5-Fluorouracil: various kinds of loaded liposomes: encapsulation efficiency, storage stability and fusogenic properties

Fresta, Massimo; Villari, A; Puglisi, Giovanni; Cavallaro, Gennara

doi:10.1016/0378-5173(93)90356-k

Cited by 52 publications

(37 citation statements)

References 35 publications

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“…CH forms a stable bilayer and is a cause of least flexibility or deformability in liposome. It was reported that 5-FU was not shown to be adsorbed to dipalmitoylphosphatidylcholine/ PC bilayer (Fresta et al, 1993). In contrast, it was observed between lipid and CH.…”

Section: Resultsmentioning

confidence: 56%

“…This limited entrapment effect was applicable to smaller liposomes due to the small ratio of trapped to external volume. Furthermore, it was reported that trapping efficiency of 5-FU was found to have only 2-6% depending on lipid composition (Ö zer, 1992;Fresta et al, 1993). On the other hand, on prolonged standing of the liposome formulation, variation in vesicular size, phase separation of the lipid bilayer and leakage of trapped drug after removal of un-entrapped drugs are another major physical instability-related issue in developing liposome.…”

mentioning

confidence: 99%

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Elastic liposome-based gel for topical delivery of 5-fluorouracil: in vitro and in vivo investigation

Hussain

Samad²,

Ramzan

et al. 2014

Drug Delivery

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Objective: This investigation has focused to characterize the elastic liposome containing 5-fluorouracil (5-FU) and to enhance drug permeation across stratum corneum (SC) of the skin (rat) using various surfactants and in vivo dermal toxicity evaluation. Methodology: 5-FU-loaded elastic liposomes were developed, prepared and characterized for their entrapment efficiency, vesicle size, number of vesicles, morphological characteristics, surface charge and turbidity. In vitro drug release profile, in vitro skin permeation potential and in vitro hemolytic ability of the formulation have been evaluated to compare with drug solution for 24 h. In vitro skin permeation potential was also compared with marketed cream. Furthermore, in vivo skin irritation potential, drug penetration into the skin using confocal laser scanning microscopy (CLSM) and in vivo toxicity studies were performed. Results and conclusions:The optimized elastic liposomes demonstrated maximum drug entrapment efficiency, optimum vesicular size and considerable elasticity. In vitro skin permeation studies showed the highest drug permeation flux like 77.07 ± 6.34, 89.74 ± 8.5 and 70.90 ± 9.6 mg/cm 2 /h for EL3-S60, EL3-S80 and EL3-T80, respectively, as compared to drug solution (8.958 ± 6.9 mg/cm 2 /h) and liposome (36.80 ± 6.4 mg/cm 2 /h). Drug deposition of optimized elastic liposome EL3-S80 was about three fold higher than drug solution. Skin irritation and CLSM studies suggested that optimized gel was free from skin irritation and capable to deliver 5-FU into the epidermal area for enhanced topical delivery than drug solution. The in vitro study showed minimum hemolysis in the optimized formulation. Finally, in vivo toxicity studies followed with hisptopathological assessment showed that elastic liposome was able to extract SC to improve drug permeation without changing general anatomy of the skin.

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Section: Resultsmentioning

confidence: 56%

mentioning

confidence: 99%

Elastic liposome-based gel for topical delivery of 5-fluorouracil: in vitro and in vivo investigation

Hussain

Samad²,

Ramzan

et al. 2014

Drug Delivery

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show abstract

“…Regretfully, these observed increments were statistically not significant in present study. Fresta et al [20] had claimed that slow rate of hydration and gentle mixing was beneficial for the entrapment efficiency due to slow annealing of multilamellar vesicle, which allowed for a longer period of contact between all the liposomes bilayers and the drug aqueous solution.…”

Section: Resultsmentioning

confidence: 99%

Development and characterisation study of liposomes-encapsulated piroxicam.

et al. 2011

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The objective of present work was to develop a novel liposomes-based drug delivery system for a lipophilic nonsteroidal anti-inflammatory drug, piroxicam. The system was prepared using proliposomes method and optimised for different preparation parameters including type of proliposomes, concentration of drug, duration of hydration and type of particle size reduction treatment used. All prepared liposomal samples were extensively characterized for their drug-entrapment and size profile using various in-vitro techniques. Present work showed that the most optimum formulation (Pro-lipo TM Duo; 12mg piroxicam per gram Prolipo TM ; 10 hours hydration time) produced highest amount of actual drug been entrapped in liposomes (800.4 mg/g Prolipo TM ) with a satisfactory entrapment efficiency of 15.36%. This formulation had also produced liposomal samples with a homogenous (polydispersity index = 0.45) and small particle size (359.95nm). Extrusion technique was found to cause significant reduction in drug-entrapment and size profile of drug-loaded liposomes. A 4-weeks storage study showed that drug-entrapment and size profile of liposomal samples were stable in both refrigerated and room temperature. Electron microscopy revealed that prepared liposomal samples were spherical-shaped and showed concentric lamellae. In conclusion, present work successfully demonstrated a simple, reproducible and practical method of preparation for liposomes-encapsulated piroxicam.

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“…[95] Statin liposomal formulations use a new and highly efficient liposomal encapsulation technique, termed micelleliposome exchange. This liposomal encapsulation greatly increases the solubility of statins, in one example more than 1000-fold.…”

Section: Liposomesmentioning

confidence: 99%

Statins therapy: a review on conventional and novel formulation approaches

Tiwari

Pathak

2011

Journal of Pharmacy and Pharmacology

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Background and objective High levels of cholesterol lead to atherosclerosis, a factor predisposing to the development of coronary artery disease. Statin drugs, i.e. HMG-CoA reductase inhibitors, have been known since the end of the last century for their benefits against cardio-and cerebrovascular diseases and are widely used clinically. This review aims at compiling the research inputs being made for developing therapeutically efficacious dosage forms that have the potential to surmount the limitations of conventional dosage forms of statins. Key findings Statin drugs can reduce the endogenous synthesis of cholesterol and prevent the onset and development of atherosclerosis, and are therefore used as an effective treatment against primary hypercholesterolemia. At present, statin drugs are most often administered orally, on a daily basis. After administration, the bioavailability and the general circulation of statin drugs is fairly low due to the first-pass metabolism in the liver and clearance by the digestive system. Extensive pharmaceutical research in understanding the causes of low oral bioavailability has led to the development of novel technologies to address these challenges. Summary These technologies vary from conventional dosage forms to nanoparticulate drug-delivery systems, and have the potential to cause improvements in bioavailability and consequently therapeutic efficacy.

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5-Fluorouracil: various kinds of loaded liposomes: encapsulation efficiency, storage stability and fusogenic properties

Cited by 52 publications

References 35 publications

Elastic liposome-based gel for topical delivery of 5-fluorouracil: in vitro and in vivo investigation

Elastic liposome-based gel for topical delivery of 5-fluorouracil: in vitro and in vivo investigation

Development and characterisation study of liposomes-encapsulated piroxicam.

Statins therapy: a review on conventional and novel formulation approaches

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