Formulation and characterization of nanoliposomal 5-fluorouracil for cancer nanotherapy

ElMeshad, Aliaa Nabil; Mortazavi, Seyyed M; Mozafari, M. R.

doi:10.3109/08982104.2013.810644

Cited by 45 publications

(19 citation statements)

References 48 publications

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“…Over the course of 3 months, the mean particle size of formulations did not change significantly ( P > 0.05). This matter could be resulted by the presence of transcutol in the formulation that may cause flexibility in vesicles [ 30 ] and cholesterol that has stabilizing effect against aggregation and fusion of the liposomes [ 37 ]. Similar results obtained by Mura et al [ 38 ] that found particle size of PEVs with different amounts of transcutol remained constant during 3 months at 4 °C.…”

Section: Resultsmentioning

confidence: 99%

Statistical optimization of tretinoin-loaded penetration-enhancer vesicles (PEV) for topical delivery

et al. 2016

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Background: The aim of this study was to develop and optimize deformable liposome for topical delivery of tretinoin. Methods: Liposomal formulations were designed based on the full factorial design and prepared by fusion method. The influence of different ratio of soy phosphatidylcholine and transcutol (independent variables) on incorporation efficiency and drug release in 15 min and 24 h (responses) from liposomal formulations was evaluated. Liposomes were characterized for their vesicle size and Differential Scanning Calorimetry (DSC) was used to investigate changes in their thermal behavior. The penetration and retention of drug was determined using mouse skin. Also skin histology study was performed. Results: Particle size of all formulations was smaller than 20 nm. Incorporation efficiency of liposomes was 79-93 %. Formulation F7 (25:5) showed maximum drug release. Optimum formulations were selected based on the contour plots resulted by statistical equations of drug release in 15 min and 24 h. Solubility properties of transcutol led to higher skin penetration for optimum formulations compared to tretinoin cream. There was no significant difference between the amount of drug retained in the skin by applying optimum formulations and cream. Histopatological investigation suggested optimum formulations could decrease the adverse effect of tretinoin in liposome compared to conventional cream. Conclusion: According to the results of the study, it is concluded that deformable liposome containing transcutol may be successfully used for dermal delivery of tretinoin.

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Section: Resultsmentioning

confidence: 99%

Statistical optimization of tretinoin-loaded penetration-enhancer vesicles (PEV) for topical delivery

et al. 2016

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“…Kaiser et al [41] argued that this effect depends on the lipid composition, the packing of the acyl chains, and particularly applies to water-soluble compounds in small liposomes, due to the small ratio between the inner and external volume. Also, Elmeshad et al [42], observed that there was a directly proportional relationship between the size of the vesicle, the subsequent aqueous space, and the amount of 5FU encapsulated. Fig.…”

Section: Physicochemical Characterization Of Udl-5fumentioning

confidence: 98%

Nano-formulation for topical treatment of precancerous lesions: skin penetration, in vitro, and in vivo toxicological evaluation

Calienni

Temprana

Prieto

et al. 2017

Drug Deliv. and Transl. Res.

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With the aim of improving the topical delivery of the antineoplastic drug 5-fluorouracil (5FU), it was loaded into ultradeformable liposomes composed of soy phosphatidylcholine and sodium cholate (UDL-5FU). The liposome populations had a mean size of 70 nm without significant changes in 56 days, and the ultradeformable formulations were up to 324-fold more elastic than conventional liposomes. The interaction between 5FU and the liposomal membrane was studied by three methods, and also release profile was obtained. UDL-5FU did penetrate the stratum corneum of human skin. At in vitro experiments, the formulation was more toxic on a human melanoma-derived than on a human keratinocyte-derived cell line. Cells captured liposomes by metabolically active processes. In vivo toxicity experiments were carried out in zebrafish (Danio rerio) larvae by studying the swimming activity, morphological changes, and alterations in the heart rate after incubation. UDL-5FU was more toxic than free 5FU. Therefore, this nano-formulation could be useful for topical application in deep skin precancerous lesions with advantages over current treatments. This is the first work that assessed the induction of apoptosis, skin penetration in a Saarbrücken penetration model, and the toxicological effects in vivo of an ultradeformable 5FU-loaded formulation.

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“…However, there appeared to be no association between the mean particle sizes of AR liposomes and the AR to lipid ratios for each method of preparation. These results could be attributed to the water-solubility of AR, which would lead to it being predominantly entrapped in the aqueous compartment rather than in the lipid bilayer of liposomes (12).…”

Section: Resultsmentioning

confidence: 99%

Anti-inflammatory activity of liposomes of Asparagus racemosus root extracts prepared by various methods

Plangsombat

Rungsardthong

Kongkaneramit

et al. 2016

Experimental and Therapeutic Medicine

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Abstract. Asparagus racemosus root extracts (AR) have been reported to possess a variety of pharmacological properties. The aim of the present study was to develop liposomes of AR and to assess their physicochemical characteristics and anti-inflammatory activity in the monocytic leukemia cell line THP-1. Liposomes containing various ratios of AR to lipid and a phosphatidylcholine to cholesterol molar ratio of 7:3 were prepared by thin-film hydration (TF), reverse-phase evaporation (REV) and polyol dilution (PD). The results showed that AR liposomes prepared by TF had a multilamellar structure and a large size, whereas those prepared by REV and PD were oligolamellar in structure, and of a smaller size. The particle sizes and zeta potentials of the liposomes ranged from 196.5 to 456.6 nm and from -4.34 to -18.94 mV, respectively. The AR to lipid ratio was shown to have no significant influence on particle size, while the zeta potential generally increased with increasing AR to lipid ratio. The highest entrapment efficiency values were detected in liposomes with an AR to lipid ratio of 1:5, and for liposomes prepared by TF, REV and PD methods, the entrapment efficiencies were 55.71±2.04, 56.21±3.59 and 67.68±1.37%, respectively. AR was found to exert no toxicity on THP-1 cells. The maximum anti-inflammatory activities of AR and AR liposomes, evaluated in terms of the percentage inhibition of tumor necrosis factor-α in THP-1 cells, were ~52% at a concentration of 1 µg/ml. It can be concluded from the present study that AR liposomes have the potential to be used a formulation for topical and/or transdermal drug delivery to provide anti-inflammatory activity.

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Formulation and characterization of nanoliposomal 5-fluorouracil for cancer nanotherapy

Cited by 45 publications

References 48 publications

Statistical optimization of tretinoin-loaded penetration-enhancer vesicles (PEV) for topical delivery

Statistical optimization of tretinoin-loaded penetration-enhancer vesicles (PEV) for topical delivery

Nano-formulation for topical treatment of precancerous lesions: skin penetration, in vitro, and in vivo toxicological evaluation

Anti-inflammatory activity of liposomes of Asparagus racemosus root extracts prepared by various methods

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