| 1. |
- 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
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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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| 2. |
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| 3. |
- 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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| 4. |
- 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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| 5. |
- 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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| 6. |
- 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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| 7. |
- 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
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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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| 8. |
- 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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