Abstract:
:This study aimed to investigate the influence of the preparation conditions on the performance of an ethosomal formulation for topical delivery of the local anesthetic agent, benzocaine (BZC). Ethosomes were prepared with different techniques, such as thin-layer evaporation, freezing and thawing, reverse-phase evaporation, extrusion and sonication, obtaining, respectively, multilayer vesicles (MLVs), frozen and thawed MLV (FATMLV), large unilamellar vesicles (LUVs), and small unilamellar vesicles (SUVs). The obtained vesicles were characterized for morphology, size, zeta potential, and entrapment efficiency (EE%), and their stability was monitored during storage at 4 degrees C. In vitro permeation properties from gels incorporating drug ethosomal dispersions were evaluated in vitro by using artificial lipophilic membranes, while their anesthetic effect was determined in vivo on rabbits. The results suggested that the vesicle preparation method plays an important role in affecting the properties and effectiveness of ethosomal formulations. MLVs and LUVs exhibited higher drug EE% and better stability than FATMLV and SUV vesicles. The In vitro drug permeation rate was directly related to the vesicle EE% and varied in the order MLV>LUV approximately FATMLV>SUV. The therapeutic efficacy of BZC ethosomal formulations was significantly improved with respect to the corresponding BZC solution. The best results, in terms of enhanced intensity of anesthetic effect, were given by formulations containing MLVs and LUVs, and the order of effectiveness was MLV approximately LUV>FATMLV approximately SUV, rather similar to that found in permeation studies. On the contrary, unexpectedly, the effectiveness order in increasing the duration of drug action was SUV> or =MLV>LUV approximately FATMLV. The highest efficacy of SUVs was probably due to the more intimate contact with the epithelium due to their greatest surface area, which allowed the longest extension of drug therapeutic action. The overall results suggest that a suitably developed ethosomal formulation of BZC can be of actual value for improving its clinical effectiveness in topical anesthesia.
journal_name
J Liposome Resjournal_title
Journal of liposome researchauthors
Maestrelli F,Capasso G,González-Rodríguez ML,Rabasco AM,Ghelardini C,Mura Pdoi
10.3109/08982100902788408subject
Has Abstractpub_date
2009-01-01 00:00:00pages
253-60issue
4eissn
0898-2104issn
1532-2394journal_volume
19pub_type
杂志文章abstract::Methotrexate (MTX) is indicated in the symptomatic control of severe, recalcitrant, and disabling psoriasis. The oral or parenteral route of administration causes systemic toxicity. The topical route of delivery, though, reduces systemic toxicity and has limited applicability due to restricted permeability. Liposomal ...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.3109/08982104.2010.492476
更新日期:2011-06-01 00:00:00
abstract::Archaeosomes, liposomes prepared from the polar ether lipids extracted from Archaea, demonstrate great potential as immunomodulating carriers of soluble antigens, promoting humoral and cell mediated immunity in the vaccinated host. The safety of unilamellar archaeosomes prepared from the total polar lipids (TPL) of Ha...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.1081/lpr-120016712
更新日期:2002-11-01 00:00:00
abstract::By selecting a unique combination of lipids and amphotericin B, the liposome composition for AmBisome® (L-AmBis) has been optimized resulting in a formulation that is minimally toxic, targets to fungal cell walls, and distributes into and remains for days to weeks in various host tissues at drug levels above the MIC f...
journal_title:Journal of liposome research
pub_type: 杂志文章,评审
doi:10.1080/08982104.2017.1327543
更新日期:2017-09-01 00:00:00
abstract:CONTEXT:Asenapine maleate (ASPM) is an antipsychotic drug for the treatment of schizophrenia and bipolar disorder. Extensive metabolism makes the oral route inconvenient for ASPM. OBJECTIVE:The objective of this study is to increase ASPM bioavailability via transdermal route by improving the skin permeation using comb...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.3109/08982104.2015.1098659
更新日期:2016-09-01 00:00:00
abstract::Propylthiouracil, a lyophobic drug with an antiproliferative activity, was formulated into niosomes using various classes of nonionic surfactants. Feasibility of vesicle formation by the sonication method was evaluated. Size and size distribution was measured by laser diffraction. Entrapment and drug release over 24 h...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.1080/08982100600992542
更新日期:2006-01-01 00:00:00
abstract::Leishmaniasis is a parasitic disease treatable and curable, however, the chemotherapeutic agents for their treatment are limited. In South American countries, pentavalent antimonials are still the first line of treatment for cutaneous leishmaniasis with an efficacy of about 75%, but the toxicity of the drug causes ser...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.1080/08982104.2020.1749067
更新日期:2020-04-13 00:00:00
abstract::Background and objective: The combination of two or more different mechanisms of drugs in the treatment of cancer has become one of the effective methods. The purpose of this study was to successfully prepare a non-viral delivery system that could efficiently co-delivery siRNA and gambogenic acid (GNA) to improve the ...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.1080/08982104.2018.1473423
更新日期:2019-12-01 00:00:00
abstract::Sonication is a simple method for reducing the size of liposomes. We report the size distributions of liposomes as a function of sonication time using three different techniques. Liposomes, mildly sonicated for just 30 sec, had bimodal distributions when surface-weighted with modes at about 140 and 750 nm. With extend...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.1080/08982100500528842
更新日期:2006-01-01 00:00:00
abstract::The current investigation aims to develop and evaluate novel ocular proniosomal gels of lomefloxacin HCl (LXN); in order to improve its ocular bioavailability for the management of bacterial conjunctivitis. Proniosomes were prepared using different types of nonionic surfactants solely and as mixtures with Span 60. The...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.3109/08982104.2016.1167737
更新日期:2017-06-01 00:00:00
abstract::Vesicular phospholipid gels (VPGs) represent semi-solid phospholipid dispersions. Their morphology is truly vesicular with aqueous compartments both within the core of the vesicles and in-between the vesicles. VPGs are suited to carry both hydrophilic, amphiphilic and lipophilic drugs. Their drug load is stable since ...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.1080/08982100601186490
更新日期:2007-01-01 00:00:00
abstract::The aim of present study was to develop conventional and PEGylated (long circulating), liposomes containing anastrozole (ANS) for effective treatment of breast cancer. ANS is a third-generation non-steroidal aromatase inhibitor of the triazole class used for the treatment of advanced and late-stage breast cancer in po...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.3109/08982104.2015.1029493
更新日期:2016-01-01 00:00:00
abstract::In the present work, we show that we obtained nanometric structures made of water, 1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine (DPPC), cholesterol (Chol), and a mixture of ethoxylated and non-ethoxylated sorbitan fatty acid esters (Tween 20, Span 20, Tween 80, and Span 80) by mixing all of them near the cloud poi...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.1080/08982104.2016.1174944
更新日期:2017-06-01 00:00:00
abstract::Co-delivery of chemotherapeutic agents using nanocarriers is a promising strategy for enhancing therapeutic efficacy of anticancer agents. The aim of this work was to develop tamoxifen and imatinib dual drug loaded temperature-sensitive liposomes to treat breast cancer. Liposomes were prepared using 1, 2-dipalmitoyl-s...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.1080/08982104.2018.1502315
更新日期:2019-06-01 00:00:00
abstract::Pulmonary lung targeting finds applications in drug delivery to the lung itself and to other body organs, via blood circulation following transfer across alveolar membranes. Understanding pulmonary drug delivery systems towards improving their efficacy needs identification of particle sizes of relevance and elucidatio...
journal_title:Journal of liposome research
pub_type: 杂志文章,评审
doi:10.3109/08982104.2013.802332
更新日期:2013-12-01 00:00:00
abstract::The evidence in this communication indicate that, unlike resident Kupffer cells, newly recruited liver macrophages (following monocyte migration from the blood to the liver) use complement receptors to recognize and internalize stearylamine-incorporated liposomes. Within two weeks of hepatic residency complement recep...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.1081/lpr-120004778
更新日期:2002-02-01 00:00:00
abstract::This work describes the preparation of a PEGylated niosomes-mediated drug delivery systems for Paeonol, thereby improving the bioavailability and chemical stability of Paeonol, prolonging its cellular uptake and enhancing its synergistic anti-cancer effects with 5-Fu. PEGylated niosomes, which are prepared from biocom...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.1080/08982104.2016.1191021
更新日期:2017-06-01 00:00:00
abstract::Simvastatin (SIM) is a lipophilic statin that has potential benefits for prevention and treatment of several types of malignancies. However, its low water solubility and the toxicity associated with administration of high doses recommend it for encapsulation in carriers able to deliver the therapeutic dose in the tumo...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.3109/08982104.2014.987787
更新日期:2015-01-01 00:00:00
abstract::The luciferase gene expression of lipoplexes, a liposome containing luciferase plasmid (pCMVLuc), in HeLa cell lines, was investigated. Cationic liposomes were prepared by the chloroform film method with sonication. The lipoplex was formed by loading the liposome with pCMVLuc. The lipoplex with an optimal weight ratio...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.1080/08982100802642457
更新日期:2009-01-01 00:00:00
abstract::In this study, the electron spin resonance (ESR) method was used to examine the effect of Amphotericin B (AmB) molecules on the fluidity of model membranes made of dipalmitoylphosphatidylcholine (DPPC). The changes occurring under increased AmB concentrations in the spectroscopic parameters of spin probes placed in li...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.3109/08982104.2013.814139
更新日期:2013-12-01 00:00:00
abstract::In this study we successfully entrapped 5-aminolevulinic acid (ALA) in liposome, although it exists as a zwitter ion. A molar ratio of 2:1:2.5 phosphatidyle-thanolamine (PE)/cholesterol/sodium stearate represented the best condition to achieve high entrapment efficiency (29.37 +/- 1.21%), and the average vehicle size ...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.1080/08982100801893952
更新日期:2008-01-01 00:00:00
abstract::Liposomal vinorelbine formulation is desirable, as it might improve the therapeutic activity of vinorelbine. However, because of its lipophilic and membrane-permeable properties, vinorelbine is hard to be formulated into liposomes using conventional drug-loading technologies. To improve vinorelbine retention, ammonium...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.3109/08982104.2011.584880
更新日期:2012-03-01 00:00:00
abstract::The imaging of sentinel lymph nodes (SLN) has been researched for its role in assessing cancer progression and postsurgical lymphedema. Indocyanine green (ICG) is a near-infrared (NIR) optical dye that has been approved by the Food and Drug Administration. It is known that liposome-encapsulated ICG (LP-ICG) has improv...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.3109/08982104.2013.801488
更新日期:2013-12-01 00:00:00
abstract::Naturally occurring antibodies to phospholipids and cholesterol are widespread; they occur commonly during the course of acute infections; they are not causally related to the anti-phospholipid syndrome; they have been associated with other clinical entities only as an epiphenomenon; and they have not been implicated ...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.1080/08982100600848553
更新日期:2006-01-01 00:00:00
abstract::Sustained release depot systems have been widely investigated for their potential to improve the efficacy of subunit vaccines and reduce the requirement for boosting. The present study aimed to further enhance the immunogenicity of a sustained release vaccine by combining a depot formulation with a particulate antigen...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.3109/08982104.2011.637502
更新日期:2012-09-01 00:00:00
abstract::The liposomalization and polyethyleneglycol (PEG) modification of antitumor agents prolongs their circulation in the blood and increases their accumulation in the tumor. It is expected that modification of the liposome surface with PEG-Lipid will prevent connection of liposome and tumor cell, so we examined the effect...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.1081/lpr-120020318
更新日期:2003-05-01 00:00:00
abstract::Skin, the largest organ of the body serves as a potential route of drug delivery for local and systemic effects. However, the outermost layer of skin, the stratum corneum (SC) acts as a tough barrier that prevents penetration of hydrophilic and high molecular weight drugs. Ethosomes are a novel phospholipid vesicular ...
journal_title:Journal of liposome research
pub_type: 杂志文章,评审
doi:10.1080/08982104.2018.1517160
更新日期:2019-06-01 00:00:00
abstract::The influence of the lipid composition of arsonoliposomes on their membrane integrity was investigated to evaluate whether it is possible to combine their action with drugs that can be encapsulated in their aqueous interior. This was investigated by measuring the retention of vesicle-encapsulated calcein (100 mM) duri...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.1080/08982100500364263
更新日期:2005-01-01 00:00:00
abstract::Intravenous injection of some liposomal drugs, diagnostic agents, micelles and other lipid-based nanoparticles can cause acute hypersensitivity reactions (HSRs) in a high percentage (up to 45%) of patients, with hemodynamic, respiratory and cutaneous manifestations. The phenomenon can be explained with activation of t...
journal_title:Journal of liposome research
pub_type: 杂志文章,评审
doi:10.1080/08982100701375118
更新日期:2007-01-01 00:00:00
abstract::This multicenter study investigated the possibility of reducing mortality rate by administering natural lung surfactant additional to standard therapy to treat patients after cardiac surgery who developed an acute respiratory failure (ARDS/ALI).A total of 78 patients (1998-2002) diagnosed with ALI or ARDS were enrolle...
journal_title:Journal of liposome research
pub_type: 杂志文章,多中心研究
doi:10.1080/08982100600850997
更新日期:2006-01-01 00:00:00
abstract::Cutaneous leishmaniasis is caused by different species of Leishmania parasites and its available treatments have not yet provided a strong consistent result. The weak response of current chemotherapeutics is due to their deficient effects on stealth parasites inside macrophages, rapid clearance from the site of action...
journal_title:Journal of liposome research
pub_type: 杂志文章
doi:10.3109/08982104.2012.762519
更新日期:2013-06-01 00:00:00