Delivery Systems for Biomolecules, From Biologic Pathway to Chemical Design
Purpose: To demonstrate the feasibility of three rationally designed synthetic systems for sustainedrelease delivery of native proteins, efficient transdermal delivery of polypeptides, and responsive carrier system for delivery of nucleotides. Methods: For protein sustained-release, an aqueous-aqueous emulsion was used to load proteins in dextran fine particles without contacting with water-oil or waterair interfaces prior to microencapsulation into PLGA microsphaeres. For transdermal delivery of polvpeptides. a phase-transition microneedle patch was developed, by which lipophobic drugs pre-loaded in the microneedles was released to the dermis layer by swelling of the needle tips. For nucleotides carriers, an endogenous gene condenser, spermine, was polymerized via a pH-responsive degradable linkage. Results: Proteins protected in the dextran microenvironment were released from PLGA microspheres in native form with minimal initial burst. Insulin was released transdermaly from the swollen microneedles without depositing the needle tip materials. The pHresponsive polyspermine showed improved gene silencing activity without causing cytotoxicity. Conclusion: Some long-standing hurdles in developing synthetic delivery systems may best be addressed by rational design on the basis of understanding of biological pathways.
protein sustained-release transdermal microneedles nucleotides cationic polymer polymersome
Tuo Jin
Shanghai Jiao Tong University School of Pharmacy, Shanghai 200240, China
国际会议
The Second Asian Symposium on Pharmaceutical Sciences and Technology(第二届亚洲药物制剂科学研讨会)
西安
英文
49-52
2011-09-19（万方平台首次上网日期，不代表论文的发表时间）