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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
Zeyu Wu, Tingting Wang, Yonghong Song, Yang Lu, Tianyun Chen, Pengpeng Chen, Ailing Hui, Yan Chen, Haixiang Wang, Wencheng Zhang
The purpose of this study was to optimize the preparation conditions of podophyllotoxin liposomes (PPT-Lips), and to investigate their effects on PC3 cells. PPT-Lips were prepared by using a thin-film dispersion method. In order to achieve maximum drug encapsulation efficiency (EE), the process and formulation variables were optimized by response surface methodology (RSM). The optimum preparation conditions were cholesterol to lecithin ratio of 3.6:40 (w/w), lipid to drug ratio of 15.8:1 (w/w), and the ultrasonic intensity of 35% (total power of 400 W)...
July 19, 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
Rui-Jun Ju, Lan Cheng, Yao Xiao, Xin Wang, Cui-Qing Li, Xiao-Ming Peng, Xue-Tao Li
CONTEXT: Non-small cell lung carcinoma (NSCLC) is a type of epithelial lung cancer that accounts for approximately 80-85% of lung carcinoma cases. Chemotherapy for the NSCLC is unsatisfactory due to multidrug resistance, nonselectively distributions and the accompanying side effects. OBJECTIVE: The objective of this study was to develop a kind of PTD modified paclitaxel anti-resistant liposomes to overcome these chemotherapy limitations. METHOD: The studies were performed on LLT cells and resistant LLT cells in vitro and on NSCLC xenograft mice in vivo, respectively...
September 2018: Journal of Liposome Research
Luciana da Silveira Cavalcante, Donald R Branch, Trang T Duong, Rae S M Yeung, Jason P Acker, Jelena L Holovati
Our in vivo studies on a rat model established safety of transfusing liposome-treated red blood cells (RBCs) but identified the potential for immune modulation as related to transfusion efficacy of liposome-treated RBCs. The aim of this study was at assessing the impact of liposome-induced membrane changes on the immune profile of liposome-treated RBCs by (a) evaluating their interaction with endothelial cells and monocytes; and (b) the resulting immune response derived from this interaction, in the form of cytokine release, adhesion molecules expression and phagocytosis...
September 2018: Journal of Liposome Research
Sushila Rathee, Anjoo Kamboj
Researchers have extensively reviewed on herbs and natural products for their marked clinical efficacy in some recent years, however, maximum of the newly discovered bioactive constituents offer poor bioavailability due to their large size molecules or to their poor miscibility with oils and lipids, thereby limiting their ability to pass across the lipid-rich outer membranes of the enterocytes of the small intestine. Phytosomes are more bioavailable as compared to herbal extracts owing to their enhanced capacity to cross the bio-membranes and thus reaching the systemic circulation...
June 2018: Journal of Liposome Research
Heba F Salem, Rasha M Kharshoum, Abdel Khalek A Halawa, Demiana M Naguib
BACKGROUND: Rosuvastatin (ROS) calcium is the latest synthetic drug in the statin group that has an anti-hyperlipidemic activity. It is available as tablets, and its poor aqueous solubility, slow dissolution rate and low-absorption extent result in less than 20% bioavailability and about 80% being excreted unchanged in the feces without absorption. OBJECTIVE: To utilize nanotechnology to reformulate ROS as a self-nano-emulsifying drug delivery system (SNEDDS), and utilizing design optimization to fabricate the SNEDDS as a tablet...
June 2018: Journal of Liposome Research
Nadia M Morsi, Ahmed A Aboelwafa, Marwa H S Dawoud
Timolol Maleate (TiM), a nonselective β-adrenergic blocker, is a potent highly effective agent for management of hypertension. The drug suffers from poor oral bioavailability (50%) due to its first pass effect and a short elimination half-life of 4 h; resulting in its frequent administration. Transdermal formulation may circumvent these problems in the form of protransfersomes. The aim of this study is to develop and optimize transdermal protransfersomal system of Timolol Maleate by film deposition on carrier method where protransfersomes were converted to transfersomes upon skin hydration following transdermal application under occlusive conditions...
June 2018: Journal of Liposome Research
Diana Guzman-Villanueva, Raymond Q Migrino, Seth Truran, Nina Karamanova, Daniel A Franco, Camelia Burciu, Subhadip Senapati, Dobrin Nedelkov, Parameswaran Hari, Volkmar Weissig
Light chain (AL) amyloidosis is a disease associated with significant morbidity and mortality arising from multi-organ injury induced by amyloidogenic light chain proteins (LC). There is no available treatment to reverse the toxicity of LC. We previously showed that chaperone glycoprotein clusterin (CLU) and nanoliposomes (NL), separately, restore human microvascular endothelial function impaired by LC. In this work, we aim to prepare PEGylated-nanoliposomal clusterin (NL-CLU) formulations that could allow combined benefit against LC while potentially enabling efficient delivery to microvascular tissue, and test efficacy on human arteriole endothelial function...
June 2018: Journal of Liposome Research
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