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Keywords = atomoxetine HCl

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14 pages, 3834 KiB  
Article
Xanthan-Gum/Pluronic-F-127-Based-Drug-Loaded Polymeric Hydrogels Synthesized by Free Radical Polymerization Technique for Management of Attention-Deficit/Hyperactivity Disorder
by Muhammad Suhail, I-Hui Chiu, Yi-Ru Lai, Arshad Khan, Noorah Saleh Al-Sowayan, Hamid Ullah and Pao-Chu Wu
Gels 2023, 9(8), 640; https://doi.org/10.3390/gels9080640 - 8 Aug 2023
Cited by 14 | Viewed by 2357
Abstract
Smart and intelligent xanthan gum/pluronic F-127 hydrogels were fabricated for the controlled delivery of atomoxetine HCl. Different parameters such as DSC, TGA, FTIR, XRD, SEM, drug loading, porosity, swelling index, drug release, and kinetics modeling were appraised for the prepared matrices of hydrogels. [...] Read more.
Smart and intelligent xanthan gum/pluronic F-127 hydrogels were fabricated for the controlled delivery of atomoxetine HCl. Different parameters such as DSC, TGA, FTIR, XRD, SEM, drug loading, porosity, swelling index, drug release, and kinetics modeling were appraised for the prepared matrices of hydrogels. FTIR confirmed the successful synthesis of the hydrogel, while TGA and DSC analysis indicated that the thermal stability of the reagents was improved after the polymerization technique. SEM revealed the hard surface of the hydrogel, while XRD indicated a reduction in crystallinity of the reagents. High gel fraction was achieved with high incorporated contents of the polymers and the monomer. An increase in porosity, drug loading, swelling, and drug release was observed with the increase in the concentrations of xanthan gum and acrylic acid, whereas Pluronic F-127 showed the opposite effect. A negligible swelling index was shown at pH 1.2 and 4.6 while greater swelling was observed at pH 7.4, indicating a pH-responsive nature of the designed hydrogels. Furthermore, a higher drug release was found at pH 7.4 compared to pH 1.2 and 4.6, respectively. The first kinetics order was followed by the prepared hydrogel formulations. Thus, it is signified from the discussion that smart xanthan gum/pluronic F-127 hydrogels have the potential to control the release of the atomoxetine HCl in the colon for an extended period of time. Full article
(This article belongs to the Special Issue Advances in Smart and Tough Hydrogels)
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29 pages, 3584 KiB  
Article
Lyophilized Nasal Inserts of Atomoxetine HCl Solid Lipid Nanoparticles for Brain Targeting as a Treatment of Attention-Deficit/Hyperactivity Disorder (ADHD): A Pharmacokinetics Study on Rats
by Mahmoud H. Teaima, Merhan Taha El-Nadi, Raghda Rabe Hamed, Mohamed A. El-Nabarawi and Rehab Abdelmonem
Pharmaceuticals 2023, 16(2), 326; https://doi.org/10.3390/ph16020326 - 20 Feb 2023
Cited by 10 | Viewed by 4384
Abstract
The study aims to investigate the ability of lyophilized nasal inserts of nanosized atomoxetine HCl solid lipid nanoparticles (ATM-SLNs) to transport atomoxetine (ATM) directly to the brain and overcome the first-pass metabolism. In this case, 16 formulae of (ATM-SLNs) were prepared using hot [...] Read more.
The study aims to investigate the ability of lyophilized nasal inserts of nanosized atomoxetine HCl solid lipid nanoparticles (ATM-SLNs) to transport atomoxetine (ATM) directly to the brain and overcome the first-pass metabolism. In this case, 16 formulae of (ATM-SLNs) were prepared using hot melt emulsification, stirring and ultrasonication method technique. A full factorial design was established with 24 trials by optimization of four variables; lipid type (Compritol 888 ATO or stearic acid) (X1), lipid to drug ratio [(1:2) or (2:1)] (X2), span 60: Pluronic f127 ratio [(1:3) or (3:1)] (X3) and probe sonication time (five or ten minutes) (X4). The prepared SLNs were characterized for entrapment efficiency (EE%), in-vitro drug release after 30 min (Q30min), particle size (PS), zeta potential (ZP) and polydispersity index (PDI). Design Expert® software was used to select the optimum two formulae. The morphological examination for the optimum two formulae was carried out using a transmission electron microscope (TEM). Furthermore, eight lyophilized nasal inserts were prepared by using a 23 full factorial design by optimization of three variables: type of (ATM-SLNs) formula (X1), type of polymer (NOVEON AA1 or HPMC K100m) (X2) and concentration of polymer (X3). They were evaluated for nasal inserts’ physicochemical properties. The two optimum inserts were selected by Design Expert® software. The two optimum insets with the highest desirability values were (S4 and S8). They were subjected to DSC thermal stability study and in-vivo study on rats. They were compared with atomoxetine oral solution, atomoxetine (3 mg/kg, intraperitoneal injection) and the pure atomoxetine solution loaded in lyophilized insert. (ATM-SLNs) showed EE% range of (41.14 mg ± 1.8% to 90.6 mg ± 2.8%), (Q30min%) of (27.11 ± 5.9% to 91.08 ± 0.15%), ZP of (−8.52 ± 0.75 to −28.4 ± 0.212% mV), PS of (320.9 ± 110.81% nm to 936.7 ± 229.6% nm) and PDI of (0.222 ± 0.132% to 0.658 ± 0.03%). Additionally, the two optimum (ATM-SLNs) formulae chosen, i.e., F7 and F9 showed spherical morphology. Nasal inserts had assay of drug content of (82.5 ± 2.5% to 103.94 ± 3.94%), Q15min% of (89.9 ± 6.4% to 100%) and Muco-adhesion strength of (3510.5 ± 140.21 to 9319.5 ± 39.425). DSC results of S4 and S8 showed compatibility of (ATM) with the other excipients. S8 and S4 also showed higher trans-nasal permeation to the brain with brain targeting efficiency of (211.3% and 177.42%, respectively) and drug transport percentages of (52.7% and 43.64%, respectively). To conclude, lyophilized nasal inserts of (ATM-SLNs) enhanced (ATM) trans-nasal drug targeting permeation and brain targeting efficiency. Full article
(This article belongs to the Special Issue Brain Theranostics: Focus on Drug Delivery and Outcomes)
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