Hydrophilic Natural Polylysine as Drug Nanocarrier for Preparation of Helical Delivery System

Abstract

Polypeptide materials have clear secondary structure and biodegradability, which can be further modified and functionalized, so that they can be employed as therapeutic agents in clinical applications. PEGylation of polylysine (PEG-PLL) is a kind of safe and effective nanocarrier that is utilized for gene and drug delivery. However, PEG-PLL needs to be produced through chemical synthesis, which is expensive and difficult to obtain. We hope to simplify the nanocarrier and use hydrophilic natural polylysine (PLL) to develop a high-efficacy delivery system. To evaluate the possibility of PLL as nanocarriers, methotrexate (MTX) is selected as a model drug and PEG-PLL is utilized as control nanocarriers. The experimental results showed that PLL is an ideal polypeptide to prepare MTX-loaded PLL nanoparticles (PLL/MTX NPs). Compared with PEG-PLL as nanocarriers, PLL/MTX NPs showed higher drug-loading content (58.9%) and smaller particle sizes (113.7 nm). Moreover, the shape of PLL/MTX NPs was a unique helical nanorod. The PLL/MTX NPs had good storage stability, media stability, and sustained release effect. Animal research demonstrated that PLL/MTX NPs could improve the anti-tumor activity of MTX, the antitumor efficacy is enhanced 1.9-fold and 1.2-fold compared with MTX injection and PEG-PLL/MTX NPs, respectively. To sum up, natural polymer PLL is an ideal nano drug delivery carrier which has potential clinical applications.

A Celastrol Drug Delivery System Based on PEG Derivatives: The Structural Effects of Nanocarriers

“…The dialysis membrane (MWCO 8000~14,000) was purchased from Spectrum Laboratories Inc. (Los Angeles, CA, USA). The 4T1 cell line, cell culture materials, including 96-well plates, an RPMI 1640 medium, phosphate-buffered saline (PBS), 0.25% trypsin, and fetal bovine serum were obtained according to previous papers [ 36 ]. Acetonitrile and methanol were chromatographically pure and purchased from Scientific Fisher (Hampton, NH, USA).…”