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载多西环素脂质体凝胶的透皮给药系统:旨在提高多西环素稳定性

Transdermal Delivery System of Doxycycline-Loaded Niosomal Gels: Toward Enhancing Doxycycline Stability.

作者信息

Zaid Alkilani Ahlam, Sharaire Zaina, Hamed Rania, Basheer Haneen A

机构信息

Department of Pharmacy, Faculty of Pharmacy, Zarqa University, Zarqa 13110, Jordan.

Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman 11733, Jordan.

出版信息

ACS Omega. 2024 Jul 23;9(31):33542-33556. doi: 10.1021/acsomega.4c01224. eCollection 2024 Aug 6.

Abstract

Doxycycline (DOX) is an antimicrobial agent that is susceptible to photosensitivity and thermal degradation. It addition, it causes gastrointestinal side effects when taken orally. Therefore, the development of alternative formulations is necessary to improve drug stability and promote patient compliance. The aim of the present study was to encapsulate DOX in niosomes as a nanocarrier to deliver DOX transdermally and enhance its stability in the formulation. DOX niosomes were prepared using nonionic surfactants, cholesterol, and dihexadecyl phosphate (DCP). After that, niosomes were characterized in terms of practical size (PS), zeta potential (ZP), morphology, and entrapment efficacy (EE%). DOX niosomal gels were then prepared using Carbopol and penetration enhancers (poly(ethylene glycol) 400 (PEG 400) and propylene glycol (PG)). The flux of DOX from the optimized formula was 322.86 μg/cm/h over 5 h, which equates to 71.2% of DOX. Furthermore, neither the DOX niosomal gel (D3) nor the comparable blank niosomal gel had a negative influence on human dermal fibroblast (HDF) cells. The findings of the antimicrobial effectiveness of DOX niosomes indicated that the niosomal formulation improved the antibacterial activity of DOX against . Permeation studies demonstrated significantly higher DOX permeation when the niosomal gel was applied to rat skin, compared to the conventional gel. Permeability parameters such as flux and the permeability coefficient increased more than 10-fold using the niosomal gels compared with those of conventional gels. In conclusion, a new niosomal gel formulation could serve as an effective alternative for the commercially available form of DOX.

摘要

多西环素(DOX)是一种易发生光敏反应和热降解的抗菌剂。此外,口服时它会引起胃肠道副作用。因此,有必要开发替代制剂以提高药物稳定性并促进患者依从性。本研究的目的是将DOX包裹在作为纳米载体的囊泡中,以实现DOX的经皮递送并提高其在制剂中的稳定性。使用非离子表面活性剂、胆固醇和磷酸二己酯(DCP)制备DOX囊泡。之后,对囊泡的实际大小(PS)、zeta电位(ZP)、形态和包封率(EE%)进行了表征。然后使用卡波姆和渗透促进剂(聚乙二醇400(PEG 400)和丙二醇(PG))制备DOX囊泡凝胶。优化配方中DOX在5小时内的通量为322.86μg/cm/h,相当于DOX的71.2%。此外,DOX囊泡凝胶(D3)和可比的空白囊泡凝胶对人皮肤成纤维细胞(HDF)均无负面影响。DOX囊泡抗菌有效性的研究结果表明,囊泡制剂提高了DOX对……的抗菌活性。渗透研究表明,与传统凝胶相比,将囊泡凝胶应用于大鼠皮肤时,DOX的渗透显著更高。与传统凝胶相比,使用囊泡凝胶时通量和渗透系数等渗透参数增加了10倍以上。总之,一种新的囊泡凝胶制剂可作为市售DOX剂型的有效替代品。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6f9e/11307314/ddf3bae43ecb/ao4c01224_0001.jpg

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