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无渗透促进剂的混合胶束提高依普菌素透皮给药效率在动物寄生虫感染治疗中的应用。

Penetration Enhancer-Free Mixed Micelles for Improving Eprinomectin Transdermal c Efficiency in Animal Parasitic Infections Therapy.

机构信息

Jiangsu Agri-Animal Husbandry Vocational College, Taizhou, Jiangsu, 225300, People's Republic of China.

Department of Pharmaceutics, China Pharmaceutical University, Nanjing, 210009, People's Republic of China.

出版信息

Int J Nanomedicine. 2024 Nov 1;19:11071-11085. doi: 10.2147/IJN.S476164. eCollection 2024.

DOI:10.2147/IJN.S476164
PMID:39502637
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11537163/
Abstract

INTRODUCTION

Eprinomectin offers promise against parasitic infections. This study develops Eprinomectin (EPR) mixed micelles for transdermal delivery, aiming to enhance efficacy and convenience against endoparasites and ectoparasites. Physicochemical characterization and pharmacokinetic studies were conducted to assess its potential as an effective treatment for parasitic infections.

METHODS

Blank and EPR mixed micelles were prepared using PEG-40 Hydrogenated castor oil (RH-40) and Nonyl phenol polyoxyethylene ether 40 (NP-40). Critical micelle concentrations (CMC) determined using the pyrene fluorescence probe method. Particle size, EE, DL, in vitro release, permeation, and skin irritation were evaluated. In vivo pharmacokinetic studies were conducted in male Sprague-Dawley rats.

RESULTS

Results show that EPR mixed micelles present suitable stability, physicochemical properties, and safety. Moreover, the rapid release and high bioavailability of EPR mixed micelles have also been verified in the study. Pharmacokinetic experiments in vivo showed that an improvement in the transdermal absorption and bioavailability of EPR after encapsulation in mixed micelles formulations.

CONCLUSION

The results proved that the novel mixed micelles are safe and effective and are expected to become a promising veterinary nano-delivery system.

摘要

简介

依普菌素有望对抗寄生虫感染。本研究开发了依普菌素（EPR）混合胶束用于透皮给药，旨在提高针对体内寄生虫和体外寄生虫的疗效和便利性。进行了理化性质表征和药代动力学研究，以评估其作为寄生虫感染有效治疗方法的潜力。

方法

使用聚乙二醇 40 氢化蓖麻油（RH-40）和壬基酚聚氧乙烯醚 40（NP-40）制备空白和 EPR 混合胶束。使用芘荧光探针法测定临界胶束浓度（CMC）。评估粒径、EE、DL、体外释放、渗透和皮肤刺激性。在雄性 Sprague-Dawley 大鼠中进行体内药代动力学研究。

结果

结果表明，EPR 混合胶束具有适宜的稳定性、理化性质和安全性。此外，研究还验证了 EPR 混合胶束的快速释放和高生物利用度。体内药代动力学实验表明，EPR 包封在混合胶束制剂中后，透皮吸收和生物利用度得到改善。

结论

结果证明，新型混合胶束安全有效，有望成为有前途的兽医纳米给药系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b27/11537163/c4b274a78265/IJN-19-11071-g0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b27/11537163/467908a86308/IJN-19-11071-g0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b27/11537163/aea027b24f66/IJN-19-11071-g0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b27/11537163/84ffaf6cfa04/IJN-19-11071-g0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b27/11537163/2b2209f1b4d4/IJN-19-11071-g0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b27/11537163/4ca2afb5bbe6/IJN-19-11071-g0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b27/11537163/c4b274a78265/IJN-19-11071-g0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b27/11537163/467908a86308/IJN-19-11071-g0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b27/11537163/aea027b24f66/IJN-19-11071-g0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b27/11537163/84ffaf6cfa04/IJN-19-11071-g0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b27/11537163/2b2209f1b4d4/IJN-19-11071-g0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b27/11537163/4ca2afb5bbe6/IJN-19-11071-g0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b27/11537163/c4b274a78265/IJN-19-11071-g0006.jpg

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