral infection. The system had advantageous mucoadhesive properties, including a suitable gelation temperature of approximately 25°C for topical delivery, a desirable textural profile, and pseudoplastic behavior. The in vitro release study showed a rapid initial release of the PE-8 in the first 3 h, and the rate of drug release remained constant for up to 24 h. The system appeared to be macroscopically and microscopically innocuous to skin tissue. Therefore, the mucoadhesive thermoresponsive system that contained the PE-8 appears to be promising for increasing bioavailability and achieving prolonged release of the PE-8 when applied to skin lesions caused by herpes simplex virus type 1.
本研究的目的是开发一种局部给药系统,该系统含有巴西绿蜂胶提取物(PE-8),以提高应用于疱疹性病变时的效率和便利性。在体外和体内测定了其细胞毒性和抗疱疹活性。将PE-8添加到含有泊洛沙姆407和卡波姆934P的系统中。该系统的体外特性包括流变学研究、质地剖面分析和粘膜粘附分析。PE-8在病毒感染阶段抑制病毒,诱导病毒体损伤,并表现出保护细胞免受病毒感染的能力。该系统具有有利的粘膜粘附特性,包括适合局部给药的约25°C的胶凝温度、理想的质地剖面和假塑性行为。体外释放研究表明,PE-8在最初3小时内迅速释放,药物释放速率在长达24小时内保持恒定。该系统在宏观和微观上对皮肤组织似乎是无害的。因此,含有PE-8的粘膜粘附热响应系统在应用于1型单纯疱疹病毒引起的皮肤病变时,似乎有望提高生物利用度并实现PE-8的长效释放。