4-amino-2-phenyl-6-(p-fluorophenyl)-5-carbonitrile-pyrimidine-bis-substituted-loaded liposomes as promising system for cancer treatment
| Autor: | JANICE V. OLIVEIRA, GLEYBSON C. ALMEIDA, MARIANE C.B.L. NOGUEIRA, FRANCISCO C.A. AGUIAR JÚNIOR, AUDENES O. MELO, THIAGO D.S. SILVA, NOEMIA P.S. SANTOS, NEREIDE S.S. MAGALHÃES, SEBASTIÃO J. MELO, EMERSON P.S. FALCÃO |
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| Jazyk: | angličtina |
| Rok vydání: | 2023 |
| Předmět: | |
| Zdroj: | Anais da Academia Brasileira de Ciências, Vol 95, Iss suppl 1 (2023) |
| Druh dokumentu: | article |
| ISSN: | 1678-2690 0001-3765 |
| DOI: | 10.1590/0001-3765202320211078 |
| Popis: | Abstract The aim of the present study was to perform in vitro and in vivo assessments of the antineoplastic action of 4-amino-pyrimidine encapsulated in liposomes. Liposomes were prepared and characterized for particle size and drug encapsulation and submitted to long-term stability tests. Cytotoxicity assays were performed in HeLa cells. Antineoplastic activity was investigated using the experimental sarcoma 180 tumor in Swiss albino mice. Encapsulation efficiency was 82.93 ± 0.04% and no significant changes were found with respect to particle size or pH after centrifugation and mechanical agitation tests. The in vitro results at concentration of 20 μg/mL indicated a considerable reduction in cell viability after treatment with encapsulated pyrimidine (75.91%). The in vivo assays using the compounds in encapsulated and free forms and 5-fluorouracil achieved tumor inhibition rates of 66.47 ± 26.8%, 50.46 ± 16.24% and 14.47 ± 9.22%, respectively. Mitotic counts demonstrated a greater reduction in the number of mitoses in animals treated with liposomal pyrimidine (32.15%) compared to those treated with the pyrimidine free (87.69%) and 5-fluorouracil (71.39%). This study demonstrated that the development of liposome formulations containing 4-amino-pyrimidine is a promising alternative for overcoming limitations related to the toxicity of current cancer treatment, ensuring greater therapeutic efficacy. |
| Databáze: | Directory of Open Access Journals |
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