Dissolving Microneedles Loaded with Gestodene: Fabrication and Characterization In Vitro and In Vivo

孕烯 药代动力学 药品 体内 医学 药理学 生物医学工程 血浆浓度 人口 研究方法 计划生育 生物 环境卫生 生物技术
作者
Xueyan Duan,Jianan Ma,Meiying Ning,Yunhua Gao
标识
DOI:10.5812/ijpr-131819
摘要

Gestodene (GEST) is widely used in female contraception. It is currently being used as an oral contraceptive. However, unfortunately, oral contraceptives are often associated with several bothersome side effects and poor compliance. Therefore, a sustained delivery system for GEST to overcome these shortcomings is highly desirable.The present study successfully developed a kind of novel dissolving microneedles (DMNs) with a potential for sustained release and a minimally invasive intradermal treatment of GEST.The dissolving microneedles containing GEST were fabricated using polyvinylpyrrolidone as the base material. The characteristics in vitro and pharmacokinetics in vivo of GEST-loaded DMNs were investigated.The results showed that the microneedle could pierce the porcine skin and release the drug at an average dose of 20µg/cm2 daily for seven days. The pharmacokinetic experiment of the microneedles indicated that the plasma level of GEST in rats increased with increasing drug dosage, and the plasma drug concentration-time curves were much flatter compared with subcutaneous injection and oral administration. In addition, no cutaneous irritation was observed.GEST-loaded DMNs may be a promising intradermal sustained delivery system for contraceptive use.
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