Thermotropic Phase Behavior of Liposome Entrapped 5-FU and LCV

Pentak, Danuta; Sułkowska, Anna; Czopek, Izabela; Bojko, Barbara; Równicka-Zubik, J.; Sułkowski, Wieslaw W.

doi:10.1080/15421401003716189

Cited by 6 publications

(5 citation statements)

References 13 publications

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“…The most significant competition in encapsulation to liposome has been previously observed for hydrophilichydrophobic (LCV-5-FU) drugs encapsulated together [14]. In that case, the difference in encapsulation amounted to 10.17%, i.e.…”

Section: Resultsmentioning

confidence: 84%

“…The fraction of drug encapsulated liposomes depends on the physico-chemical properties of the drugs used in multidrug therapy [14].…”

Section: Resultsmentioning

confidence: 99%

“…The study performed with 5-FU and Ara-C allowed us to make a comparative analysis with the data obtained previously for 5-FU and 5-formyl-5,6,7,8-tetrahydropteroyl-Lglutamic acid calcium salt (leucovorin; LCV) [14].…”

Section: Resultsmentioning

confidence: 99%

“…packing) and their mobility. The above parameters decide about the increase or decrease of temperature T c of phospholipids phase transition [14]. Influence of some physical properties of 5-fluorouracil 69 UV study…”

Section: Resultsmentioning

confidence: 99%

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Influence of some physical properties of 5-fluorouracil on encapsulation efficiency in liposomes

Pentak

Sułkowski

Sułkowska

2011

J Therm Anal Calorim

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The aim of this study is to encapsulate two drugs: 5-fluorouracil (5-FU) with the hydrophobic properties and 1-b-D-arabinofuranosylcytosine (Ara-C) with the amphiphilic properties into liposomes prepared by the modified reverse-phase evaporation method (mREV) from L-a-phosphatidylcholine dipalmitoyl (DPPC). We studied the thermotropic phase behavior of liposome entrapped 5-FU and Ara-C. It is known that the stability of liposomes depends not only on the method of chemical gradient loading, the use of membrane stabilizer such as sterols, but also on the phase transition temperature (T c ) of phospholipids, which undergoes an alteration after encapsulation of drugs to liposomes. The competition of these two drugs entrapped in liposomes was analyzed by the use of two spectroscopies: 1 H NMR and UV on the basis of the analysis of the signals of each drug in the liposome-drug system. The percent of encapsulation in DPPC/Ara-C/5-FU liposome obtained by the use of UV spectroscopy amounted 93.84 and 96.05% for 5-FU and Ara-C, respectively. Phase transition temperature T c of liposomes containing Ara-C did not significantly change while for the liposomes containing 5-FU it increased in comparison with T c of the reference liposomes formed from DPPC.

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Section: Resultsmentioning

confidence: 84%

“…The fraction of drug encapsulated liposomes depends on the physico-chemical properties of the drugs used in multidrug therapy [14].…”

Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

See 2 more Smart Citations

Influence of some physical properties of 5-fluorouracil on encapsulation efficiency in liposomes

Pentak

Sułkowski

Sułkowska

2011

J Therm Anal Calorim

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“…The gadoteridol concentration and the pH of the buffer strongly affected all calorimetric responses, which suggests that the pH of the formulation and lipid interaction with the contrast agent influence the thermotropic phase behavior of the lipid bilayer. It is recognized that encapsulation of drugs can have a drastic effect on the lateral organization and the order of lipid bilayers and consequently on the thermotropic phase behavior of liposomes. − Interaction between the lipid headgroups and gadoteridol may affect the fluidity and permeability of the bilayers and the packing of the membranes, eventually reducing the Δ H and influencing the T m and Δ T 1/2 . This interaction is more pronounced at higher contrast agent concentration, which is evident from the quadratic effect observed in the T m response model.…”

Section: Discussionmentioning

confidence: 99%

Design of Gadoteridol-Loaded Cationic Liposomal Adjuvant CAF01 for MRI of Lung Deposition of Intrapulmonary Administered Particles

et al. 2019

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Designing effective and safe tuberculosis (TB) subunit vaccines for inhalation requires identification of appropriate antigens and adjuvants and definition of the specific areas to target in the lungs. Magnetic resonance imaging (MRI) enables high spatial resolution, but real-time anatomical and functional MRI of lungs is challenging. Here, we describe the design of a novel gadoteridol-loaded cationic adjuvant formulation 01 (CAF01) for MRI-guided vaccine delivery of the clinically tested TB subunit vaccine candidate H56/CAF01. Gadoteridol-loaded CAF01 liposomes were engineered by using a quality-by-design approach to (i) increase the mechanistic understanding of formulation factors governing the loading of gadoteridol and (ii) maximize the loading of gadoteridol in CAF01, which was confirmed by cryotransmission electron microscopy. The encapsulation efficiency and loading of gadoteridol were highly dependent on the buffer pH due to strong attractive electrostatic interactions between gadoteridol and the cationic lipid component. Optimal gadoteridol loading of CAF01 liposomes showed good in vivo stability and safety upon intrapulmonary administration into mice while generating 1.5-fold MRI signal enhancement associated with approximately 30% T 1 relaxation change. This formulation principle and imaging approach can potentially be used for other mucosal nanoparticle-based formulations, species, and lung pathologies, which can readily be translated for clinical use.

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Liposomes as nonspecific nanocarriers for 5-Fluorouracil in the presence of cyclodextrins

Buczek

Kupka

Broda

et al. 2021

Journal of Molecular Liquids

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Thermotropic Phase Behavior of Liposome Entrapped 5-FU and LCV

Cited by 6 publications

References 13 publications

Influence of some physical properties of 5-fluorouracil on encapsulation efficiency in liposomes

Influence of some physical properties of 5-fluorouracil on encapsulation efficiency in liposomes

Design of Gadoteridol-Loaded Cationic Liposomal Adjuvant CAF01 for MRI of Lung Deposition of Intrapulmonary Administered Particles

Liposomes as nonspecific nanocarriers for 5-Fluorouracil in the presence of cyclodextrins

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