Folate Modified Long Circulating Nano-Emulsion as a Promising Approach for Improving the Efficiency of Chemotherapy Drug
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RESEARCH PAPER
Folate Modified Long Circulating Nano-Emulsion as a Promising Approach for Improving the Efficiency of Chemotherapy Drugs in Cancer Treatment Baohui Song 1 & Shiyang Wu 1 & Wenpan Li 1 & Dawei Chen 1 & Haiyang Hu 1
Received: 10 November 2019 / Accepted: 1 April 2020 # Springer Science+Business Media, LLC, part of Springer Nature 2020
ABSTRACT Purpose In order to improve the therapeutic efficiency of the chemotherapeutic drug paclitaxel in tumors, a folate-based Paclitaxel nanoemulsion (FNEs) was developed for tumor targeted treatment. Methods In this study, we designed a folate-targeted nanoemulsion (folate/PEG-DSPE/nanoemulsion, FNEs) based on the traditional nanoemulsion using the principle of longcirculation targeting receptor mediated. The nanoemulsion (folate/PEG-DSPE/nanoemulsion, FNEs) was fabricated using high-pressure homogenization with a microfluidizer. Results The nanoemulsion (folate/PEG-DSPE/nanoemulsion, FNEs) can improve the delivery efficiency of nanocarriers at the tumor site by virtue of the high expression of folate receptors on the tumor surface. Malvern Nanoseries device and transmission electron microscopy (TEM) analyses showed that the nanoemulsions were spherical with an average diameter of 140 nm. The nanoemulsions can effectively carry paclitaxel (PTX) with an encapsulation rate of about 95%. And in vitro experiments have shown that it can efficiently increase the uptake of PTX in 4 T1 breast cancer cells and FNEs had a targeting capability hundredfold higher than that of PTXloaded nanoemulsions (PTX-NEs) without folate. In vivo experiments have shown that the pharmacokinetic parameters of FNEs were better than those of other PTX groups and FNEs can significantly enhance circulation time in the body of the subcutaneously implanted 4 T1 breast cancer in mice, Electronic supplementary material The online version of this article (https://doi.org/10.1007/s11095-020-02811-1) contains supplementary material, which is available to authorized users. * Haiyang Hu [email protected] 1
School of Pharmacy, Shenyang Pharmaceutical University, 103Wenhua Road, Shenyang 110016, Liaoning Province, China
increase the accumulation of chemotherapy drugs at tumor sites and effectively inhibit tumor growth with lower system toxicity. Conclusions This study can effectively improve the therapeutic efficiency of chemotherapy drugs for tumors, and provide an useful reference for solving the problem of low efficacy of chemotherapy drugs in clinical treatment of tumors.
KEY WORDS cancer treatment . chemotherapy drugs . folate modified . nanoemulsion
INTRODUCTION Chemotherapy is one of the main methods of tumor treatment, but due to non-specificity, most of the chemotherapeutic drugs are harmful to normal as well as cancerous tissues, therefore, chemotherapeutic drugs are facing with great challenge such as poor delivery and strong side effects. Meanwhile, the poor aqueous solubility and low bioavailability also result in the phenomenon that chemotherapeutic active ingredients cannot effecti
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