• 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

用于增强乙酰唑胺眼部递送的转凝胶体的制备：统计优化、体外表征和体内研究。

Fabrication of Transgelosomes for Enhancing the Ocular Delivery of Acetazolamide: Statistical Optimization, In Vitro Characterization, and In Vivo Study.

作者信息

Mazyed Eman A, Abdelaziz Abdelaziz E

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, Kaferelsheikh University, Kaferelsheikh POB 33516, Egypt.

出版信息

Pharmaceutics. 2020 May 20;12(5):465. doi: 10.3390/pharmaceutics12050465.

DOI:10.3390/pharmaceutics12050465
PMID:32443679
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7284610/
Abstract

Acetazolamide (ACZ) is a potent carbonic anhydrase inhibitor that is used for the treatment of glaucoma. Its oral administration causes various undesirable side effects. This study aimed to formulate transgelosomes (TGS) for enhancing the ocular delivery of ACZ. ACZ-loaded transfersomes were formulated by the ethanol injection method, using phosphatidylcholine (PC) and different edge activators, including Tween 80, Span 60, and Cremophor RH 40. The effects of the ratio of lipid to surfactant and type of surfactant on % drug released after 8 h (Q) and entrapment efficiency (EE%) were investigated by using Design-Expert software. The optimized formula was formulated as TGS, using poloxamers as gelling agents. In vitro and in vivo characterization of ACZ-loaded TGS was performed. According to optimization study, F8 had the highest desirability value and was chosen as the optimized formula for preparing TGS. F8 appeared as spherical elastic nanovesicles with Q of 93.01 ± 3.76% and EE% of 84.44 ± 2.82. Compared to a free drug, TGS exhibited more prolonged drug release of 71.28 ± 0.46% after 8 h, higher ex vivo permeation of 66.82 ± 1.11% after 8 h and a significant lowering of intraocular pressure (IOP) for 24 h. Therefore, TGS provided a promising technique for improving the corneal delivery of ACZ.

摘要

乙酰唑胺（ACZ）是一种强效碳酸酐酶抑制剂，用于治疗青光眼。口服该药物会引起各种不良副作用。本研究旨在制备转凝胶体（TGS）以增强ACZ的眼部给药效果。采用乙醇注入法，使用磷脂酰胆碱（PC）和不同的边缘活化剂（包括吐温80、司盘60和聚氧乙烯蓖麻油RH 40）制备载ACZ的传递体。利用Design-Expert软件研究了脂质与表面活性剂的比例以及表面活性剂类型对8小时后药物释放百分比（Q）和包封率（EE%）的影响。使用泊洛沙姆作为胶凝剂，将优化后的配方制成TGS。对载ACZ的TGS进行了体外和体内表征。根据优化研究，F8具有最高的可取性值，被选为制备TGS的优化配方。F8呈现为球形弹性纳米囊泡，Q为93.01±3.76%，EE%为84.44±2.82。与游离药物相比，TGS在8小时后表现出更长时间的药物释放，释放率为71.28±0.46%，8小时后的离体渗透率更高，为66.82±1.11%，并且眼内压（IOP）显著降低达24小时。因此，TGS为改善ACZ的角膜给药提供了一种有前景的技术。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/18c9a22ccf56/pharmaceutics-12-00465-g014.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/da872f6b6377/pharmaceutics-12-00465-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/2ccd89aaee73/pharmaceutics-12-00465-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/440c2522523c/pharmaceutics-12-00465-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/91e81f9b0b58/pharmaceutics-12-00465-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/5d1330a017bb/pharmaceutics-12-00465-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/5ceffe4213d9/pharmaceutics-12-00465-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/1d74d9566736/pharmaceutics-12-00465-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/e89fae42359d/pharmaceutics-12-00465-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/fff9fc1ad8b8/pharmaceutics-12-00465-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/195ff54d2ad9/pharmaceutics-12-00465-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/728b0f343004/pharmaceutics-12-00465-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/1df832e2a8d8/pharmaceutics-12-00465-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/587efc5077ce/pharmaceutics-12-00465-g013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/18c9a22ccf56/pharmaceutics-12-00465-g014.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/da872f6b6377/pharmaceutics-12-00465-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/2ccd89aaee73/pharmaceutics-12-00465-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/440c2522523c/pharmaceutics-12-00465-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/91e81f9b0b58/pharmaceutics-12-00465-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/5d1330a017bb/pharmaceutics-12-00465-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/5ceffe4213d9/pharmaceutics-12-00465-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/1d74d9566736/pharmaceutics-12-00465-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/e89fae42359d/pharmaceutics-12-00465-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/fff9fc1ad8b8/pharmaceutics-12-00465-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/195ff54d2ad9/pharmaceutics-12-00465-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/728b0f343004/pharmaceutics-12-00465-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/1df832e2a8d8/pharmaceutics-12-00465-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/587efc5077ce/pharmaceutics-12-00465-g013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fe1/7284610/18c9a22ccf56/pharmaceutics-12-00465-g014.jpg

相似文献

1
Fabrication of Transgelosomes for Enhancing the Ocular Delivery of Acetazolamide: Statistical Optimization, In Vitro Characterization, and In Vivo Study.用于增强乙酰唑胺眼部递送的转凝胶体的制备：统计优化、体外表征和体内研究。
Pharmaceutics. 2020 May 20;12(5):465. doi: 10.3390/pharmaceutics12050465.
2
Formulation of Nanospanlastics as a Promising Approach for ‎Improving the Topical Delivery of a Natural Leukotriene Inhibitor (3-‎Acetyl-11-Keto-β-Boswellic Acid): Statistical Optimization, in vitro ‎Characterization, and ex vivo Permeation Study.将纳米弹性体制剂作为一种有前途的方法来提高天然白三烯抑制剂（3-乙酰基-11-酮-β-乳香酸）的局部递送：统计优化、体外特性和体外渗透研究。
Drug Des Devel Ther. 2020 Sep 15;14:3697-3721. doi: 10.2147/DDDT.S265167. eCollection 2020.
3
Nanogel loaded with surfactant based nanovesicles for enhanced ocular delivery of acetazolamide.载有表面活性剂纳米囊泡的纳米凝胶用于增强乙酰唑胺的眼部递药。
Int J Nanomedicine. 2019 Apr 29;14:2973-2983. doi: 10.2147/IJN.S201891. eCollection 2019.
4
Formulation of Sodium Valproate Nanospanlastics as a Promising Approach for Drug Repurposing in the Treatment of Androgenic Alopecia.丙戊酸钠纳米弹性体的配方作为雄激素性脱发治疗中药物重新利用的一种有前景的方法。
Pharmaceutics. 2020 Sep 11;12(9):866. doi: 10.3390/pharmaceutics12090866.
5
Fabrication of acetazolamide loaded leciplex for intraocular delivery: Optimization by 3 full factorial design, in vitro, ex vivo and in vivo pharmacodynamics.载乙酰唑胺的 Leciplex 的制备：通过 3 因素完全设计进行优化，体外、离体和体内药效学。
Int J Pharm. 2024 Aug 15;661:124391. doi: 10.1016/j.ijpharm.2024.124391. Epub 2024 Jun 25.
6
Development, in vitro and in vivo characterization of Eudragit RL 100 nanoparticles for improved ocular bioavailability of acetazolamide.Eudragit RL 100 纳米粒的制备、体外与体内评价及其用于提高乙酰唑胺眼部生物利用度的研究
Drug Deliv. 2013 Sep-Oct;20(7):269-76. doi: 10.3109/10717544.2013.834417.
7
Acetazolamide encapsulated dendritic nano-architectures for effective glaucoma management in rabbits.用于有效治疗兔青光眼的乙酰唑胺包封树枝状纳米结构
Int J Pharm. 2014 Jan 30;461(1-2):380-90. doi: 10.1016/j.ijpharm.2013.11.043. Epub 2013 Nov 28.
8
Sustained ocular delivery of Dorzolamide-HCl via proniosomal gel formulation: in-vitro characterization, statistical optimization, and in-vivo pharmacodynamic evaluation in rabbits.通过前体脂质体凝胶制剂实现盐酸多佐胺的眼部持续递送：在兔体内的体外特征描述、统计优化和药效动力学评价。
Drug Deliv. 2018 Nov;25(1):1340-1349. doi: 10.1080/10717544.2018.1477861.
9
Design and optimization of acetazolamide nanoparticle-laden contact lens using statistical experimental design for controlled ocular drug delivery.采用统计实验设计的载乙酰唑胺纳米粒子隐形眼镜的设计和优化用于控制眼部药物传递。
J Biomater Sci Polym Ed. 2024 Dec;35(18):2884-2908. doi: 10.1080/09205063.2024.2391233. Epub 2024 Aug 19.
10
Corneal targeted fenticonazole nitrate-loaded novasomes for the management of ocular candidiasis: Preparation, characterization, and assessments.载有硝酸芬替康唑的角膜靶向诺瓦索姆用于眼部念珠菌病的治疗：制备、表征和评估。
Drug Deliv. 2022 Dec;29(1):2428-2441. doi: 10.1080/10717544.2022.2103600.

引用本文的文献

1
Fabrication and appraisal of targeted axitinib loaded bilosomes for the enhanced breast and ovarian anticancer activity.用于增强乳腺癌和卵巢癌抗癌活性的靶向阿昔替尼负载双分子层脂质体的制备与评价
PLoS One. 2025 Jul 17;20(7):e0325511. doi: 10.1371/journal.pone.0325511. eCollection 2025.
2
Polyol-modified deformable liposomes fortified contact lenses for improved ocular permeability.多元醇修饰的可变形脂质体强化隐形眼镜以提高眼部通透性。
Nanomedicine (Lond). 2025 Apr;20(7):649-662. doi: 10.1080/17435889.2025.2463867. Epub 2025 Feb 18.
3
Development and Evaluation of Nano-Vesicular Emulsion-Based Gel as a Promising Approach for Dermal Atorvastatin Delivery Against Inflammation.

本文引用的文献

1
Disulfiram thermosensitive in-situ gel based on solid dispersion for cataract.基于固体分散体的用于白内障治疗的双硫仑热敏原位凝胶
Asian J Pharm Sci. 2018 Nov;13(6):527-535. doi: 10.1016/j.ajps.2018.02.010. Epub 2018 Apr 23.
2
Topical delivery of acetazolamide by encapsulating in mucoadhesive nanoparticles.通过包裹在粘膜粘附纳米颗粒中进行乙酰唑胺的局部给药。
Asian J Pharm Sci. 2017 Nov;12(6):550-557. doi: 10.1016/j.ajps.2017.04.005. Epub 2017 May 16.
3
Poloxamer Hydrogels for Biomedical Applications.用于生物医学应用的泊洛沙姆水凝胶
基于纳米囊泡乳液的凝胶的研制与评价：一种有前途的经皮递送阿托伐他汀治疗炎症的方法。
Int J Nanomedicine. 2024 Nov 7;19:11415-11432. doi: 10.2147/IJN.S477001. eCollection 2024.
4
Ocular mucoadhesive and biodegradable spanlastics loaded cationic spongy insert for enhancing and sustaining the anti-inflammatory effect of prednisolone Na phosphate; Preparation, I-optimal optimization, and In-vivo evaluation.用于增强和维持磷酸泼尼松龙抗炎作用的眼用粘膜粘附性和可生物降解的Spanlastics负载阳离子海绵插入物；制备、I-最优优化和体内评价
Int J Pharm X. 2024 Oct 16;8:100293. doi: 10.1016/j.ijpx.2024.100293. eCollection 2024 Dec.
5
Maximizing the Use of Ivermectin Transethosomal Cream in the Treatment of Scabies.最大限度地利用伊维菌素转质体乳膏治疗疥疮。
Pharmaceutics. 2024 Aug 1;16(8):1026. doi: 10.3390/pharmaceutics16081026.
6
Formulation Development of Meloxicam Binary Ethosomal Hydrogel for Topical Delivery: In Vitro and In Vivo Assessment.用于局部给药的美洛昔康二元醇质体水凝胶的制剂开发：体外和体内评估
Pharmaceutics. 2024 Jul 4;16(7):898. doi: 10.3390/pharmaceutics16070898.
7
Vesicular Drug Delivery Systems: Promising Approaches in Ocular Drug Delivery.囊泡药物递送系统：眼部药物递送的有前景的方法。
Pharmaceuticals (Basel). 2024 Apr 16;17(4):511. doi: 10.3390/ph17040511.
8
Formulation of Deformable Liponiosomal Hybrid of Repaglinide: In vitro Characterization and Evaluation of the Anti-Diabetic Effect.瑞格列奈变形脂质体杂化物的制剂：体外特性分析及抗糖尿病作用评价。
Int J Nanomedicine. 2023 Dec 7;18:7417-7440. doi: 10.2147/IJN.S434840. eCollection 2023.
9
Curcumin Transferosome-Loaded Thermosensitive Intranasal in situ Gel as Prospective Antiviral Therapy for SARS-Cov-2.姜黄素传递体负载温敏型鼻内原位凝胶作为 SARS-CoV-2 的新型抗病毒治疗策略。
Int J Nanomedicine. 2023 Oct 17;18:5831-5869. doi: 10.2147/IJN.S423251. eCollection 2023.
10
Reinvestigation of Passerini and Ugi scaffolds as multistep apoptotic inducers dual modulation of caspase 3/7 and P53-MDM2 signaling for halting breast cancer.重新研究Passerini和Ugi支架作为多步凋亡诱导剂：对caspase 3/7和P53-MDM2信号进行双重调节以阻止乳腺癌
RSC Adv. 2023 Sep 20;13(40):27722-27737. doi: 10.1039/d3ra04029a. eCollection 2023 Sep 18.
Pharmaceutics. 2019 Dec 10;11(12):671. doi: 10.3390/pharmaceutics11120671.
4
Promising Approach in the Treatment of Glaucoma Using Nanotechnology and Nanomedicine-Based Systems.利用纳米技术和基于纳米医学的系统治疗青光眼的有前途的方法。
Molecules. 2019 Oct 22;24(20):3805. doi: 10.3390/molecules24203805.
5
Cubic and hexagonal liquid crystal gels for ocular delivery with enhanced effect of pilocarpine nitrate on anti-glaucoma treatment.用于眼部给药的立方相和六方相液晶凝胶，增强硝酸毛果芸香碱的抗青光眼治疗效果。
Drug Deliv. 2019 Dec;26(1):952-964. doi: 10.1080/10717544.2019.1667451.
6
Poloxamer-based in situ gelling thermoresponsive systems for ocular drug delivery applications.泊洛沙姆基原位凝胶温敏递药系统及其在眼部给药中的应用。
Drug Discov Today. 2019 Aug;24(8):1575-1586. doi: 10.1016/j.drudis.2019.05.036. Epub 2019 Jun 5.
7
Proniosomal gel-derived niosomes: an approach to sustain and improve the ocular delivery of brimonidine tartrate; formulation, in-vitro characterization, and in-vivo pharmacodynamic study.原前体凝胶衍生的尼莫司汀：一种持续改善酒石酸溴莫尼定眼部递药的方法；制剂、体外特征及体内药效学研究。
Drug Deliv. 2019 Dec;26(1):509-521. doi: 10.1080/10717544.2019.1609622.
8
Gellan Gum Based Transforming System of Natamycin Transfersomes Improves Topical Ocular Delivery.基于结冷胶的那他霉素传递体转化系统改善了局部眼用递药。
J Pharmacol Exp Ther. 2019 Sep;370(3):814-822. doi: 10.1124/jpet.119.256446. Epub 2019 Mar 14.
9
The Role of Surface Active Agents in Ophthalmic Drug Delivery: A Comprehensive Review.表面活性剂在眼科药物传递中的作用：全面综述。
J Pharm Sci. 2019 Jun;108(6):1923-1933. doi: 10.1016/j.xphs.2019.01.016. Epub 2019 Jan 23.
10
In Situ Gel of Triamcinolone Acetonide-Loaded Solid Lipid Nanoparticles for Improved Topical Ocular Delivery: Tear Kinetics and Ocular Disposition Studies.用于改善眼部局部给药的载曲安奈德固体脂质纳米粒原位凝胶：泪液动力学和眼部处置研究
Nanomaterials (Basel). 2018 Dec 27;9(1):33. doi: 10.3390/nano9010033.