Core–shell-type polymer–lipid nanoparticles for the transdermal delivery of daidzein

Micro & nano letters

article

Zaitongguli Wusiman¹  Liang Sun¹  Tiantian Zuo¹  Yunzhi Yin¹  Xiaoming Yang¹  Qi Shen¹ 

[1] Department of Pharmaceutics, School of Pharmacy, Shanghai Jiao Tong University

关键词: nanoparticles;    drugs;    skin;    particle size;    encapsulation;    drug delivery systems;    polymers;    nanomedicine;    diseases;    optical microscopy;    core–shell-type polymer–lipid nanoparticles;    transdermal delivery;    daidzein;    drug-loading rate;    DZ–polymer-azone–lipid nanoparticles;    skin penetration experiment;    DZ–polymer–lipid nanoparticles;    Chinese herb;    water solubility;    confocal laser scanning microscopy;    encapsulation efficiency;   

DOI  :  10.1049/mnl.2018.5095

学科分类：计算机科学（综合）

来源: Wiley

【 摘 要 】

5-Fluorouracil is one of the commonly used chemotherapy drugs in anticancer therapy; unfortunately treatment with 5-FU by solely has many drawbacks  low lipophilicity, low permeability, low molecular weight, and its relatively poor plasma protein binding; also a brief half-life therefore frequent administration is required to maintain the optimal therapeutic plasma level which in addition to its poor selectivity, drug resistance and limited penetration to cancer cells; leads to increased incidence of side-effects to healthy cells/tissues and low response rates. In order to minimize these drawbacks; 5-FU was chemically  conjugated with pyrrolidine dithiocarbamate (PDTC) in a mutual prodrug moiety (S-(9H-purin-6-yl) 3-((pyrrolidine-1-carbonothioyl)thio)propanethioate) "compound [IV]" with (chloroacetic acid) and (chloroethanol) being the linkers ;synthesized prodrug and intermediates were characterized and identified using FTIR ,1H NMR and all the results shown good agreements with the proposed chemical structures of the synthesized compounds.  ; in-vitro preliminary cytotoxicity study was conducted for compound [IV] and 5-FU on CAL 51 and B16V cell lines ,results showed  enhanced cytotoxic effects for [IV] over 5-FU.

【 授权许可】

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