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Journal of Liposome Research

Meenakumari V, Hideo Utsumi, A Jawahar, A Milton Franklin Benial
In this work, the detailed studies of electron spin resonance (ESR) and Overhauser enhanced magnetic resonance imaging (OMRI) were carried out for permeable nitroxyl spin probe, MC-PROXYL as a function of agent concentration in liposomal solution. In order to compare the impermeable nature of nitroxyl radical, the study was also carried out only at 2mM concentration of carboxy-PROXYL. The ESR parameters were estimated using L- band and 300 MHz ESR spectrometers. The line width broadening was measured as a function of agent concentration in liposomal solution...
November 28, 2016: Journal of Liposome Research
Bianca Sylvester, Alina Porfire, Dana-Maria Muntean, Laurian Vlase, Lavinia Lupuţ, Emilia Licarete, Alina Sesarman, Marius Costel Alupei, Manuela Banciu, Marcela Achim, Ioan Tomuţă
Quality by design principles (QbD) were used to assist the formulation of prednisolone-loaded long-circulating liposomes (LCL-PLP) in order to gain a more comprehensive understanding of the preparation process. This approach enables us to improve the final product quality in terms of liposomal drug concentration, encapsulation efficiency and size, and to minimize preparation variability. A 19-run D-optimal experimental design was used to study the impact of the highest risk factors on PLP liposomal concentration (Y1- μg/ml), encapsulation efficiency (Y2-%) and size (Y3-nm)...
November 16, 2016: Journal of Liposome Research
Nida Akhtar, Anurag Verma, Kamla Pathak
CONTEXT: Atopic dermatitis (AD) is a chronic skin disease characterized by inflammation of the skin and has exhibited remarkable repercussions on human life across the globe. Fluocinolone acetonide (FA), a topical corticosteroid is employed in the treatment of atopic dermatitis, but suffers from limited penetration into deeper epidermis of atopic skin. OBJECTIVE: The present investigation was focused to explore the utility of β-cylcoethosomes in improvising the penetration deep into the skin...
November 16, 2016: Journal of Liposome Research
Mohammad Najlah, Mohit Jain, Ka-Wai Wan, Waqar Ahmed, Mohamed Albed Alhnan, David A Phoenix, Kevin M G Taylor, Abdelbary Elhissi
In this study the anticancer activity of paclitaxel-loaded nano-liposomes on glioma cell lines was investigated. Soya phosphatidylcholine: cholesterol (SPC:Chol), hydrogenated soya phosphatidylcholine: cholesterol (HSPC:Chol) or dipalmitoylphosphatidylcholine: cholesterol (DPPC:Chol) in 1:1 mole ratio were used to prepare ethanol-based proliposomes. Following hydration of proliposomes, the size of resulting vesicles was subsequently reduced to nanometre scale via probe-sonication. The resulting formulations were characterised in terms of size, zeta potential and morphology of the vesicles, and entrapment efficiency of paclitaxel (PX) as well as the final pH of the preparations...
November 11, 2016: Journal of Liposome Research
Therese Klemetsrud, Anna-Lena Kjøniksen, Marianne Hiorth, Jette Jacobsen, Gro Smistad
In this study we investigated the in vitro toxicity, impact on cell permeability and mucoadhesive potential of polymer coated liposomes intended for use in the oral cavity. A TR146 cell line was used as a model. The overall aim was to end up with a selection of safe polymer coated liposomes with promising mucoadhesive properties for drug delivery to the oral cavity. The following polymers were tested: chitosan, low-methoxylated pectin (LM-pectin), high-methoxylated pectin (HM-pectin), amidated pectin (AM-pectin), Eudragit, poly(N-isopropylacrylamide-co-methacrylic acid) (p(NIPAAM-co-MAA)), hydrophobically modified hydroxyethyl cellulose (HM-HEC), and hydrophobically modified ethyl hydroxyethyl cellulose (HM-EHEC)...
November 3, 2016: Journal of Liposome Research
Mona Mahmoud 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...
October 19, 2016: 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
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
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
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