Encapsulation efficiency of water-soluble and insoluble drugs in liposomes prepared by the microencapsulation vesicle method

Nii, Tomoko; Ishii, Fumiyoshi

doi:10.1016/j.ijpharm.2005.04.029

Cited by 276 publications

(156 citation statements)

References 16 publications

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“…However, co-encapsulation rates of both 5-FU and its modulator were relatively poor (11 and 26%, respectively). Such a moderate encapsulation rate for 5-FU is not surprising when considering the polar and amphoterous properties of this drug, that render its handling quite difficult when preparing standard pegylated liposomes, as used here (Nii and Ishii, 2005). Indeed, our strategy was to develop a stealth delivery system as basic and as simple as possible, to easily standardise a fabrication process that could be performed in most laboratories equipped with standard apparatus and reagents.…”

Section: Discussionmentioning

confidence: 98%

“…Beside these higher plasma levels, sustained exposure to the drug was achieved, as liposomal d-Ino remained fully detectable 2 h after administration, whereas free d-Ino was totally cleared. Despite its extremely widespread use in clinical oncology, few reports have focused on encapsulating 5-FU in simple carriers, probably as a result of its polar and amphotereous properties that render it particularly difficult to entrap in standard liposomes (Simmons and Krame, 1977;Nii and Ishii, 2005). However, as a prodrug, 5-FU presents an opportunity to increase its therapeutic efficacy by combining it with biochemical modulators that can improve its intratumoural activation pattern.…”

Section: Discussionmentioning

confidence: 99%

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In vitro and in vivo reversal of resistance to 5-fluorouracil in colorectal cancer cells with a novel stealth double-liposomal formulation

Fanciullino¹,

Giacometti²,

Mercier³

et al. 2007

Br J Cancer

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Drug resistance is a major cause of treatment failure in cancer chemotherapy, including that with the extensively prescribed antimetabolite, 5-fluorouracil (5-FU). In this study, we tried to reverse 5-FU resistance by using a double-punch strategy: combining 5-FU with a biochemical modulator to improve its tumoural activation and encapsulating both these agents in one same stealth liposome. Experiments carried out in the highly resistant, canonical SW620 human colorectal model showed a up to 80% sensitisation to 5-FU when these cells were treated with our liposomal formulation. Results with this formulation demonstrated 30% higher tumoural drug uptake, better activation with increased active metabolites including critical-5-fluoro-2-deoxyuridine-5-monophosphate, superior inhibition (98%) of tumour thymidylate synthase, and subsequently, higher induction of both early and late apoptosis. Drug monitoring showed that higher and sustained exposure was achieved in rats treated with liposomal formulation. When examined in a xenograft animal model, our dual-agent liposomal formulation caused a 74% reduction in tumour size with a mean doubling in survival time, whereas standard 5-FU failed to exhibit significant antiproliferative activity as well as to increase the lifespan of tumour-bearing mice. Taken collectively, our data suggest that resistance to 5-FU can be overcome through a better control of its intratumoural activation and the use of an encapsulated formulation.

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Section: Discussionmentioning

confidence: 98%

Section: Discussionmentioning

confidence: 99%

In vitro and in vivo reversal of resistance to 5-fluorouracil in colorectal cancer cells with a novel stealth double-liposomal formulation

Fanciullino¹,

Giacometti²,

Mercier³

et al. 2007

Br J Cancer

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“…Centrifugation method was used to separate free molecules from the micelles based on their different ability to cross through the membrane with different sizes of pores upon centrifugation [13]. We first evaluated the recovery of free CPT-11 solution in the procedure.…”

Section: The Centrifugation Methodsmentioning

confidence: 99%

Development and Validation of a Method for Determination of Encapsulation Efficiency of CPT-11/DSPE-mPEG2000 Nanoparticles

Li¹,

Li²

2016

Med chem (Los Angeles)

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“…For the latter application, one typically employs liposomes encapsulating a sufficient amount of therapeutic agents. These liposomes have the ability to carry the substance in aqueous fluids (bloodstream) and modulate the drug biodistribution 12. The light exposure of liposomes, made of photoswitchable lipids can indeed trigger a rapid release of the vesicle content 13…”

Section: Introductionmentioning

confidence: 99%

Area Increase and Budding in Giant Vesicles Triggered by Light: Behind the Scene

et al. 2018

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Biomembranes are constantly remodeled and in cells, these processes are controlled and modulated by an assortment of membrane proteins. Here, it is shown that such remodeling can also be induced by photoresponsive molecules. The morphological control of giant vesicles in the presence of a water‐soluble ortho‐tetrafluoroazobenzene photoswitch (F‐azo) is demonstrated and it is shown that the shape transformations are based on an increase in membrane area and generation of spontaneous curvature. The vesicles exhibit budding and the buds can be retracted by using light of a different wavelength. In the presence of F‐azo, the membrane area can increase by more than 5% as assessed from vesicle electrodeformation. To elucidate the underlying molecular mechanism and the partitioning of F‐azo in the membrane, molecular dynamics simulations are employed. Comparison with theoretically calculated shapes reveals that the budded shapes are governed by curvature elasticity, that the spontaneous curvature can be decomposed into a local and a nonlocal contribution, and that the local spontaneous curvature is about 1/(2.5 µm). The results show that exo‐ and endocytotic events can be controlled by light and that these photoinduced processes provide an attractive method to change membrane area and morphology.

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Encapsulation efficiency of water-soluble and insoluble drugs in liposomes prepared by the microencapsulation vesicle method

Cited by 276 publications

References 16 publications

In vitro and in vivo reversal of resistance to 5-fluorouracil in colorectal cancer cells with a novel stealth double-liposomal formulation

In vitro and in vivo reversal of resistance to 5-fluorouracil in colorectal cancer cells with a novel stealth double-liposomal formulation

Development and Validation of a Method for Determination of Encapsulation Efficiency of CPT-11/DSPE-mPEG2000 Nanoparticles

Area Increase and Budding in Giant Vesicles Triggered by Light: Behind the Scene

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