| 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
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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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