Maitani Yoshie, Nakamura Koji, Kawano Kumi
Institute of Medicinal Chemistry and Hoshi University, Ebara 2-4-41, Shinagawa-ku, Tokyo, Japan.
Curr Pharm Biotechnol. 2005 Feb;6(1):81-93. doi: 10.2174/1389201053167194.
Recent advances in biotechnology have promoted biomolecular targeting of drugs, peptides and genes in the treatment and management of major diseases and infections. Therapeutic development of drugs and delivery systems may have various objectives: Systemic drugs require optimal delivery and uptake at target sites; peptide drugs require alternative routes of administration, such as nasal or intestinal absorption; gene medicines need to be delivered efficiently, safely and selectively to diseased areas. The propensity of ligand-modified liposomes to carry drugs and genes to desirable sites has been extensively examined and current reports show considerable progress in this field. Sterylglucoside (SG) is a novel absorption-enhancer of peptide drugs across nasal and intestinal mucosae. Physico-chemical properties and biodistribution of liposomes incorporating SG were studied and compared against the profiles of aglycon and sitosterol derivatives of SG. It was shown that SG particles aided colon drug delivery and increased bioavailability of peptide drugs after nasal and intestinal administration. In addition, they were able to enhance anticancer effects in liver cancer chemotherapy. Biological fate and interaction of SG with hepatocytes support the novel proposition of liver-targeting SG-liposomes.
生物技术的最新进展推动了药物、肽和基因在重大疾病和感染的治疗与管理中的生物分子靶向作用。药物和递送系统的治疗性开发可能有多种目标：全身性药物需要在靶部位实现最佳递送和摄取；肽类药物需要替代给药途径，如鼻腔或肠道吸收；基因药物需要高效、安全且选择性地递送至患病区域。配体修饰脂质体将药物和基因携带至理想部位的倾向已得到广泛研究，目前的报告显示该领域取得了显著进展。甾醇糖苷（SG）是一种新型的肽类药物跨鼻腔和肠道黏膜的吸收增强剂。研究了掺入SG的脂质体的物理化学性质和生物分布，并与SG的苷元及甾醇衍生物的情况进行了比较。结果表明，SG颗粒有助于结肠药物递送，并提高肽类药物经鼻腔和肠道给药后的生物利用度。此外，它们能够增强肝癌化疗中的抗癌效果。SG与肝细胞的生物学命运及相互作用支持了肝靶向SG脂质体这一新概念。
