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Journal of Liposome Research

Pushpendra Singh, Zoltan Beck, Gary R Matyas, Carl R Alving
Liposomes containing cholesterol and monophosphoryl lipid A (such as ALFQ and AS01B) are vaccine adjuvants. During construction of the formulations, addition of QS21 to nano-size (50-100 nm) liposomes resulted in extremely large (up to ∼30 micron) liposomes in ALFQ, but AS01B liposomes remained small nano-vesicles. Here, we show that saturation of phospholipid chains is essential for production of large liposomes by QS21.
October 23, 2018: Journal of Liposome Research
Mariia Nesterkina, Sergii Smola, Iryna Kravchenko
The influence of esters based on gamma-aminobutyric acid (GABA) and mono-/bicyclic terpenoids on membrane structure was investigated. The mechanism of action for terpenoid esters on phospholipids of artificial membranes and lipids isolated from the rat stratum corneum was studied by fluorescence and FT-IR spectroscopy. We report here, that inclusion of monocyclic terpenoid esters in phospholipid liposomes leads to growth of excimer to monomer ratio (IE /IM ) indicating a decrease of membrane microviscosity...
October 23, 2018: Journal of Liposome Research
Sandip Honmane, Ashok Hajare, Harinath More, Riyaz Ali M Osmani, Sachin Salunkhe
The motive behind present work was to discover a solution for overcoming the problems allied with deprived oral bioavailability of salbutamol sulphate (SS) due to its first pass hepatic metabolism, shorter half life and systemic toxicity at high doses. Pulmonary delivery provides alternative route of administration to avoid hepatic metabolism of SS, moreover facilitated diffusion and prolonged retention can be achieved by incorporation into liposomes. Liposomes were prepared by thin film hydration technique using 32 full factorial design and formulation was optimized based on the vesicle size and percent drug entrapment (PDE) of liposomes...
October 8, 2018: Journal of Liposome Research
Mohammad A Obeid, Christine Dufès, Sukrut Somani, Alexander B Mullen, Rothwelle J Tate, Valerie A Ferro
RNA interference (RNAi) is an effective and naturally occurring post-transcriptional gene regulatory mechanism. This mechanism involves the degradation of a target messenger RNA (mRNA) through the introduction of short interfering RNA (siRNA) that is complementary to the target mRNA. The application of siRNA-based therapeutics is limited by the development of an effective delivery system, as naked siRNA is unstable and cannot penetrate the cell membrane. In this study, we investigated the use of cationic niosomes (CN) prepared by microfluidic mixing for siRNA delivery...
October 8, 2018: Journal of Liposome Research
Xing YaBing, Liu Xin, Li Xiao, Ding Fang, Zhang JunYa, Guo XinHong
The primary purpose of the present study was to design and optimize a solid lipid nanoparticle (SLN) formulation of the poorly water-soluble drug 2-methoxyestradiol (2-ME) to improve its oral bioavailability and prolong the duration of therapeutic drug level. SLN was modified by amphipathic PEG-PCL (PLN) and then encapsulated in pH-sensitive microparticles (MP) by spray drying technology. Several properties of 2-ME PLN-MP were characterized including particle size, drug loading and drug or PLN release. After oral administration of 2-ME PLN-MP, retention time in mice were evaluated by in vivo imaging technology and the pharmacokinetic parameters in rats were determined by HPLC...
October 3, 2018: Journal of Liposome Research
Tarek M Ibrahim, Marwa H Abdallah, Nagia A El-Megrab, Hanan M El-Nahas
The current study was conducted to develop vesicular ethosomal gel (ethogel) systems for upgrading the transdermal delivery of anti-hypertensive carvedilol. Ethosomes composed of Phospholipone 100 H, cholesterol, ethanol and Transcutol P at different ratios, were prepared by thin-film hydration method with sonication. Carvedilol-loaded ethosomes were characterized by microscopic examinations followed by other in-vitro assessments. Selected ethosomal formulation (E10) was incorporated into different concentrations of gelling agents to prepare the ethogel formulations...
October 1, 2018: Journal of Liposome Research
Samira Tajvar, Soheila Mohammadi, Alireza Askari, Sajjad Janfaza, Maryam Nikkhah, Elnaz Tamjid, Saman Hosseinkhani
In recent years there has been much interest in development of multifunctional drug delivery systems. In this work, liposomes that contain doxorubicin (Dox), a potent anticancer drug, and graphene nanosheets (GNS) were prepared. The GNSs have excellent optical properties, such as photoluminescence which enables tracking of the liposomes, high absorption in ultra violet region of electromagnetic spectrum which can be exploited in photodynamic and photothermal therapy, and low toxicity to mammalian cells. Nanoliposomes were prepared using the thin film hydration method...
September 20, 2018: Journal of Liposome Research
Heba F Salem, Rasha M Kharshoum, Ossama M Sayed, Lekaa F Abdel Hakim
BACKGROUND: The oral administration of celecoxib (CLX) is a real problem because of its low aqueous solubility that results in high variability in absorption and its severe adverse effect such as cardio toxic effects and gastrointestinal toxicity. Self-nanoemulsifying drug delivery systems (SNEDDS) can enhance the poor dissolution and erratic absorption of poorly-water soluble drugs like CLX. AIMS: This study was conducted to investigate the potential of SNEDDS to enhance the efficacy of CLX on inflamed mucous tissue and reduce systemic adverse effects by increasing its poor dissolution properties...
September 16, 2018: Journal of Liposome Research
Rawia M Khalil, Ahmed Abdelbary, Silvia Kocova El Arini, Mona Basha, Hadeer A El-Hashemy
Bilosomes were developed in order to investigate their efficacy as nanocarriers for transdermal delivery of Tizanidine HCl (TZN), a skeletal muscle relaxant with low oral bioavailability. Full factorial experimental design consisting of 27 combinations was generated to study the effects of surfactant type, surfactant to cholesterol ratio and the amount of bile salt on the entrapment efficiency, the vesicle size and in-vitro dissolution of the TZN-loaded bilosomes. The permeation through the stratum cornea (SC) was optimized with the vertical diffusion assembly using excised rat skin...
September 16, 2018: Journal of Liposome Research
Heba F Salem, Rasha M Kharshoum, Heba A AbouTaleb, Hisham A Abou Taleb, Kariman M AbouElhassan
Bio-identical progesterone (PRG) is an exogenous female steroidal hormone which is used for treatment of polycystic ovary syndrome. However, it suffers from poor bioavailability due to hepatic metabolism and poor solubility. The target of this work was to evaluate and statistically optimize PRG-loaded nanovesicle transethosomes(NVTEs) based in mucoadhesive gel for transvaginal delivery of PRG as potential luteal-phase support. A 24 full factorial design was used to explore the effect of phosphatidylcholine (PC), Tween 80, cetyltrimethyl ammonium bromide and ethanol concentration on particle size, entrapment efficiency (EE %), % in vitro PRG release after 24h and transvaginal flux...
September 16, 2018: Journal of Liposome Research
Anup Jose, Kunal Manoj Ninave, Sriravali Karnam, Venkata Vamsi Krishna Venuganti
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-sn-glycero-3-phosphocholine (DPPC), monopalmitoyl-2-hydroxy-sn-glycero-3-phosphocholine (MPPC), and different surface active agents. The liposomes were characterized for the average particle size, zeta potential, transition temperature, and drug release below and above liposomal transition temperature...
September 11, 2018: Journal of Liposome Research
Magdalini Rovoli, Ioannis Pappas, Stavros Lalas, Olga Gortzi, George Kontopidis
Vitamin A (VA) is an essential nutrient needed in small amounts by humans and supports a wide range of biological actions. Retinol, the most common and most biologically active form of VA has also been found to inhibit peroxidation processes in membranes and it has been widely used as an ingredient with pharmaceutical and nutritional applications. VA is a lipophilic molecule, sensitive to air, oxidizing agents, ultraviolet light and low pH levels. For these reasons, it is necessary for VA to be protected against oxidation...
September 6, 2018: Journal of Liposome Research
Ana Cláudia Pedreira de Almeida, Luciana Matos Alves Pinto, Giuliana Piovesan Alves, Lígia Nunes de Morais Ribeiro, Maria Helena Andrade Santana, Cíntia Maria Saia Cereda, Leonardo Fernandes Fraceto, Eneida de Paula
This study describes the encapsulation of the local anaesthetic lidocaine (LDC) in large unilamellar liposomes (LUV) prepared in a scalable procedure, with hydrogenated soybean phosphatidylcholine, cholesterol and mannitol. Structural properties of the liposomes were assessed by dynamic light scattering, nanoparticle tracking analysis and transmission electron microscopy. A modified, two-compartment Franz-cell system was used to evaluate the release kinetics of LDC from the liposomes. The in vivo anaesthetic effect of liposomal LDC 2% (LUVLDC ) was compared to LDC 2% solution without (LDCPLAIN ) or with the vasoconstrictor epinephrine (1:100 000) (LDCVASO ), in rat infraorbital nerve blockade model...
September 6, 2018: Journal of Liposome Research
Nidhi Nainwal, Sunil Jawla, Ranjit Singh, Vikas Anand Saharan
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 carrier containing high ethanol concentrations and offer improved skin permeability and efficient bioavailability due to their structure and composition. This article gives a review of ethosomes including their compositions, types, mechanism of drug delivery, stability, and safety behavior...
August 29, 2018: Journal of Liposome Research
Fariba Malekpour-Galogahi, Ashrafalsadat Hatamian-Zarmi, Fariba Ganji, Bahman Ebrahimi-Hosseinzadeh, Fahimeh Nojoki, Razi Sahraeian, Zahra Beagom Mokhtari-Hosseini
Rivastigmine hydrogen tartrate (RHT) is a pseudo-irreversible inhibitor of cholinesterase and is used for the treatment of Alzheimer's. However, RHT delivery to the brain is limited by the blood-brain barrier (BBB). The purpose of this study was to improve the brain-targeting delivery of RHT by producing and optimizing rivastigmine hydrogen tartrate-loaded tocopherol succinate-based solid lipid nanoparticles (RHT-SLNs). RHT-SLNs were prepared using the microemulsion technique. The impact of significant variables, such as surfactant concentration and drug/lipid ratio, on the size of RHT-SLNs and their drug loading and encapsulation efficiency was analysed using a five-level central composite design (CCD)...
September 2018: Journal of Liposome Research
Artur Wrona, Krystian Kubica
CONTEXT: The molecular bases of pore formation in the lipid bilayer remain unclear, as do the exact characteristics of their sizes and distributions. To understand this process, numerous studies have been performed on model lipid membranes including cell-sized giant unilamellar vesicles (GUV). The effect of an electric field on DPPC GUV depends on the lipid membrane state: in the liquid crystalline phase the created pores have a cylinder-like shape, whereas in the gel phase a crack has been observed...
September 2018: Journal of Liposome Research
Maria Chountoulesi, Nikolaos Naziris, Natassa Pippa, Costas Demetzos
Liposomes are considered to be one of the most extensively investigated drug delivery nanosystems. Each drug can be loaded either in the liposomal hydrophilic core or within the lipidic bilayer and delivered eventually to the proper site into the organism. There are already many marketed approved liposomal products. The development of a liposomal product is a quite complicated process, while many critical parameters have to be investigated during the preparation process. The present study deals with the drug-to-lipid ratio (D/L ratio), which is a critical process parameter, expresses the actual capacity of the liposome to accommodate the drug and can play a key role at the optimization of every liposomal formulation...
September 2018: Journal of Liposome Research
Amal A Sultan, Sanaa A El-Gizawy, Mohamed A Osman, Gamal M El Maghraby
Niosomes have been claimed to enhance intestinal absorption and to widen the absorption window of acidic drugs. This was reported after monitoring the intestinal absorption in situ. Accordingly, the aim of this work was to investigate the effect of niosomal encapsulation on intestinal absorption and oral bioavailability of nateglinide. This was conducted with the goal of correlation between in situ intestinal absorption and in vivo availability. The drug was encapsulated into proniosomes. The niosomes resulting after hydration of proniosomes were characterized with respect to vesicle size and drug entrapment efficiency...
September 2018: Journal of Liposome Research
Amelia M Avachat, Pooja J Takudage
Various dressings are available to heal chronic wounds which many times fail to achieve the expected results. To overcome some of their drawbacks, formulation of a novel dressing; lyophilized liposomal wafers having better wound healing potential has been proposed in the present study. The drug incorporated in the formulation is gatifloxacin (GTX) which is a fourth-generation fluoroquinolone antibiotic having in vitro activity against both Gram-negative and Gram-positive bacteria. The formulation was designed in three stages where at first liposomes were prepared, the liposomes were converted to gel using chitosan and lastly this gel was lyophilized to form liposomal wafers...
September 2018: Journal of Liposome Research
Sinar Sayed, Basant A Habib, Ghada M Elsayed
This study aimed to prepare, optimize and characterize novel felodipine-loaded polymeric nanomicelles, using a pluronic mixture of F127 and P123. Thin-film hydration method was adopted for the preparation of different polymeric nanomicelles (T1-T12) according to a 41 .31 full factorial design. Factors studied were: Pluronic®:drug ratio (P:D ratio) (10, 20, 30 and 40 w/w) and percent of hydrophilic polymer (F127%) (33.33%, 50% and 66.67% w/w). Optimization criteria were to maximize transmittance percent (T%) and entrapment efficiency percent (EE%) and to minimize particle size (PS) and polydispersity index (PDI)...
September 2018: Journal of Liposome Research
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