Physico-chemical characteristics of methotrexate-entrapped oleic acid-containing deformable liposomes for in vitro transepidermal delivery targeting psoriasis treatment

Srisuk, Pathomthat; Thongnopnua, Phensri; Raktanonchai, Uracha; Kanokpanont, Sorada

doi:10.1016/j.ijpharm.2012.01.045

Cited by 124 publications

(56 citation statements)

References 39 publications

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“…The highest entrapment efficiencies of PMX were obtained for PMX at a dose of 5 mg/mL. These results are in agreement with those of Srisuk et al 39) who found that, while the percentage loading of methotrexate increased with increasing methotrexate dose, the entrapment efficiency decreased with increasing methotrexate dose.…”

Section: Effect Of Phospholipid Type and The Presence Of Cholesterol supporting

confidence: 91%

Liposomal Pemetrexed: Formulation, Characterization and <i>in Vitro</i> Cytotoxicity Studies for Effective Management of Malignant Pleural Mesothelioma

Eldin

El-Nahas

Mahdy

et al. 2015

Biological & Pharmaceutical Bulletin

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Pemetrexed (PMX) is a newly developed multi-targeted anti-folate with promising clinical activity in many solid tumors including malignant pleural mesothelioma (MPM). However, PMX does not show sufficient anti-tumor activity in vivo when used alone either due to inefficient delivery of adequate concentrations to tumor tissue or dose-limiting side effects. In order to overcome these problems and to achieve potent anti-tumor activity, PMX was encapsulated into a liposomal delivery system. In the present study, various formulations of liposomal PMX were prepared. The effect of formulation parameters on the encapsulation efficiency of PMX within liposomes was evaluated. In addition, the influence of drug release rate on the in vitro cytotoxicity was investigated. Encapsulation of PMX within liposomes was remarkably increased by the incorporation of cholesterol within liposomal membranes and by increasing the total lipid concentration. Encapsulation efficiency was found to be unaffected by the type of phospholipid used or the inclusion of a cation lipid, DC-6-14. Interestingly, encapsulation of PMX within "fluid" liposomes was found to allow efficient release of PMX from liposomes resulting in a potent in vitro cytotoxicity against MPM MSTO-211H cell line. On the other hand, entrapment of PMX within "solid" liposomes substantially hindered PMX release from liposomes, and thus PMX failed to exert any in vitro cytotoxicity. These results suggest that encapsulation of PMX within "fluid" liposomes might represent a novel strategy to enhance the therapeutic efficacy of PMX while minimizing the side effect encountered by the non selective delivery of free PMX to various body tissues.Key words liposome; malignant pleural mesothelioma; polyethylene glycol; pemetrexed Pemetrexed (PMX) is a new-generation anti-folate, approved for the treatment of malignant pleural mesothelioma (MPM) and non-small cell lung cancer, currently being evaluated for the treatment of a variety of other solid tumors.

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Section: Effect Of Phospholipid Type and The Presence Of Cholesterol supporting

confidence: 91%

Liposomal Pemetrexed: Formulation, Characterization and <i>in Vitro</i> Cytotoxicity Studies for Effective Management of Malignant Pleural Mesothelioma

Eldin

El-Nahas

Mahdy

et al. 2015

Biological & Pharmaceutical Bulletin

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“…10,11 Most of these carriers have insufficient drugloading capacity. Recently, peptide-targeted PEGylated liposomes encapsulating MTX caused a significant improvement in clinical scores in the experimental autoimmune encephalomyelitis in mice.…”

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confidence: 99%

Liposomal formulation of a methotrexate lipophilic prodrug: assessment in tumor cells and mouse T-cell leukemic lymphoma

Алексеева¹,

Моисеева²,

Onishchenko³

et al. 2017

IJN

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In a previous study, a formulation of methotrexate (MTX) incorporated in the lipid bilayer of 100-nm liposomes in the form of diglyceride ester (MTX-DG, lipophilic prodrug) was developed. In this study, first, the interactions of MTX-DG liposomes with various human and mouse tumor cell lines were studied using fluorescence techniques. The liposomes composed of egg phosphatidylcholine (PC)/yeast phosphatidylinositol/MTX-DG, 8:1:1 by mol, were labeled with fluorescent analogs of PC and MTX-DG. Carcinoma cells accumulated 5 times more MTX-DG liposomes than the empty liposomes. Studies on inhibitors of liposome uptake and processing by cells demonstrated that the formulation used multiple mechanisms to deliver the prodrug inside the cell. According to the data from the present study, undamaged liposomes fuse with the cell membrane only 1.5–2 hours after binding to the cell surface, and then, the components of liposomal bilayer enter the cell separately. The study on the time course of plasma concentration in mice showed that the area under the curve of MTX generated upon intravenous injection of MTX-DG liposomes exceeded that of intact MTX 2.5-fold. These data suggested the advantage of using liposomal formulation to treat systemic manifestation of hematological malignancies. Indeed, the administration of MTX-DG liposomes to recipient mice bearing T-cell leukemic lymphoma using a dose-sparing regimen resulted in lower toxicity and retarded lymphoma growth rate as compared with MTX.

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“…Methotrexate has been widely used as a chemotherapy agent for cancer and arthritis. As shown in Figure 6, MTX-PLLA-PEG-PLLA prepared by the microencapsulation process can provide desirable sustained in vitro release of methotrexate, which can be used in the treatment of ectopic pregnancy 32 and leukemia 33 by intravenous injection, in breast cancer 34 by pulmonary delivery, and in psoriasis 35 and rheumatoid arthritis 36 by percutaneous administration.…”

Section: Drug Release Profilesmentioning

confidence: 99%

Formation of methotrexate-PLLA-PEG-PLLA composite microspheres by microencapsulation through a process of suspension-enhanced dispersion by supercritical CO2

Chen¹,

Wang²,

Wang³

et al. 2012

IJN

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Background:The aim of this study was to improve the drug loading, encapsulation efficiency, and sustained-release properties of supercritical CO 2 -based drug-loaded polymer carriers via a process of suspension-enhanced dispersion by supercritical CO 2 (SpEDS), which is an advanced version of solution-enhanced dispersion by supercritical CO 2 (SEDS). Methods: Methotrexate nanoparticles were successfully microencapsulated into poly (L-lactide)-poly(ethylene glycol)-poly(L-lactide) (PLLA-PEG-PLLA) by SpEDS. Methotrexate nanoparticles were first prepared by SEDS, then suspended in PLLA-PEG-PLLA solution, and finally microencapsulated into PLLA-PEG-PLLA via SpEDS, where an "injector" was utilized in the suspension delivery system. Results: After microencapsulation, the composite methotrexate (MTX)-PLLA-PEG-PLLA microspheres obtained had a mean particle size of 545 nm, drug loading of 13.7%, and an encapsulation efficiency of 39.2%. After an initial burst release, with around 65% of the total methotrexate being released in the first 3 hours, the MTX-PLLA-PEG-PLLA microspheres released methotrexate in a sustained manner, with 85% of the total methotrexate dose released within 23 hours and nearly 100% within 144 hours. Conclusion: Compared with a parallel study of the coprecipitation process, microencapsulation using SpEDS offered greater potential to manufacture drug-loaded polymer microspheres for a drug delivery system.

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Physico-chemical characteristics of methotrexate-entrapped oleic acid-containing deformable liposomes for in vitro transepidermal delivery targeting psoriasis treatment

Cited by 124 publications

References 39 publications

Liposomal Pemetrexed: Formulation, Characterization and <i>in Vitro</i> Cytotoxicity Studies for Effective Management of Malignant Pleural Mesothelioma

Liposomal Pemetrexed: Formulation, Characterization and <i>in Vitro</i> Cytotoxicity Studies for Effective Management of Malignant Pleural Mesothelioma

Liposomal formulation of a methotrexate lipophilic prodrug: assessment in tumor cells and mouse T-cell leukemic lymphoma

Formation of methotrexate-PLLA-PEG-PLLA composite microspheres by microencapsulation through a process of suspension-enhanced dispersion by supercritical CO2

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