• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
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
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
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 @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

基于聚乙烯吡咯烷酮 K-30 的交联快速溶胀纳米凝胶:改善药物溶解度的完美方法。

Polyvinylpyrrolidone K-30-Based Crosslinked Fast Swelling Nanogels: An Impeccable Approach for Drug's Solubility Improvement.

机构信息

College of Pharmacy, University of Sargodha, Sargodha City Punjab, Pakistan.

Quaid-e-Azam College of Pharmacy, Sahiwal, Punjab, Pakistan.

出版信息

Biomed Res Int. 2022 Aug 26;2022:5883239. doi: 10.1155/2022/5883239. eCollection 2022.

DOI:10.1155/2022/5883239
PMID:36060130
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9439932/
Abstract

Poor solubility is a global issue of copious pharmaceutical industries as large number of drugs in development stage as well as already marketed products are poorly soluble which results in low dissolution and ultimately dosage increase. Current study is aimed at developing a polyvinylpyrrolidone- (PVP-K30-) based nanogel delivery system for solubility enhancement of poorly soluble drug olanzapine (OLP), as solubilization enhancement is the most noteworthy application of nanosystems. Crosslinking polymerization with subsequent condensation technique was used for the synthesis of nanogels, a highly responsive polymeric networks in drug's solubility. Developed nanogels were characterized by percent entrapment efficiency, sol-gel, percent swelling, percent drug loaded content (%DLC), percent porosity, stability, solubility, in vitro dissolution studies, FTIR, XRD, and SEM analysis. Furthermore, cytotoxicity study was conducted on rabbits to check the biocompatibility of the system. Particle size of nanogels was found with 178.99 ± 15.32 nm, and in vitro dissolution study exhibited that drug release properties were considerably enhanced as compared to the marketed formulation OLANZIA. The solubility studies indicated that solubility of OLP was noticeably improved up to 36.7-fold in phosphate buffer of pH 6.8. In vivo cytotoxicity study indicated that prepared PVP-K30-based formulation was biocompatible. On the basis of results obtained, the developed PVP-K30-co-poly (AMPS) nanogel delivery system is expected to be safe, effective, and cost-effective for solubility improvement of poorly soluble drugs.

摘要

溶解度差是众多制药行业面临的全球性问题,因为大量处于研发阶段和已上市的药物溶解度较差,导致溶解度低,最终需要增加剂量。本研究旨在开发一种基于聚乙烯吡咯烷酮(PVP-K30)的纳米凝胶给药系统,以提高难溶性药物奥氮平(OLP)的溶解度,因为增溶是纳米系统最值得注意的应用。通过交联聚合和随后的缩合技术合成纳米凝胶,这是一种对药物溶解度具有高响应性的聚合物网络。所开发的纳米凝胶通过包封效率、溶胶-凝胶、溶胀度、载药量(%DLC)、孔隙率、稳定性、溶解度、体外溶解研究、FTIR、XRD 和 SEM 分析进行了表征。此外,还对兔子进行了细胞毒性研究,以检查系统的生物相容性。纳米凝胶的粒径为 178.99 ± 15.32nm,体外溶解研究表明,与市售奥氮平制剂相比,药物释放性能得到了显著提高。溶解度研究表明,在 pH 6.8 的磷酸盐缓冲液中,OLP 的溶解度提高了 36.7 倍。体内细胞毒性研究表明,所制备的基于 PVP-K30 的制剂具有生物相容性。基于所获得的结果,所开发的 PVP-K30-共-聚(AMPS)纳米凝胶给药系统有望成为提高难溶性药物溶解度的安全、有效和具有成本效益的方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec63/9439932/b8e8514ca276/BMRI2022-5883239.009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec63/9439932/bb1def64cddd/BMRI2022-5883239.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec63/9439932/ed3820ea43fd/BMRI2022-5883239.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec63/9439932/5735c94ab10e/BMRI2022-5883239.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec63/9439932/e9f2afdf4a7f/BMRI2022-5883239.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec63/9439932/4156d7631dda/BMRI2022-5883239.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec63/9439932/f2064033bf42/BMRI2022-5883239.006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec63/9439932/6a8a1da17572/BMRI2022-5883239.007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec63/9439932/b2882c161176/BMRI2022-5883239.008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec63/9439932/b8e8514ca276/BMRI2022-5883239.009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec63/9439932/bb1def64cddd/BMRI2022-5883239.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec63/9439932/ed3820ea43fd/BMRI2022-5883239.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec63/9439932/5735c94ab10e/BMRI2022-5883239.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec63/9439932/e9f2afdf4a7f/BMRI2022-5883239.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec63/9439932/4156d7631dda/BMRI2022-5883239.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec63/9439932/f2064033bf42/BMRI2022-5883239.006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec63/9439932/6a8a1da17572/BMRI2022-5883239.007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec63/9439932/b2882c161176/BMRI2022-5883239.008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec63/9439932/b8e8514ca276/BMRI2022-5883239.009.jpg

相似文献

1
Polyvinylpyrrolidone K-30-Based Crosslinked Fast Swelling Nanogels: An Impeccable Approach for Drug's Solubility Improvement.基于聚乙烯吡咯烷酮 K-30 的交联快速溶胀纳米凝胶:改善药物溶解度的完美方法。
Biomed Res Int. 2022 Aug 26;2022:5883239. doi: 10.1155/2022/5883239. eCollection 2022.
2
Synthesis of PEG-4000-co-poly (AMPS) nanogels by cross-linking polymerization as highly responsive networks for enhancement in meloxicam solubility.通过交联聚合合成 PEG-4000-co-聚(AMPS)纳米凝胶作为高响应性网络,以提高美洛昔康的溶解度。
Drug Dev Ind Pharm. 2021 Mar;47(3):465-476. doi: 10.1080/03639045.2021.1892738. Epub 2021 Mar 2.
3
Poloxamer-407-Co-Poly (2-Acrylamido-2-Methylpropane Sulfonic Acid) Cross-linked Nanogels for Solubility Enhancement of Olanzapine: Synthesis, Characterization, and Toxicity Evaluation.泊洛沙姆-407 共聚物(2-丙烯酰胺基-2-甲基丙磺酸)交联纳米胶用于奥氮平增溶:合成、表征和毒性评价。
AAPS PharmSciTech. 2020 May 17;21(5):141. doi: 10.1208/s12249-020-01694-0.
4
Development of β-cyclodextrin/polyvinypyrrolidone-co-poly (2-acrylamide-2-methylpropane sulphonic acid) hybrid nanogels as nano-drug delivery carriers to enhance the solubility of Rosuvastatin: An in vitro and in vivo evaluation.β-环糊精/聚乙烯基吡咯烷酮共聚物-聚(2-丙烯酰胺基-2-甲基丙烷磺酸)杂化纳米凝胶作为纳米药物载体提高瑞舒伐他汀溶解度的研究:体外和体内评价。
PLoS One. 2022 Jan 21;17(1):e0263026. doi: 10.1371/journal.pone.0263026. eCollection 2022.
5
Crosslinked PVA--poly(AMPS) Nanogels for Enhanced Solubility and Dissolution of Ticagrelor: Synthesis, Characterization, and Toxicity Evaluation.用于增强替格瑞洛溶解度和溶出度的交联聚乙烯醇-聚(2-丙烯酰胺基-2-甲基丙磺酸)纳米凝胶:合成、表征及毒性评价
ACS Omega. 2024 May 2;9(19):21401-21415. doi: 10.1021/acsomega.4c01721. eCollection 2024 May 14.
6
Preparation, In Vitro Characterization, and Evaluation of Polymeric pH-Responsive Hydrogels for Controlled Drug Release.用于控释药物的聚合物pH响应水凝胶的制备、体外表征及评价
ACS Omega. 2024 Feb 19;9(9):10498-10516. doi: 10.1021/acsomega.3c08107. eCollection 2024 Mar 5.
7
Crystalline Ethylene Oxide and Propylene Oxide Triblock Copolymer Solid Dispersion Enhance Solubility, Stability and Promoting Time- Controllable Release of Curcumin.结晶环氧乙烷和环氧丙烷三嵌段共聚物固体分散体提高姜黄素的溶解度、稳定性并促进其时间可控释放。
Recent Pat Drug Deliv Formul. 2018;12(1):65-74. doi: 10.2174/1872211312666180118104920.
8
Retracted: Polyvinylpyrrolidone K-30-Based Crosslinked Fast Swelling Nanogels: An Impeccable Approach for Drug's Solubility Improvement.撤回:基于聚乙烯吡咯烷酮K-30的交联快速溶胀纳米凝胶:改善药物溶解度的完美方法。
Biomed Res Int. 2024 Jan 9;2024:9817465. doi: 10.1155/2024/9817465. eCollection 2024.
9
Bi-polymeric Spongy Matrices Through Cross-linking Polymerization: Synthesized and Evaluated for Solubility Enhancement of Acyclovir.双聚合物海绵基质的交联聚合:为提高阿昔洛韦的溶解度而合成并评价。
AAPS PharmSciTech. 2021 Jun 15;22(5):181. doi: 10.1208/s12249-021-02054-2.
10
Design of Isoniazid Smart Nanogel by Gamma Radiation-Induced Template Polymerization for Biomedical Application.γ辐射诱导模板聚合制备用于生物医学应用的异烟肼智能纳米凝胶的设计
Pharm Res. 2017 Sep;34(9):1872-1885. doi: 10.1007/s11095-017-2196-1. Epub 2017 Jun 15.

引用本文的文献

1
Crosslinked PVA--poly(AMPS) Nanogels for Enhanced Solubility and Dissolution of Ticagrelor: Synthesis, Characterization, and Toxicity Evaluation.用于增强替格瑞洛溶解度和溶出度的交联聚乙烯醇-聚(2-丙烯酰胺基-2-甲基丙磺酸)纳米凝胶:合成、表征及毒性评价
ACS Omega. 2024 May 2;9(19):21401-21415. doi: 10.1021/acsomega.4c01721. eCollection 2024 May 14.
2
Nanomedicines: Emerging Platforms in Smart Chemotherapy Treatment-A Recent Review.纳米药物:智能化疗治疗中的新兴平台——近期综述
Pharmaceuticals (Basel). 2024 Feb 28;17(3):315. doi: 10.3390/ph17030315.
3
Preparation and Characterization of Theophylline Controlled Release Matrix System Incorporating Poloxamer 407, Stearyl Alcohol, and Hydroxypropyl Methylcellulose: A Novel Formulation and Development Study.

本文引用的文献

1
Off-Stoichiometric Thiol-Ene Chemistry to Dendritic Nanogel Therapeutics.用于树枝状纳米凝胶疗法的非化学计量硫醇-烯化学
Adv Funct Mater. 2019 May 2;29(18):1806693. doi: 10.1002/adfm.201806693. Epub 2019 Mar 7.
2
Synthesis of novel combinatorial drug delivery system (nCDDS) for co-delivery of 5-fluorouracil and leucovorin calcium for colon targeting and controlled drug release.新型组合药物递送系统(nCDDS)的合成,用于共递送 5-氟尿嘧啶和亚叶酸钙用于结肠靶向和控释药物。
Drug Dev Ind Pharm. 2021 Dec;47(12):1952-1965. doi: 10.1080/03639045.2022.2072514. Epub 2022 May 12.
3
Overview of nanoparticulate strategies for solubility enhancement of poorly soluble drugs.
含泊洛沙姆407、硬脂醇和羟丙基甲基纤维素的茶碱控释基质系统的制备与表征:一项新型制剂研发研究
Polymers (Basel). 2024 Feb 27;16(5):643. doi: 10.3390/polym16050643.
4
Retracted: Polyvinylpyrrolidone K-30-Based Crosslinked Fast Swelling Nanogels: An Impeccable Approach for Drug's Solubility Improvement.撤回:基于聚乙烯吡咯烷酮K-30的交联快速溶胀纳米凝胶:改善药物溶解度的完美方法。
Biomed Res Int. 2024 Jan 9;2024:9817465. doi: 10.1155/2024/9817465. eCollection 2024.
5
Development of olanzapine solid dispersion by spray drying technique using screening design for solubility enhancement.采用筛选设计通过喷雾干燥技术制备奥氮平固体分散体以提高溶解度
ADMET DMPK. 2023 Oct 6;11(4):615-627. doi: 10.5599/admet.1998. eCollection 2023.
6
Effect of Excipients on the Quality of Drug Formulation and Immediate Release of Generic Metformin HCl Tablets.辅料对药物制剂质量及盐酸二甲双胍仿制药片速释性能的影响
Pharmaceuticals (Basel). 2023 Apr 4;16(4):539. doi: 10.3390/ph16040539.
7
Polymeric Gel Systems Cytotoxicity and Drug Release as Key Features for their Effective Application in Various Fields of Addressed Pharmaceuticals Delivery.聚合物凝胶系统的细胞毒性和药物释放是其在靶向药物递送各个领域有效应用的关键特性。
Pharmaceutics. 2023 Mar 3;15(3):830. doi: 10.3390/pharmaceutics15030830.
纳米颗粒策略概述:提高难溶性药物的溶解度。
Life Sci. 2022 Feb 15;291:120301. doi: 10.1016/j.lfs.2022.120301. Epub 2022 Jan 6.
4
Bi-polymeric Spongy Matrices Through Cross-linking Polymerization: Synthesized and Evaluated for Solubility Enhancement of Acyclovir.双聚合物海绵基质的交联聚合:为提高阿昔洛韦的溶解度而合成并评价。
AAPS PharmSciTech. 2021 Jun 15;22(5):181. doi: 10.1208/s12249-021-02054-2.
5
Synthesis of PEG-4000-co-poly (AMPS) nanogels by cross-linking polymerization as highly responsive networks for enhancement in meloxicam solubility.通过交联聚合合成 PEG-4000-co-聚(AMPS)纳米凝胶作为高响应性网络,以提高美洛昔康的溶解度。
Drug Dev Ind Pharm. 2021 Mar;47(3):465-476. doi: 10.1080/03639045.2021.1892738. Epub 2021 Mar 2.
6
Porous and highly responsive cross-linked β-cyclodextrin based nanomatrices for improvement in drug dissolution and absorption.多孔且高响应性的交联 β-环糊精纳米基质,用于改善药物溶解和吸收。
Life Sci. 2021 Feb 15;267:118931. doi: 10.1016/j.lfs.2020.118931. Epub 2020 Dec 30.
7
Segmental hair analysis of olanzapine and N-desmethyl-olanzapine in postmortem hair from mentally ill patients by LC-MS/MS.应用 LC-MS/MS 对精神疾病患者死后毛发中奥氮平和 N-去甲基奥氮平进行分段分析。
J Pharm Biomed Anal. 2020 Oct 25;190:113510. doi: 10.1016/j.jpba.2020.113510. Epub 2020 Aug 2.
8
Formulation of Curcumin-β-cyclodextrin-polyvinylpyrrolidone supramolecular inclusion complex: experimental, molecular docking, and preclinical anti-inflammatory assessment.姜黄素-β-环糊精-聚乙烯吡咯烷酮超分子包合物的制备:实验、分子对接及临床前抗炎评估
Drug Dev Ind Pharm. 2020 Sep;46(9):1524-1534. doi: 10.1080/03639045.2020.1810268. Epub 2020 Aug 27.
9
Measurement of the amorphous fraction of olanzapine incorporated in a co-amorphous formulation.奥氮平共无定形制剂中无定形部分的测量。
Int J Pharm. 2020 Oct 15;588:119716. doi: 10.1016/j.ijpharm.2020.119716. Epub 2020 Aug 3.
10
Poloxamer-407-Co-Poly (2-Acrylamido-2-Methylpropane Sulfonic Acid) Cross-linked Nanogels for Solubility Enhancement of Olanzapine: Synthesis, Characterization, and Toxicity Evaluation.泊洛沙姆-407 共聚物(2-丙烯酰胺基-2-甲基丙磺酸)交联纳米胶用于奥氮平增溶:合成、表征和毒性评价。
AAPS PharmSciTech. 2020 May 17;21(5):141. doi: 10.1208/s12249-020-01694-0.