期刊
PHOTODIAGNOSIS AND PHOTODYNAMIC THERAPY
卷 19, 期 -, 页码 284-297出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.pdpdt.2017.06.016
关键词
Biodegradable polymers; Hypericin; Photodynamic therapy; Biological evaluation; Natural products; Physicochemical properties
类别
资金
- Brazilian funding agency CAPES (Coordenacao de Apeifeicoamento de Pessoal de Nivel Superior)
- Brazilian funding agency CNPq (Conselho Nacional de Desenvolvimento Cientifico e Tecnologico)
- SETI/UGF-Parana
- FINEP (Financiadora de Estudos e Projetos)
- State University of Maringa
Hypericin (Hyp) is a natural photoactive pigment utilized in the treatment of different types of cancer and antimicrobial inactivation using photodynamic therapy (PDT). Hyp is poorly soluble in water leading to problems of administration, getting close contact with the site, and bio-availability. Therefore, this study aimed to develop bioadhesive thermoresponsive system containing Hyp for local PDT. Carbomer 934P, poloxamer 407, and Hyp were used to prepare the thermoresponsive bioadhesive formulations. They were characterized for sol-gel transition temperature, mechanical, mucoadhesive, rheological (continuous flow and oscillatory) and dielectric properties, syringeability, in vitro Hyp release kinetics, ex vivo permeability, and photodynamic activity. The formulations displayed suitable gelation temperature and rheological characteristics. The compressional, mechanical and mucoadhesive properties, as well the syringeability showed the easiness of administration and the permanence of the system adhered to the mucosa or skin. The dielectric analysis helped to understand the Hyp availability, and its release presented an anomalous behavior. The system did not permeate the pig skin nor rat intestine and showed good biological photodynamic activity. Therefore, data obtained from the bioadhesive system indicate a potentially useful role as a platform for local hypericin delivery in PDT, suggesting it is worthy of in vivo evaluation.
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