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Carriers for Brain Targeting
Published in Raj K. Keservani, Anil K. Sharma, Rajesh K. Kesharwani, Nanocarriers for Brain Targeting, 2019
Md. Sahab Uddin, Mst. Marium Begum
Nasal administration constitutes a potentially efficacious way to achieve the brain uptake of neuroactive agents (Fine et al., 2014, 2015; Illum, 2000; Vyas et al., 2005). Drugs deposited on the olfactory epithelium of the nose can obtain direct access to the CNS, precisely the CSF, via transcellular transport through olfactory epithelial cells. The absorbed drugs in the CSF then diffuse into the ISF and then penetrate the brain parenchyma (Illum, 2000, 2004; Thorne and Frey, 2001). Furthermore, drugs that are deposited on the olfactory epithelium can be transported into the brain parenchyma by olfactory neurons or trigeminal nerves that reach the nasal cavity (Finger et al., 1990; Illum, 2000; Johnson et al., 2010). Ultimately, the nasally administered drugs can be absorbed into the systemic circulation from the respiratory epithelium (Cho et al., 2014), and if they are capable of crossing the BBB, they can then reach the CNS (Illum, 2000).
The modern pharmacological approach to diabetes: innovative methods of monitoring and insulin treatment
Published in Expert Review of Medical Devices, 2022
Iulian Tătaru, Oana M. Dragostin, Iuliu Fulga, Florentina Boros, Adelina Carp, Ariadna Maftei, Carmen L. Zamfir, Aurel Nechita
The intranasal route of administration is noninvasive and can be approached for insulin administration [55]. The nasal cavity has a large absorption surface, a rich vascularization [56] and the advantage of avoiding the first-pass metabolism. The permeability of the nasal mucosa to large insulin molecules is increased with the help of ‘absorption enhancers,’ and its transport is done by passive diffusion [57] or carrier-mediated pathway [58]. To overcome the disadvantages of this route of administration, mucoadhesive formulations are used, which by prolonging the contact time, reduce the mucociliary clearance effect [59], and through proteolytic enzyme inhibitors, enzymatic degradation [60] or local irritation is avoided. Thus, the ease with which the patient approaches this route of administration for long-term therapies, increases his adherence to treatment [60]. In addition, nasal administration of insulin also provides better control of postprandial hypoglycemia [61].
Spray-dried nanoparticle-loaded pectin microspheres for dexamethasone nasal delivery
Published in Drying Technology, 2019
Bisera Jurišić Dukovski, Lea Mrak, Katarzyna Winnicka, Marta Szekalska, Marina Juretić, Jelena Filipović-Grčić, Ivan Pepić, Jasmina Lovrić, Anita Hafner
DNM and DM microspheres were characterized by high entrapment efficiency, showing no significant difference in drug content (3.3 ± 0.3 and 3.8 ± 0.9%, respectively). Considering the targeted daily dose of Dex (400–800 µg[3]) and the quantity of powder that can be administered per nostril per shot (about 10–25 mg[18]), the obtained drug content within the microspheres is sufficient to enable nasal administration of Dex therapeutic dose. In addition, complex carrier developed to improve the Dex bioavailability/therapeutic effect, acts at the same time as a filler excipient that contributes largely to the total mass of the powder to be delivered, ensuring accurate Dex dosing.[18]
Nasal mucoadhesive in situ gelling liquid crystalline fluid precursor system of polyene antibiotic for potential treatment of localized sinuses aspergillosis post COVID infection
Published in Journal of Dispersion Science and Technology, 2023
Marzooka Kazi-Chishti, Javeed Shaikh, Nazimuddin Chishti, Mohamed Hassan Dehghan
The pharmacokinetic and tissue distribution of NYS were determined for IGFPS (FG9). For these studies IGFPS was administered to Wistar rats by the nasal route and the drug solution to another group of Wistar rats by IV route. Both groups were given the same dose of NYS, that is, 8 mg/kg. The mean plasma concentrations of NYS for FG9 and intravenous injection of NYS solution over time is depicted in Figure 12. The data obtained for pharmacokinetic parameters and tissue distribution of NYS is shown in Table 5. Subsequent to I.V. administration of the drug solution, the Cmax (34.66 ± 2.51 μg/ml) was achieved in 10 ± 1.11 mins and declined swiftly. Following intranasal administration of FG9, the Cmax value 11.79 ± 2.31 μg/ml was realized in 20 min and the curve showed a decline similar to I.V. The possible reason for such kind of behavior can be attributed to some amount of drug being directly absorbed from the nasal cavity into the central nervous system via the olfactory epithelium.[20] The study performed by Girotra and her coworkers have identified multi-targeted receptor activity of nystatin for anti-migraine potential and have developed its brain targeted chitosan nanoformulation.[89] The values of AUC0-∞, Cmax, and Tmax for i.v. solution and intranasal FG9 formulation were found to be significantly different (P < 0.05); though, both groups demonstrated similar curve profile. The apparent distribution of the drug from the test (FG9) after nasal administration was insignificantly (P > 0.05) in comparison to IV solution. The elimination was similar for i.v. and intranasal groups, as the means of t1/2, Kel, and Cl for the two groups showed no significant statistical deviation. Tissue distribution was also estimated and compared among both the groups it was seen that for intranasal formulation FG9 the amount of NYS was minimal in the lungs whereas higher concentration of drug was seen in kidneys but was comparatively lower than the I.V. groups. This kind of tissue distribution could be due to single dose regimen study. So as to achieve higher concentration of drug in lungs it may either require high doses or multiple dose regimen administration.[90] As polyene treatment has been related to nephrotoxicity, lower levels of nystatin in the kidneys following intranasal administration implies the possibility of reduced toxicity.[31,91]