RESUMEN
In this work, a drug delivery system for perillyl alcohol based on the peptide self-assembly containing 3-(2-benzothiazolyl)-7-(diethylamino)coumarin (C6) as a fluorescent additive is obtained, and its photophysical characteristics as well as its release dynamics were studied by steady-state and time-resolved fluorescence spectroscopy. Results proved the dynamics of drug release from the peptide nanostructures and showed that the system formed by the self-assembled peptide and C6, along with perillyl alcohol, presents unique photophysical properties that can be exploited to generate singlet oxygen (1O2) upon irradiation, which is not achieved by the sole components. Through epifluorescence microscopy combined with time-correlated single photon counting fluorescence spectroscopy, the release mechanism was proven to occur upon peptide structure interconversion, which is controlled by environmental changes.
RESUMEN
Herein, we describe the production of poly(hydroxybutyrate-co-hydroxyvalerate) [P(HB-HV)]-based microspheres containing coumarin-6 (C6) or pyrene (Py) fluorophores as additives and models for hydrophobic and hydrophilic drug encapsulation. Their photophysical and morphological properties, as well as encapsulation efficiencies, are studied as this work aims to describe the influence of additive hydrophobicity/hydrophilicity on microparticle formation. These properties were studied by scanning electron microscopy, fluorescence confocal laser scanning microscopy (FCLSM), and steady-state fluorescence spectroscopy. The results show that the surfactant concentration, polymer molar mass, emulsification stirring rate, and the presence of the fluorophore and its nature are determinants of the P(HB-HV) microsphere properties. Also, encapsulation efficiency is shown to be governed by synergic effects of these parameters on the formation of microspheres. Moreover, size distribution is proved to be strongly influenced by the surfactant poly(vinyl alcohol) content. FCLSM showed that the fluorophores were efficiently encapsulated in P(HB-HV) microspheres at distinct distributions within the copolymer matrix. Surprisingly, nanospheres were observed in the microsphere surface, suggesting that microspheres are formed from nanosphere coalescence.
RESUMEN
The new heterocyclic derivative LQFM048 (3) (2,4,6-tris ((E)-ethyl 2-cyano-3-(4-hydroxy-3-methoxyphenyl)acrylate)-1,3,5-triazine) was originally designed through the molecular hybridization strategy from Uvinul® T 150 (1) and (E)-ethyl 2-cyano-3-(4hydroxy-3-methoxyphenyl)acrylate (2) sunscreens, using green chemistry approach. This compound was obtained in global yields (80%) and showed an interesting redox potential. In addition, it is thermally stable up to temperatures around 250°C. It was observed that LQFM048 (3) showed a low degradation after 150min of sunlight exposure at 39°C, whereas the extreme radiation conditions induced a considerable photodegradation of the LQFM048 (3), especially when irradiated by VIS and VIS+UVA. During the determination of sun protection factor, LQFM048 (3) showed interesting results, specially as in association with other photoprotective compounds and commercial sunscreen. Additionally, the compound (3) did not promote cytotoxicity for 3T3 fibroblasts. Moreover, it was not able to trigger acute oral systemic toxicity in mice, being classified as a compound with low acute toxicity hazard (2.000mg/kg>LD50<5.000mg/kg). Therefore, this compound synthesized using green chemistry approach is promising showing potential to development of a new sunscreen product with advantage of presenting redox potential, indicating antioxidant properties.