Dataset Information

Microneedle Patches with O₂ Propellant for Deeply and Fast Delivering Photosensitizers: Towards Improved Photodynamic Therapy.

ABSTRACT: Photodynamic therapy (PDT) is an emerging technique for treating tumors. Especially, topical administration of photosensitizers (PSs) is more favorable for superficial tumor treatments with low systematic phototoxicity. Yet, ineffective migration of PSs to targeted tumor tissues and rapid consumption of O₂ during PDT greatly limit their effects. Herein, PS-loaded microneedle (MN) patches with O₂ propellant for a deeper and faster transdermal delivery of PS and improved PDT by embedding sodium percarbonate (SPC) into dissolving poly(vinyl pyrrolidone) MNs are presented. It is shown that SPC in the MNs can react with surrounding fluid to generate gaseous oxygen bubbles, forming vigorous fluid flows and thus greatly enhancing PS of chlorin e6 (Ce6) penetration in both hydrogel models and skin tissues. Reactive oxygen species (ROS) in hypoxic breast cancer cells (4T1 cells) are greatly increased by rapid penetration of PS and relief of hypoxia in vitro, and Ce6-loaded SPC MNs show an excellent cell-killing effect. Moreover, lower tumor growth rate and tumor mass after a 20-d treatment in tumor-bearing mice model verify the improved PDT in gaseous oxygen-droved delivery of PS. This study demonstrates a facile yet effective route of MN delivery of PSs for improved PDT in hypoxic tumor treatment.

SUBMITTER: Liu P

PROVIDER: S-EPMC9443460 | biostudies-literature | 2022 Sep

REPOSITORIES: biostudies-literature

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Publications

Microneedle Patches with O2 Propellant for Deeply and Fast Delivering Photosensitizers: Towards Improved Photodynamic Therapy.

Liu Pei P Fu Yangxue Y Wei Fulong F Ma Teng T Ren Jingli J Xie Zhanjun Z Wang Shanzheng S Zhu Jinjin J Zhang Lianbin L Tao Juan J Zhu Jintao J

Advanced science (Weinheim, Baden-Wurttemberg, Germany) 20220715 25

Photodynamic therapy (PDT) is an emerging technique for treating tumors. Especially, topical administration of photosensitizers (PSs) is more favorable for superficial tumor treatments with low systematic phototoxicity. Yet, ineffective migration of PSs to targeted tumor tissues and rapid consumption of O2 during PDT greatly limit their effects. Herein, PS-loaded microneedle (MN) patches with O2 propellant for a deeper and faster transdermal delivery of PS and improved PDT ...[more]

PMID: 35839467

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Project description:There are a number of lipophilic cations that can be chosen; the triphenylphosphonium (TPP) ion is particularly unique for mitochondrion targeting, mainly due to its simplicity in structure and ease to be linked to the target molecules. In this work, mitochondrion-targeted AB3-type novel phthalocyanine and porphyrin photosensitizers (PSs) were synthesized and their photophysical photochemical properties were defined. Fluorescence quantum yields (ΦF) are 0.009, 0.14, 0.13, and 0.13, and the singlet-oxygen quantum yields (ΦΔ) are 0.27, 0.75, 0.57, and 0.58 for LuPcPox(OAc), AB 3 TPP-Pc, AB 3 TPP-Por-C4, and AB 3 TPP-Por-C6, respectively. To evaluate the photodynamic efficacy of the TPP-conjugated PS cell viabilities of A549 and BEAS-2B lung cells were comparatively measured and IC-50 values were determined. AB 3 TPP-Por-C4, AB 3 TPP-Por-C6, and AB 3 TPP-Pc compounds compared to the reference molecules ZnPc and H 2 TPP were found to be highly cytotoxic (sub-micromolar concentration) under the light. LuPcPox(OAc) is the most effective molecule regarding cell killing (the activity). The cell killing of the TPP-conjugated porphyrin derivatives exhibits a similar response compared to LuPcPox(OAc) when the light absorbing factor of the PS is normalized at 660 nm: TPP-conjugated porphyrins absorb less light (lower extinction coefficient) but produce more radical species (higher singlet-oxygen quantum yield) and therefore effectively kill the cells. The singlet oxygen-producing capacity of AB 3 TPP-Pc is almost 3 times higher compared to LuPcPox(OAc) and 50% more efficient with respect to ZnPc, suggesting that TPP-conjugated phthalocyanine may serve as a good photosensitizer for photodynamic therapy (PDT). The high singlet oxygen generation capacity of these novel TPP-conjugated porphyrin and phthalocyanine PS suggests that they might be useful for PDT requiring lower photosensitizer concentration and reduced energy deposited through less light exposure.

Dataset Information

Microneedle Patches with O₂ Propellant for Deeply and Fast Delivering Photosensitizers: Towards Improved Photodynamic Therapy.

Publications

Microneedle Patches with O<sub>2</sub> Propellant for Deeply and Fast Delivering Photosensitizers: Towards Improved Photodynamic Therapy.

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