2022
DOI: 10.3390/pharmaceutics14030588
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Strategies to Improve Drug Strength in Nasal Preparations for Brain Delivery of Low Aqueous Solubility Drugs

Abstract: Intranasal administration is a promising route for brain drug delivery. However, it can be difficult to formulate drugs that have low water solubility into high strength intranasal solutions. Hence, the purpose of this work was to review the strategies that have been used to increase drug strength in intranasal liquid formulations. Three main groups of strategies are: the use of solubilizers (change in pH, complexation and the use cosolvents/surfactants); incorporation of the drugs into a carrier nanosystem; m… Show more

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Cited by 43 publications
(38 citation statements)
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“…They are slightly shifted from the accepted range. The pH of the prepared formulations should be close to the nasal mucosa’s (5.0 to 6.5) to avoid causing sensations of discomfort, irritation or toxicity in the nasal epithelium and/or enhanced mucociliary clearance (Pires et al., 2022 ). The mucoadhesion force of the prepared nasal inserts was ranged from 7063.2 ± 2.06 to 9319.5 ± 2.02 dyne/cm2 ( Table 6 ).…”
Section: Resultsmentioning
confidence: 99%
“…They are slightly shifted from the accepted range. The pH of the prepared formulations should be close to the nasal mucosa’s (5.0 to 6.5) to avoid causing sensations of discomfort, irritation or toxicity in the nasal epithelium and/or enhanced mucociliary clearance (Pires et al., 2022 ). The mucoadhesion force of the prepared nasal inserts was ranged from 7063.2 ± 2.06 to 9319.5 ± 2.02 dyne/cm2 ( Table 6 ).…”
Section: Resultsmentioning
confidence: 99%
“…Drug absorption and bioavailability of clozapine administered using the nasal route may be limited by its poor solubility. , Large, undissolved drug particles may cause nasal irritation and trigger the mucociliary clearance of the nasal cavity . In this study, the clozapine-encapsulated nanoemulsion sol–gel (CLZ-NESG) was developed using the aqueous titration method to determine the oil, surfactant, and cosurfactant with the highest drug solubility, followed by sonication.…”
Section: Resultsmentioning
confidence: 99%
“…There are several types of nanosystems, with the main categories being: polymeric nanosystems (polymeric nanoparticles, polymeric micelles), lipid nanoparticles (solid lipid nanoparticles, nanostructured lipid carriers), liposomes and related nanosystems (transfersomes, cubosomes, ethosomes), and nanometric emulsions [ 11 ]. Nevertheless, most of these systems have been reported to have short/low physical stability, low encapsulation efficiency, and non-biocompatible components, while requiring complex preparation methods, that are time- and resource-consuming, and that frequently use toxic organic solvents [ 12 , 13 , 14 ]. Yet, nanometric emulsions, which consist of colloidal liquid-in-liquid dispersions, can form spontaneously, evidencing the great advantage of having straightforward methods of preparation, that are not quite common.…”
Section: Potential Of Nanosystems For Brain Drug Deliverymentioning
confidence: 99%