Abstract
Natural amino acids and their derivatives are excellent building blocks of polymers for various biomedical applications owing to the non-toxicity, biocompatibility, and ease of multifunctionalization. In the present review, we summarized the common approaches to designing and constructing functional polymeric micelles based on basic amino acids including lysine, histidine, and arginine and highlighted their applications as drug carriers for cancer therapy. Different polypeptide architectures including linear polypeptides and dendrimers were developed for efficient drug loading and delivery. Besides, polylysine- and polyhistidine-based micelles could enable pH-responsive drug release, and polyarginine can realize enhanced membrane penetration and gas therapy by generating metabolites of nitric oxide (NO). It is worth mentioning that according to the structural or functional characteristics of basic amino acids and their derivatives, key points for designing functional micelles with excellent drug delivery efficiency are importantly elaborated in order to pave the way for exploring micelles based on basic amino acids.
Highlights
In the past few decades, micelles, as an effective drug delivery system, have considerably attracted worldwide attention for the treatment of tumors
This review describes the design and construction of drugloaded micelles based on the three basic amino acids or their derivatives from the following perspectives: 1) Design of micelles based on the position and role of lysine in the micelle skeleton
The non-cross-linked and cross-linked micelles were separately incubated in PBS with 50% serum for 30 min, and the scattered light intensity of the former decreased to 49% of the initial intensity, while that of the latter dropped about 5%
Summary
In the past few decades, micelles, as an effective drug delivery system, have considerably attracted worldwide attention for the treatment of tumors. As pH is below 7.0, the hydrophilicity of poly(L-histidine) chain segment increased for ionization of histidine imidazole groups, leading to instability of micellar core (Jin et al, 2014) This pHresponsive property is good for drug release outside tumor cells. The added amount of PLLA-b-PEG block copolymer had an effect on the pH value of micellar dissociation These results suggested that appropriate proportion of PLLA-b-PEG polymer could improve the discrimination and sensitivity of the mixed micelles to the acidic extracellular pH of the tumoral microenvironment. In another example, poly(histidine-co-phenylalanine) (PHP) was synthesized via the ring-opening polymerization of the benzyl-protected L-histidine NCA and L-phenylalanine NCA. It is helpful for designing arginine-rich micelles to enhance the therapeutic effect of tumor
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
