由 Mafenide 和吲哚美辛开发的超分子水凝胶作为一种合理的多药自递送系统作为抗菌和抗炎外用凝胶,ACS Applied Bio Materials

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由 Mafenide 和吲哚美辛开发的超分子水凝胶作为一种合理的多药自递送系统作为抗菌和抗炎外用凝胶
ACS Applied Bio Materials ( IF 4.6 ) Pub Date : 2022-02-10 , DOI: 10.1021/acsabm.1c01089
Rajdip Roy ₁ , Joydeb Majumder ₁ , Hemanta Kumar Datta ₁ , Rumana Parveen ₁ , Parthasarathi Dastidar ₁

Affiliation

根据结构原理，一系列简单的有机盐衍生自 mafenide（一种用于治疗烧伤的药物）和正烷基羧酸（Me-(CH ₂ ) _n -COOH；n = 1-3, 10-15）和各种非甾体抗炎药 (NSAID)，即消炎痛 ( IND)、双氯芬酸 ( DIC)、甲氯芬那酸 ( MEC )、托芬那酸 ( TOL ) 和氟芬那酸 ( FLU )（分别命名为盐1-14）被合成为潜在的水凝胶剂。凝胶化研究表明，mafenide n-烷基羧酸盐与n= 11-14，即盐5-8，和 mafenide 的吲哚美辛盐，即盐10，是水凝胶剂。相应的水凝胶，即5(HG) - 8(HG)和10(HG)，通过桌面和动态流变学以及高分辨率透射电子显微镜 (HR-TEM) 进行了表征。非凝胶盐1-3和凝胶盐 10的单晶结构由 X 射线衍射确定。从各种研究中获得的结果，包括盐10的溶解度、生物稳定性、生物相容性（MTT 测定）和抗炎（PGE ₂测定）反应，盐10、其组分和10 ( HG )的抗菌反应（区域抑制测定），以及盐10在体外在 37 °C 下 24 小时内从相应的水凝胶床释放到本体溶剂中，表明它们的合理性用于开发用于自递送应用的多药衍生的局部水凝胶。

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Supramolecular Hydrogels Developed from Mafenide and Indomethacin as a Plausible Multidrug Self-Delivery System as Antibacterial and Anti-inflammatory Topical Gels

Following a structural rationale, a series of simple organic salts derived from mafenide (a drug for treating burn wounds) and n-alkyl carboxylic acids (Me–(CH₂)_n–COOH; n = 1–3, 10–15) and various nonsteroidal anti-inflammatory drugs (NSAIDs), namely, indomethacin (IND), diclofenac (DIC), meclofenamic acid (MEC), tolfenamic acid (TOL), and flufenamic acid (FLU) (designated as salts 1–14, respectively) were synthesized as potential hydrogelators. Gelation studies revealed that mafenide n-alkyl carboxylates with n = 11–14, i.e., salts 5–8, and the indomethacin salt of mafenide, i.e., salt 10, were hydrogelators. The corresponding hydrogels, namely, 5(HG)–8(HG) and 10(HG), were characterized by table-top and dynamic rheology and high-resolution transmission electron microscopy (HR-TEM). Single-crystal structures of the nongelator salts 1–3 and the gelator salt 10 were determined by X-ray diffraction. The results obtained from various studies, which included the solubility, biostability, biocompatibility (MTT assay), and anti-inflammatory (PGE₂ assay) response of salt 10, the antibacterial response (zone inhibition assay) of salt 10, its components, and 10(HG), and the release of salt 10in vitro from the corresponding hydrogel bed to the bulk solvent at 37 °C in 24 h, suggested their plausible use in developing multidrug-derived topical hydrogels for self-delivery applications.

更新日期：2022-02-10

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