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Syed Mahmood, Uttam Kumar Mandal, Bappaditya Chatterjee
Raloxifene HCl belongs to a class of selective estrogen receptor modulators (SERMs) which is used for the management of breast cancer. The major problem reported with raloxifene is its poor bioavailability which is only up to 2%. The main objective of the present work was to formulate raloxifene loaded ethosomal preparation for transdermal application and compare it with an oral formulation of the drug. Five ethosomal formulations with different concentrations of ethanol and a conventional liposomes formulation were prepared by rotary evaporation method...
February 28, 2018: International Journal of Pharmaceutics
Bhupinder Kapoor, Reena Gupta, Sachin Kumar Singh, Monica Gulati, Saranjit Singh
With the advent from the laboratory bench to patient bedside in last five decades, vesicular systems have now come to be widely accepted as pragmatic means for controlled delivery of drugs. Their success stories include those of liposomes, niosomes and even the lately developed ethosomes and transferosomes. Pharmacosomes, which, as delivery systems offer numerous advantages and have been widely researched, however, remain largely unacknowledged as a successful delivery system. Though a large number of drugs have been derivatized and formulated into self-assembled vesicular systems, the term pharmacosomes has not been widely used while reporting them...
February 7, 2018: Advances in Colloid and Interface Science
Babar Iqbal, Javed Ali, Sanjula Baboota
Skin is the largest and easily accessible organ of the body. Increases in incidences of dermatological disorders, demand for drug targeting, and patient compliance have increased the popularity of topical drug delivery amongst the people. However, drug delivery across the skin is still a challenge for researchers because permeation of maximum drugs is hindered by the upper layer of the epidermis (stratum corneum). Several approaches like use of chemical permeation enhancers and physical methods such as sonophoresis, iontophoresis, electroporation, microneedles, etc...
February 12, 2018: International Journal of Dermatology
Basant A Habib, Sinar Sayed, Ghada M Elsayed
This study aimed to formulate suitable nanovesicles (NVs) for transdermal delivery of Ondansetron. It also illustrated a practical example for the importance of Box-Cox transformation. A 23 full factorial design was used to enable testing transfersomes, ethosomes, and transethosomes of Ondansetron simultaneously. The independent variables (IVs) studied were sodium taurocholate amount, ethanol volume in hydration medium and sonication time. The studied dependent variables (DVs) were: particle size (PS), zeta potential (ZP) and entrapment efficiency (EE)...
January 30, 2018: European Journal of Pharmaceutical Sciences
Xiao Zheng, Fei Wu, Xiao Lin, Lan Shen, Yi Feng
The bioactive alkaloids (e.g. vincristine, hydroxycamptothecin, ligustrazine, and so on) from traditional Chinese medicine (TCM) have exerted potent efficacies (e.g. anti-tumor, anti-inflammation, immunosuppression, etc.). However, a series of undesirable physicochemical properties (like low solubility and weak stability) and baneful pharmacokinetic (PK) profiles (e.g. low bioavailability, short half time, rapid clearance, etc.) have severely restricted their applications in clinic. In addition, some side effects (like cumulative toxicities caused by high-frequency administration and their own toxicities) have recently been reported and also confined their clinical uses...
November 2018: Drug Delivery
Nauman Rahim Khan, Tin Wui Wong
This study focuses on the use of ethosome and microwave technologies to facilitate skin penetration and/or deposition of 5-fluorouracil in vitro and in vivo. Low ethanol ethosomes were designed and processed by mechanical dispersion technique and had their size, zeta potential, morphology, drug content and encapsulation efficiency characterized. The skin was pre-treated with microwave at 2450 MHz for 2.5 min with ethosomes applied topically and subjected to in vitro and in vivo skin drug permeation as well as retention evaluation...
January 29, 2018: Artificial Cells, Nanomedicine, and Biotechnology
Muhammad Zia Ullah Khan, Shujaat Ali Khan, Muhammad Ubaid, Aamna Shah, Rozina Kousar, Ghulam Murtaza
Androgenetic alopecia, generally recognized as male pattern baldness, is a gradually developing medical and physiological change, which is manifested by continuous hair-loss from scalp. Finasteride (4-aza-3-oxosteroid) is a potent anti-baldness compound that selectively and competitively inhibits the 5α-reductase isoenzymes. Prolonged oral use of finasteride leads to the emergence of sexual disorders including decrease in libido, gynecomastia, erectile dysfunction, ejaculation disorder, orgasm disorders and mood disturbances...
January 23, 2018: Current Drug Delivery
Zhen Zhang, Jun Chen, Jun Huang, Yan Wo, Yixin Zhang, Xiangdong Chen
OBJECTIVE: This study is designed to explore permeability of ethosomes encapsulated with 5-florouracil (5-FU) mediated by CO2 fractional laser on hypertrophic scar tissues. Moreover, therapeutic and duration effect of CO2 fractional laser combined with 5-FU encapsulated ethosomes in rabbit ear hypertrophic scar model will be evaluated. METHODS: The permeated amount of 5-FU and retention contents of 5-FU were both determined by high-performance liquid chromatography (HPLC)...
January 18, 2018: Nanoscale Research Letters
Sanjoy Kumar Das, Soumalya Chakraborty, Chhandita Roy, Rajan Rajabalaya, Amal Widaad Mohaimin, Jasmina Khanam, Arunabha Nanda, Sheba R David
BACKGROUND: In the study of lipid vesicular carriers in permeation enhancement of drug molecules across skin after the success story of liposomes, ethosomes are a recent addition. There are a number of published reviews but still, there is a lack of reviews representing various aspects in a systematic way with a detailed description of current research works. This review serves to fill this deficiency along with a special emphasize on its preparation methods and application. METHODS: Information was collected from previously published literatures which were represented after analysis in terms of various aspects such as principles, composition, preparation, mechanism of penetration, modified forms, characterization, marketed preparation and its application...
January 15, 2018: Current Drug Delivery
Kamla Pathak, Ankur Vaidya, Vijay Sharma
BACKGROUND: Improvisation of the nanosized vesicular systems has led to a series of useful developments including the deformable vesicles namely transfersomes, ethosomes and invasomes. While the former two have been explored extensively, literature on invasomes is relatively scanty. METHOD: Invasomal formulations researched for various applications have been reviewed using search engine "Scopus". The present review focuses on the update on the research activity on effectiveness and permeation enhancing effects of invasomes for dermal and topical delivery...
January 8, 2018: Current Drug Delivery
Zheng Zhang, Yunsheng Chen, Jiayue Ding, Chunlei Zhang, Amin Zhang, Dannong He, Yixin Zhang
Biocompatible 5-aminolevulinic acid/Au nanoparticle-loaded ethosomal vesicle (A/A-ES) is prepared via ultrasonication for synergistic transdermal photodynamic/photothermal therapy (PDT/PTT) of hypertrophic scar (HS). Utilizing ultrasonication, Au nanoparticles (AuNPs) are synthesized and simultaneously loaded in ethosomal vesicles (ES) without any toxic agents, and 5-aminolevulinic acid (ALA) is also loaded in ES with 20% of the entrapment efficiency (EE). The prepared A/A-ES displays strong absorbance in 600-650 nm due to the plasmonic coupling effect between neighboring AuNPs in the same A/A-ES, which can simultaneously stimulate A/A-ES to produce heat and enhance quantum yields of reactive oxygen species (ROS) by using 632 nm laser...
December 15, 2017: Nanoscale Research Letters
Shahira F El-Menshawe, Adel Ahmed Ali, Abdelkhalk Ali Halawa, Ahmed Sg Srag El-Din
Background: Betahistine dihydrochloride (BDH) is a histamine analog used to control weight gain, with short elimination half-life and gastric irritation as side effects. Objective: The aim of the current investigation is to formulate and optimize a topical BDH ethosomal gel for weight gain control. Materials and methods: Box-Behnken design was applied to study the effect of independent variables: phosphatidylcholine (PC), propylene glycol (PG), and ethanol on vesicle size; entrapment efficiency; % drug release; and flux...
2017: Drug Design, Development and Therapy
Keke Li, Shanshan Gao, Baocheng Tian, Yanan Shi, Qingzhi Lv, Jingtian Han
BACKGROUND: Ethosomes, a novel type of percutaneous drug delivery carrier with a lipid bilayer structure, penetrate the skin barrier due to their deformability and malleability, and presence of ethanol that fluidizes lipids in the skin. In order to further enhance the delivery of drugs through the skin, penetration enhancers are widely used. OBJECTIVE: The objective of this work was to develop an optimized formulation of lornoxicam ethosomal gels, investigate skin permeability with the addition of penetration enhancers, and evaluate the in vivo pharmacodynamics of these formulations...
December 7, 2017: Current Drug Delivery
M Sala, R Diab, A Elaissari, H Fessi
During the past decades, lipid nanocarriers are gaining momentum with their multiple advantages for the management of skin diseases. Lipid nanocarriers enable to target the therapeutic payload to deep skin layers or even to reach the blood circulation making them a promising cutting-edge technology. Lipid nanocarriers refer to a large panel of drug delivery systems. Lipid vesicles are the most conventional, known to be able to carry lipophilic and hydrophilic active agents. A variety of lipid vesicles with high flexibility and deformability could be obtained by adjusting their composition; namely ethosomes, transfersomes and penetration enhancer lipid vesicles which achieve the best results in term of skin permeation...
January 15, 2018: International Journal of Pharmaceutics
Emine Kahraman, Sevgi Güngör, Yıldız Özsoy
Nanocarriers used for alternative drug-delivery strategies have gained interest due to improved penetration and delivery of drugs into specific regions of the skin in recent years. Dermal drug delivery via polymeric-based nanocarriers (polymeric nanoparticles, micelles, dendrimers) and lipid-based nanocarriers (solid-lipid nanoparticles and nanostructured lipid carriers, vesicular nanocarriers including liposomes, niosomes, transfersomes and ethosomes) has been widely investigated. Although penetration of nanocarriers through the intact skin could be restricted, these carriers are particularly considered as feasible for the treatment of dermatological diseases in which the skin barrier is disrupted and also for follicular delivery of drugs for management of skin disorders such as acne...
November 2017: Therapeutic Delivery
Amanda C Caritá, Josimar O Eloy, Marlus Chorilli, Robert J Lee, Gislaine Ricci Leonardi
The cutaneous route is attractive for the delivery of drugs in the treatment of a wide variety of diseases. However the stratum corneum (SC) is an effective barrier that hampers skin penetration. Within this context, liposomes emerge as a potential carrier for improving topical delivery of therapeutic agents. In this review, we aimed to discuss key aspects for the topical delivery by drug-loaded liposomes. Phospholipid type and phase transition temperature have been shown to affect liposomal topical delivery...
October 9, 2017: Current Medicinal Chemistry
Tunyaluk Limsuwan, Prapaporn Boonme, Thanaporn Amnuaikit
The high performance liquid chromatography (HPLC) was used for quantitative determination of phenylethyl resorcinol (PR) which was loaded in the novel vesicle carriers including ethosome, invasome and transfersome formulations, and permeated into pig skin membrane and receptor fluid for skin permeation study. The reverse-phase chromatography was carried out with a C18 column (150 × 4.6 mm2, 5 μm, HypersilTM, Thermo Fisher Scientific Inc, USA) with the column temperature at 25°C. A mixture of acetonitrile-methanol-Milli-Q water in the ratio of 40:20:40%, v/v/v was used as a mobile phase by maintaining the flow rate at 0...
November 1, 2017: Journal of Chromatographic Science
Tunyaluk Limsuwan, Prapaporn Boonme, Pasarat Khongkow, Thanaporn Amnuaikit
Ethosome formulations containing phenylethyl resorcinol (PR) were developed. The formulation was produced from 0.5% w/v PR, 0.5% w/v cholesterol from lanolin, 3% w/v L-α-phosphatidylcholine from soybean, 30% v/v absolute ethanol, and water up to 100% v/v. It was characterized by a vesicular size of 389 nm, low polydispersity index of 0.266, zeta potential of -34.19 ± 0.44 mV, high PR entrapment efficiency of 71%, and good stability on storage at 4 and 30°C at 75% RH for 4 months. In vitro studies using pig skin revealed that permeation coefficient of PR from ethosomes was significantly higher than that from liposomes...
2017: BioMed Research International
K Malinovskaja-Gomez, S Espuelas, M J Garrido, J Hirvonen, T Laaksonen
This study was aimed to evaluate the in vitro transdermal direct/pulsed current iontophoretic delivery of an amphiphilic model compound from various lipid vesicle-encapsulated formulations compared to free-drug formulation. Conventional, pegylated, ultradeformable liposomes (transfersomes) and ethosomes loaded with a negatively charged drug diclofenac sodium (DS) were prepared and characterized. All the liposomes possessed an average size of ≈100-150nm and negative zeta potential. No changes in colloidal stability were detected after 8h incubation of any vesicle formulation under constant or pulsed iontophoretic current...
August 30, 2017: European Journal of Pharmaceutical Sciences
Jing Zhao, Yuan Li, Ming-Xin Shi, Xue Wang, Jing-Qing Zhang
OBJECTIVES: To study the oral phamacokinetics of curcumin ethosomes in rats. METHODS: Pharmacokinetics parameters were detected by DAS 2.1.1 software analysis through data of blood concentrations harvested from HPLC after oral administration of curcumin ethosomes in rats. RESULTS: Analyzed by non-compartmental method, the area under concentration-time curve from 0 to last time [AUC(0-72h)] of curcumin ethosomes was 1.6 times larger than that of free curcumin, the peak concentration (C max) of curcumin ethosomes was 1...
March 2017: Sichuan da Xue Xue Bao. Yi Xue Ban, Journal of Sichuan University. Medical Science Edition
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