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用于靶向皮肤肿瘤治疗的卡波姆基卟啉凝胶的配方与表征:物理化学和药剂学见解

Formulation and Characterization of Carbopol-Based Porphyrin Gels for Targeted Dermato-Oncological Therapy: Physicochemical and Pharmacotechnical Insights.

作者信息

Ozon Emma Adriana, Anastasescu Mihai, Musuc Adina Magdalena, Burloiu Andreea Mihaela, Socoteanu Radu Petre, Atkinson Irina, Mitran Raul-Augustin, Culita Daniela C, Lupuliasa Dumitru, Mihai Dragos Paul, Gird Cerasela Elena, Boscencu Rica

机构信息

Faculty of Pharmacy, "Carol Davila" University of Medicine and Pharmacy, 6 Traian Vuia St., 020956 Bucharest, Romania.

Institute of Physical Chemistry-Ilie Murgulescu, Romanian Academy, 202 Spl. Independentei, 060021 Bucharest, Romania.

出版信息

Int J Mol Sci. 2025 Apr 11;26(8):3641. doi: 10.3390/ijms26083641.

Abstract

Malignant skin conditions are classified as the most common forms of cancer, with an evolution of one million new cases reported every year. Research efforts in the medical field are focused on developing innovative strategies for the dissemination of measures for preventing cancer and providing new antitumor compounds. The present research examines the development and evaluation of 1% Carbopol-based hydrogels incorporating two porphyrin derivatives-5,10,15,20-tetrakis-(4-acetoxy-3-methoxyphenyl) porphyrin (P2.1) and 5-(4-hydroxy-3-methoxyphenyl)-10,15,20-tris-(4-acetoxy-3-methoxyphenyl) porphyrin (P2.2)-to create formulations suitable for topical photodynamic therapy (PDT) applications. The physicochemical properties of the obtained hydrogels were carefully evaluated, revealing the successful integration of the porphyrins into the 1% Carbopol hydrogel matrix. Rheological analysis demonstrated pseudoplastic behavior, with an increase in viscosity properties for P2.1 and P2.2, suggesting interactions with the Carbopol polymer structure. UV-visible and fluorescence spectroscopy confirmed the maintenance of the porphyrins' photodynamic properties, essential for therapeutic efficacy. Pharmacotechnical studies highlighted the hydrogels' suitability for topical applications. The formulations maintained an optimal pH range, ensuring skin compatibility and minimizing the potential for skin irritation. Their mechanical properties, including elasticity and rigidity, provided stability during handling and application. The high swelling capacity indicated effective moisture retention, enhancing skin hydration and drug release potential. Furthermore, the hydrogels demonstrated excellent spreadability, enabling uniform application and coverage, crucial for efficient light activation of the photosensitizers. The combination of robust physicochemical and pharmacotechnical properties highlights the potential of these porphyrin-loaded 1% Carbopol hydrogels as promising carriers for topical PDT. These results permit further biological and therapeutic investigations to optimize the formulation for clinical use, advancing the development of effective localized photodynamic therapies.

摘要

恶性皮肤疾病被归类为最常见的癌症形式,每年报告的新病例达100万例。医学领域的研究工作集中在制定传播癌症预防措施的创新策略以及提供新的抗肿瘤化合物。本研究考察了含两种卟啉衍生物——5,10,15,20-四-(4-乙酰氧基-3-甲氧基苯基)卟啉(P2.1)和5-(4-羟基-3-甲氧基苯基)-10,15,20-三-(4-乙酰氧基-3-甲氧基苯基)卟啉(P2.2)的1%卡波姆水凝胶的开发与评估,以制备适用于局部光动力疗法(PDT)应用的制剂。对所得水凝胶的物理化学性质进行了仔细评估,结果表明卟啉成功地整合到了1%卡波姆水凝胶基质中。流变学分析表明其具有假塑性行为,P2.1和P2.2的粘度特性增加,表明与卡波姆聚合物结构存在相互作用。紫外可见光谱和荧光光谱证实了卟啉光动力性质的保持,这对治疗效果至关重要。药物技术研究突出了这些水凝胶在局部应用方面的适用性。这些制剂保持了最佳的pH范围,确保了皮肤相容性并将皮肤刺激的可能性降至最低。它们的机械性能,包括弹性和刚性,在处理和应用过程中提供了稳定性。高溶胀能力表明其具有有效的保湿性,增强了皮肤水合作用和药物释放潜力。此外,这些水凝胶表现出优异的铺展性,能够均匀涂抹和覆盖,这对于光敏剂的有效光激活至关重要。强大的物理化学和药物技术性质相结合,突出了这些负载卟啉的1%卡波姆水凝胶作为局部PDT有前景载体的潜力。这些结果允许进一步进行生物学和治疗学研究,以优化制剂用于临床,推动有效的局部光动力疗法的发展。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cca5/12026875/b81680f26768/ijms-26-03641-g001.jpg

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