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Current Drug Delivery

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https://www.readbyqxmd.com/read/29219057/formulation-optimization-and-in-vitro-and-in-vivo-evaluation-of-lornoxicam-ethosomal-gels-with-penetration-enhancers
#1
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
https://www.readbyqxmd.com/read/29219056/in-vitro-and-in-vivo-pharmacokinetic-evaluation-of-guar-gum-eudragit%C3%A2-s100-based-colon-targeted-spheroids-of-sulfasalazine-co-administered-with-probiotics
#2
Abhinav Sharma, Bimlesh Kumar, Sachin Kumar Singh, Monica Gulati, Yogyata Vaidya, Manik Sadotra, Harish Rathee, Deepak Ghai, Adil Hussain Malik, Ankit Kumar Yadav, Peddi Maharshi, Palak Bawa, Sarvi Yadav Rajesh, Parth Sharma, Narendra Kumar Pandey, Souvik Mohant
Polysaccharide based delivery systems have been successfully used to target drugs to colon. In some recent reports, the superiority of concomitant administration of probiotics with such systems has been established. However, the pharmacokinetics of such symbiotic therapy remain unexplored hitherto. This study deciphers the pharmacokinetic parameters of guar gum based colon targeted spheroids of sulfasalazine with co-administration of probiotics in experimental rats. Thirty rats were divided into five groups using Latin square design...
December 7, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/29219055/the-role-of-nanoparticles-in-the-inhibition-of-multidrug-resistant-bacteria-and-biofilms
#3
Manaf AlMatar, Essam A Makky, Isil Var, Fatih Koksal
BACKGROUND: Until recently, one of the main reasons for mortality has been infectious diseases, and bacteria that are drug-resistant have emerged as a result of the wide application, as well as the misuse, of antibacterial medications. Having multidrug-resistance, bacteria present a great problem for the efficient management of bacterial infections and this challenge has resulted in the creation of other means of dealing with bacterial diseases. Of late, metallic nanoparticles (NPs), employed as antibacterial agents, have the potential for use against resistance to bacterial drugs...
December 7, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/29189154/brain-targeted-intranasal-zaleplon-nano-emulsion-in-vitro-characterization-and-assessment-of-gamma-aminobutyric-acid-levels-in-rabbits-brain-and-plasma-at-low-and-high-doses
#4
Eman Abd-Elrasheed, Sara Nageeb El-Helaly, Manal M El-Ashmoony, Salwa Salah
BACKGROUND: Zaleplon is a pyrazolopyrimidin derivative hypnotic drug indicated for the short-term management of insomnia. Zaleplon belongs to Class II drugs, according to the biopharmaceutical classification system (BCS), showing poor solubility and high permeability. It undergoes extensive first-pass hepatic metabolism after oral absorption, with only 30% of Zaleplon being systemically available. It is available in tablet form which is unable to overcome the previous problems. OBJECTIVE: The aim of this study is to enhance solubility and bioavailability via utilizing nanotechnology in the formulation of intranasal Zaleplon nano-emulsion (ZP-NE) to bypass the barriers and deliver an effective therapy to the brain...
November 30, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/29189155/fabrication-and-characterization-of-timolol-maleate-and-brinzolamide-loaded-nanostructured-lipid-carrier-system-for-ocular-drug-delivery
#5
Nupur Shrivastava, Saba Khan, Sanjula Baboota, Javed Ali
BACKGROUND: The combination of timolol maleate (TM) and brinzolamide (BRZ) has potential therapeutic prospects for treating glaucoma. However, the conventional formulation of TM and BRZ exhibits sub optimal therapeutic effects attributable to the poor ocular bioavailability of these drugs. OBJECTIVE: Therefore, the aim of the present study was to design and evaluate TM and BRZ loaded nanostructured lipid carrier (NLC) to enhance the bioavailabilities, permeation and precorneal residence time of these drugs that would result in efficacious treatment of glaucoma...
November 29, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/29189153/antiviral-effects-of-saffron-and-its-major-ingredients
#6
Sepehr Soleymani, Rezvan Zabihollahi, Sepideh Shahbazi, Azam Bolhassani
The lack of an effective vaccine against viral infections, toxicity of the synthetic anti-viral drugs and the generation of resistant viral strains led to discover novel inhibitors. Recently, saffron and its compounds were used to treat different pathological conditions. In this study, we tested the anti-HSV-1 and anti-HIV-1 activities of Iranian saffron extract and its major ingredients including crocin and picrocrocin as well as cytotoxicity in vitro. The data showed that the aqueous saffron extract was not active against HIV-1 and HSV-1 virions at certain doses (i...
November 29, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/29165081/rheological-characteristics-of-novel-meloxicam-loaded-complex-organogels-based-on-fumed-silica-and-poloxamer
#7
Tomasz Osmalek, Anna Froelich, Barbara Jadach, Katarzyna Ancukiewicz, Piotr Gadzinski
The objective of the presented work was to formulate and investigate the rheological behavior of non-aqueous gels containing 0.5% of meloxicam (MLX) in a non-ionic, dissolved form. Fumed silica and SynperonicTM PE/L 62 were used as structure forming components. Arlasolve®, Transcutol®, ethanol and DMSO were applied as solubilizers and potential skin absorption enhancers. In the first step, the preformulation studies were conducted in order to optimize the composition of the vehicle. The main acceptance criterion was the ability of the medium to dissolve MLX, which was confirmed by the lack of drug crystals and proper clarity of the formulation...
November 20, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/29165080/tuberculosis-treated-by-multiple-drugs-an-overview
#8
Gyanendra Singh, Prashant Kesharwani, A K Shrivastava
Current tuberculosis (TB) treatment is established on an amalgamation of drugs that were evolved mostly in the central decades of the hind century. Cure rates are elevated for drug-sensitive strains of Mycobacterium tuberculosis (M.Tb) when the recommended complex and prolonged treatment protocols adhere. However, the difficulty in accurately prescribing and adhering to these protocols and the emergence of M. Tb strains resistant to multiple drugs and drug-drug interactions that interfere with optimal treatment of Tuberculosis and co-infected patients with the different disease has generated a pressing need for improved Tuberculosis therapies...
November 20, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/29165079/comparison-of-clobetasol-propionate-generics-using-simplified-in-vitro-bioequivalence-method-for-topical-drug-products
#9
Kelen Carine Costa Soares, Weidson Carlos de Souza, Leonardo de Souza Texeira, Marcilio Sergio Soares da Cunha-Filho, Guilherme Martins Gelfuso, Tais Gratieri
The aim of this paper is to propose a simple in vitro skin penetration experiment in which the drug is extracted from the whole skin piece as a test valid for formulation screening and optimization during development process, equivalence assessment during quality control or post-approval after changes to the product. Twelve clobetasol propionate (CP) formulations (six creams and six ointments) from the local market were used as a model to challenge the proposed methodology in comparison to in vitro skin penetration following tape-stripping for drug extraction...
November 20, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/29165078/pharmaceutical-product-lead-optimization-for-better-in-vivo-bioequivalence-performance-a-case-study-of-diclofenac-sodium-extended-release-matrix-tablets
#10
Aliasgar Shahiwala, Aisha Zarar
BACKGROUND: In order to prove the validity of a new formulation, a considerable amount of efforts is required to study bioequivalence, not only increases the burden of carrying out a number of bioequivalence studies but eventually increase the cost of the optimization process. OBJECTIVE: The aim of the present study was to develop sustained release matrix tablets containing diclofenac sodium using natural polymers and to demonstrate step by step process of product development till the prediction of in vivo marketed product equivalence of the developed product...
November 20, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/29165077/physicochemical-and-toxic-properties-of-novel-genipin-drug-delivery-systems-prepared-by-mechanochemistry
#11
Wenhao Xu, Murong Wen, Weike Su, Alexander V Dushkin, Lubov P Suntsova, Irina D Markova, Olga Yu Selyutina, Nikolay E Polyakov
Complexes of Genipin and differents water-soluble adjuvant polysaccharides such as arabinogalactane, hydroxyethyl starch, fibergum,and oligosaccharides β-CD and HP-β-CD,were synthesized as drug delivery system using mechanochemical technology. We have investigated physicochemical properties, stability, and hepatotoxicity of the synthesized complexes in solid state and aqueous solution. The formation of the complexes was evidenced by different physical and spectroscopy assays, and the stability constants of our synthesized Genipin-based complexes were also calculated...
November 20, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/29165076/pasylation-as-a-powerful-technology-for-improving-the-pharmacokinetic-properties-of-biopharmaceuticals
#12
Sajjad Ahmadpour, Seyed Jalal Hosseinimehr
One of the major challenges of short plasma half-life biopharmaceuticals is to daily high dose administration that leads to economic problems, patient inconvenience and undesirable side effects. Increasing the hydrodynamic volume beyond the pore size of the glomerular basal membrane is a general approach to increase the size of the small biopharmaceuticals with low half-life in blood circulation. PASylation technology is one of these approaches that are designed based on the genetic fusion of biopharmaceutical with a hydrophilic random coil sequence of tri proline (Pro), alanine (Ala), and serine (Ser) amino acids...
November 20, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/29165075/preferential-formulation-of-second-generation-antipsychotic-asenapine-as-inclusion-complex-with-sulphobutylether-%C3%AE-cd-captisol-in-vitro-and-in-vivo-evaluation
#13
Amelia Makarand Avachat, Juilee A Kulkarni, Charul M Avachat, Rohan Pradhan, Tushar S Suryawanshi, E M Khan, Elvis A F Martis, Evans C Coutinho, Subhash Padhye
Asenapine is an anti-psychotic agent approved by the US-FDA for treatment of acute schizophrenia and manic or bipolar I disorder in adults. It is poorly absorbed when administered orally, hence exhibits poor oral bioavailability, which limits its use in clinical practice. Consequently, enhancement in its solubility through complexation with three different cyclodextrins, viz. βCD (β cyclodextrin), HPβCD (Hydroxypropyl β cyclodextrin) and sulphobutylether-βCD (Captisol®) was attempted and compared. Kneading method was used for preparation of inclusion complexes which were characterized by FTIR, DSC, and XRD methods...
November 20, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/29165074/state-of-the-art-of-dental-adhesive-systems
#14
Jefferson Ricardo Pereira, Saulo Pamato, Marcos Vargas, Newton Fahl
BACKGROUND: The large dependence on a dental substrate type to bond strength has leveraged the research on materials and techniques that perform different clinical behavior, promoting a stable bonding over time. Bonding to tooth structure has different clinical behaviors and is dependent on several factors. OBJECTIVE: The aim of this paper is to reflect on the state of the art of adhesive systems since Buonocore's experiments to current days. METHODS: An electronic search was conducted on PubMed databases and supplemented with a manual study of relevant references...
November 20, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/29165071/minocycline-loaded-in-situ-hydrogel-for-periodontitis-treatment
#15
Xiaoqing Wang, Jianli Ma, Xiaoming Zhu, Fang Wang, Liang Zhou
In situ hydrogel based on phase separation by solvent exchange has emerged as an attractive alternative for periodontal pocket injection. In this study, an minocycline (MCL)-loaded in situ hydrogel was prepared composed of poly(lactide-co-glycolide) (PLGA) and N-methylpyrrolidone (NMP) to enhance the topical treatment of periodontitis. A series of reasonable and applicable formulations were optimized by investigating their syringeability, viscosity and in vitro drug release. The rheological profiles, antimicrobial activities and pharmacodynamics were further studied to evaluate its effect on periodontitis treatment...
November 20, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/29165073/recent-progress-in-delivery-of-therapeutic-and-imaging-agents-utilizing-organic-inorganic-hybrid-nanoparticles
#16
Haque Sheikh Tanzina, Ezharul Chowdhury
Delivery of conventional small molecule drugs and currently evolving nucleic acid-based therapeutics, such as small interfering RNAs (siRNAs) and genes, and contrast agents for high resolution imaging, to the target site of action is highly demanding to increase the therapeutic and imaging efficacy while minimizing the off-target effects of the delivered molecules, as well as develop novel therapeutic and imaging approaches. Organic-inorganic hybrid nanoparticles offer a number of advantages by combining the unique properties of the organic and inorganic counterparts, thus improving the pharmacokinetic behavior and targetability of drugs and contrast agents, and conferring the exclusive optical and magnetic properties for both therapeutic and imaging purposes...
November 19, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/29165072/mpeg-pla-micelle-for-delivery-of-effective-parts-of-andrographis-paniculata
#17
Hailu Yao, Shiyong Song, Xiaolu Miao, Xiao Liu, Zhen Wang, Xiaoting Shao, Yu Zhang, Guang Han
Many studies have shown that Andrographis paniculata (Burm. f.) Nees has a good anti-tumor effect, but poor solubility in water and poor bioavailability hinder the modernization of it. To formulate the effective parts (mainly diterpene lactones) of Andrographis paniculata (AEP) into targeting drug delivery system, a series of poly(ethylene glycol)-poly(D.L-lactic acid)(mPEG-PLA) with different ratio of hydrophilic and hydrophobic segment were synthetized to encapsulate AEP. AEP micelles were prepared by a simple solvent-evaporation method...
November 19, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/29110612/influence-of-implants-composition-on-melatonin-release-from-ethylcellulose-matrix
#18
Emilie Duffau, Etienne Harte, Jean Toutain, Florence Guimberteau, Sophie Lecomte, Fernando Leal-Calderon, Chrystel Faure
We report a comprehensive study about the influence of the drug loading on its release from solid implants, from both a kinetic and structural point of view. The study was performed on binary implants, composed of melatonin (M), as a model drug, and of ethyl cellulose (EC), as a polymeric carrier matrix. Cylindrical implants differing in their M:EC ratio were fabricated to cover a large range of compositions. Drug release was assayed by in vitro dissolution tests in CTAB micellar solutions. The 2D imaging of implant chemical composition during M release, performed by confocal Raman spectroscopy, evidenced a drug radial leakage, whatever the implant composition...
November 3, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/29065835/hydroxypropyl-%C3%AE-cyclodextrin-formulated-in-nasal-chitosan-microspheres-as-candidate-therapeutic-agent-in-alzheimer-s-disease
#19
Giovanna Rassu, Elisabetta Gavini, Antonio Carta, Antonella Obinu, Elena Piera Porcu, Paolo Giunchedi
Hydroxypropyl-β-cyclodextrin (HP-CD) is a hydroxyalkyl derivative of native β-cyclodextrin, cyclic oligosaccharide able to form inclusion complexes with many drugs and biomolecules [1]. Cyclodextrins have a possible neuroprotective effect due to their capability to extract and deplete cholesterol from cell membranes [1]. HP-CD is classified as an excipient (cyclodextrins are in fact widely used to improve solubility of poorly water soluble drugs) and it is not been FDA-approved as therapeutic agent. However HP-CD received the "orphan drug designation" in the United States and Europe because it is employed in individual compassionate use for patients suffering from Niemann-Pick type C...
October 19, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/29065834/polymeric-nano-encapsulation-of-curcumin-enhances-its-anti-cancer-activity-in-breast-mda-mb231-and-lung-a549-cancer-cells-through-reduction-in-expression-of-hif-1a-and-nuclear-p65-rel-a
#20
Mohammed N Khan, Yusuf A Haggag, Majella E Lane, Paul A McCarron, Murtaza M Tambuwala
BACKGROUND: The anti-cancer potential of curcumin, a natural NFkβ inhibitor, has been reported extensively in breast, lung and other cancers. In vitro and in vivo studies indicate that the therapeutic efficacy of curcumin is enhanced when formulated in a nanoparticulate carrier. However, the mechanism of action of curcumin at the molecular level in the hypoxic tumour micro-environment is not fully understood. Hence, the aim of our study was to investigate the mechanism of action of curcumin formulated as nanoparticles in in vitro models of breast and lung cancer under a hypoxic micro-environment...
October 19, 2017: Current Drug Delivery
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