Development and evaluation of multiparticulate biphasic system for the treatment of circadian diseases

Martins, Sarah Moherdaui; Muller, Vinícius; Galan, Vanderson; Souza, Fabio Pinheiro de; Andreazza, Itamar Francisco; Rosa, Mauricio Ferreira da

doi:10.1590/s2175-97902018000417167

Cited by 1 publication

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References 23 publications

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“…This finding was in accordance with two studies also having hydrophobic agents displaying a similar biphasic release pattern upon in vitro release study ( Nguyen et al, 2011 ; Madheswaran et al, 2014 ). This biphasic drug delivery system is ideal in pharmaceutical applications in which the drug can be released at two fractions, one is at initial release (fast) and another modified constant release (slow) to achieve the treatment efficacy ( Jha et al, 2011 ; Martins et al, 2018 ). With the Re(I) complex bearing the ideal biphasic release pattern, no extra excipient is needed to modify the drug release pattern in future studies.…”

Section: Discussionmentioning

confidence: 99%

Novel Gemcitabine-Re(I) Bisquinolinyl Complex Combinations and Formulations With Liquid Crystalline Nanoparticles for Pancreatic Cancer Photodynamic Therapy

et al. 2022

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With less than 10% of 5-year survival rate, pancreatic ductal adenocarcinoma (PDAC) is known to be one of the most lethal types of cancer. Current literature supports that gemcitabine is the first-line treatment of PDAC. However, poor cellular penetration of gemcitabine along with the acquired and intrinsic chemoresistance of tumor against it often reduced its efficacy and hence necessitates the administration of high gemcitabine dose during chemotherapy. Photodynamic therapy (PDT), a more selective and minimally invasive treatment, may be used synergistically with gemcitabine to reduce the doses utilized and dose-related side effects. This study reports the synergistic use of Re(I) bisquinolinyl complex, a transition metal complex photosensitizer with gemcitabine against PDAC. Re(I) bisquinolinyl complex was found to act synergistically with gemcitabine against PDAC in vitro at various ratios. With the aim to enhance cellular uptake and therapeutic efficiency, the Re(I) bisquinolinyl complex and gemcitabine were encapsulated into liquid crystalline nanoparticles (LCNPs) system. The formulations were found to produce homogeneous drug-loaded LCNPs (average size: 159–173 nm, zeta potential +1.06 to −10 mV). Around 70% of gemcitabine and 90% of the Re(I) bisquinolinyl complex were found to be entrapped efficiently in the formulated LCNPs. The release rate of gemcitabine or/and the Re(I) bisquinolinyl complex loaded into LCNPs was evaluated in vitro, and the hydrophilic gemcitabine was released at a faster rate than the lipophilic Re(I) complex. LCNPs loaded with gemcitabine and Re(I) bisquinolinyl complex in a 1:1 ratio illustrated the best anti-cancer activity among the LCNP formulations (IC50 of BxPC3: 0.15 μM; IC50 of SW 1990: 0.76 μM) through apoptosis. The current findings suggest the potential use of transition metal-based photosensitizer as an adjunctive agent for gemcitabine-based chemotherapy against PDAC and the importance of nano-formulation in such application.

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Section: Discussionmentioning

confidence: 99%