| 1. |
- Adane, M., et al.
(författare)
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The use of extragranular disintegrants in multiple-unit tablet formulations : effect on compressibility, compactibility and disintegration
- 2007
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Ingår i: Journal of drug delivery science and technology. - 1773-2247. ; 17:4, s. 279-284
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Tidskriftsartikel (refereegranskat)abstract
- Multiple-unit tablets formed from mixtures of microcrystalline cellulose pellets and disintegrants (Ac-Di-Sol, Primojel or Kollidon CL) by compaction were investigated with the aim of controlling tablet tensile strength and disintegration time. The effects of pellet porosity, compaction pressure, and type and amount of disintegrant were studied. Primojel made the pellets less prone to deformation during compression, while the other two disintegrants had very minor effects on the compression behavior. Ac-Di-Sol and Primojel generally increased the tablet tensile strength, whereas the effect of Kollidon CL was dependent on the initial pellet porosity. Kollidon CL was found to significantly reduce the disintegration time, but the other two disintegrants had variable efficacy, and for the low-porosity pellets significantly increased the disintegration time. These results are interpreted as resulting from the interplay between the mechanical characteristics of the pellets and the mechanisms of action of the disintegrants.
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| 2. |
- Ahnfelt, Emelie, et al.
(författare)
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Lipiodol-based emulsions used for transarterial chemoembolization and drug delivery : Effects of composition on stability and product quality
- 2019
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Ingår i: Journal of Drug Delivery Science and Technology. - : ELSEVIER. - 1773-2247. ; 53
-
Tidskriftsartikel (refereegranskat)abstract
- Transarterial chemoembolization with emulsion-based formulations using doxorubicin hydrochloride (DOX) and Lipiodol (R) is the golden standard for the loco-regional treatment of unresectable hepatocellular carcinoma (HCC). However, from a pharmaceutical quality perspective these emulsions are poorly characterized. In this study, clinically relevant Lipiodol (R)-based emulsions were characterized in terms of emulsion stability, continuous phase classification and droplet-size distribution. Also, the solubility of DOX in the different emulsion components and the distribution of DOX to the lipid phase were investigated. These are key features to investigate due to the claimed tumor-seeking properties of Lipiodol (R). The in vitro release of DOX was studied in a miniaturized dialysis method and an empirical release model was applied to adjust for the passage of DOX across the dialysis membrane. The most stable emulsion ( > 72 h) was classified as water-in-oil (w/o), had the highest distribution of DOX to the lipid phase (20%) and an aqueous-to-lipid phase ratio of 1:4. The composition of the aqueous phase was a mixture (v/v) of iohexol (85%) and water (15%). Emulsions containing iohexol and a high aqueousto-lipid phase ratio (1:2-1:4) displayed prolonged in vitro release profiles of DOX. This study further emphasizes the medical need to standardize these emulsion-based drug delivery systems.
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| 3. |
- Ahrenstedt, Lage, et al.
(författare)
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Sustained zero-order release of dexamethasone after incorporation into crosslinked PEG-dendrons using click reactions
- 2024
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Ingår i: Journal of Drug Delivery Science and Technology. - : Elsevier BV. - 1773-2247. ; 95
-
Tidskriftsartikel (refereegranskat)abstract
- Hydrogel-based localised drug delivery minimises systemic side effects and a linear release profile ensuring a sustained drug release over time, crucial for long-term therapy. The current paper describes the use of the Copper(I)-catalyzed Azide-Alkyne Cycloaddition (CuAAc) to append azidified Dexamethasone (Dex) onto dendrons of first- and second-generation PEGs. Crosslinking with thiolated PEGs using either thiol-acrylate or nucleophilic addition reactions yielded gels containing β-thio-ether ester groups that imparted enhanced hydrolytic susceptibility. In vitro gel degradation was followed gravimetrically and expressed as swelling ratios. Thiol-acrylate crosslinked hydrogels exhibited zero-order Dex release kinetics over 11, 27, and 16 days (G1, G1-star, and G2). Crosslinking the G1-gels by nucleophilic addition also resulted in linear release and the end point was reached in 5 days. Hydrolysis was accounted as the main release mechanism for covalently bound Dex, while physically incorporated Dex showed undefined rapid burst or first-order release, with most of the drug released in the initial 1–3 days. Eluates from covalently bound Dex maintained high activity, whereas Trap-Dex gels lost activity over time, as detected by the upregulation of luciferase expression from a transformed cell line. This novel chemistry combination offers precise drug release control applicable beyond Dex to drugs with suitable nucleophilic groups.
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| 4. |
- AlHayali, Amani, et al.
(författare)
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Silodosin oral films : Development, physico-mechanical properties and in vitro dissolution studies in simulated saliva
- 2019
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Ingår i: Journal of Drug Delivery Science and Technology. - : Elsevier. - 1773-2247. ; 53
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Tidskriftsartikel (refereegranskat)abstract
- Sublingual film dosage forms for drugs used for fast symptomatic treatment have promise because they allow a rapid onset of action. The aim of this study was to prepare films of silodosin intended for sublingual administration for the symptomatic treatment of benign prostatic hyperplasia in men. Hydroxypropyl methylcellulose (HPMC) or hydroxypropyl methylcellulose acetate succinate (HPMC-AS) were used as film-forming polymers. The effects of the polymers and the surfactant tocopherol polyethylene glycol succinate (TPGS) on the physico-mechanical properties and dissolution behavior of the films in simulated saliva were investigated. The eight silodosin oral films developed (F1–F8) contained 8 mg silodosin per 6 cm2 film and HPMC or HPMC-AS in drug:polymer ratios of 1:5 or 1:3, while four also contained TPGS (0.5% w/w). The films were characterized using DSC, TGA, SEM, and PXRD and the mechanical properties were investigated by measuring tensile strength, elongation at break and Young's modulus. The mechanical properties of the films were dependent on the ratio of polymer used. The in vitro dissolution and drug release studies indicated that HPMC-AS films disintegrated more quickly than HPMC films. Silodosin was shown to be dispersed within the polymers. Despite silodosin being submicronized in the HPMC films, the dissolution and drug release rate (time for 80% release) from HPMC films was significantly faster than from HPMC-AS films. TPGS increased the drug release rate to a greater extent with HPMC than with HPMC-AS. The degree of saturation of formulation F4 was >1, which shows potential for improving oral absorption of silodosin.
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| 5. |
- Ali, Abdullah, 1985-, et al.
(författare)
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Will a water gradient in oral mucosa affect transbuccal drug absorption?
- 2018
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Ingår i: Journal of Drug Delivery Science and Technology. - : Elsevier. - 1773-2247. ; 48, s. 338-345
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Tidskriftsartikel (refereegranskat)abstract
- Formulations for buccal drug delivery often comprise polymers to facilitate mucoadhesion based on water sorption. The main objective of the current study was therefore to evaluate the effect of dehydration on drug uptake through oral mucosa. We have used diffusion cells with excised porcine mucosa to study uptake of three alternative drugs (i.e., Metronidazole, Benzydamine and Xylometazoline) together with polyethylene glycol (PEG) as the model polymer for adjusting water activity in the test solutions. Taking drug activity into account, we can conclude that addition of PEG results in a drug flux through mucosa that is about two times lower for Metronidazole and more than 40 times lower for Xylometazoline compared to that from a pure PBS-solution. However, for Benzydamine the uptake through mucosa was more or less the same, which could possibly be due to the high PEG-concentration (65 wt%) affecting the dissociation constant and thus the permeability. These results indicate that an increased water gradient may have the same limiting effect on permeability through oral mucosa as previously seen for skin. Thus, water gradient effects should be a factor to consider when developing buccal adhesive formulations.
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| 6. |
- Bakardzhiev, Pavel, et al.
(författare)
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Novel polyglycidol-lipid conjugates create a stabilizing hydrogen-bonded layer around cholesterol-containing dipalmitoyl phosphatidylcholine liposomes
- 2015
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Ingår i: Journal of Drug Delivery Science and Technology. - : Elsevier. - 1773-2247. ; 29, s. 90-98
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Tidskriftsartikel (refereegranskat)abstract
- Hybrid liposomes resulting from co-assembly of dipalmitoylphosphatidylcholine and polyglycidol-derivatized lipids were prepared. The latter were composed of a lipid-mimetic residue to which a linear polyglycidol chain (degree of polymerization, DP, in the 23–110 range) was conjugated. Formulations with varying copolymer type and content were prepared by film hydration technique followed by extrusion. The hybrid structures were studied by means of dynamic and electrophoretic light scattering, cryogenic transmission electron microscopy, and fluorescence spectroscopy. Cytotoxicity towards OPM-2 (multiple myeloma) and EJ (human urinary bladder carcinoma) cell lines was assessed as well. Predominantly unilamellar liposomes with mean hydrodynamic diameters in the 113–134 nm range and neutral to slightly negative surface potential were prepared. The integrity of liposomes containing copolymers with DP of the polyglycidol chain 23 and 30 was preserved at copolymer contents up to 10 mol%. Bilayer disks were observed at somewhat lower contents of the copolymers of the highest DP of the polyglycidol chain. The hybrid structures were less leaky than the plain liposomes, which was attributed to formation of a strongly hydrogen-bonded polyglycidol layer around the bilayer membrane. They exhibited low toxicological potential, favorable physicochemical characteristics, and ability to act as containers for sustained release.
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| 7. |
- Bramer, Tobias, et al.
(författare)
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Effects of pH and ionic strength on catanionic drug-surfactant mixtures used for prolonged release from gels.
- 2007
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Ingår i: Journal of drug delivery science and technology. - 1773-2247. ; 17:4, s. 285-291
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Tidskriftsartikel (refereegranskat)abstract
- The purpose of this study was to investigate the influence of pH and ionic strength on the phase behavior of two different catanionic drug-surfactant mixtures, and to study drug release from gels facilitated by the catanionic aggregates. Simplified phase diagrams were constructed for diphenhydramine or tetracaine mixed with SDS, varying the pH approximately between 6 and 11, and the NaCI concentration from 0.45 to 1.8%. The phases formed were studied visually, rheologically and with cryo-TEM. Some mixtures containing catanionic vesicles and micelles were selected for drug release studies from gels, varying the pH and NaCI concentration here as well. Both catanionic systems investigated proved relatively resilient to changes in the ionic strength. Changes in pH, on the other hand, caused marked effects to the phase behavior in both systems. The influence of pH was particularly strong in the drug-rich part of the tetracaine/SDS system, where increasing the pH causes precipitation. As expected, the drug release in both systems was somewhat affected by changes in both pH and ionic strength, but remained in all cases significantly prolonged as compared to the release of free, non-complexed, drug. These studies show that catanionic mixtures may be used to obtain prolonged drug release from gels, and that the concept also works when the gels are exposed to a pH that is a couple of units above the pKa of the cationic component. Furthermore, the ionic strength has no pronounced effect on the drug release, as long as it is kept within reasonable pharmaceutical levels.
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| 8. |
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| 9. |
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| 10. |
- Fichtner, Frauke, et al.
(författare)
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Drug release from compacted single inert matrix agglomerates
- 2007
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Ingår i: Journal of Drug Delivery Science and Technology. - 1773-2247. ; 17:4, s. 273-277
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Tidskriftsartikel (refereegranskat)abstract
- The effect of compaction on the drug release from single, sodium chloride loaded, microcrystalline cellulose agglomerates of different porosities was investigated in this study. The drug release from uncompacted agglomerates and from agglomerates regained from tablets compacted at a range of different compaction pressures was monitored measuring the conductivity of the dissolution medium in a recirculation flow-through system. The drug release profiles were described using the mean dissolution time (MDT), the variation of dissolution time (VDT) and the relative dispersion coefficient (RD). It was found that depending on physical structure changes of the matrix, the drug release rate of compacted agglomerates could be enhanced or retarded in comparison with uncompacted agglomerates. The retardation is suggested to be due to a densification of the matrix and the enhancement due to a crack formation in the external surface of the matrix.
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| 11. |
- Fransén, Nelly, et al.
(författare)
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The in vitro transport of dihydroergotamine across porcine nasal respiratory and olfactory mucosa and the effect of a novel powder formulation
- 2007
-
Ingår i: Journal of Drug Delivery Science and Technology. - 1773-2247. ; 17:4, s. 267-271
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Tidskriftsartikel (refereegranskat)abstract
- The objective was to investigate the transport of dihydroergotamine (DHE) across porcine nasal respiratory and olfactory mucosa and to evaluate the absorption enhancing effect of a novel dry powder formulation compared with a reference solution with the horizontal Ussing chamber method. The powder formulation was obtained by mixing micronized DHE particles and mucoadhesive carrier particles (sodium starch glycolate) to create an interactive mixture. The horizontal Ussing chamber method was chosen as the in vitro model since it provides the opportunity to apply a dry powder formulation and compare the transport across the two types of nasal mucosa. A histological evaluation confirmed that the mucosa had been correctly isolated. The results showed no significant difference in the absorption from the powder formulation compared with the reference solution, but the transport of DHE was significantly higher across olfactory mucosa than across respiratory mucosa. This may be explained by facilitated transport through paracellular transfer along the olfactory nerve cells.
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| 12. |
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| 13. |
- Gulsun, T., et al.
(författare)
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Preparation and characterization of furosemide nanosuspensions
- 2018
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Ingår i: Journal of Drug Delivery Science and Technology. - : Elsevier BV. - 1773-2247. ; 45, s. 93-100
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Tidskriftsartikel (refereegranskat)abstract
- Furosemide, a widely used loop diuretic, has a low aqueous solubility, and low permeability. Nanosuspensions have been widely used to increase the solubility of poorly soluble drugs. The aim of this study was to develop and characterize furosemide containing nanosuspensions. Furosemide nanosuspensions with Tween 80, were prepared using high pressure homogenization method using ultrasonic probe or ultra turrax, ball milling method, and combination of these methods. The physicochemical properties of furosemide, physical mixture and nanosuspensions were evaluated by FT-IR, DSC and X-ray analyses. Particle size, polydispersity index, zeta potential, solubility and permeability of nanosuspensions were also determined. FT-IR analysis revealed that characteristic peaks of furosemide were seen in all formulations. X-ray analysis indicated that crystalline structure of furosemide was preserved in nanosuspensions. The particle size of furosemide decreased significantly (p < 0.05) by using nanosuspension technology. Furosemide solubility was pH-dependent, and impact of nanosuspension on the solubility was more pronounced at lower pH values (e.g. pH 1.2). Furosemide permeability seemed to be influenced by nanosuspension preparation method. In conclusion, nanosuspension technology seems to be a promising approach for enhancement of solubility and permeability properties of poorly water soluble compounds, and it has an excellent potential to improve the bioavailability of such compounds. © 2018 Elsevier B.V.
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| 14. |
- Hagen, Eirik, et al.
(författare)
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Use of interactive mixtures to obtain mini-tablets with high dose homogeneity for paediatric drug delivery
- 2016
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Ingår i: Journal of Drug Delivery Science and Technology. - : Elsevier BV. - 1773-2247. ; 34, s. 51-59
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Tidskriftsartikel (refereegranskat)abstract
- Mini-tablets are suitable for children since they are easy to swallow and offer dose flexibility by adjustment of the number of units. The main objective was to investigate the use of interactive mixtures as a means to obtain high dose homogeneity in mini-tablets. The effect of carrier particle properties, mixing time, mixing equipment and sample size on homogeneity was evaluated. Micronized sodium salicylate (1% w/w) was mixed with different size fractions of spray-dried and granulated mannitol. The degree of homogeneity was expressed as the relative standard deviation (RSD). Mini-tablets were prepared from the interactive mixtures and characterized with respect to uniformity of mass and content, dose homogeneity, tablet strength, wetting time and disintegration time. Generally, RSD decreased with increasing mixing times, and levelled out around 3-4%. The lowest RSD was achieved with carrier particles of intermediate sizes; 125-180 mu m, 180-250 mu m and 250-355 mu m. The tumbling mixer was considered to be more suitable than the planetary mixer and longer mixing times were required to reach high degree of homogeneity in the smaller sample size. Mini-tablets showed high dose homogeneity as well as appropriate tensile strength and disintegration time to be suitable as orally disintegrating mini-tablets for children.
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| 15. |
- Hellberg, Emma, et al.
(författare)
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Evaluation of dissolution techniques for orally disintegrating mini-tablets
- 2021
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Ingår i: Journal of Drug Delivery Science and Technology. - : Elsevier. - 1773-2247. ; 61
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Tidskriftsartikel (refereegranskat)abstract
- Mini-tablets are suitable for paediatric as well as geriatric use since they may provide flexible and accurate dosing and administration. Due to the minute tablet size, there is a need for new standardized quality evaluation procedures and conventional techniques may have to be adopted. The main objective of the study was to evaluate different dissolution techniques for orally disintegrating mini-tablets. Dissolution tests using mini-paddle apparatus were compared with standard size paddle apparatus, and the effect of paddle rotation speed was evaluated. Also, the filter choice, and its impact on dissolution, was considered. Sodium salicylate was used as a model drug substance and was mixed with different size fractions of mannitol. The powder mixtures were compacted into 2 mm flat faced tablets. The mini-tablets were characterized regarding weight and content uniformity, tensile strength, friability, disintegration and dissolution. Similar dissolution profiles were obtained with both mini and standard equipment. The paddle rotation speed affected the dissolution profiles; a low paddle speed resulted in a slower dissolution. Furthermore, choosing a chemically inert filter will increase the likelihood of obtaining reliable and accurate results. An appropriately designed dissolution test using mini-paddle apparatus is required prior to further implementation in quality control procedures.
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| 16. |
- Kirejev, Vladimir, 1984, et al.
(författare)
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Multiphoton microscopy – a powerful tool in skin research and topical drug delivery science
- 2012
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Ingår i: Journal of Drug Delivery Science and Technology. - 1773-2247. ; 22:3, s. 250-259
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Tidskriftsartikel (refereegranskat)abstract
- Multiphoton microscopy (MPM) has become a powerful complementary tool in biomedical research, enabling non-invasive three-dimensional imaging of tissue with high resolution. The major advantage is that investigations and visualization can be performed without mechanical destruction of the sample through tissue sectioning. This review will give a brief introduction to the technology, accompanied by examples of how the technique can be implemented within the field of skin research. Specifically, MPM has already made it possible to visualize cellular morphology and the cutaneous distribution of topically applied compounds applied to intact skin. MPM provides information that can be used to assess the bioavailability of drugs and to visualize drug penetration pathways into skin. MPM has also been implemented as a tool for obtaining non-invasive tissue biopsy based on skin autofluorescence in connection to diagnostics of skin cancer. We will also briefly present some recent results where MPM has been used to track cyclodextrin based drugs applied topically. Finally, we will discuss some future challenges of the technology, including label-free imaging, multimodal techniques, and quantitative imaging.
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| 17. |
- Lennernäs, Hans, et al.
(författare)
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Oral drug absorption and the biopharmaceutics classification system
- 2007
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Ingår i: Journal of drug delivery science and technology. - 1773-2247. ; 17:4, s. 237-244
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Forskningsöversikt (refereegranskat)abstract
- Bioavailability (BA) and bioequivalence (BE) play a central role in pharmaceutical product development and BE studies are presently being conducted for New Drug Application (NDAs) of new compounds, in supplementary NDAsfor new medical indications and product line extensions, in Abbreviated New Drug Applications (ANDAs) of generic products and in applications for scale-up and post-approval changes. The Biopharmaceutics Classification System (BCS) has been developed to provide a scientific approach for classifying drug compounds based on solubility as related to dose and intestinal permeability in combination with the dissolution properties of the oral immediate release (IR) dosage form. The aim of BCS is to provide a regulatory tool for replacing certain BE studies by accurate in vitro dissolution tests. The aim of the present review is to present the status of BCS and discuss its future application in pharmaceutical product development. This will be discussed in relation to novel findings in human intestinal absorption, permeability and solubility. The future application of BCS is likely to be increasingly important if the BCS borders for certain Class II and III drugs are extended. The BCS is also a simple tool in early drug development to determine the rate-limiting step in the oral absorption process, which has facilitated the information between different experts involved in the overall drug development process. In the future, this increased awareness of a proper biopharmaceutical characterization of new drugs may result in drug molecules with a sufficiently high permeability, solubility and dissolution rate that will automatically increase the importance of BCS as a regulatory tool over time.
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| 18. |
- Michel, Bastien, et al.
(författare)
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Inclusion complex formation between sulfadiazine and various modified β-cyclodextrins and characterization of the complexes
- 2022
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Ingår i: Journal of Drug Delivery Science and Technology. - : Editions de Sante. - 1773-2247. ; 76
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Tidskriftsartikel (refereegranskat)abstract
- β-Cyclodextrin (β-CD) and its derivatives are cyclic oligosaccharides which present the ability to form inclusion complexes with hydrophobic molecules and can bring new functionalities to a wide range of materials. As of today, the most used prophylactic drugs for wound dressing applications are sulfadiazine (SD) and its derivatives silver sulfadiazine (SSD). These drugs are used to prevent infections of the wounds; however, their low intrinsic water-solubility is a hindrance to their use. In this study, the inclusion complex formation between SD/SSD and the various β-CDs were assessed with various protocols. Isothermal Titration Calorimetry (ITC) experiments led to the conclusion that the formation constants measured for SD and SSD are sufficiently similar meaning that SD can be considered as a satisfactory model molecule. Phase Solubility Diagram (PSD) were built for SD and the various β-CDs, highlighting a 1:1 stoichiometry of inclusion and a linear increase in solubility of SD with increasing concentration of β-CDs- The formation constant ranged from 197 M−1 to 245 M−1 for the different β-CDs. X-Ray diffraction (XRD) and Differential Scanning Calorimetry (DSC) experiments revealed the different physico-chemical properties affected by the formation of an inclusion complex. Finally, Nuclear Magnetic Resonance (NMR) experiments confirmed the depth of penetration of SD inside the β-CDs cavity as well as the orientation of SD, highlighting the fact that CM-β-CDs induce a deeper penetration than other β-CDs.
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| 19. |
- Neuhoff, Sibylle, et al.
(författare)
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Advantages and disadvantages of using bovine serum albumin and/or Cremophor EL as extracellular additives during transport studies of lipophilic compounds across Caco-2 monolayers
- 2007
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Ingår i: Journal of drug delivery science and technology. - 1773-2247. ; 17:4, s. 259-266
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Tidskriftsartikel (refereegranskat)abstract
- The effects of Cremophor EL (CEL) and bovine serum albumin (BSA) on the active and passive permeation of BCS class II compounds (felodipine, asimadoline) were studied across Caco-2 cells. The effect of BSA on either or both sides of the monolayers, apically applied CEL in the presence ofbasolateral BSA and the effect ofaddition of CEL on P-gp by the use ofquinidine were investigated. Presence of 4% BSA improved sink conditions and recovery from 60 to 95% for both felodipine and asimadoline. Efflux ratios obtained under comparable sink conditions, indicated that felodipine was transported by passive diffusion, while quinidine and asimadoline were transported actively. CEL decreased the transport rate for felodipine and asimadoline in the absorptive direction and increased in the secretory direction at different CEL concentrations, most likely due to the incorporation of drug into micelles. Our results indicate that inclusion of BSA is generally sufficient to increase the recovery for lipophilic BCS class II compounds. The overall effect of CEL on the permeability of a drug is compound specific and, therefore, less predictable and cannot be recommended.
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| 20. |
- Patel, Vyoma K., et al.
(författare)
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Tackling the cytokine storm using advanced drug delivery in allergic airway disease
- 2023
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Ingår i: Journal of Drug Delivery Science and Technology. - : Elsevier. - 1773-2247. ; 82
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Forskningsöversikt (refereegranskat)abstract
- Asthma is one of the leading causes of mortality worldwide presenting a huge socio-economic burden with rising morbidity and mortality rates. It is a chronic inflammatory airway disease that is eminent with multiple epidemiological and pathophysiological features such as over production of pro-inflammatory cytokines that triggers an uncontrolled aberrant inflammatory response known as 'cytokine storm'. This phenomenon interferes with the signalling and production of cytokines over time leading to the progression of disease and the development of complications that lead to fatal consequences in many individuals. Targeting this overproduction and signalling of cytokines may prove a promising approach to develop novel cytokine specific therapies in the treatment of asthma. This review discusses on the various pharmacological strategies, recent advancements in drug delivery systems and significant findings from clinical trials that may have a potential to outweigh the limitations of the current therapies in the treatment of asthma.
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| 21. |
- Persson, Eva M., et al.
(författare)
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Is there an effect of food on the biliary secretion of cyclosporine and three in vivo formed metabolites in a porcine model?
- 2007
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Ingår i: Journal of Drug Delivery Science and Technology. - 1773-2247. ; 17:4, s. 253-258
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Tidskriftsartikel (refereegranskat)abstract
- The aim of this study was to investigate the effect of lipids and P-glycoprotein (P-gp) inhibition on the biliary secretion of cyclosporine (CsA) and in vivo formed metabolites in pigs. A parallel group design including 12 pigs in four groups and a combined single-pass intestinal perfusion and bile collection method was employed. CsA was perfused through the jejunum in an isotonic fluid alone and with verapamil or lipids added. The study showed that there was no difference between the administration groups, except for the fraction of the absorbed dose that was excreted in bile was twice as high when CsA was administered together with lipids. In conclusion, CsA is excreted via the biliary route in pigs without any significant involvement of P-gp. Concomitant food-intake could increase the secretion to the bile, presumably by prolonged associations between the CsA and the lipid species.
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| 22. |
- Reijmar, K., et al.
(författare)
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Bactericidal and hemolytic properties of mixed LL-37/surfactant systems
- 2007
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Ingår i: Journal of drug delivery science and technology. - 1773-2247. ; 17:4, s. 293-297
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Tidskriftsartikel (refereegranskat)abstract
- The interaction between acyl chain homologues (C10 and C12) of n-acyl β-D-maltoside and the antimicrobial peptide LL-37 (LLGDFFRKSKEKIGKEFKRIVQRIKDFLRNLVPRTES) was investigated. Emphasis was placed on peptide-micelle complexation and its consequences for peptide proteolytic stability, as well as bactericidal and hemolytic effects of the mixed systems. From circular dichroism and liposome leakage experiments, it was found that LL-37 interacts with both surfactants investigated, and that this reduces the effective free peptide concentration. Analogously, LL-37 displayed increased proteolytic stability towards Pseudomonas aeruginosa elastase in surfactant solution. Despite this, conditions can be found at which the bactericidal effect of mixed peptide-surfactant systems is comparable to that of free LL-37. However, also a number of challenges to this type of antimicrobial peptide (AMP) carrier system were identified, notably related to reduction of bactericidal effect for some systems, and occurrence of hemolysis for mixed peptide-surfactant systems displaying advantageous bactericidal effects. Any use of such AMP carrier systems will therefore have to be carefully optimized in order to retain bactericidal activity and minimize toxicity.
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| 23. |
- Sartaj, Km, et al.
(författare)
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Detailed investigation on FAME capped metal nanocomposite synthesis as potential antifungal agent
- 2024
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Ingår i: Journal of Drug Delivery Science and Technology. - : Elsevier. - 1773-2247. ; 98
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Tidskriftsartikel (refereegranskat)abstract
- Oleaginous yeast lipid derived fatty acid methyl esters (FAMEs) are renowned for their exceptional potential towards bioenergy production specially in biodiesel domain. FAME application in other realms of biotechnology including nanotechnology (offer large possibilities for industry and contemporary science) has hitherto remained unexplored. Present study has investigated the novel use of FAME as biogenic capping agents to synthesize amphotericin B loaded CuO-CT (CT: chitosan) nanocomposites. The utilization of FAME-modified formulation (CuO-CTY@.L.F-AmpB) is evident in providing steric stability, as indicated by various physiochemical characterization techniques, accompanied by a low polydispersity index 0.24 ± 0.06 and a partial negative surface charge. Additional insights from HRTEM reveal a nanocarrier with a rod-shaped morphology, featuring 40–50 nm length and a 5–6 nm diameter. Amphotericin B release from CuO-CT@Y.L.F-AmpB followed a sustained pattern for up to 100 h, suggested FAME coating facilitated the drug release for a longer time duration. FAME stabilization has improved antibiofilm activity against Candida albicans (BEC50: 15 μg/mL) evinced by multitude assays that were found concordant with each other. A comprehensive FAME profiling conducted through GC-MS unveiled the predominance of oleic (84.02 ± 0.30 %) and palmitic acid methyl esters (9.40 ± 0.15 %) in the sample. This observation identifies them as concealed factors contributing to the stability of the nanocomposite. Conclusively, present study stipulated FAME as an efficient capping agent where it impart stability as well as efficacy to the nanocarrier. Moreover, current research work opens an innovative path for biorefinery approach integrating simultaneous production of lipid and multiphase nano-material synthesis, vital for a sustainable and circular bio-economy.
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| 24. |
- Shakir, Nida, et al.
(författare)
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Pirarubicin loaded biodegradable nanoparticles downregulate IL-6, COX-II and TNF-alpha along with oxidative stress markers in comparison to conventional pirarubicin in healthy albino rats
- 2023
-
Ingår i: Journal of Drug Delivery Science and Technology. - : Elsevier. - 1773-2247. ; 84
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Tidskriftsartikel (refereegranskat)abstract
- Pirarubicin (PRB) is an anthracycline antibiotic that has shown equal or superior cytotoxicity compared to doxorubicin. However, the detailed toxicological profile for Pirarubicin has not yet been investigated. The present study was designed to access the acute and chronic toxicity of the nanoformulation coupled with in-flammatory and oxidative stress responses. PRB was encapsulated in PLGA nanoparticles and was physico-chemically evaluated. The nanoparticle size was found to be 420.0 +/- 8.2 nm with an encapsulation efficiency of 80.3 +/- 3.1%. The SEM images showed spherical nanoparticles while the drug release in PBS (pH 7.4) was estimated to be 72.5 +/- 3.5%. Acute toxicity in female albino rats was conducted for 14 days at two dosage levels (i.e., 5 and 300 mg/kg) once a week through an intravenous route. A repeated toxicity study was conducted for 28 days at 3 different dosage levels (i.e., 30, 60 and 100 mg/kg) weekly. No mortality was observed during the experimentation period. Toxicity assessment of body weights, hematological parameters, blood biochemistry, histopathological evaluation of internal organs and relative organ weight percentage was done. Inflammatory markers quantification (COX-II, TNF-alpha, IL-6) along with the generation of oxidative stress (SOD, GSH-ST, GSH-PX, MDA, and H2O2) was also investigated in a repeated 28 days toxicity study. The nanoformulation did not have any effect on the behavioral pattern, food, water consumption or body weights. The abnormalities in function and morphology of the organs produced by nano-formulated PRB were dose-dependent and reversible. The serum sample of rats treated with nanoparticles exhibited a non-significant difference in levels of COX-II, TNF-alpha, and IL-6 as compared to the normal saline (NS) group. Altogether the results offered us evidence about the safety profile of Pirarubicin loaded PLGA nanoparticles (PRB-NP) as compared to PRB alone.
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| 25. |
- Tariq, Imran, et al.
(författare)
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Ameliorative delivery of docetaxel and curcumin using PEG decorated lipomers : A cutting-edge in-vitro/ in-vivo appraisal
- 2024
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Ingår i: Journal of Drug Delivery Science and Technology. - : Elsevier. - 1773-2247. ; 97
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Tidskriftsartikel (refereegranskat)abstract
- The development of a PEG-decorated lipid-polymer hybrid system camouflaged with natural and synthetic chemotherapeutic moieties is an influential approach melding the biomimetic properties of long-circulating vesicles to utilize different mechanisms to dwindle the tumor growth. Therefore, a safe and efficient lipid-coated nano-particulate system (LCNPs) was proposed to investigate the in-vitro, ex-vivo and in-vivo demeanors of such amalgamation.Docetaxel loaded PLGA nanoparticles (DTX-NPs) were prepared by solvent evaporation while curcumin liposomes were mapped out using the film hydration method. Physicochemical characterizations were executed in terms of size, surface morphology, differential scanning calorimetry (DSC) and fourier-transform infrared spectroscopy (FTIR). In-vitro cytotoxicity was effectuated using MCF-7 cell line. Hemolysis, erythrocyte aggregation and acute in-vivo toxicity were carried out to establish the biocompatibility. The hydrodynamic diameters of samples were in the nano-range and corresponded to the findings of scanning electron microscopy (SEM) and atomic force microscopy (AFM). The absence of distinctive peaks of DTX-NPs in FTIR and DSC analysis of LCNPs depicts the shielding of the lipid bilayer over the nanoparticle. Cytotoxicity induced by the LCNPs represented the efficient delivery of cargo to the tumor cells. LCNPs also exhibited the least toxicity under ex-vivo and in-vivo circumstances compared to free drugs. Additionally, histological studies showed no evidence of substantial necrosis. Additionally, histological studies showed no evidence of notable necrosis.
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| 26. |
- Vijayakumar, Mahalingam Rajamanickam, et al.
(författare)
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Trans resveratrol loaded DSPE PEG 2000 coated liposomes: An evidence for prolonged systemic circulation and passive brain targeting
- 2016
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Ingår i: Journal of Drug Delivery Science and Technology. - : Elsevier BV. - 1773-2247. ; 33, s. 125-135
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Tidskriftsartikel (refereegranskat)abstract
- Trans resveratrol (RSV) is a natural molecule proved for cardioprotective effects, vasodilation, anti-inflammatory, cancer preventive and therapeutic activities devoid of any potential side effects. Recently, anti cancer potential against glioma cells were also reported with proven molecular mechanisms. However, the therapeutic application of RSV in clinical disease management is restricted because of its rapid elimination from systemic circulation and thereby low biological half life in mammals. Therefore, the main objective of this study was to improve the systemic circulation and biological half life of RSV using DSPE PEG 2000 decorated (PEGylated) liposomes. Moreover, brain distribution of RSV loaded PEGylated liposomes (RSV-PEG-Lipo) and non-PEGylated liposomes (RSV-Lipo) was also evaluated for proving their passive brain targeting ability. In vitro drug release of both liposomes was found to be sustained up to 48 h. RSV-PEG-Lipo showed higher area under the curve, plasma half life and mean residence time and lower volume of distribution and clearance than that of pristine RSV solution and RSV-Lipo. Pharmaokinetics results clearly indicated that the RSV-PEG-Lipo will be promising tool for enhancing plasma half life and prolong the systemic circulation of RSV. Brain distribution studies revealed that the liposomal formulations can be applied as an effective tool for passive brain targeting useful in the treatment of glioma.
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