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International Journal of Pharmaceutics

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https://www.readbyqxmd.com/read/29138048/in-vitro-and-in-vivo-cytotoxicity-and-efficacy-evaluation-of-novel-glycyl-glycine-and-alanyl-alanine-conjugates-of-chitosan-and-trimethyl-chitosan-nano-particles-as-carriers-for-oral-insulin-delivery
#1
Nersi Jafary Omid, Nika Bahari Javan, Ahmad-Reza Dehpour, Alireza Partoazar, Morteza Rafiee Tehrani, Farid Dorkoosh
PURPOSE: The aim of this research work was to explore the possibility of providing multifunctional oral insulin delivery system by conjugating several types of dipeptides on chitosan and trimethyl chitosan to be used as drug carriers. METHOD: Conjugates of Glycyl-glycine and alanyl-alanine of chitosan and trimethyl chitosan (on primary alcohol group of polymer located on carbon 6) were synthesized and nanoparticles containing insulin were prepared for oral delivery...
November 11, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29138047/antibacterial-effect-and-dna-delivery-using-a-combination-of-an-arsonium-containing-lipophosphoramide-with-an-n-heterocyclic-carbene-silver-complex-potential-benefits-for-cystic-fibrosis-lung-gene-therapy
#2
Angélique Mottais, Mathieu Berchel, Yann Sibiril, Véronique Laurent, Deborah Gill, Stephen Hyde, Paul-Alain Jaffrès, Tristan Montier, Tony Le Gall
Cystic Fibrosis (CF), the most common chronic genetic disorder among the Caucasian population, is a life-threatening disease mainly due to respiratory failures resulting from chronic infections and inflammation. Although research in the pharmacological field has recently made significant progress, gene therapy still remains a promising strategy to cure CF, especially because it should be applicable to any patient whatever the mutation profile. Until now, little attention has been paid to bacterial lung infections with regard to gene delivery to the airways; yet, this could greatly impact on the success of gene therapy...
November 11, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29138046/novel-cremochylomicrons-for-improved-oral-bioavailability-of-the-antineoplastic-phytomedicine-berberine-chloride-optimization-and-pharmacokinetics
#3
Manal A Elsheikh, Yosra S R Elnaggar, Dalia A Hamdy, Ossama Y Abdallah
Berberine chloride (BER) is an antineoplastic phytomedicine that combat non-Hodgkin lymphoma. BER suffers from low oral bioavailability due to P-glycoprotein efflux and first-pass metabolism. Lymphatic drug targeting recently gained a profound attention due to circumventing hepatic first-pass metabolism and targeting lymph diseases. Therefore, novel BER-loaded cremochylomicrons were elaborated to mitigate BER drawbacks and enhance its lymphatic targeting and bioavailability. Optimized cremochylomicron was prepared with 2...
November 11, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29138045/cyclodextrins-structure-physicochemical-properties-and-pharmaceutical-applications
#4
Phatsawee Jansook, Noriko Ogawa, Thorsteinn Loftsson
Since their discovery over 100 years ago cyclodextrins (CDs) have been the subject of numerous scientific publications. In 2016 alone CDs were the subject of over 2200 research articles published in peer-reviewed journals and mentioned in over 2300 patents and patent applications, many of which were on pharmaceutical applications. Natural CDs and their derivatives are used as enabling pharmaceutical excipients that enhance aqueous solubility of poorly soluble drugs, increase drug permeability through biological membranes and improve drug bioavailability...
November 11, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29104056/taste-evaluation-of-a-novel-midazolam-tablet-for-pediatric-patients-in-vitro-drug-dissolution-in-vivo-animal-taste-aversion-and-clinical-taste-perception-profiles
#5
Laurence C Cheung, Minh Nguyen, Edith Tang, Britta S von Ungern Sternberg, Sam Salman, Catherine Tuleu, Abeer H A Mohamed Ahmed, Jessica Soto, Lee Yong Lim
Harmonized methodologies are urgently required for the taste evaluation of novel pediatric medicines. This study utilized in vitro, in vivo and clinical data to evaluate the palatability of a novel midazolam chocolate tablet. In vitro dissolution experiments showed the crushed tablet to release within 5 min 1.68 mg of midazolam into simulated saliva. This translated to a drug level of 0.84 mg/ml in the oral cavity, which would be higher than the midazolam bitterness detection threshold concentration of 0...
November 11, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29133207/oral-hepatitis-b-vaccine-chitosan-or-glucan-based-delivery-systems-for-efficient-hbsag-immunization-following-subcutaneous-priming
#6
Edna Soares, Sandra Jesus, Olga Borges
The World Health Organization encourages "the development of oral formulations to simplify their transport, storage and administration in poor countries", and to "facilitate an effective immunization program to prevent sexually transmitted hepatitis B". Thus, two distinct and promising delivery systems were developed: recombinant hepatitis B surface antigen (HBsAg) encapsulated into alginate-coated chitosan particles (AlgChiPs) and into glucan particles (GPs) mainly composed of β-1,3-D-glucan. In vitro preliminary studies showed that both could be internalized by peripheral blood mononuclear cells and murine Peyer's patches, an imperative aspect regarding oral immunization...
November 10, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29133206/relationship-between-polarities-of-antibiotic-and-polymer-matrix-on-nanoparticle-formulations-based-on-aliphatic-polyesters
#7
J A S Ritsema, E M A Herschberg, S E Borgos, C Løvmo, R Schmid, Y M Te Welscher, G Storm, C F van Nostrum
In the field of nanomedicine, nanoparticles are developed to target antibiotics to sites of bacterial infection thus enabling adequate drug exposure and decrease development of resistant bacteria. In the present study, we investigated the encapsulation of two antibiotics with different polarity into different PEGylated polymeric nanoparticles based on aliphatic polyesters, to obtain a better understanding of critical factors determining encapsulation and release. The nanoparticles were prepared from diblock copolymers comprising of a poly(ethylene glycol) block attached to an aliphatic polyester block of varying polarity: poly(lactic-co-glycolic acid) (mPEG-PLGA), poly(lactic-co-hydroxymethyl glycolic acid) (mPEG-PLHMGA) and poly(lactic-co-benzyloxymethyl glycolic acid) (mPEG-PLBMGA)...
November 10, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29133205/hpma-copolymer-conjugate-with-pirarubicin-in-vitro-and-ex-vivo-stability-and-drug-release-study
#8
Waliul Islam, Jun Fang, Tomas Etrych, Petr Chytil, Karel Ulbrich, Akihiro Sakoguchi, Katsuki Kusakabe, Hiroshi Maeda
We have developed a tumor environment-responsive polymeric anticancer prodrug containing pirarubicin (THP) conjugated to N-(2-hydroxypropyl) methacrylamide copolymer (PHPMA), [P-THP], through a spacer containing pH-sensitive hydrazone bond, that showed remarkable therapeutic effect against various tumor models and in a human pilot study. Toward clinical development, here we report THP release profile from its HPMA copolymer conjugate, the conjugate stability, protein and cell-binding and solubility of P-THP...
November 10, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29133204/investigating-phase-separation-in-amorphous-solid-dispersions-via-raman-mapping
#9
Christian Luebbert, Christian Klanke, Gabriele Sadowski
The bioavailability of poorly-water-soluble active pharmaceutical ingredients (APIs) can be significantly improved by so-called amorphous solid dispersions (ASDs). However, the long-term stability of ASDs might be impaired by API recrystallization and/or amorphous phase separation (APS). So far, no methods have been reported to quantify APS in ASDs. In this work, phase-separation kinetics as well as the compositions of the two amorphous phases evolving due to APS were quantitatively determined for the first time using confocal Raman spectroscopy...
November 10, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29129572/biocompatible-fluorinated-poly-%C3%AE-amino-ester-s-for-safe-and-efficient-gene-therapy
#10
Jia-Hui Gong, Yi Wang, Lei Xing, Peng-Fei Cui, Jian-Bin Qiao, Yu-Jing He, Hu-Lin Jiang
Cationic polymers have been widely used as one of the most promising non-viral vehicles for gene delivery due to their potential safety and ease of large-scale production. Here, we report the design and synthesis of a series of novel biodegradable fluorinated poly(β-amino ester)s (FPBAEs) by simple Michael-addition reaction as safe and efficient gene carrier. The results of transfection efficacy assay demonstrated the optimal FPBAE could mediated much higher GFP expression than the commercial transfection agents, polyethyleneimine (PEI, Mw = 25K) and Lipo 2000, as well as the non-fluorinated poly(β-amino ester)s (PBAE) on both HeLa and HEK-293T cell lines (higher than 70 and 90%, respectively), which was largely attributed to fluorination...
November 10, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29129573/3d-printed-uv-light-cured-polydimethylsiloxane-devices-for-drug-delivery
#11
Jenny Holländer, Risto Hakala, Jaakko Suominen, Niko Moritz, Jouko Yliruusi, Niklas Sandler
The goal of this work was to study the printability of PDMS with a semi-solid extrusion printer in combination with the UV-assisted crosslinking technology using UV-LED light to manufacture drug containing structures. Structures with different pore sizes and different drug loadings were prepared containing prednisolone as a model drug. The work showed that it was possible to print drug-free and drug-loaded drug delivery devices of PDMS with the 3D printing technique used in this study. The required UV-curing time to get sufficient crosslinking yield and mechanical strength was minimum three minutes...
November 9, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29128423/amorphous-solid-dispersions-and-nanocrystal-technologies-for-poorly-water-soluble-drug-delivery-an-update
#12
Scott V Jermain, Chris Brough, Robert O Williams
Poor water-solubility remains a typical property of drug candidates in pharmaceutical development pipelines today. Various processes have been developed to increase the solubility, dissolution rate, and bioavailability of these active ingredients belonging to biopharmaceutical classification system (BCS) II and IV classifications. Since the early 2000s, nanocrystal delivery and amorphous solid dispersions are more established techniques to overcome the limitations of poorly-water soluble drugs in FDA available products...
November 8, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29128422/ampholytic-starch-excipients-for-high-loaded-drug-formulations-mechanistic-insights
#13
Khalil Sakeer, Pompilia Ispas-Szabo, Nassim Benyerbah, Mircea Alexandru Mateescu
Ampholytic starch derivatives are proposed as a new class of excipients carrying simultaneously anionic carboxymethyl (CM) and cationic aminoethyl (AE) groups on starch (St) polymeric chains. Three different types of derivatives were obtained by using the same reagents and varying only the order of their addition in the reaction medium: in one step method (OS) the two reactants were added simultaneously, whereas in two steps method (TS) either CMSt or AESt were prepared separately in the first step, followed by subsequent addition of the second reactant...
November 8, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29104057/high-payload-nanostructured-lipid-carriers-fabricated-with-alendronate-polyethyleneimine-ion-complexes
#14
Basma N Abd El-Hamid, Nitin K Swarnakar, Ghareb M Soliman, Mohamed A Attia, Giovanni M Pauletti
Oral bioavailability of the anti-osteoporotic drug alendronate (AL) is limited to ≤ 1% due to unfavorable physicochemical properties. To augment absorption across the gastrointestinal mucosa, an ion pair complex between AL and polyethyleneimine (PEI) was formed and incorporated into nanostructured lipid carriers (NLCs) using a modified solvent injection method. When compared to free AL, ion pairing with PEI increased drug encapsulation efficiency in NLCs from 10% to 87%. Drug release from NLCs measured in vitro using fasted state simulated intestinal fluid, pH 6...
November 8, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29126908/a-novel-formulation-of-6-gingerol-proliposomes-with-enhanced-oral-bioavailability-and-antitumor-effect
#15
Qilong Wang, Qiuyu Wei, Qiuxuan Yang, Xia Cao, Qiang Li, Feng Shi, ShanShan Tong, Chunlai Feng, Qingtong Yu, Jiangnan Yu, Ximing Xu
[6]-Gingerol, one of the components of the rhizome of Ginger, has a variety of biological activities such as anticoagulant, antioxidative, antitumor, anti-inflammatory, antihypertensive, and so forth. However, as one of the homologous phenolic ketones, [6]-gingerol is insoluble in water which limits its applications. Herein, we prepared [6]-gingerol proliposomes through modified thin-film dispersion method, which was spherical or oval, and physicochemically stable with narrow size distribution. Surprisingly, in vitro release of [6]-gingerol loaded proliposome compared with the free [6]-gingerol was significantly higher and its oral bioavailability increased 5-fold in vivo...
November 7, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29126907/influence-of-cholesterol-inclusion-on-the-doxorubicin-release-characteristics-of-lysolipid-based-thermosensitive-liposomes
#16
Negar Sadeghi, Roel Deckers, Burcin Ozbakir, Sohail Akthar, Robbert Jan Kok, Twan Lammers, Gert Storm
Fast hyperthermia (i.e. 39-42 °C) triggered doxorubicin release from lysolipid-containing thermosensitive liposomes (LTSL) in the tumor vasculature has been demonstrated to result in considerable enhancement of bioavailable drug levels in heated tumor tissue in preclinical tumor models. However, there is also significant leakage of doxorubicin already at 37 °C in the bloodstream, making these LTSL less efficient and increasing the risk for systemic toxicity. In conventional liposomes, cholesterol is incorporated in the bilayer to increase the stability of the liposomes...
November 7, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29126906/development-and-characterization-of-an-organic-solvent-free-proliposomal-formulation-of-busulfan-using-quality-by-design-approach
#17
Dhawal Chobisa, Ketan Patel, Jasmin Monpara, Mayank Patel, Pradeep Vavia
Parenteral administration of Busulfan (BU) conquers the bioavailability and biovariability related issues of oral BU by maintaining the plasma drug concentration in therapeutic range with minimal fluctuations thereby significantly reducing the side effects. Busulfex(®) is the only commercially available parenteral formulation of BU composed of organic solvents N, N-dimethylacetamide and polyethylene glycol 400. Since, BU is highly susceptible to hydrolytic degradation; Busulfex(®) has poor physical and chemical stability in IV fluids...
November 7, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29126905/failure-of-active-targeting-by-a-cholesterol-anchored-ligand-and-improvement-by-altering-the-lipid-composition-to-prevent-ligand-desorption
#18
Shoshiro Yamamoto, Yu Sakurai, Hideyoshi Harashima
Although anti-angiogenic therapy is predicted to be an effective therapy for treating cancer, selectively targeting tumor endothelial cells (TECs), and not normal endothelial cells, remains a major obstacle. Modifying a drug carrier with a targeting ligand is a popular strategy for developing an active-targeting type drug delivery system (DDS). We previously reported that a cyclo(Arg-Gly-Asp-D-Phe-Lys) (cRGD)-equipped liposome that contains encapsulated siRNA (RGD-MEND) achieved an efficient therapeutic outcome in a murine cancer model...
November 7, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29126904/enhancement-of-tioconazole-ungual-delivery-combining-nanocapsule-formulation-and-nail-poration-approaches
#19
Fernanda C Flores, Wing Sin Chiu, Ruy C R Beck, Cristiane B da Silva, M Begoña Delgado-Charro
This work investigated the impact of formulation including in vitro release profile, repeated dosing, and nail poration on the ex vivo nail delivery performance of antifungal formulations. Chitosan coated and uncoated tioconazole-loaded nanocapsules and a nano-based film-forming vehicle were assessed via in vitro release and in vitro permeation tests using an artificial membrane and human nail clippings, respectively. The later involved single and daily dosing experiments with intact and porated nails. Additional experiments with Nile Red-loaded formulations evaluated the depth of penetration of the fluorescent marker into the nail by laser scanning confocal microscopy...
November 7, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29104058/ionic-liquid-microemulsions-assisting-in-the-transdermal-delivery-of-dencichine-preparation-in-vitro-and-in-vivo-evaluations-and-investigation-of-the-permeation-mechanism
#20
Chengxiao Wang, Junxiao Zhu, Ding Zhang, Ye Yang, Luyao Zheng, Yuan Qu, Xiaoyan Yang, Xiuming Cui
A novel microemulsion was developed and characterized for topical delivery of Dencichine (Den). Two imidazaolium ionic liquid, 1-hydroxyethyl-3-methylimidazolium chloride ([HOEIM]Cl) and 1-butyl-3-methylimidazolium dodecanesulfate ([BMIM]C12SO3) were incorporated into the aqueous and surfactant phases respectively for the remarkable enhancement on skin permeation. The nano-carrier was developed and optimized based on a pseudo-ternary phase diagram. The optimized formulation was composed of 50% water/[HOEIM]Cl mix (1:1) as water phase, 20% Tween 80/[BMIM]C12SO3 mix (1:1) as surfactant, 10% propylene glycol as co-surfactant and 20% IPM as oil phase...
November 7, 2017: International Journal of Pharmaceutics
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