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노규빈,금태광,Bashyal Santosh,Seo Jo-Eun,Shrawani Lamichhane,Kim Jeong Hwan,이상길 한국약제학회 2022 Journal of Pharmaceutical Investigation Vol.52 No.1
Background The biopharmaceuticals market has grown rapidly in recent years owing to the low toxicity and high therapeutic efficacy of peptide and protein drugs. However, due to their low stability, biopharmaceuticals have to be administrated via invasive routes, and there is an unmet need for alternative routes. The most familiar and preferred alternative route of administration is the oral route; however, peptide and protein drugs are readily affected by the harsh gastrointestinal environment, resulting in low oral bioavailability. Lipid-based drug delivery systems (LDDSs) for oral administration protect the incorporated drugs and enhance their absorption in the GI tract. However, only lipophilic substances can be stably incorporated in LDDSs, and hydrophilic peptides and proteins require lipidation via, e.g., hydrophobic ion pairing (HIP). Area covered This review discusses the issues that hamper the oral administration of peptides and proteins and introduces HIP and LDDSs as strategies to overcome these. The principle of HIP complexation, the parameters to be considered for complexation, and the various counterions used are described. As for LDDSs, the advantages of self-emulsifying drug delivery systems (SEDDSs), which are suitable for oral peptide and protein delivery, and in vivo study results are described. Expert opinion HIP complexes are prepared based on an understanding of the characteristics of drugs and counterions. HIP complexes of peptides and proteins in the oil phase of SEDDSs are protected from the GI environment and therefore, improved absorption is expected. Although their fundamental mechanisms remain unclear and require further study, HIPincorporated SEDDSs provide a potential strategy for oral peptide and protein delivery.
Cell penetrating peptides as an innovative approach for drug delivery; then, present and the future
Santosh Bashyal,노규빈,금태광,최영욱,이상길 한국약제학회 2016 Journal of Pharmaceutical Investigation Vol.46 No.3
With the rapid development of biotechnology, various macromolecules as therapeutic agents have made drug delivery an important field of research. However, these are being commercialized as injection form. Due to low patient compliance, various non-invasive routes emerge as a promising strategy. Cell penetrating peptides (CPPs) have shown to assist in efficient and non-toxic manner. They provide ample evidence to deliver of many cargoes ranging from small molecules to proteins and even nanocarriers for various applications. This review briefly discusses about introduction of CPPs, history, cellular uptake mechanisms and various possible alternative routes for CPP-conjugated drug delivery system. It also aims to give a perspective on present status of CPP-mediated research, clinical development, possible obstacles as well as future opportunities. Thus, development of novel CPPs that are safe, tissue-specific and highly efficient will be exemplified and become ideal vehicles for therapeutic delivery in near future.