PMID: 26328448Sep 4, 2015Paper

Liposomal Entrapment of 4-Nerolidylcatechol: Impact on Phospholipid Dynamics, Drug Stability and Bioactivity

Journal of Nanoscience and Nanotechnology
Marilisa P N GaetilEliana M Lima

Abstract

Liposomes containing 4-nerolidylcatechol (4-NC), the major metabolite isolated from Pothomorphe umbellata, were obtained and characterized. Influence of liposomal encapsulation on chemical stability of 4-NC and on cytotoxicity profile of this drug was evaluated. Soybean phosphatidylcholine liposomes were prepared by lipid film hydration followed by extrusion. Entrapment efficiency for 4-NC was approximately 92%. Mean diameter of liposomes was 100 nm with a polydispersity index below 0.13. Liposomal 4-NC (L4-NC) and free drug (F4-NC) were submitted to forced degradation assays, monitored by HPLC. Photodegradation assay followed ICH Guidelines, using a photostability chamber equipped with both UV and white light sources. Liposomal encapsulation was able to markedly reduce 4-NC degradation rates under all the conditions tested. L4-NC showed a half-live approximately 15% higher than F4-NC under light exposure. After 72 hours, acid and base hydrolysis of F4-NC lead to 13 and 16% of degradation, respectively. However, no degradation was observed in L4-NC. EPR spectra of liposomal membrane showed that greatest changes in membrane properties were obtained when 5-doxyl stearic acid was used as the spin label, indicating a marked decreas...Continue Reading

Citations

Jan 18, 2015·Toxicology in Vitro : an International Journal Published in Association with BIBRA·Lívia Palmerston MendesMarize Campos Valadares
May 26, 2016·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Iqbal AhmadArif Sabah
Oct 27, 2017·Drug Delivery·Giuseppina IoeleGaetano Ragno
Dec 17, 2020·Antibiotics·Vanessa Raquel GreattiRosemeire Cristina Linhari Rodrigues Pietro
Apr 21, 2018·Life Sciences·Bruna Dos Santos RodriguesMarize Campos Valadares

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