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单甲氧基聚（乙二醇）-脱氧胆酸的热敏核-刚性胶束

Thermosensitive core-rigid micelles of monomethoxy poly(ethylene glycol)-deoxy cholic acid.

作者信息

Han Jin Ok, Lee Hyun Jung, Jeong Byeongmoon

机构信息

Department of Chemistry and Nanoscience, Ewha Womans University, 52 Ewhayeodae-gil, Seodaemun-gu, Seoul, Korea.

出版信息

Biomater Res. 2022 Apr 28;26(1):16. doi: 10.1186/s40824-022-00263-9.

DOI:10.1186/s40824-022-00263-9
PMID:35484562
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9052506/
Abstract

BACKGROUND

Thermosensitive micelles with rigid cores that exhibit a reversible lower critical solution temperature at 30-35 °C can be applied for drug delivery.

METHOD

Hydrophilic monomethoxy poly(ethylene glycol) was conjugated to hydrophobic deoxycholic acid to prepare monomethoxy poly(ethylene glycol)-deoxycholic acid (mPEG-DC). Micelle formation and thermosensitive solution behavior were studied using various methods, including hydrophobic dye solubilization, transmission electron microscopy, dynamic light scattering, turbidity measurement, microcalorimetry, and H-NMR spectroscopy. Drug release from the thermosensitive micelles was demonstrated using estradiol, a model drug.

RESULTS

The mPEG-DC formed micelles with a critical micelle concentration of 0.05 wt.% and an average size of 15 nm. Aqueous mPEG-DC solutions exhibit a lower critical solution temperature (LCST) that is independent of concentration and reversible over heating and cooling cycles. The LCST transition is an entropically driven process involving dehydration of the PEG shell. The thermosensitive mPEG-DC micelles with rigid DC cores were applied as an estradiol delivery system in which estradiol was released, without initial burst, over the 16 days in a diffusion-controlled manner.

CONCLUSIONS

This study suggests that mPEG-DCs form thermosensitive micelles with rigid cores that can function as an excellent diffusion-controlled hydrophobic drug delivery system without initial burst release. Thermosensitive core-rigid micelles of monomethoxy poly(ethylene glycol)-deoxy cholic acid.

摘要

背景

具有刚性核且在30 - 35°C表现出可逆的低临界溶液温度的热敏胶束可用于药物递送。

方法

将亲水性单甲氧基聚（乙二醇）与疏水性脱氧胆酸偶联以制备单甲氧基聚（乙二醇）-脱氧胆酸（mPEG-DC）。使用多种方法研究胶束形成和热敏溶液行为，包括疏水性染料增溶、透射电子显微镜、动态光散射、浊度测量、微量量热法和H-NMR光谱法。使用模型药物雌二醇证明了从热敏胶束中的药物释放。

结果

mPEG-DC形成临界胶束浓度为0.05 wt.%且平均尺寸为15 nm的胶束。mPEG-DC水溶液表现出与浓度无关且在加热和冷却循环中可逆的低临界溶液温度（LCST）。LCST转变是一个由熵驱动的过程，涉及PEG壳的脱水。具有刚性DC核的热敏mPEG-DC胶束被用作雌二醇递送系统，其中雌二醇在16天内以扩散控制方式无初始突释地释放。

结论

本研究表明mPEG-DC形成具有刚性核的热敏胶束，其可作为优异的扩散控制的疏水性药物递送系统且无初始突释。单甲氧基聚（乙二醇）-脱氧胆酸的热敏核刚性胶束。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61c9/9052506/3feaced242c2/40824_2022_263_Fig9_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61c9/9052506/bda6e2851c0f/40824_2022_263_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61c9/9052506/b1e47506631e/40824_2022_263_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61c9/9052506/940c6c7d591b/40824_2022_263_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61c9/9052506/391e94c72c42/40824_2022_263_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61c9/9052506/bafe84ab85dc/40824_2022_263_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61c9/9052506/4058200a439a/40824_2022_263_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61c9/9052506/825514ea2a2e/40824_2022_263_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61c9/9052506/d050faa7c25a/40824_2022_263_Fig8_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61c9/9052506/3feaced242c2/40824_2022_263_Fig9_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61c9/9052506/bda6e2851c0f/40824_2022_263_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61c9/9052506/b1e47506631e/40824_2022_263_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61c9/9052506/940c6c7d591b/40824_2022_263_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61c9/9052506/391e94c72c42/40824_2022_263_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61c9/9052506/bafe84ab85dc/40824_2022_263_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61c9/9052506/4058200a439a/40824_2022_263_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61c9/9052506/825514ea2a2e/40824_2022_263_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61c9/9052506/d050faa7c25a/40824_2022_263_Fig8_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61c9/9052506/3feaced242c2/40824_2022_263_Fig9_HTML.jpg

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