文献检索文档翻译深度研究
Suppr Zotero 插件Zotero 插件
邀请有礼套餐&价格历史记录

新学期，新优惠

限时优惠:9月1日-9月22日

30天高级会员仅需29元

1天体验卡首发特惠仅需5.99元

了解详情
不再提醒
插件&应用
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
高级版
套餐订阅购买积分包
AI 工具
文献检索文档翻译深度研究
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2025

新型可生物降解聚酯。合成及其作为药物载体用于制备载盐酸雷洛昔芬纳米颗粒的应用。

Novel biodegradable polyesters. Synthesis and application as drug carriers for the preparation of raloxifene HCl loaded nanoparticles.

作者信息

Bikiaris Dimitrios, Karavelidis Vassilios, Karavas Evangelos

机构信息

Laboratory of Organic Chemical Technology, Chemistry Department, Aristotle University of Thessaloniki, 541 24 Thessaloniki, Greece.

出版信息

Molecules. 2009 Jul 7;14(7):2410-30. doi: 10.3390/molecules14072410.

DOI:10.3390/molecules14072410
PMID:19633613
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6255325/
Abstract

Raloxifene HCl is a drug with poor bioavailability and poor water solubility. Furthermore nomicron pharmaceutically acceptable organic solvent has been reported before to dilute the drug. It was observed that Raloxifene HCl can be diluted in a solvent mixture of acetone/water or ethanol/water. The aim of this study was to use biodegradable polymers in order to prepare Raloxifene HCl nanoparticles. For this purpose a series of novel biodegradable poly(ethylene succinate-co-propylene adipate) P(ESu-co-PAd) polyesters were synthesized following the polycondensation method and further, poly(ethylene succinate) (PESu) and poly(propylene adipate) (PPAd) were used. The prepared polyesters were characterized by intrinsic viscosity measurements, end group analysis, enzymatic hydrolysis, Nuclear Magnetic Resonance Spectroscopy ((1H)-NMR and (13)C-NMR) and Wide-angle X-ray Diffractometry (WAXD). The drug nanoparticles have been prepared by a variation of the co-precipitation method and were studied by Wide-angle X-ray Diffractometry (WAXD), FTIR spectrometry, light scattering size distribution, Scanning Electron Microscopy (SEM) and release behavior measurements. The interactions between the polymers and the drug seem to be limited, so the drug occurs in crystalline form in all nanoparticles. The size of the nanoparticles seems to be in the range of 150-350 nm, depending on the polymer that was used. The drug release depends on the melting point and degree of crystallinity of the polyesters used. An initial high release rate was recorded followed by very slow rates of controlled release.

摘要

盐酸雷洛昔芬是一种生物利用度差且水溶性差的药物。此外，之前已有报道称使用纳米级药学上可接受的有机溶剂来稀释该药物。据观察，盐酸雷洛昔芬可在丙酮/水或乙醇/水的溶剂混合物中稀释。本研究的目的是使用可生物降解的聚合物来制备盐酸雷洛昔芬纳米颗粒。为此，采用缩聚法合成了一系列新型可生物降解的聚（琥珀酸乙烯酯 - 共 - 己二酸丙酯）P（ESu - 共 - PAd）聚酯，此外，还使用了聚（琥珀酸乙烯酯）（PESu）和聚（己二酸丙酯）（PPAd）。通过特性粘度测量、端基分析、酶水解、核磁共振光谱（（1H）-NMR和（13C）-NMR）以及广角X射线衍射（WAXD）对所制备的聚酯进行了表征。通过共沉淀法的改进制备了药物纳米颗粒，并通过广角X射线衍射（WAXD）、傅里叶变换红外光谱（FTIR）、光散射尺寸分布、扫描电子显微镜（SEM）和释放行为测量对其进行了研究。聚合物与药物之间的相互作用似乎有限，因此药物在所有纳米颗粒中均以结晶形式存在。纳米颗粒的尺寸似乎在150 - 350 nm范围内，这取决于所使用的聚合物。药物释放取决于所用聚酯的熔点和结晶度。记录到初始高释放速率，随后是非常缓慢的控释速率。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/8d7d95b43f30/molecules-14-02410-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/89e39bb66fe6/molecules-14-02410-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/ceabf9110d54/molecules-14-02410-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/b0ea9fcf8032/molecules-14-02410-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/5a59ef05fd94/molecules-14-02410-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/8dbb3e66fc4f/molecules-14-02410-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/5df2473c3176/molecules-14-02410-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/d4c25bbe81d7/molecules-14-02410-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/0677ae3b8e76/molecules-14-02410-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/5ffa6bcec945/molecules-14-02410-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/d4274eb57004/molecules-14-02410-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/ec970dd6c0d7/molecules-14-02410-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/8d7d95b43f30/molecules-14-02410-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/89e39bb66fe6/molecules-14-02410-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/ceabf9110d54/molecules-14-02410-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/b0ea9fcf8032/molecules-14-02410-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/5a59ef05fd94/molecules-14-02410-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/8dbb3e66fc4f/molecules-14-02410-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/5df2473c3176/molecules-14-02410-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/d4c25bbe81d7/molecules-14-02410-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/0677ae3b8e76/molecules-14-02410-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/5ffa6bcec945/molecules-14-02410-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/d4274eb57004/molecules-14-02410-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/ec970dd6c0d7/molecules-14-02410-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/197f/6255325/8d7d95b43f30/molecules-14-02410-g012.jpg

相似文献

[1]
Novel biodegradable polyesters. Synthesis and application as drug carriers for the preparation of raloxifene HCl loaded nanoparticles.

Molecules. 2009-7-7

[2]
Effectiveness of various drug carriers in controlled release formulations of raloxifene HCl prepared by melt mixing.

Curr Drug Deliv. 2009-10

[3]
Nanoencapsulation of a water soluble drug in biocompatible polyesters. Effect of polyesters melting point and glass transition temperature on drug release behavior.

Eur J Pharm Sci. 2010-9-21

[4]
Preparation of New Risperidone Depot Microspheres Based on Novel Biocompatible Poly(Alkylene Adipate) Polyesters as Long-Acting Injectable Formulations.

J Pharm Sci. 2018-8-7

[5]
Novel self-assembled core-shell nanoparticles based on crystalline amorphous moieties of aliphatic copolyesters for efficient controlled drug release.

J Control Release. 2009-5-14

[6]
Development of l-Amino-Acid-Based Hydroxyl Functionalized Biodegradable Amphiphilic Polyesters and Their Drug Delivery Capabilities to Cancer Cells.

Biomacromolecules. 2020-1-13

[7]
Poly(methyl vinyl ether-co-maleic acid) for enhancement of solubility, oral bioavailability and anti-osteoporotic effects of raloxifene hydrochloride.

Eur J Pharm Sci. 2017-12-5

[8]
Synthesis and characterization of poly-alpha,beta-[N-(2-hydroxyethyl)-L-aspartamide]-g-poly(L-lactide) biodegradable copolymers as drug carriers.

J Biomed Mater Res A. 2006-1

[9]
Development of biodegradable nanoparticles for delivery of quercetin.

Colloids Surf B Biointerfaces. 2010-6-11

[10]
Novel self-assembled amphiphilic poly(epsilon-caprolactone)-grafted-poly(vinyl alcohol) nanoparticles: hydrophobic and hydrophilic drugs carrier nanoparticles.

J Mater Sci Mater Med. 2009-3

引用本文的文献

[1]
Multivariate Analysis of Solubility Parameters for Drug-Polymer Miscibility Assessment in Preparing Raloxifene Hydrochloride Amorphous Solid Dispersions.

AAPS PharmSciTech. 2024-6-6

[2]
Revisiting Non-Conventional Crystallinity-Induced Effects on Molecular Mobility in Sustainable Diblock Copolymers of Poly(propylene adipate) and Polylactide.

Molecules. 2022-11-2

[3]
Mg,Si-Co-Substituted Hydroxyapatite/Alginate Composite Beads Loaded with Raloxifene for Potential Use in Bone Tissue Regeneration.

Int J Mol Sci. 2021-3-13

[4]
Development and Characterization of Venetoclax Nanocrystals for Oral Bioavailability Enhancement.

AAPS PharmSciTech. 2021-3-8

[5]
Folate and Pegylated Aliphatic Polyester Nanoparticles for Targeted Anticancer Drug Delivery.

Int J Nanomedicine. 2020-7-10

[6]
Selectively Biodegradable Polyesters: Nature-Inspired Construction Materials for Future Biomedical Applications.

Polymers (Basel). 2019-6-19

[7]
Design of a transdermal formulation containing raloxifene nanoparticles for osteoporosis treatment.

Int J Nanomedicine. 2018-9-6

[8]
Taribavirin and 5-Fluorouracil-Loaded Pegylated-Lipid Nanoparticle Synthesis, p38 Docking, and Antiproliferative Effects on MCF-7 Breast Cancer.

Pharm Res. 2018-2-27

[9]
Effects of Particle Hydrophobicity, Surface Charge, Media pH Value and Complexation with Human Serum Albumin on Drug Release Behavior of Mitoxantrone-Loaded Pullulan Nanoparticles.

Nanomaterials (Basel). 2015-12-25

[10]
Controlled release of raloxifene by nanoencapsulation: effect on in vitro antiproliferative activity of human breast cancer cells.

Int J Nanomedicine. 2014-6-17

本文引用的文献

[1]
Dissolution rate enhancement of the poorly water-soluble drug Tibolone using PVP, SiO2, and their nanocomposites as appropriate drug carriers.

Drug Dev Ind Pharm. 2009-9

[2]
Novel self-assembled core-shell nanoparticles based on crystalline amorphous moieties of aliphatic copolyesters for efficient controlled drug release.

J Control Release. 2009-5-14

[3]
Novel biodegradable polyester poly(propylene succinate): synthesis and application in the preparation of solid dispersions and nanoparticles of a water-soluble drug.

AAPS PharmSciTech. 2009

[4]
Enhanced electrostatic interaction between chitosan-modified PLGA nanoparticle and tumor.

Int J Pharm. 2009-4-17

[5]
Active targeting schemes for nanoparticle systems in cancer therapeutics.

Adv Drug Deliv Rev. 2008-12-14

[6]
Thermosensitive polymer-conjugated albumin nanospheres as thermal targeting anti-cancer drug carrier.

Eur J Pharm Sci. 2008-11-15

[7]
Correlation between chemical and solid-state structures and enzymatic hydrolysis in novel biodegradable polyesters. The case of poly(propylene alkanedicarboxylate)s.

Macromol Biosci. 2008-8-11

[8]
Possibility of active targeting to tumor by local hyperthermia with temperature-sensitive nanoparticles.

Med Hypotheses. 2008-8

[9]
Cytocompatibility of aliphatic polyesters--in vitro study on fibroblasts and macrophages.

J Biomed Mater Res A. 2008-11

[10]
Characterization of the distribution, polymorphism, and stability of nimodipine in its solid dispersions in polyethylene glycol by micro-Raman spectroscopy and powder X-ray diffraction.

AAPS J. 2007-12-7

文献AI研究员

20分钟写一篇综述，助力文献阅读效率提升50倍

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

推荐工具

医学文档翻译智能文献检索