STUDY OF STABILITY OF LIPOSOMES LOADED WITH TETRAKIS(4-BENZYLOXYPHENYL)TETRACYANOPORPHYRAZINE
Abstract and keywords
Abstract (English):
Photosensitizers from the group of tetra(aryl)tetracyanoporphyrazines are the promising dyes for photodynamic therapy of tumors with unique properties. However, in vivo application of such photosensitizers (PS) requires the use of special drug carriers that ensure effective delivery and selective accumulation in the tumor site. The present study is focused on obtaining liposomes with different lipid composition loaded with tetrakis(4-benzyloxyphenyl)tetracyanoporphyrazine (Pz) and examining their stability. An efficient loading of the dye (with loading efficiency up to 33 %) was proved for the neutral and negatively charged liposomes composed of phosphatidylcholine with cholesterol and phosphatidylglycerol. It was found that porphyrazine do not affect the size of these vesicles. Surface modification of the liposomes by adding polyethylene glycol (in the composition of phosphatidylethanolamine-N-[carboxy (polyethylene glycol)-2000]) increases the loading efficiency of the photosensitizer by 2,2-2,5 times (up to 80 %). At the same time, the size of liposomes coated with polyethylene glycol is doubled after Pz loading compared to vesicles without Pz. This result indicates that Pz causes the aggregation of such liposomes. The high loading efficiency of Pz into liposomes gives the prerequisites for the further development of the liposomal form of photosensitizers of this class by means of optimization of the method of surface coating.

Keywords:
porphyrazine, liposomes, photodynamic therapy, photosensitizer
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