Preparation and evaluation of N3-O-toluyl-fluorouracil-loaded liposomes

Sun, Weitong; Zhang, Na; Li, Aiguo; Zou, Weiwei; Xu, Wenfang

doi:10.1016/j.ijpharm.2007.11.017

Cited by 89 publications

(42 citation statements)

References 24 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Methods to determine the fraction of encapsulated material within liposomes typically rely on destruction of the lipid bilayer and subsequent quantification of the released material. In the present study, the drug encapsulation efficiency was determined using the protamine aggregation method, as described by Wang et al [23] and Sun et al [24]. Briefly, the total amount of vitamin E (TA) was determined after disrupting and dissolving vitamin E-loaded liposomes in ethanol using an ultrasound bath for 10 min.…”

Section: Characterization Of Liposomesmentioning

confidence: 99%

Preparation of liposomes: a novel application of microengineered membranes - investigation of the process parameters and application to the encapsulation of vitamin E

et al. 2013

View full text Add to dashboard Cite

Liposomes with a mean size of 59-308 nm suitable for pulmonary drug delivery were prepared by the ethanol injection method using nickel microengineered flat disc membranes with a uniform pore size of 5-40 mm and a pore spacing of 80 or 200 mm. An ethanolic phase containing 20-50 mg ml 21 phospholipid (1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC) or Lipoid1 E80), 5-12.5 mg ml 21 stabilizer (cholesterol, stearic acid or cocoa butter), and 0 or 5 mg ml 21 vitamin E was injected through the membrane into an agitated aqueous phase at a controlled flux of 142-355 l m 22 h 21 and a shear stress on the membrane surface of 0.80-16 Pa. The mean particle size obtained under optimal conditions was 84 and 59 nm for Lipoid E80 and POPC liposomes, respectively. The particle size of the prepared liposomes increased with an increase in the pore size of the membrane and decreased with an increase in the pore spacing. Lipoid E80 liposomes stabilized by cholesterol or stearic acid maintained their initial size within 3 months. A high entrapment efficiency of 99.87% was achieved when Lipoid E80 liposomes were loaded with vitamin E. Transmission electron microscopy images revealed spherical multi-lamellar structure of vesicles. The reproducibility of the developed fabrication method was high.

show abstract

Section: Characterization Of Liposomesmentioning

confidence: 99%

Preparation of liposomes: a novel application of microengineered membranes - investigation of the process parameters and application to the encapsulation of vitamin E

et al. 2013

View full text Add to dashboard Cite

show abstract

“…Liposomes are spherical vesicles with concentric phospholipid bilayers that can act as biocompatible, biodegradable and nonimmunogenic drug carriers [2]. The advantages of nano-carriers are their ability to entrap both lipophilic and hydrophilic drugs, selective delivery of entrapped drug to the targeted site, protecting encapsulated agents from metabolic processes, improved therapeutic indices, and increased circulation life times of the drug [2].…”

Section: Introductionmentioning

confidence: 99%

“…The advantages of nano-carriers are their ability to entrap both lipophilic and hydrophilic drugs, selective delivery of entrapped drug to the targeted site, protecting encapsulated agents from metabolic processes, improved therapeutic indices, and increased circulation life times of the drug [2]. Despite worldwide interest in therapeutic applications of liposomes in biotechnology, their preparation remains as a challenging issue [3].…”

Section: Introductionmentioning

confidence: 99%

Formulation of a New Generation of Liposomes from Bacterial and Archeal Lipids

Ameri¹,

Moghimipour²,

Ramezani³

et al. 2016

Trop. J. Pharm Res

View full text Add to dashboard Cite

“…7 Based on the advantages of lipidbased materials and nanostructures, lipid-based nanocarriers present many favorable characteristics, such as: 1) improved drug dispersibility; 2) enhanced drug solubility; 3) enhanced drug transmembrane transport capability; 4) increased therapeutic efficacy by passive targeting; and 5) reduced toxicity with biocompatible or biodegradable components. [8][9][10][11] TFU has been previously encapsulated in several kinds of lipid-based formulations, such as liposomes 1,12 and two types (cationic and anionic) of solid lipid nanoparticles. [13][14][15] All three formulations enhanced the gastrointestinal absorption of TFU by oral administration, which was about twice that of TFU suspension.…”

Section: Introductionmentioning

confidence: 99%

Preclinical studies of N3-O-toluyl-fluorouracil-loaded lipid-based nanosuspensions in H22-bearing mice

Zhang¹,

Li²,

Liu³

et al. 2014

IJN

View full text Add to dashboard Cite

Purpose N 3 -O-toluyl-fluorouracil (TFU) is a potential antitumor prodrug of 5-fluorouracil (5-FU), but its poor solubility has limited its use in clinic. This study aimed to improve the bioavailability of TFU by preparing TFU-loaded lipid-based nanosuspensions (TFU-LNS) and perform a preclinical evaluation. Methods TFU-LNS were prepared through high-pressure homogenization and were lyophilized afterwards. For in vitro test, the physicochemical properties and cytotoxicity against HegG2 cells were conducted. For in vivo evaluation, the pharmacokinetics, tissue distribution, and antitumor efficacy were investigated in H 22 -bearing Kunming mice. Results TFU showed different degradability in four media; in particular, nearly all of it converted to an equimolar amount of 5-FU in blank plasma of Wistar rats. The lyophilized TFU-LNS had a mean particle size of 180.03±3.11 nm and zeta potential of −8.02±1.43 mV and showed no discernible changes after storage at 4°C for 3 months. In the in vivo antitumor study, the antitumor efficacy of TFU-LNS was consistent with that of 5-FU injection. Furthermore, TFU-LNS released a lower concentration of 5-FU in heart and kidney throughout the tissue distribution studies. Conclusion TFU-LNS exhibited convincing antitumor activity and easy scale-up opportunity, which suggests that TFU-LNS might be a promising drug delivery system for cancer therapy.

show abstract

Preparation and evaluation of N3-O-toluyl-fluorouracil-loaded liposomes

Cited by 89 publications

References 24 publications

Preparation of liposomes: a novel application of microengineered membranes - investigation of the process parameters and application to the encapsulation of vitamin E

Preparation of liposomes: a novel application of microengineered membranes - investigation of the process parameters and application to the encapsulation of vitamin E

Formulation of a New Generation of Liposomes from Bacterial and Archeal Lipids

Preclinical studies of N3-O-toluyl-fluorouracil-loaded lipid-based nanosuspensions in H22-bearing mice

Contact Info

Product

Resources

About