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视黄醇包裹的低分子水溶性壳聚糖纳米粒

Retinol-encapsulated low molecular water-soluble chitosan nanoparticles.

作者信息

Kim Dong-Gon, Jeong Young-Il, Choi Changyong, Roh Sung-Hee, Kang Seong-Koo, Jang Mi-Kyeong, Nah Jae-Woon

机构信息

Department of Polymer Science and Engineering, Sunchon National University, Jeonnam 540-742, Republic of Korea.

出版信息

Int J Pharm. 2006 Aug 17;319(1-2):130-8. doi: 10.1016/j.ijpharm.2006.03.040. Epub 2006 Apr 6.

Abstract

This aim of this study was to encapsulate retinol into chitosan nanoparticles and reconstitute it into aqueous solution. Retinol-encapsulated chitosan nanoparticles were prepared for application of cosmetic and pharmaceutical applications. Retinol-encapsulated chitosan nanoparticle has a spherical shape and its particle sizes were around 50-200 nm according to the drug contents. Particle size was increased according to the increase of drug contents. Solubility of retinol is able to increase by encapsulation into chitosan nanoparticles more than 1600-fold. It was suggested that retinol was encapsulated into chitosan nanoparticles by ion complex as a result of FT-IR spectra. Specific peak of chitosan at 1590 cm(-1) was divided to semi-doublet due to the electrostatic interaction between amine group of chitosan and hydroxyl group of retinol. At (1)H NMR spectra, specific peaks of retinol disappeared when retinol-encapsulated chitosan nanoparticles were reconstituted into D(2)O while specific peaks both of retinol and chitosan appeared at D(2)O/DMSO (1/4, v/v) mixture. XRD patterns also showed that crystal peaks of retinol were disappeared by encapsulation into chitosan nanoparticles. Retinol-encapsulated nanoparticles were completely reconstituted into aqueous solution as same as original aqueous solution and zeta potential of reconstituted chitosan nanoparticles was similar to their original solution. At HPLC study, retinol was stably and efficiently encapsulated into chitosan nanoparticles.

摘要

本研究的目的是将视黄醇包封于壳聚糖纳米粒中并将其重构成水溶液。制备了视黄醇包封的壳聚糖纳米粒以用于化妆品和药物应用。视黄醇包封的壳聚糖纳米粒呈球形,根据药物含量其粒径约为50 - 200 nm。粒径随药物含量的增加而增大。通过包封于壳聚糖纳米粒中,视黄醇的溶解度能够提高超过1600倍。傅里叶变换红外光谱(FT - IR)结果表明视黄醇通过离子络合作用被包封于壳聚糖纳米粒中。壳聚糖在1590 cm(-1)处的特定峰由于壳聚糖的胺基与视黄醇的羟基之间的静电相互作用而分裂为半双峰。在氢核磁共振((1)H NMR)光谱中,当视黄醇包封的壳聚糖纳米体重构成重水(D₂O)时,视黄醇的特定峰消失,而在D₂O/二甲亚砜(DMSO,1/4,v/v)混合物中视黄醇和壳聚糖的特定峰均出现。X射线衍射(XRD)图谱也表明视黄醇的晶体峰通过包封于壳聚糖纳米粒中而消失。视黄醇包封的纳米粒能够完全重构成与原始水溶液相同的水溶液,并且重构后的壳聚糖纳米粒的zeta电位与其原始溶液相似。在高效液相色谱(HPLC)研究中,视黄醇被稳定且有效地包封于壳聚糖纳米粒中。

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