The application of co-melt-extruded poly( ε-caprolactone) as a controlled release drug delivery device when combined with novel bioactive drug candidates: Membrane permeation and Hanson dissolution studies
Publication date: May 2011 Source:Results in Pharma Sciences, Volume 1, Issue 1 Author(s): Stephen J. Gardyne, Michael R. Mucalo, Michael J. Rathbone Eight bioactive drug compounds (abamectin, amoxicillin, dexamethasone, dexamethasone valerate, ketoprofen, melatonin, oestradiol 17β, and oestradiol benzoate) were combined via melt extrusion and disc pressing processes with a polycaprolactone (PCL) matrix and were then evaluated and compared via membrane diffusion and Hanson dissolution studies. This investigation was to determine the potential of this matrix to act as a controlled release drug delivery vehicle fo...
Source: Results in Pharma Sciences - June 17, 2016 Category: Drugs & Pharmacology Source Type: research
Oral bioavailability of a poorly aqueous drug from three different SBE7- β-cyclodextrin based formulations in beagle dogs
Publication date: May 2011 Source:Results in Pharma Sciences, Volume 1, Issue 1 Author(s): René Holm, Lene Andresen, Claus Strange Oral administration of Lu 35-138, a low aqueous soluble compound, was investigated in three different formulations containing sulfobutylether β-cyclodextrin (SBE7βCD) in fasted beagle dogs. The evaluated formulations was (i) a SBE7βCD solution, (ii) a spray dried solution filled into hard gelatine capsules, and (iii) a direct compressible tablet containing SBE7βCD. The three formulations did not lead any significant differences in the obtained AUCs, though a trend was observed fo...
Source: Results in Pharma Sciences - June 17, 2016 Category: Drugs & Pharmacology Source Type: research
Two-step nanoprecipitation for the production of protein-loaded PLGA nanospheres
Publication date: 2012 Source:Results in Pharma Sciences, Volume 2 Author(s): Moraima Morales-Cruz, Giselle M. Flores-Fernández, Myreisa Morales-Cruz, Elsie A. Orellano, José A. Rodriguez-Martinez, Mercedes Ruiz, Kai Griebenow One of the first methods to encapsulate drugs within polymer nanospheres was developed by Fessi and coworkers in 1989 and consisted of one-step nanoprecipitation based on solvent displacement. However, proteins are poorly encapsulated within polymer nanoparticles using this method because of their limited solubility in organic solvents. To overcome this limitation, we developed a ...
Source: Results in Pharma Sciences - June 17, 2016 Category: Drugs & Pharmacology Source Type: research
Moxifloxacin in situ gelling microparticles –bioadhesive delivery system
Publication date: 2012 Source:Results in Pharma Sciences, Volume 2 Author(s): Qiongyu Guo, Ahmed Aly, Oliver Schein, Morgana M. Trexler, Jennifer H. Elisseeff Antibiotic use for ocular treatments has been largely limited by poor local bioavailability with conventional eyedrops formulations. Here, we developed a controlled delivery system composed of moxifloxacin-loaded poly(lactic-co-glycolic acid) (PLGA) microparticles encapsulated in a chondroitin sulfate-based, two-component bioadhesive hydrogel. Using a simple and fast electrohydrodynamic spray drying (electrospraying) technique, surfactant-free moxifloxa...
Source: Results in Pharma Sciences - June 17, 2016 Category: Drugs & Pharmacology Source Type: research
Relationship between the usability and physicochemical properties of triamcinolone acetonide ointments
Publication date: 2013 Source:Results in Pharma Sciences, Volume 3 Author(s): Yutaka Inoue, Rikimaru Maeda, Kayoko Furuya, Murata Isamu, Kimura Masayuki, Ikuo Kanamoto The purpose of this study was to examine the physicochemical properties of TA ointments and conduct a human sensory test to assess the properties of those ointments. Physicochemical assessment was done via near-infrared (NIR) absorption spectroscopy, measurement of water content, microscopy, and measurement of viscoelasticity. The human sensory test examined 5 aspects (texture, cohesiveness, spreadability, smell, and feel). Three TA ointments...
Source: Results in Pharma Sciences - June 17, 2016 Category: Drugs & Pharmacology Source Type: research
Enzymatic activity in the presence of surfactants commonly used in dissolution media, Part 1: Pepsin
Publication date: 2016 Source:Results in Pharma Sciences, Volume 6 Author(s): Maria L Guzman, Margareth R Marques, Maria E Olivera ME, Erika S Stippler The United States Pharmacopeia (USP) General Chapters Dissolution 〈711〉 and Disintegration and Dissolution of Dietary Supplements 〈2040〉 allows the use of enzymes in dissolution media when gelatin capsules do not conform to dissolution specifications due to cross linking. Possible interactions between enzymes and surfactants when used together in dissolution media could result in loss of the enzymatic activity. Pepsin is an enzyme commonly used in dissol...
Source: Results in Pharma Sciences - March 16, 2016 Category: Drugs & Pharmacology Source Type: research
Enzymatic activity in the presence of surfactants commonly used in dissolution media. part 1: PEPSIN
Publication date: Available online 2 March 2016 Source:Results in Pharma Sciences Author(s): Maria L Guzman, Margareth R Marques, Maria E Olivera ME, Erika S Stippler The United States Pharmacopeia (USP) General Chapters Dissolution <711> and Disintegration and Dissolution of Dietary Supplements <2040> allows the use of enzymes in dissolution media when gelatin capsules do not conform to dissolution specifications due to cross linking. Possible interactions between enzymes and surfactants when used together in dissolution media could result in loss of the enzymatic activity. Pepsin i...
Source: Results in Pharma Sciences - March 2, 2016 Category: Drugs & Pharmacology Source Type: research
Differences in the rheological properties and mixing compatibility with heparinoid cream of brand name and generic steroidal ointments: The effects of their surfactants
Publication date: Available online 13 February 2016 Source:Results in Pharma Sciences Author(s): Shuji Kitagawa, Reiko Yutani, Rhu-ichi Kodani, Reiko Teraoka Most steroidal ointments contain propylene glycol (PG) and surfactants, which improve the solubility of corticosteroids in white petrolatum. Surfactants aid the uniform dispersal of PG within white petrolatum. Since the surfactants used in generic ointments are usually different from those used in brand name ointments, we investigated the effects of surfactants on the rheological properties of three brand name ointments and six equivalent generic ointments...
Source: Results in Pharma Sciences - February 14, 2016 Category: Drugs & Pharmacology Source Type: research
The importance of binder moisture content in Metformin HCL high-dose formulations prepared by moist aqueous granulation (MAG)
Publication date: Available online 3 October 2015 Source:Results in Pharma Sciences Author(s): Hiroshi Takasaki, Etsuo Yonemochi, Masanori Ito, Koichi Wada, Katsuhide Terada The aim of this study was to evaluate binders to improve the flowability of granulates and compactibility of Metformin HCL (Met) using the moist aqueous granulation (MAG) process. The effect of the binder moisture content on granulate and tablet quality was also evaluated. Vinylpyrrolidone-vinyl acetate copolymer (Kollidon VA64 fine: VA64), polyvidone (Povidone K12: PVP), hydroxypropyl cellulose (HPC SSL SF: HPC) and hydroxypropyl methylc...
Source: Results in Pharma Sciences - October 4, 2015 Category: Drugs & Pharmacology Source Type: research
Development and characterization of in-situ gel for ophthalmic formulation containing ciprofloxacin Hydrochloride
Publication date: Available online 8 July 2015 Source:Results in Pharma Sciences Author(s): S.B. Makwana , V.A. Patel , S.J. Parmar In situ gels are systems which are applied as solutions or suspensions and are capable of undergoing rapid sol-to-gel transformation triggered by external stimulus such as temperature, pH etc. on instillation. The aim of the present study was to formulate and evaluate pH responsive in-situ gel for ophthalmic delivery. Ciprofloxacin hydrochloride is popularly used as a broad spectrum anti biotic in the treatment of corneal ulcers of ocular infections. However, rapid dilution on instilla...
Source: Results in Pharma Sciences - July 8, 2015 Category: Drugs & Pharmacology Source Type: research
Glycosylation improves α-chymotrypsin stability upon encapsulation in poly(lactic-co-glycolic)acid microspheres
Publication date: 2012 Source:Results in Pharma Sciences, Volume 2 Author(s): Giselle M. Flores-Fernández , Kai Griebenow Enhancing protein stability upon encapsulation and release from polymers is a key issue in sustained release applications. In addition, optimum drug dispersion in the polymer particles is critical for achieving release profiles with low unwanted initial “burst” release. Herein, we address both issues by formulating the model enzyme α-chymotrypsin (α-CT) as nanoparticles to improve drug dispersion and by covalently modifying it with glycans to afford improved stability during encapsulation i...
Source: Results in Pharma Sciences - January 23, 2015 Category: Drugs & Pharmacology Source Type: research
Biological conversion of aripiprazole lauroxil − An N-acyloxymethyl aripiprazole prodrug
Publication date: 2014 Source:Results in Pharma Sciences, Volume 4 Author(s): Morten Rohde , Niels M∅rk , Anders E. Håkansson , Klaus G. Jensen , Henrik Pedersen , Tina Dige , Erling B. J∅rgensen , René Holm N-acyloxyalkylation of NH-acidic compounds can be a prodrug approach for e.g. tertiary or some N-heterocyclic amines and secondary amides and have the potential to modify the properties of the parent drug for specific uses, for example its physicochemical, pharmacokinetic or biopharmaceutical properties. Aripiprazole lauroxil was prepared as a model compound for such prodrugs and its bioconversion wa...
Source: Results in Pharma Sciences - December 23, 2014 Category: Drugs & Pharmacology Source Type: research
The application of co-melt-extruded poly(ε-caprolactone) as a controlled release drug delivery device when combined with novel bioactive drug candidates: Membrane permeation and Hanson dissolution studies
Publication date: May 2011 Source:Results in Pharma Sciences, Volume 1, Issue 1 Author(s): Stephen J. Gardyne , Michael R. Mucalo , Michael J. Rathbone Eight bioactive drug compounds (abamectin, amoxicillin, dexamethasone, dexamethasone valerate, ketoprofen, melatonin, oestradiol 17β, and oestradiol benzoate) were combined via melt extrusion and disc pressing processes with a polycaprolactone (PCL) matrix and were then evaluated and compared via membrane diffusion and Hanson dissolution studies. This investigation was to determine the potential of this matrix to act as a controlled release drug delivery vehicle for...
Source: Results in Pharma Sciences - October 12, 2014 Category: Drugs & Pharmacology Source Type: research
A microdialysis study of topically applied diclofenac to healthy humans: Passive versus iontophoretic delivery
Publication date: May 2011 Source:Results in Pharma Sciences, Volume 1, Issue 1 Author(s): Birgit Falk Riecke , Else Marie Bartels , Søren Torp-Pedersen , Søren Ribel-Madsen , Henning Bliddal , Bente Danneskiold-Samsøe , Lars Arendt-Nielsen Topical application of NSAIDs is an alternative route to systemic administration when a local anti-inflammatory effect of the underlying tissue is a treatment option. The aim of the present microdialysis study was to assess and compare plasma and tissue levels of diclofenac when topically applied with or without iontophoresis in healthy adults. Fourteen healthy adults (26...
Source: Results in Pharma Sciences - October 12, 2014 Category: Drugs & Pharmacology Source Type: research
Effects of doxorubicin-encapsulating AG73 peptide-modified liposomes on tumor selectivity and cytotoxicity
In this study, to develop a safer and more selective liposomal formulation, we prepared doxorubicin-encapsulating AG73 peptide-modified liposomes (AG73–Dox). First, we assessed the selectivity of AG73–Dox for cancer cells, including syndecan-2 over-expressing cells, using flow cytometry and confocal microscopy. AG73–Dox showed selective cellular uptake on cancer cells and enhancement of the intracellular uptake. Next, we examined the cytotoxicity of AG73–Dox using a WST assay. AG73–Dox exhibited a higher cytotoxicity against cancer cells than other control liposomes. In addition, we showed that the antitumor effi...
Source: Results in Pharma Sciences - October 12, 2014 Category: Drugs & Pharmacology Source Type: research
