- Development of novel amisulpride-loaded solid self-nanoemulsifying tablets: preparation and pharmacokinetic evaluation in rabbits. [Journal Article]
- DDDrug Dev Ind Pharm 2017 Apr 27; :1-29
- CONCLUSIONS: S-SNEDDS can be a very useful approach for providing patient acceptable dosage forms with improved oral dissolution and biovailability.
- Development of novel amisulpride-loaded liquid self-nanoemulsifying drug delivery systems via dual tackling of its solubility and intestinal permeability. [Journal Article]
- DDDrug Dev Ind Pharm 2017 Apr 27; :1-31
- CONCLUSIONS: the present study proved that AMS could be successfully incorporated into L-SNEDDS for improved dissolution and intestinal permeation leading to enhanced oral delivery.
- Recent Achievements in Tc-99m Radiopharmaceutical Direct Production by Medical Cyclotrons. [Journal Article]
- DDDrug Dev Ind Pharm 2017 Apr 26; :1-43
- (99m)Tc is the most commonly used radionuclide in the field of diagnostic imaging, a noninvasive method intended to diagnose a disease, assess the disease state and monitor the effects of treatments....
(99m)Tc is the most commonly used radionuclide in the field of diagnostic imaging, a noninvasive method intended to diagnose a disease, assess the disease state and monitor the effects of treatments. Annually, the use of (99m)Tc, covers about 85% of nuclear medicine applications. This isotope releases gamma rays at about the same wavelength as conventional X-ray diagnostic equipment, and owing to its short half-life (t½ = 6 hours) is ideal for diagnostic nuclear imaging. A patient can be injected with a small amount of (99m)Tc and within 24 hours almost 94% of the injected radionuclide would have decayed and left the body, limiting the patient's radiation exposure. (99m)Tc is usually supplied to hospitals through a (99)Mo/(99m)Tc radionuclide generator system where it is produced from the β decay of the parent nuclide (99)Mo (t½ = 66 h), which is produced in nuclear reactors via neutron fission. Recently, the interruption of the global supply chain of reactor-produced (99)Mo, has forced the scientific community to investigate alternative production routes for (99m)Tc. One solution was to consider cyclotron-based methods as potential replacement of reactor-based technology and the nuclear reaction (100)Mo(p,2n)(99m)Tc emerged as the most worthwhile approach. This review reports some achievements about (99m)Tc produced by medical cyclotrons. In particular, the available technologies for target design, the most efficient extraction and separation procedure developed for the purification of (99m)Tc from the irradiated targets, the preparation of high purity (99m)Tc radiopharmaceuticals and the first clinical studies carried out with cyclotron produced (99m)Tc are described.
- Synthesis and characterization of poly(N-vinylcaprolactam)-based spray-dried microparticles exhibiting temperature and pH-sensitive properties for controlled release of ketoprofen. [Journal Article]
- DDDrug Dev Ind Pharm 2017 Apr 22; :1-31
- Poly(N-vinylcaprolactam) (PNVCL) and poly(N-vinylcaprolactam-co-acrylic acid) (poly(NVCL-co-AA)) were synthesized by solution free radical polymerization and displayed thermo-responsive behavior, wit...
Poly(N-vinylcaprolactam) (PNVCL) and poly(N-vinylcaprolactam-co-acrylic acid) (poly(NVCL-co-AA)) were synthesized by solution free radical polymerization and displayed thermo-responsive behavior, with lower critical solution temperatures (LCSTs) of 35°C and 39°C, respectively. The incorporation of AA unities made the poly(NVCL-co-AA) sensitive to both pH- and temperature. They were exploited in this work in preparing microparticles loaded with ketoprofen via spray-drying to modulate the drug release rate by changing pH or temperature. The interaction between polymer and drug was studied using x-ray diffractometry, Raman spectrometry and scanning electron microscopy (SEM). The biocompatibility of pure polymers, free ketoprofen as well as the spray-dried particles was demonstrated in vitro by low cytotoxicity and a lack of nitric oxide production in macrophages at concentrations as high as 100 µg mL(-1). The release profile of ketoprofen was evaluated by in vitro assays at different temperatures and pH values. Drug diffusion out of PNVCL's hydrated polymer network is increased at temperatures below the LCST. However, when poly(NVCL-co-AA) was used as the matrix, the release of Ketoprofen was primarily controlled by the pH of the medium. These results indicated that PNVCL and the novel poly(NVCL-co-AA) could be promising candidates for pH and temperature responsive drug delivery systems.
- Mydriatics release from solid and semi-solid ophthalmic formulations using different in vitro methods. [Journal Article]
- DDDrug Dev Ind Pharm 2017 Apr 20; :1-23
- The aim of the present paper was the development of semisolid (hydrogels) and solid (film) ophthalmic formulations for the controlled release of two mydriatics: phenylephrine and tropicamide. The for...
The aim of the present paper was the development of semisolid (hydrogels) and solid (film) ophthalmic formulations for the controlled release of two mydriatics: phenylephrine and tropicamide. The formulations - based on polyvinylalchol and hyaluronic acid - were characterized, and release studies were performed with three different in vitro set-ups, i.e. Franz-type diffusion cell, vial method and inclined plane; for comparison, a solution and a commercial insert, both clinically used to induce mydriasis, were evaluated. Both gels and film allowed for a controlled release of drugs, appearing a useful alternative for mydriatics administration. However, the release kinetic was significantly influenced by the method used, highlighting the need for optimization and standardization of in vitro models for the evaluation of drug release from ophthalmic dosage forms.
- Enhanced Solubility of Piperine using Hydrophilic carrier based Potent Solid Dispersion Systems. [Journal Article]
- DDDrug Dev Ind Pharm 2017 Apr 20; :1-32
- CONCLUSIONS: Results suggest that the piperine solid dispersions prepared with improved in-vitro release exhibit potential advantage in delivering poorly water-soluble piperine as an oral supplement.
- Development of a Soluplus® Budesonide Freeze-Dried Powder for Nasal Drug Delivery. [Journal Article]
- DDDrug Dev Ind Pharm 2017 Apr 20; :1-31
- CONCLUSIONS: The small volume of fluid present in the nasal cavity limits the absorption of a poorly soluble drug. Budesonide is a corticosteroid, practically insoluble, and normally administered as a suspension-based nasal spray.Soluplus has been shown to be a promising polymer for the formulation of budesonide amorphous solid suspension/solution. This opens up opportunities to develop new formulations of poorly soluble drug for nasal delivery.
- Evaluation of polyvinyl alcohols as mucoadhesive polymers for mucoadhesive buccal tablets prepared by direct compression. [Journal Article]
- DDDrug Dev Ind Pharm 2017 Apr 20; :1-56
- The purpose of the present work was to evaluate polyvinyl alcohols (PVAs) as a mucoadhesive polymer for mucoadhesive buccal tablets prepared by direct compression. Various polymerization degree and p...
The purpose of the present work was to evaluate polyvinyl alcohols (PVAs) as a mucoadhesive polymer for mucoadhesive buccal tablets prepared by direct compression. Various polymerization degree and particle diameter PVAs were investigated for their usability. The tensile strength, in vitro adhesive force and water absorption properties of the tablets were determined to compare the various PVAs. The highest values of the tensile strength and the in vitro adhesive force were observed for PVAs with a medium viscosity and small particle size. The optimal PVA was identified by a factorial design analysis. Mucoadhesive tablets containing the optimal PVA were compared with carboxyvinyl polymer and hydroxypropyl cellulose formulations. The optimal PVA gives a high adhesive force, has a low viscosity and resulted in relatively rapid drug release. Formulations containing carboxyvinyl polymer had high tensile strengths but short disintegration times. Higher hydroxypropyl cellulose concentration formulations had good adhesion forces and very long disintegration times. We identified the optimal characteristics of PVA, and the usefulness of mucoadhesive buccal tablets containing this PVA was suggested from their formulation properties.
- Implant Compositions for the Unidirectional Delivery of Drugs to the Brain. [Journal Article]
- DDDrug Dev Ind Pharm 2017 Apr 19; :1-28
- The overall objective of this study was to design and characterize the properties of a bioadhesive trilayer sustained-release implant device for the unidirectional local delivery of anticancer compou...
The overall objective of this study was to design and characterize the properties of a bioadhesive trilayer sustained-release implant device for the unidirectional local delivery of anticancer compounds to the brain following the removal of glioblastoma multiforme tumors. Using acetaminophen as a model drug compound, we compressed trilayer wafers that contained (a) a bioadhesive layer, (b) a drug layer that contained a lipid and a pore-forming hydrophilic polymer, and (c) a third layer comprising a lipid substance. To maintain a unidirectional pathway of drug release from these trilayer wafers, the edges and the surface lipophilic layer were coated with molten wax followed by cooling of the wafer. These wafers were subsequently heat cured to promote interlayer adhesion in the device. Polyethylene oxide was utilized both as the bioadhesive layer and the pore-forming hydrophilic polymer. Glyceryl behenate was employed as the lipid. The drug release properties of the trilayer wafer were a function of (a) the molecular weight and concentration of polyethylene oxide in the drug-containing lipid layer, (b) the presence of the bioadhesive layer on the wafer, and (c) the lipid coating applied to the top and sides of the delivery system. The unidirectional release of the drug occurred from the device through the bioadhesive layer, and zero-order release kinetics resulted over a 10-day period after a three-day lag time. During this period, less than 10% of the drug had been released from the wafer. All of the drug was released by 21 days.
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- Optimization of methotrexate loaded niosomes by Box-Behnken design: an understanding of solvent effect and formulation variability. [Journal Article]
- DDDrug Dev Ind Pharm 2017 Apr 27; :1-10
- Dermal drug delivery system which localizes methotrexate (MTX) in the skin is advantageous in topical treatment of psoriasis. The aim of the current study was to understand dilution effects and formu...
Dermal drug delivery system which localizes methotrexate (MTX) in the skin is advantageous in topical treatment of psoriasis. The aim of the current study was to understand dilution effects and formulation variability for the potential formation of niosomes from proniosome gels of MTX. Box-Behnken's design was employed to prepare a series of MTX proniosome gels of Span 40, cholesterol (Chol-X1) and Tween 20 (T20-X2). Short chain alcohols (X3), namely ethanol (Et), propylene glycol (Pg) and glycerol (G) were evaluated for their dilution effects on proniosomes. The responses investigated were niosomal vesicles size (Y1), MTX entrapment efficiency percent (EE%-Y2) and zeta potential (Y3). MTX loaded niosomes were formed immediately upon hydration of the proniosome gels with the employed solvents. Addition of Pg resulted in a decrease of vesicular size from 534 nm to 420 nm as Chol percentage increased from 10% to 30%, respectively. In addition, increasing the hydrophilicity of the employed solvents was enhancing the resultant zeta potential. On the other hand, using Et in proniosomal gels would abolish Chol action to increase the zeta potential value and hence less stable niosomal dispersion was formed. The optimized formula of MTX loaded niosomes showed vesicle size of 480 nm, high EE% (55%) and zeta potential of -25.5 mV, at Chol and T20 concentrations of 30% and 23.6%, respectively, when G was employed as the solvent. Hence, G was the solvent of choice to prepare MTX proniosomal gels with a maintained stability and highest entrapment.