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AAPS PharmSciTech ; 20(5): 198, 2019 May 24.
Artigo em Inglês | MEDLINE | ID: mdl-31127389

RESUMO

In this work, several normal, oil-in-water (o/w) microemulsions (MEs) were prepared using peppermint essential oil, jojoba oil, trans-anethole, and vitamin E as oil phases to test their capacity to load paclitaxel (PTX). Initially, pseudo-ternary partial phase diagrams were constructed in order to find the normal microemulsion region using d-α-tocopherol polyethylene glycol 1000 succinate (TPGS-1000) as surfactant and isobutanol (iso-BuOH) as co-surfactant. Selected ME formulations were loaded with PTX reaching concentrations of 0.6 mg mL-1 for the peppermint oil and trans-anethole MEs, while for the vitamin E and jojoba oil MEs, the maximum concentration was 0.3 mg mL-1. The PTX-loaded MEs were stable according to the results of heating-cooling cycles and mechanical force (centrifugation) test. Particularly, drug release profile for the PTX-loaded peppermint oil ME (MEPP) showed that ∼ 90% of drug was released in the first 48 h. Also, MEPP formulation showed 70% and 90% viability reduction on human cervical cancer (HeLa) cells after 24 and 48 h of exposure, respectively. In addition, HeLa cell apoptosis was confirmed by measuring caspase activity and DNA fragmentation. Results showed that the MEPP sample presented a major pro-apoptotic capability by comparing with the unloaded PTX ME sample.


Assuntos
Antineoplásicos Fitogênicos/síntese química , Apoptose/efeitos dos fármacos , Citotoxinas/síntese química , Nanosferas/química , Paclitaxel/síntese química , Óleos de Plantas/síntese química , Antineoplásicos Fitogênicos/farmacocinética , Apoptose/fisiologia , Sobrevivência Celular/efeitos dos fármacos , Sobrevivência Celular/fisiologia , Citotoxinas/farmacocinética , Relação Dose-Resposta a Droga , Liberação Controlada de Fármacos , Células HeLa , Humanos , Mentha piperita , Paclitaxel/farmacocinética , Óleos de Plantas/farmacocinética , Polietilenoglicóis/síntese química , Polietilenoglicóis/farmacocinética , Tensoativos/síntese química , Tensoativos/farmacocinética , Vitamina E/síntese química , Vitamina E/farmacocinética
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