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Current Drug Delivery

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https://www.readbyqxmd.com/read/28606033/tc-99m-radiolabeled-alendronate-sodium-microemulsion-characterization-and-permeability-studies-across-caco-2-cells
#1
Yetkin Elitez, Meliha Ekinci, Derya Ilem-Ozdemir, Evren Gundogdu, Makbule Asikoglu
BACKGROUND: Alendronate sodium (ALD) is used orally but it is poorly absorbed from the gastrointestinal (GI) tract. For this reason, microemulsion system was chosen to evaluate ALD from the GI tract after oral delivery. OBJECTIVE: This study was aimed to prepare water-in-oil (w/o) microemulsion formulation of ALD and evaluate the permeability of ALD microemulsion from Caco-2 cell lines with radioactive and non-radioactive studies. METHOD: The ALD microemulsion was developed by using pseudo-ternary phase diagram and composed of Soybean oil, Colliphor EL, Tween 80, Transcutol and distilled water...
June 12, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28595530/encapsulation-of-solid-dispersion-in-solid-lipid-particles-for-dissolution-enhancement-of-poorly-water-soluble-drug
#2
Khanh Thi My Tran, Toi Van Vo, Phuong Ha-Lien Tran, Beom-Jin Lee, Wei Duan, Thao Truong-Dinh Tran
BACKGROUND: The aim of this research was to engineer solid dispersion lipid particles (SD-SLs) in which a solid dispersion (SD) was encapsulated to form the core of solid lipid particles (SLs), thereby achieving an efficient enhancement in the dissolution of a poorly water-soluble drug. METHODS: Ultrasonication was introduced into the process to obtain micro/nanoscale SLs. The mechanism of dissolution enhancement was investigated by analysing the crystalline structure, molecular interactions, and particle size of the formulations...
June 5, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28595529/development-and-optimization-by-quality-by-design-strategies-of-frovatriptan-orally-disintegrating-tablets-for-migraine-management
#3
Natascia Mennini, Serena Orlandini, Sandra Furlanetto, Benedetta Pasquini, Paola Mura
BACKGROUND: Frovatriptan is a potent anti-migraine agent with unfavourable slow onset of action, available on the market as film-coated tablets. OBJECTIVE: optimization, by Quality by Designs strategies, of an orally disintegrating tablet (ODT) formulation of frovatriptan aimed to make its oral administration easier and its dissolution faster than the commercial tablets, thus improving its effectiveness in migraine management. METHOD: A screening D-optimal design was applied to investigate the effects of different levels of kind and amount of ODT special excipient and disintegrant agents (identified as the critical variables) on disintegration time (DT) and % drug dissolved at 30 s (%Diss), selected as the responses to optimize...
June 5, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28571542/folic-acid-targeted-polymeric-micelles-based-on-tocopherol-succinate-pulluan-as-an-effective-carrier-for-epirubicin-preparation-characterization-and-in-vitro-cytotoxicity-assessment
#4
Farshid Hassanzadeh, Mozhdeh Mehdifar, Jaleh Varshosaz, Ghadam Ali Khodarahmi, Mahboubeh Rostami
BACKGROUND: Chemotherapy still encounters a serious drawback, the lack of selectivity of anticancer drugs toward neoplastic cells, thus, the normal cells are affected by the cytotoxic action of the drugs. This causes a narrow therapeutic index in most anticancer drugs. OBJECTIVE: We describe here the preparation of pullulan-tocopherol succinate-folic acid (Pu-TS-FA) micelles for the first time to targeted delivery of epirubicin (EPI) to Hela and MCF-7 cell lines...
June 1, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28571541/investigation-of-methylene-blue-release-from-functional-polymeric-systems-using-dielectric-analysis
#5
Marcos Luciano Bruschi, Mariana Volpato Junqueira, Fernanda Belincanta Borghi-Pangoni, Tao Yu, Gavin Paul Andrews, David Simon Jones
BACKGROUND: Methylene blue (MB) is a photosensitizer used in photodynamic therapy (PDT) to treat colorectal cancer tumors and leishmaniasis infection. The clinical efficacy of PDT using MB is dependent on the physicochemical characteristics of the formulation. Bioadhesive thermoresponsive systems containing poloxamer 407 and Carbopol 934P have been proposed as platforms for PDT. However, the effect of MB on the physicochemical properties of these platforms is not fully understood, particularly in light of the MB availability...
June 1, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28545355/emerging-trends-on-drug-delivery-strategy-of-momordica-charantia-against-diabetes-and-its-complications
#6
Zar Chi Thent, Srijit Das, Nurul Hannim Zaidun
The incidence of diabetes mellitus has increased drastically over the past few decades. This oxidant-antioxidant imbalance resulting in complication of diabetes mellitus includes macro- and microvascular complications. Resistance to conventional treatment and patient compliance has paved the way to the usage of effective natural products and supplements. Momordica charantia (bitter gourd) is widely consumed in many parts of Malaysia as a vegetable. Momordica charantia (MC) is mainly used in the management of diabetes mellitus...
May 25, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28545354/solid-lipid-nanoparticles-approach-for-lymphatic-targeting-through-intraduodenal-delivery-of-quetiapine-fumarate
#7
Mohd Yasir, Praveen Kumar Gaur, Dinesh Puri, Preeti Shekar, S Sadish Kumar
BACKGROUND: Lymphatic route is one of the prominent route for improving the poor bioavailability of the drugs which undergoes extensive hepatic first pass metabolism. Nanocarriers (solid lipid nanoparticles) offers a new drug delivery system that could hold great promise for attaining the bioavailability enhancement along with controlled and site specific drug delivery. OBJECTIVE: The aim of the present research work was to prepare and optimized the Quetiapine fumarate (an antipsychotic drug) loaded solid lipid nanoparticles for lymphatic targeting through intraduodenal administration Method: Thirteen quetiapine fumarate loaded solid lipid nanoparticle formulations were developed using different lipids by Microemulsion technique and optimized by box behnken design...
May 25, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28521675/chemotherapy-with-si-rna-and-anti-cancer-drugs
#8
Kamaljeet Kaur, Goutam Rath, Saket Chandra, Ranjit Singh, Amit K Goyal
To treat cancer, chemotherapy is a key therapeutic approach which is associated with several limitations. This chemotherapeutical agents exhibit multi drug resistance coupled with undesirable side effects. This multidrug resistance is exhibited by tumor cell due to actuation of drug out flow mechanism, programmed cell death and protection mechanisms etc. One of the therapeutic approaches to cure cancer is RNA interference (RNAi). Small interfering RNA (si-RNA) is considered as a major therapeutic tool used to control expression of a particular gene...
May 18, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28521674/sorbitane-monostearate-and-cholesterol-based-niosomes-for-oral-delivery-of-telmisartan-from-bench-to-preclinical-implementation-in-wistar-albino-rats
#9
Abdul Ahad, Mohammad Raish, Fahad I Al-Jenoobi, Abdullah M Al-Mohizea
BACKGROUND: Niosomes are non-ionic surfactant vesicles used as drug carriers for encapsulating both hydrophobic and hydrophilic drugs. The aim of the present study was to prepare and characterize niosomes formulations for oral delivery of telmisartan and evaluated for its antihypertensive activity. METHOD: Telmisartan loaded niosomes were prepared using thin film hydration method by varying the Span 60 and cholesterol at several molar ratios and characterized for vesicles size, polydispersity index, zeta potential, entrapment efficiency...
May 18, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28521673/simple-strategy-to-protect-lactase-activity-in-solid-formulation
#10
Aline Gravinez Perissinato, André Luis Morais Ruela, Gislaine Ribeiro Pereira, Jerusa Simone Garcia, Marcello Garcia Trevisan
Lactose intolerance is characterized by the absence of the enzyme lactase (beta-galactosidase) and affects two thirds of the world adult population. Our aim was to evaluate a lactase gastro formulation to ensure increased activity in the action site of the enzyme (lumen of the small intestine). Simultaneously, we also evaluated the commercial product stability and enzyme activity. When carrying out dissolution test in commercial product it is noted that the existing formulation is not able to protect the enzyme from degrading action of gastric environment (a loss of 86...
May 18, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28521697/an-accelerated-release-method-of-risperidone-loaded-plga-microspheres-with-good-ivivc
#11
Hu Xiaoqin, Jianwei Zhang, Xuemei Tang, Mingyuan Li, Siyu Ma, Cheng Liu, Gao Yue, Yue Zhang, Yan Liu, Fanglin Yu, Yang Yang, Guo Jia, Zhiping Li, Xingguo Mei
The purpose of this study was to obtain an accelerated release method of risperidone loaded poly(lactic-co-glycolic acid) (PLGA) microspheres with good in vitro/in vivo correlation (IVIVC). Two formulations of risperidone loaded PLGA microspheres used for evaluating IVIVC were prepared by O/W method. The accelerated release condition was optimized by investigating the effect of pH, osmotic pressure, temperature and ethanol concentration on the release of risperidone from microspheres and the in vitro accelerated release profiles of risperidone from PLGA microspheres were obtained under this optimized accelerated release condition...
May 15, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28521696/nanotechnology-as-a-promising-strategy-for-anticancer-drug-delivery
#12
Mona Basha
Cancer was and still a very stressful and urgent disease condition representing a leading cause of death in developed as well as developing countries. Although, much research work in both medical and pharmaceutical fields has evolved in the past few years in addition to some promising clinical trials and few market products, cancer becomes much wilder, threatening and getting more lives. Most approaches have focused on the synthesis of new active ingredients or chemical modification of available ones, formulating them in suitable dosage forms aiming for targeted and effective drug delivery with minimal side effects...
May 15, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28482784/recent-advancemnts-in-biodegradable-ocular-implants
#13
Oshin Miranda, Swati Mittal
The perpetuation of healthy vision is paramount in an individual. It has been observed that various drug delivery systems are been fabricated to develop vision quality in individuals. Systemic ocular drug therapies have limited efficacy due to poor bioavailability, systemic and toxic side effects and low patient compliance. Various drug systems which follow the ocular route of administration are manufactured to achieve optimized bioavailability along with better patient compliance. Ocular implants is one such example...
May 7, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28472909/impact-of-surfactants-on-skin-penetration-of-dexpanthenol
#14
Flavia Laffleur, Stefan Pschick, Jan Barthelmes, Sabine Hauptstein, Andreas Bernkop-Schnürch
OBJECTIVE: It was the aim of this study to evaluate the impact of nonionic and ionic surfactants on skin penetration of dexpanthenol. METHODS: The relative potency of three surfactants (two nonionic and one ionic) as enhancers in the permeability of a series of compounds was investigated. The influence of the enhancers was also studied. For this purpose porcine abdominal skin was prepared and mounted on Franz diffusion cells, while different mixtures of Dexpanthenol containing Tween®85, SDS and Span®80 in concentrations of 0...
May 3, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28472908/targeted-nanostructured-lipid-carriers-for-delivery-of-paclitaxel-to-cancer-cells-preparation-characterization-and-cell-toxicity
#15
Mahboubeh Rezazadeh, Jaber Emami, Farshid Hassanzadeh, Hojjat Sadeghi, Mahboubeh Rostami, Hamid Mohammadkhani
Low water solubility, high systemic toxicity and insignificant cellular uptake has limited efficient clinical applications of the anti-tumor agent paclitaxel (PTX). To overcome these limitations, a novel nanostructured lipid carrier (NLC) modified with folic acid (FA) and polyethylene glycol (PEG) was prepared by emulsion solvent evaporation method using cholesterol, α-tocopherol, lecithin and Poloxamer. A partial factorial design was applied to determine the appropriate levels of variables for optimized formulation...
May 3, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28425869/development-of-a-chitosan-based-nanoparticle-formulation-for-ophthalmic-delivery-of-honokiol
#16
Feng Deng, Wenjing Hu, Huali Chen, Yalan Tang, Liangke Zhang
In this study, honokiol-loaded chitosan/sulfobutylether-β-cyclodextrin nanoparticles (HK-CS-NPs) were prepared for ophthalmic drug delivery systems. An inclusion complex of honokiol and sulfobutylether-β-cyclodextrin was used to generate large amounts of insoluble honokiol to be incorporated into chitosan nanoparticles, which were prepared through ionotropic gelation. HK-CS-NPs featured a spherical surface with a narrow size distribution of polydispersity index less than 0.250, a mean size range of 373-523 nm, a positive surface charge of +19...
April 19, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28578642/studies-on-solubility-enhancement-of-poorly-soluble-nsaid-by-dual-approach-of-melt-granulation-and-micro-environmental-ph-modulation
#17
Abhijeet Kadam, Namita D Desai
The present work describes the role of melt granulation and microenvironmental pH modulation technique in solubility enhancement of a poorly water soluble NSAID, Aceclofenac (ACL). ACL is a BCS Class II drug showing dissolution rate limited absorption and pH dependent solubility, with higher solubility at alkaline pH. The limited solubility of ACL affects drug absorption and hence, therapeutic effect as the drug is indicated in conditions of pain where rapid onset of action is desired. Solubility enhancement of ACL was carried out by melt granulation technique using Gelucire 50/13 as molten carrier...
April 13, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28530536/leuprolide-acetate-release-study-from-%C3%AE-irradiated-plga-based-in-situ-forming-system
#18
Mona Shapourgan, Hamid Mobedi, Nasrin Sheikh, Aliasghar Behnamghader, Arezou Mashak
It is well known that the properties of polymers can be altered by exposure to γ- ray. γ-irradiation has been used as a sterilization method for biodegradable polymeric drug delivery devices, and its drug release profile must not be significantly changed. In this study, the effect of γ-irradiation with 8 kGy doses on the release profile of leuprolide acetate from PLGA-based in situ forming system was evaluated. PLGA-based in situ forming systems were prepared by injecting some specific amount of irradiated solution of PLGA /NMP containing drug into a buffer phosphate pH 7...
March 28, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28322165/anti-inflammatory-and-anti-arthritic-activity-of-different-milk-based-formulation-of-curcumin-in-rat-model
#19
Sumeet Gupta
Inflammation is the key mediator for arthritis. Plant based products are most useful for treating various disorders, but at the same time drug absorbtion is utmost important for effective therapy. The aim of the study was to find out the therapeutic concern in pharmacokinetic and pharmacodynamic parameters in an arthritis induced rat model. Carrageenan and complete Freud's adjuvant, both were used for an arthritis induction as an animal model. Five different formulations of curcumin were prepared in single toned milk, double toned milk, full fat milk, full fat milk with ghee and in an aqueous suspension...
March 20, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28322164/solubilization-and-enhancement-of-ex-vivo-vaginal-delivery-of-progesterone-using-solid-dispersions-inclusion-complexes-and-micellar-solubilization
#20
Abeer S Hassan, Ghareb M Soliman, Mona M El-Mahdy, Gamal El-Din A El-Gindy
Progesterone (PG), a natural female sex hormone is used clinically in menopausal hormone replacement therapy and to control reproductive functions. Its very limited aqueous solubility of 7 µg/ml results in reduced oral bioavailability and low patient compliance when administered in high doses. The aim of this study was to enhance PG aqueous solubility and vaginal delivery using solid dispersion, inclusion complex and micellar solubilization techniques. PG solid dispersions and inclusion complexes were prepared by solvent evaporation method using different polymers, such as cyclodextrins, polyvinyl pyrrolidone (PVP), poly (ethylene glycol) 6000, Pluronic® F-127 and Pluronic® F-68...
March 20, 2017: Current Drug Delivery
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