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Molecules 2016, 21(10), 1347; doi:10.3390/molecules21101347

Evaluation of Hydrogel Suppositories for Delivery of 5-Aminolevulinic Acid and Hematoporphyrin Monomethyl Ether to Rectal Tumors

1
Cardiovascular Medicine, Tianjin First Center Hospital, Tianjin 300192, China
2
Laser Medicine Laboratory, Institute of Biomedical Engineering, Chinese Academy of Medical Sciences & Peking Union Medical College, Tianjin 300192, China
*
Author to whom correspondence should be addressed.
Academic Editor: Norbert Lange
Received: 25 August 2016 / Revised: 6 October 2016 / Accepted: 7 October 2016 / Published: 12 October 2016
(This article belongs to the Special Issue Photodynamic Therapy)
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Abstract

We evaluated the potential utility of hydrogels for delivery of the photosensitizing agents 5-aminolevulinic acid (ALA) and hematoporphyrin monomethyl ether (HMME) to rectal tumors. Hydrogel suppositories containing ALA or HMME were administered to the rectal cavity of BALB/c mice bearing subcutaneous tumors of SW837 rectal carcinoma cells. For comparison, ALA and HMME were also administered by three common photosensitizer delivery routes; local administration to the skin and intratumoral or intravenous injection. The concentration of ALA-induced protoporphyrin IX or HMME in the rectal wall, skin, and subcutaneous tumor was measured by fluorescence spectrophotometry, and their distribution in vertical sections of the tumor was measured using a fluorescence spectroscopy system. The concentration of ALA-induced protoporphyrin IX in the rectal wall after local administration of suppositories to the rectal cavity was 9.76-fold (1 h) and 5.8-fold (3 h) higher than in the skin after cutaneous administration. The maximal depth of ALA penetration in the tumor was ~3–6 mm at 2 h after cutaneous administration. Much lower levels of HMME were observed in the rectal wall after administration as a hydrogel suppository, and the maximal depth of tumor penetration was <2 mm after cutaneous administration. These data show that ALA more readily penetrates the mucosal barrier than the skin. Administration of ALA as an intrarectal hydrogel suppository is thus a potential delivery route for photodynamic therapy of rectal cancer. View Full-Text
Keywords: photosensitizer; drug delivery; photodynamic therapy; hematoporphyrin monomethyl ether; 5-aminolevulinic acid; rectal cancer photosensitizer; drug delivery; photodynamic therapy; hematoporphyrin monomethyl ether; 5-aminolevulinic acid; rectal cancer
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Ye, X.; Yin, H.; Lu, Y.; Zhang, H.; Wang, H. Evaluation of Hydrogel Suppositories for Delivery of 5-Aminolevulinic Acid and Hematoporphyrin Monomethyl Ether to Rectal Tumors. Molecules 2016, 21, 1347.

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