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Journal of Liposome Research

Stephan Holzschuh, Kathrin Kaeß, Guilherme Volpe Bossa, Christiane Decker, Alfred Fahr, Sylvio May
Liposomal delivery constitutes a promising approach for i.v. administration of mTHPC because lipid membranes can host these drug molecules. This study investigates the transfer and release of temoporfin (mTHPC) to plasma proteins and stability of various liposomal formulations. To this end, we employed traces of radioactive markers and studied the effects of fatty acid chain length and the degree of saturation in the lipophilic tail, addition of cholesterol, and PEGylation of the membrane surface and different drug-to-lipid ratios...
October 18, 2016: Journal of Liposome Research
Xiao-Qing Wang, Zhou-Na Li, Qi-Ming Wang, Zhonggao Gao, Zhe-Hu Jin
Keloids were characterized by excessive growth of fibrous tissues, and shared several pathological characteristics with cancer. They did put physical and emotional stress on patients in that keloids could badly change appearance of patients. N-(4-hydroxyphenyl) retinamide (4HPR) showed cytotoxic activity on a wide variety of invasive-growth cells. Our work was aim to prepare N-(4-hydroxyphenyl) retinamide-loaded lipid microbubbles (4HPR-LM) combined with ultrasound for anti-keloid therapy. 4HPR-loaded liposomes (4HPR-L) were first prepared by film evaporation method, and then 4HPR-LM were manufactured by mixing 4HPR-L and perfluoropentane (PFP) with ultrasonic cavitation method...
October 13, 2016: Journal of Liposome Research
Qiying Shen, Liyan Qiu
Multidrug resistance (MDR) is a major obstacle to successful clinical cancer chemotherapy. Currently, there is still unsatisfactory demand for innovative strategies as well as effective and safe reversing agent to overcome MDR. In this study, we developed a novel nanoformulation, in which doxorubicin hydrochloride (DOX) and quinine hydrochloride (QN) were simultaneously loaded into liposomes by a pH-gradient method for overcoming MDR and enhancing cytotoxicity in a doxorubicin-resistant human breast cancer cell line (MCF-7/ADR)...
October 11, 2016: Journal of Liposome Research
Noriyuki Maeda, Kazuhito Ikeda, Masaki Matsumoto, Yukihiro Namba
Phospholipids and cholesterols are being spotlighted as raw materials for preparing liposomes, one of the key compounds for drug delivery systems (DDS), and as base compounds for converting water-soluble drugs to fat-soluble drugs. Other applications of phospholipids also are being explored. Nippon Fine Chemical, aware of the future of such lipids, has developed new processes for synthesizing and purifying phospholipids and is supplying them on an industrial scale. These products - used worldwide - are highly regarded as raw materials for preparing liposomes...
October 9, 2016: Journal of Liposome Research
Jin Ren, Zhengjie Fang, Liqun Jiang, Qian Du
The purpose of this study was to develop a liquid self-assemble proliposome for quercetin oral delivery. This liquid proliposome was prepared by dissolving phospholipids, surfactants and drug in ethanol. There was only one step in the preparation process of this liquid self-assemble proliposome and no special devices were required. The mechanism about proliposome transformation was discussed. Quercetin proliposomes with different cremorphor RH40 concentrations (0%, 20%, 23%, 26%, 30%) were prepared. The particle size and polydispersity index decreased as cremorphor RH40 concentration increased...
September 25, 2016: Journal of Liposome Research
Waleed Faisal, Ghareb M Soliman, Ahmed M Hamdan
Despite its broad-spectrum antifungal properties, voriconazole has many side effects when administered systemically. The aim of this work was to develop an ethosomal topical delivery system for voriconazole and test its potential to enhance the antifungal properties and skin delivery of the drug. Voriconazole was encapsulated into various ethosomal preparations and the effect of phospholipid and ethanol concentrations on the ethosomes properties were evaluated. The ethosomes were evaluated for drug encapsulation efficiency, particle size and morphology and antifungal efficacy...
September 25, 2016: Journal of Liposome Research
Mona M Abousamra, Alaa Hamed Salama
Tolnaftate is a thiocarbamate antifungal drug which is therapeutically active against dermatophytes that cause various forms of tinea. Due to the small amount of tolnaftate released from ordinary ointment bases and insufficient penetration through the infected skin layers the need to incorporate the drug in a more suitable pharmaceutical form has evolved. A provesicular system is one such form that can solve these problems. Once in contact with the skin, dilution with moisture occurs and the provesicular system rapidly transforms into a vesicular one...
September 25, 2016: Journal of Liposome Research
Tian Fu, Jinglin Yi, Songyi Lv, Bing Zhang
CONTEXT: Fungal keratitis, a corneal fungal infection of the eye caused mainly by Candida species, has become the leading cause of blindness resulting from corneal disease in China. Present limitations in the management of ophthalmic fungal infections include the inability to provide long-term extraocular drug delivery without compromising intraocular structures and/or systemic drug exposure. OBJECTIVE: The aim of this study was to construct amphotericin B (AmB) loaded, chitosan-modified, nanostructured lipid carriers (AmB-CH-NLC) for prolonged ocular application and for the improvement of the targeted delivery of AmB to the ocular mucosa...
September 7, 2016: Journal of Liposome Research
Hui Zhang, Xuemin Zhu, Jingjing Shen, Haiheng Xu, Min Ma, Wei Gu, Qiudong Jiang, Jun Chen, Jinao Duan
A prerequisite for successful transdermal or dermal drug therapy is the drug ability to penetration through the skin, especially stratum corneum (SC). The most acceptable technique for measuring skin permeation in vitro is the application of both the Franz diffusion cell device and the skin model. As the skin model, a liposome-based artificial skin membrane (LASM) consisting of tight layers of liposomes immobilized on a filter was prepared and characterized. Using porcine ear skin, rat skin and Strat-M(TM) artificial membrane as control, the LASM was then evaluated in permeation studies with five active compounds, i...
August 31, 2016: Journal of Liposome Research
Shery Jacob, Anroop B Nair, Bandar E Al-Dhubiab
Niosomes suggest a versatile vesicle delivery system with possible transport of drugs via topical route for skin delivery. The aim of the present research was to optimize niosome gel formulation of acyclovir and evaluate in both in vitro and in vivo rabbit model. Niosome formulations were formulated by coacervation phase separation technique with different ratios of non-ionic surfactants, phospholipids and cholesterol using 3(2) factorial design. Altering the surfactant concentration has influenced the drug entrapment, but not vesicle size...
August 25, 2016: Journal of Liposome Research
Nikolaos Naziris, Natassa Pippa, Anastasia Meristoudi, Stergios Pispas, Costas Demetzos
The application of stimuli-responsive medical practices has emerged, in which pH-sensitive liposomes figure prominently. This study investigates the impact of the incorporation of different amounts of pH-sensitive polymer, C12H25-PAA (poly(acrylic acid) with a hydrophobic end group) in L-α-phosphatidylcholine, hydrogenated (Soy) (HSPC) phospholipidic bilayers, with respect to biomimicry and functionality. PAA is a poly(carboxylic acid) molecule, classified as a pH-sensitive polymer, whose pH-sensitivity is attributed to its regulative -COOH groups, which are protonated under acidic pH (pKa∼4...
August 25, 2016: Journal of Liposome Research
Yoochan Myung, Seongyeol Yeom, Sanghwa Han
Bilayers prepared from sorbitan fatty acid esters (Span) have been frequently used for delivery of drugs including flavonoids. We applied molecular dynamics simulation to characterize the structure of a sorbitan monostearate (Span 60) bilayer in complex with three representative flavones, a subclass of flavonoids. At a low concentration, unsubstituted flavone, the most hydrophobic member, was able to flip over and cross the bilayer with a large diffusion coefficient. At a high concentration, it was accumulated at the bilayer center resulting in a phase separation...
December 2016: Journal of Liposome Research
Heba F Salem, Rasha M Kharshoum, Lekaa F Abdel Hakim, Mohamed E Abdelrahim
PURPOSE: Voriconazole has both low aqueous solubility and stability. We hypothesize that designing voriconazole in the form of a nano powder inhaler at a geometric diameter within 1-5 μm will enhance its stability and solubility. Therefore, we prepared nanoagglomerates of voriconazole which will collapse in the lungs to reform the nanoparticles. METHOD: The nanoparticles were formulated using both stearic acid and sodium deoxycholate as edge activators. Osmogenic polycation polyethyleneimine (PEI) was used to form agglomerates of controllable size...
December 2016: Journal of Liposome Research
Paola Ringhieri, Alessandra Pannunzio, Angelina Boccarelli, Giancarlo Morelli, Mauro Coluccia, Diego Tesauro
Gynecological tumors are major therapeutic areas of platinum-based anticancer drugs. Here, we report the characterization and in vitro biological assays of cisplatin-containing Egg L-α-phosphatidylcholine liposomes with different amounts of cholesterol. Dynamic light scattering estimated sizes of all obtained liposomes in the 100 nm range that are suitable for in vivo use. On the basis of these data and of the drug loading values, the best formulation has been selected. Stability and drug release properties of platinum-containing liposomes have been verified in serum...
December 2016: Journal of Liposome Research
Ratnesh Mishra, Kedar S Prabhavalkar, Lokesh Kumar Bhatt
CONTEXT: Zaltoprofen, a non-steroidal anti-inflammatory drug, has potent inhibitory action against nociceptive responses. However, gastrointestinal ulcer accompanied with anemia due to the bleeding are most cited side effects associated with it. Due to this, administration of Zaltoprofen is not suitable for individuals with gastric ulcer. Thus, there is unmet need to develop an alternative delivery system that will be easy to administer and can avoid ulcerogenic side effects associated with it...
December 2016: Journal of Liposome Research
Mallesh Kurakula, Osama A A Ahmed, Usama A Fahmy, Tarek A Ahmed
CONTEXT: Avanafil (AVA) is used in the treatment of erectile dysfunction, but is reported for its poor aqueous solubility. Solid lipid nanoparticles (SLNs) are lipid carriers that can greatly enhance drug solubility and bioavailability. OBJECTIVE: This work was aimed to formulate and optimize AVA SLNs with subsequent loading into hydrogel films for AVA transdermal delivery. MATERIALS AND METHODS: AVA SLNs were prepared utilizing homogenization followed by ultra-sonication technique...
December 2016: Journal of Liposome Research
Shivani Rai Paliwal, Rishi Paliwal, Govind Prasad Agrawal, Suresh Prasad Vyas
CONTEXT: Surface-modified pH-sensitive liposomal system may be useful for intracellular delivery of chemotherapeutics. OBJECTIVE: Achieving site-specific targeting with over-expressed hyaluronic acid (HA) receptors along with using pH sensitive liposome carrier for intracellular drug delivery was the aim of this study. MATERIALS AND METHODS: Stealth HA-targeted pH-sensitive liposomes (SL-pH-HA) were developed and evaluated to achieve effective intracellular delivery of doxorubicin (DOX) vis-a-vis enhanced antitumor activity...
December 2016: Journal of Liposome Research
Santosh Shelke, Sadhana Shahi, Sunil Jalalpure, Dinesh Dhamecha
Zolmitriptan is the drug of choice for migraine, but low oral bioavailability (<50%) and recurrence of migraine lead to frequent dosing and increase in associated side effects. Increase in the residence time of drug at the site of drug absorption along with direct nose to brain targeting of zolmitriptan can be a solution to the existing problems. Hence, in the present investigation, thermoreversible intranasal gel of zolmitriptan-loaded nanoethosomes was formulated by using mucoadhesive polymers to increase the residence of the drug into the nasal cavity...
December 2016: Journal of Liposome Research
Helena Ferreira, Raquel Silva, Teresa Matamá, Carla Silva, Andreia C Gomes, Artur Cavaco-Paulo
Chronic wounds usually remain in the inflammatory phase of the healing process during several months or even years. Hence, a continuous research has been resulting in the development of wound dressings with improved performance. Herein, we report a delivery system for cutaneous wound healing, consisting of a textile material (non-woven gauzes) covered with lipidic vesicles containing diclofenac, a non-steroidal anti-inflammatory drug (NSAID). This study also aims to compare the entrapment efficiency data with previous works and confirm that this parameter and drug amount are not directly correlated...
December 2016: Journal of Liposome Research
Michael E Wagner, Katherine A Spoth, Lena F Kourkoutis, Syed S H Rizvi
Niosomes were prepared using a novel supercritical carbon dioxide based method to simultaneously encapsulate ferrous sulfate and vitamin D3 as hydrophilic and hydrophobic cargo, respectively. Vesicle particle size was determined to be bimodal with peak diameters of 1.44 ± 0.16 μm and 7.21 ± 0.64 μm, with the smaller peak comprising 98.8% of the total niosomal volume. Encapsulation efficiency of ferrous sulfate was 25.1 ± 0.2% and encapsulation efficiency of vitamin D3 was 95.9 ± 1...
December 2016: Journal of Liposome Research
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