de Oliveira Évelin L, Ferreira Sabrina B S, de Castro-Hoshino Lidiane V, Campanholi Katieli da S S, Calori Italo R, de Morais Flávia A P, Kimura Elza, da Silva Junior Ranulfo C, Bruschi Marcos L, Sato Francielle, Hioka Noboru, Caetano Wilker
Department of Chemistry, Research Nucleus of Photodynamic Therapy, State University of Maringá, Avenue Colombo 5790, Maringá, Paraná 87020-900, Brazil.
Department of Pharmacy, Laboratory of Research and Development of Drug Delivery Systems, State University of Maringá, Avenue Colombo 5790, Maringá, Paraná 87020-900, Brazil.
Langmuir. 2021 Mar 16;37(10):3202-3213. doi: 10.1021/acs.langmuir.1c00148. Epub 2021 Mar 8.
Phthalocyanine aluminum chloride (Pc) is a clinically viable photosensitizer (PS) to treat skin lesions worsened by microbial infections. However, this molecule presents a high self-aggregation tendency in the biological fluid, which is an direct administration obstacle. This study proposed the use of bioadhesive and thermoresponsive hydrogels comprising triblock-type Pluronic F127 and Carbopol 934P (FCarb) as drug delivery platforms of Pc (FCarbPc)-targeting topical administration. Carbopol 934P was used to increase the F127 hydrogel adhesion on the skin. Rheological analyses showed that the Pc presented a low effect on the hydrogel matrix, changing the gelation temperature from 27.2 ± 0.1 to 28.5 ± 0.9 °C once the Pc concentration increases from zero to 1 mmol L. The dermatological platform showed matrix erosion effects with the release of loaded Pc micelles. The permeation studies showed the excellent potential of the FCarb platform, which allowed the partition of the PS into deeper layers of the skin. The applicability of this dermatological platform in photodynamic therapy was evaluated by the generation of reactive species which was demonstrated by chemical photodynamic efficiency assays. The low effect on cell viability and proliferation in the dark was demonstrated by assays using L929 fibroblasts. The FCarbPc fostered the inhibition of strain, therefore demonstrating the platform's potential in the treatment of dermatological infections of microbial nature.
酞菁氯化铝（Pc）是一种临床上可行的用于治疗因微生物感染而恶化的皮肤损伤的光敏剂（PS）。然而，该分子在生物流体中呈现出较高的自聚集倾向，这是直接给药的障碍。本研究提出使用包含三嵌段型普朗尼克F127和卡波姆934P（FCarb）的生物粘附性和热响应性水凝胶作为Pc（FCarbPc）靶向局部给药的药物递送平台。卡波姆934P用于增强F127水凝胶在皮肤上的粘附性。流变学分析表明，Pc对水凝胶基质的影响较小，当Pc浓度从零增加到1 mmol/L时，凝胶化温度从27.2±0.1℃变为28.5±0.9℃。该皮肤病学平台显示出基质侵蚀效应以及负载的Pc胶束的释放。渗透研究表明FCarb平台具有出色的潜力，它能使PS分配到皮肤的更深层。通过化学光动力效率测定法证明的活性物质的产生，评估了该皮肤病学平台在光动力疗法中的适用性。使用L929成纤维细胞的测定法证明了在黑暗中对细胞活力和增殖的影响较小。FCarbPc促进了对菌株的抑制，因此证明了该平台在治疗微生物性皮肤病感染方面的潜力。
