Hydrogels containing porphyrin-loaded nanoparticles for topical photodynamic applications.
5,10,15,20-tetrakis(1-methylpyridinium-4-yl)-porphyrin tetra-iodide (TMPyP), a potent water-soluble photosensitizer (PS) used in antimicrobial applications, was encapsulated into poly(lactic-co-glycolic acid) (PLGA) nanoparticles (TMPyP-PLGA) for topical delivery purposes. Nanoparticles resulted in a mean particle size around 130nm, narrow polydispersity index (PdI), spherical morphology and association efficiency up to 93%. Free TMPyP and TMPyP-PLGA nanoparticles were incorporated into Carbopol(®) hydrogels, resulting in controlled TMPyP release of about 60% and 20% after 4.5h, respectively. Critical properties such as appearance, clarity, viscosity and pH were maintained over time, as hydrogels were stable during 6 months at 4°C, 25°C/60% RH and 40°C/75% RH. For photodynamic applications, the photoproduction of singlet oxygen from these hydrogels was quite efficient being both formulations very photostable after 20min. No TMPyP permeation through pig ear skin was observed after 24h, and histological assays did not show relevant damages in surrounding tissues. All these excellent characteristics make them promising platforms for photodynamic applications through topical clinical use.
Inovapotek, Pharmaceutical Research & Development, Edifício Inovar e Crescer, Salas 23 e 39, Rua Alfredo Allen, 455/461, 4200-135 Porto, Portugal; QOPNA and Department of Chemistry, University of Aveiro, 3810-193 Aveiro, Portugal. Electronic address: jose.delgado@inovapotek.com.
José A
JA
González-Delgado
CBQF - Centro de Biotecnologia e Química Fina - Laboratório Associado, Escola Superior de Biotecnologia, Universidade Católica Portuguesa/Porto, Rua Arquiteto Lobão Vital Apartado 2511, 4202-401 Porto, Portugal; CESPU, Instituto de Investigação e Formação Avançada em Ciências e Tecnologias da Saúde, Instituto Universitário de Ciências da Saúde, Rua Central de Grandra, 1317, 4585-116 Gandra, Portugal.
Pedro M
PM
Castro
I3 S-Instituto de Investigação e Inovação em Saúde, University of Porto, Rua Alfredo Allen, 208, 4200-135 Porto, Portugal; INEB-Instituto de Engenharia Biomédica, University of Porto, Rua Alfredo Allen, 208, 4200-135 Porto, Portugal.
Alexandra
A
Machado
I3 S-Instituto de Investigação e Inovação em Saúde, University of Porto, Rua Alfredo Allen, 208, 4200-135 Porto, Portugal; INEB-Instituto de Engenharia Biomédica, University of Porto, Rua Alfredo Allen, 208, 4200-135 Porto, Portugal.
Francisca
F
Araújo
REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Porto, Portugal.
Francisca
F
Rodrigues
Inovapotek, Pharmaceutical Research & Development, Edifício Inovar e Crescer, Salas 23 e 39, Rua Alfredo Allen, 455/461, 4200-135 Porto, Portugal; QOPNA and Department of Chemistry, University of Aveiro, 3810-193 Aveiro, Portugal.
Bárbara
B
Korsak
Inovapotek, Pharmaceutical Research & Development, Edifício Inovar e Crescer, Salas 23 e 39, Rua Alfredo Allen, 455/461, 4200-135 Porto, Portugal.
Marta
M
Ferreira
QOPNA and Department of Chemistry, University of Aveiro, 3810-193 Aveiro, Portugal; Centro de Química Estrutural, Instituto Superior Técnico, Universidade de Lisboa, Av. Rovisco Pais, 1049-001 Lisboa, Portugal.
João P C
JP
Tomé
Inovapotek, Pharmaceutical Research & Development, Edifício Inovar e Crescer, Salas 23 e 39, Rua Alfredo Allen, 455/461, 4200-135 Porto, Portugal; CESPU, Instituto de Investigação e Formação Avançada em Ciências e Tecnologias da Saúde, Instituto Universitário de Ciências da Saúde, Rua Central de Grandra, 1317, 4585-116 Gandra, Portugal; I3 S-Instituto de Investigação e Inovação em Saúde, University of Porto, Rua Alfredo Allen, 208, 4200-135 Porto, Portugal; INEB-Instituto de Engenharia Biomédica, University of Porto, Rua Alfredo Allen, 208, 4200-135 Porto, Portugal. Electronic address: bruno.sarmento@ineb.up.pt.
Bruno
B
Sarmento
D000287:Administration, Topical; D000818:Animals; D020100:Hydrogels / Q000008:administration & dosage* / Q000737:chemistry; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D017319:Photosensitizing Agents / Q000008:administration & dosage* / Q000737:chemistry; D011166:Porphyrins / Q000008:administration & dosage* / Q000737:chemistry; D013552:Swine
D020100:Hydrogels; D017319:Photosensitizing Agents; D011166:Porphyrins
Hydrogels; Photodynamic therapy; Photosensitizers; Polymeric nanoparticles; Porphyrins