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微囊化α-生育酚的卡波姆水凝胶:聚焦微胶囊的生物相容性、局部应用特性及体外释放研究

Carbomer Hydrogels with Microencapsulated α-Tocopherol: Focus on the Biocompatibility of the Microcapsules, Topical Application Attributes, and In Vitro Release Study.

作者信息

Đekić Ljiljana, Milinković Budinčić Jelena, Stanić Dušanka, Fraj Jadranka, Petrović Lidija

机构信息

Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, University of Belgrade, 11221 Belgrade, Serbia.

Department of Pharmaceutical Engineering, Faculty of Technology Novi Sad, University of Novi Sad, 21000 Novi Sad, Serbia.

出版信息

Pharmaceutics. 2024 May 7;16(5):628. doi: 10.3390/pharmaceutics16050628.

Abstract

The microencapsulation of α-tocopherol based on the complex coacervation of low-molecular-weight chitosan (LMWC) and sodium lauryl ether sulphate (SLES) without harmful crosslinkers can provide biocompatible carriers that protect it from photodegradation and air oxidation. In this study, the influence of the microcapsule wall composition on carrier performance, compatibility with a high-water-content vehicle for topical application, and release of α-tocopherol were investigated. Although the absence of aldehyde crosslinkers decreased the encapsulation efficiency of α-tocopherol (~70%), the variation in the LMWC/SLES mass ratio (2:1 or 1:1) had no significant effect on the moisture content and microcapsule size. The prepared microcapsule-loaded carbomer hydrogels were soft semisolids with pseudoplastic flow behavior. The integrity of microcapsules embedded in the hydrogel was confirmed by light microscopy. The microcapsules reduced the pH, apparent viscosity, and hysteresis area of the hydrogels, while increasing their spreading ability on a flat inert surface and dispersion rate in artificial sweat. The in vitro release of α-tocopherol from crosslinker-free microcapsule-loaded hydrogels was diffusion-controlled. The release profile was influenced by the LMWC/SLES mass ratio, apparent viscosity, type of synthetic membrane, and acceptor medium composition. Better data quality for the model-independent analysis was achieved when a cellulose nitrate membrane and ethyl alcohol 60% as acceptor medium were used.

摘要

基于低分子量壳聚糖(LMWC)和月桂醇聚醚硫酸酯钠(SLES)的复凝聚作用对α-生育酚进行微囊化,无需使用有害交联剂,可提供生物相容性载体,保护其免受光降解和空气氧化。在本研究中,研究了微胶囊壁组成对载体性能、与高含水量局部应用载体的相容性以及α-生育酚释放的影响。尽管不含醛类交联剂降低了α-生育酚的包封效率(约70%),但LMWC/SLES质量比(2:1或1:1)的变化对水分含量和微胶囊尺寸没有显著影响。制备的微胶囊负载卡波姆水凝胶为具有假塑性流动行为的软半固体。通过光学显微镜确认了嵌入水凝胶中的微胶囊的完整性。微胶囊降低了水凝胶的pH值、表观粘度和滞后面积,同时提高了它们在平坦惰性表面上的铺展能力和在人工汗液中的分散速率。无交联剂的微胶囊负载水凝胶中α-生育酚的体外释放是扩散控制的。释放曲线受LMWC/SLES质量比、表观粘度、合成膜类型和受体介质组成的影响。当使用硝酸纤维素膜和60%乙醇作为受体介质时,模型无关分析可获得更好的数据质量。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b2b/11125425/d5060ca41fd8/pharmaceutics-16-00628-g001.jpg

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