Development of copolymeric nanoparticles of hypocrellin B: Enhanced phototoxic effect and ocular distribution
| Autor: | Ragupathy Madiyalakan, Subramanian Natesan, Muthuselvam Paulsamy, Venkateshwaran Krishnaswami, Senthilkumar Sankareswaran, Chandrasekar Ponnusamy, Rajaguru Palanichamy, Ruckmani Kandasamy |
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| Rok vydání: | 2018 |
| Předmět: |
Male
0301 basic medicine Silver Light Bulk polymerization Cell Survival Surface Properties Stereochemistry Pharmaceutical Science Nanoparticle 02 engineering and technology Eye Macular Degeneration 03 medical and health sciences chemistry.chemical_compound Polylactic Acid-Polyglycolic Acid Copolymer Copolymer Zeta potential Animals Humans Tissue Distribution Photosensitizer Particle Size Perylene Drug Carriers Photosensitizing Agents Singlet Oxygen Chemistry Aqueous humour Singlet oxygen Quinones Silver Nano 021001 nanoscience & nanotechnology Drug Liberation 030104 developmental biology A549 Cells Nanoparticles Rabbits 0210 nano-technology Nuclear chemistry |
| Zdroj: | European Journal of Pharmaceutical Sciences. 116:26-36 |
| ISSN: | 0928-0987 |
| Popis: | In the present work, we have developed a photosensitizer hypocrellin B (HB) and nano silver loaded PLGA-TPGS nanoparticles with improved singlet oxygen production for enhanced photodynamic effect for the efficient treatment of age related macular degeneration. Random copolymer (PLGA-TPGS) synthesized by ring opening and bulk polymerization was characterized by IR, 1H NMR and TGA analysis. HBS-CP-NPs prepared by nanoprecipitation techniques were spherical shaped 89.6–753.6 nm size particles with negative zeta potential. The average encapsulation efficiency was 84.06 ± 11.43% and HB release from the HBS-CP-NPs was found to be biphasic with a slow release of 1.41% in the first 8 h and 48.91% during 3 days as measured by RP-HPLC. DSC thermograms indicate that HB was dispersed as amorphous form in HBS-CP-NPs. The ROS generation level of HBS-CP-NPs was significantly higher than that of HB/HB-CP-NPs. The production of 1O2 of HBS-CP-NPs has been assessed using EPR spectrometer. The 1O2 generating efficiency follows the order of nano silver > HB-CP-NPs > HBS-CP-NPs > pure HB drug solution. The superior phototoxic effect of HBS-CP-NPs (85.5% at 50 μM) was attained at 2 h irradiation in A549 cells. Significant anti angiogenic effect of HBS-CP-NPs was observed in treated CAM embryos. Following intravenous injection of HBS-CP-NPs to rabbits, the maximum amount of HB was found in retina (3 h), iris (9 h), aqueous humour (9 h) and vitreous humour (9 h). |
| Databáze: | OpenAIRE |
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