Development of a Self-Assembled Hydrogels Based on Carboxymethyl Chitosan and Oxidized Hyaluronic Acid Containing Tanshinone Extract Nanocrystals for Enhanced Dissolution and Acne Treatment.
Development of a Self-Assembled Hydrogels Based on Carboxymethyl Chitosan and Oxidized Hyaluronic Acid Containing Tanshinone Extract Nanocrystals for Enhanced Dissolution and Acne Treatment.
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开发基于羧甲基壳聚糖和含丹参酮提取物纳米晶体的氧化透明质酸的自组装水凝胶，用于增强溶解和痤疮治疗
DOI：
10.3390/ph15121534
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发表时间：
2022-12-09
期刊：
影响因子：
--
通讯作者：
Gao R
中科院分区：
文献类型：
--
作者：
Tang X;Liu Y;Yuan H;Gao R
本研究旨在基于羧甲基壳聚糖（CMC）和氧化透明质酸（OHA）的自组装行为构建pH响应性纳米晶水凝胶药物递送系统，用于局部递送不溶性药物。采用介电研磨法制备丹参酮纳米晶（TNCs）提取物，考察药物稳定剂的种类和配比优化处方，并采用效应面法优化制备工艺。采用高碘酸钠氧化法制备OHA，并以凝胶形成时间为指标优化CMC和OHA的浓度。将OHA溶解在TNCs中，与CMC溶液自组装形成丹参酮提取物纳米晶水凝胶（CMC-OHA/TNCs），并对其理化性质和体外抗菌活性进行评价。结果表明，优化处方和工艺可制得丹参酮提取物纳米晶，粒径为（223.67±4.03）nm，多分散指数（PDI）为0.2173±0.0008。根据SEM和XRD结果，TNCs以纳米粒子的形式完全包裹在水凝胶中，TNCs的结晶度降低，CMC-OHA/TNCs中的衍射峰几乎消失。体外透皮试验结果表明，CMC-OHA/TNCs可以在痤疮皮损处持续释放药物。细胞计数试剂盒8（CCK-8）检测证实CMC-OHA/TNCs没有明显的细胞毒性。 CMC-OHA/TNCs对痤疮丙酸杆菌和金黄色葡萄球菌的最低抑菌浓度（MIC）和最低杀菌浓度（MBC）均显着低于TNCs和丹参酮提取物粗悬液，且抑菌圈直径显着大于TNCs和丹参酮提取物粗悬液。这项研究表明，CMC-OHA/TNCs 是一种有前途的局部递送不溶性药物的递送系统，它可以提高丹参酮提取物的溶解度并增强其体外细菌抑制活性。
This study aimed to construct a pH-responsive nanocrystalline hydrogel drug delivery system for topical delivery of insoluble drugs based on the self-assembly behavior of carboxymethyl chitosan (CMC) and oxidized hyaluronic acid (OHA). The tanshinone nanocrystal (TNCs) extract was prepared by dielectric milling method, the type and ratio of stabilizer of the drug were investigated to optimize the prescription, and the effector surface method was used to optimize the preparation process. OHA was prepared by the sodium periodate oxidation method, and the concentration of CMC and OHA was optimized using gel formation time as an indicator. OHA was dissolved in TNCs and self-assembled with CMC solution to form tanshinone extract nanocrystal hydrogels (CMC-OHA/TNCs), of which the physicochemical properties and in vitro antibacterial activity were evaluated. Results showed that the optimized prescription and process could produce tanshinone extract nanocrystals with a particle size of (223.67 ± 4.03) nm and a polydispersity index (PDI) of 0.2173 ± 0.0008. According to SEM and XRD results, TNCs were completely wrapped in the hydrogel as nanoparticles, and the crystallinity of TNCs was reduced and the diffraction peaks in CMC-OHA/TNCs almost disappeared. In vitro, transdermal test results showed that CMC-OHA/TNCs could release the drug continuously at the acne lesions. The cell-counting kit-8 (CCK-8) assay confirmed that the CMC-OHA/TNCs had no obvious cytotoxicity. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of CMC-OHA/TNCs against Propionibacterium acnes and Staphylococcus aureus were significantly lower and the diameter of the inhibition circle was obviously higher than that of TNCs and tanshinone extract crude suspension. This study demonstrated that CMC-OHA/TNCs was a promising delivery system for topical delivery of insoluble drugs, which could improve the solubility of tanshinone extract and enhance its in vitro bacterial inhibitory activity.
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DOI：
10.3390/ph14080712
发表时间：
2021-07-23
期刊：
Pharmaceuticals (Basel, Switzerland)
影响因子：
--
作者：
Sip S;Paczkowska-Walendowska M;Rosiak N;Miklaszewski A;Grabańska-Martyńska K;Samarzewska K;Cielecka-Piontek J
通讯作者：
Cielecka-Piontek J
影响因子：
18.9
作者：
Hu B;Gao M;Boakye-Yiadom KO;Ho W;Yu W;Xu X;Zhang XQ
通讯作者：
Zhang XQ
影响因子：
4.4
作者：
Li Y;Xi P;Wang T;Miao MS
通讯作者：
Miao MS
影响因子：
5.4
作者：
Navarro-Partida J;Castro-Castaneda CR;Santa Cruz-Pavlovich FJ;Aceves-Franco LA;Guy TO;Santos A
通讯作者：
Santos A
影响因子：
4.5
作者：
Say YH;Heng AHS;Reginald K;Wong YR;Teh KF;Rawanan Shah SM;Sio YY;Ng YT;Matta SA;Pang SL;Chew FT
通讯作者：
Chew FT