生物大分子药物口腔黏膜递送研究进展

Research progress of the oral mucosal delivery of biomacromolecules

生物大分子药物的替代给药方式一直是生物大分子药物研究的热点。口腔黏膜因其"柔和"的给药环境、无肝首过效应以及患者依从性好等优点,是生物大分子药物理想的给药部位。由于相对分子质量大、亲水性强的特点,生物大分子药物存在口腔黏膜渗透吸收差、生物利用度低的问题。黏膜促透技术的发展,为生物大分子药物的口腔黏膜递送提供了契机。笔者综述了生物大分子药物口腔黏膜给药中的渗透促进技术、剂型设计、渗透评价3个方面的研究与应用,并对其发展趋势进行了探讨,以期促进生物大分子药物口腔黏膜给药的深入研究。

The alternative administration of biomacromolecules has been a hot topic in the study of biomacromolecules. Oral mucosa is an ideal drug administration site for biomacromolecules because of its gentle drug delivery environment,no hepatic first-pass effect,and good patient compliance. Due to its large molecular weight and strong hydrophilicity,biomacromolecules have poor oral absorption and low bioavailability. The development of mucosal penetration technology provides opportunities for oral mucosal delivery of biomacromolecules. In order to study the oral mucosal administration of biomacromolecules more deeply,we reviewed the research and application of penetration promotion technology,dosage form design,and penetration evaluation in the oral mucosal administration of biomacromolecules,and explored its development trend.