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基于纤维素衍生物的热敏凝胶用于治疗痤疮时局部递送蜂胶。

Thermosensitive gel based on cellulose derivative for topical delivery of propolis in acne treatment.

机构信息

Laboratory of Research and Development of Drug Delivery Systems, Postgraduate Program in Pharmaceutical Sciences, Department of Pharmacy, State University of Maringa, Maringa, Brazil.

Laboratory of Basic and Applied Bacteriology NIP3, Department of Microbiology, Center of Biological Sciences, State University of Londrina, Londrina, Brazil.

出版信息

Pharm Dev Technol. 2022 Apr;27(4):490-501. doi: 10.1080/10837450.2022.2080221. Epub 2022 May 29.

Abstract

Thermosensitive bioadhesive formulations can display increased retention time, skin permeation, and improve the topical therapy of many drugs. Acne is an inflammatory process triggered by several factors like the proliferation of the bacteria . Aiming for a new alternative treatment with a natural source, propolis displays great potential due to its antibiotic, anti-inflammatory, and healing properties. This study describes the development of bioadhesive thermoresponsive platform with cellulose derivatives and poloxamer 407 for propolis skin delivery. Propolis ethanolic extract (PES) was added to the formulations with sodium carboxymethylcellulose (CMC) or hydroxypropyl methylcellulose (HPMC) and poloxamer 407 (Polox). The formulations were characterized as rheology, bioadhesion, and mechanical analysis. The selected formulations were investigated as propolis release, cytotoxicity, skin permeation by Fourier Transform Infrared Photoacoustic Spectroscopy, and the activity against . Formulations showed suitable sol-gel transition temperature, shear-thinning behavior, and texture profile. CMC presence decreased the cohesiveness and adhesiveness of formulations. Polox/HPMC/PES system displayed less cytotoxicity, modified propolis release governed by anomalous transport, skin permeation, and activity against . These results indicate important advantages in the topical treatment of acne and suggest a potential formulation for clinical evaluation.

摘要

热敏型生物黏附制剂可以增加滞留时间、增加皮肤渗透,从而改善许多药物的局部治疗效果。痤疮是一种由多种因素引发的炎症过程,如细菌增殖。为了寻找一种新的天然来源替代疗法,蜂胶由于其具有抗生素、抗炎和愈合特性而显示出巨大的潜力。本研究描述了以纤维素衍生物和泊洛沙姆 407 为载体制备用于蜂胶皮肤给药的热敏型生物黏附性平台。将蜂胶乙醇提取物(PES)加入到含有羧甲基纤维素钠(CMC)或羟丙基甲基纤维素(HPMC)和泊洛沙姆 407(Polox)的制剂中。对制剂进行了流变学、生物黏附性和机械性能分析。选择的制剂进行了蜂胶释放、细胞毒性、傅里叶变换红外光声光谱法皮肤渗透以及对 的活性研究。制剂具有合适的溶胶-凝胶转变温度、剪切稀化行为和质构特性。CMC 的存在降低了制剂的内聚性和黏附性。Polox/HPMC/PES 体系显示出较低的细胞毒性、改性的蜂胶释放由非定常传输控制、皮肤渗透和对 的活性。这些结果表明在痤疮的局部治疗中有重要的优势,并为临床评估提供了一种有潜力的制剂。

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