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AAPS PharmSciTech ; 20(5): 198, 2019 May 24.
Article in English | MEDLINE | ID: mdl-31127389

ABSTRACT

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.


Subject(s)
Antineoplastic Agents, Phytogenic/chemical synthesis , Apoptosis/drug effects , Cytotoxins/chemical synthesis , Nanospheres/chemistry , Paclitaxel/chemical synthesis , Plant Oils/chemical synthesis , Antineoplastic Agents, Phytogenic/pharmacokinetics , Apoptosis/physiology , Cell Survival/drug effects , Cell Survival/physiology , Cytotoxins/pharmacokinetics , Dose-Response Relationship, Drug , Drug Liberation , HeLa Cells , Humans , Mentha piperita , Paclitaxel/pharmacokinetics , Plant Oils/pharmacokinetics , Polyethylene Glycols/chemical synthesis , Polyethylene Glycols/pharmacokinetics , Surface-Active Agents/chemical synthesis , Surface-Active Agents/pharmacokinetics , Vitamin E/chemical synthesis , Vitamin E/pharmacokinetics
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