Abstract
The use of nanocarrier delivery systems for direct nose to brain drug delivery shows promise for achieving increased brain drug levels as compared to simple solution systems. An example of such nanocarriers is emulsomes formed from lipid cores surrounded and stabilised by a corona of phospholipids (PC) and a coating of Tween 80, which combines the properties of both liposomes and emulsions. Oxcarbazepine (OX), an antiepileptic drug, was entrapped in emulsomes and then localized in a poly(lactic acid-co-glycolic acid)-poly(ethylene glycol)-poly(lactic acid-co-glycolic acid) (PLGA-PEG-PLGA) triblock copolymer thermogel. The incorporation of OX emulsomes in thermogels retarded drug release and increased its residence time (MRT) in rats. The OX-emulsome and the OX-emulsome-thermogel formulations showed in vitro sustained drug release of 81.1 and 53.5%, respectively, over a period of 24 h. The pharmacokinetic studies in rats showed transport of OX to the systemic circulation after nasal administration with a higher uptake in the brain tissue in case of OX-emulsomes and highest MRT for OX-emulsomal-thermogels as compared to the IN OX-emulsomes, OX-solution and Trileptal® suspension. Histopathological examination of nasal tissues showed a mild vascular congestion and moderate inflammatory changes around congested vessels compared to saline control, but lower toxic effect than that reported in case of the drug solution.
Highlights
IntroductionHydrogels that are prepared from “intelligent” or “smart” polymers and capable of exhibiting a physicochemical response in a nonlinear manner to an external stimuli, such as temperature [1,2], pH [3], light [4], counter-ion changes [5] and biological molecules [6] have been extensively investigated
Hydrogels that are prepared from “intelligent” or “smart” polymers and capable of exhibiting a physicochemical response in a nonlinear manner to an external stimuli, such as temperature [1,2], pH [3], light [4], counter-ion changes [5] and biological molecules [6] have been extensively investigatedPharmaceutics 2018, 10, 217; doi:10.3390/pharmaceutics10040217 www.mdpi.com/journal/pharmaceuticsPPhhaarrmmaacceeuuttiiccss22001188,1100,2x1F7OR PEER REVIEW22 ooff 2109 in the literature
The use of nanocarrier delivery systems for direct nose to brain drug delivery shows promise for achieving increased brain drug levels as compared to simple solution systems. An example of such nanocarriers is emulsomes formed from lipid cores surrounded and stabilised by a corona of phospholipids (PC) and a coating of Tween 80, which combines the properties of both liposomes and emulsions
Summary
Hydrogels that are prepared from “intelligent” or “smart” polymers and capable of exhibiting a physicochemical response in a nonlinear manner to an external stimuli, such as temperature [1,2], pH [3], light [4], counter-ion changes [5] and biological molecules [6] have been extensively investigated. These polymers have great potential in drug delivery and tissue engineering [7,8,9], iinn tahdedliittieornattuorsee.nTshoerseapnodlyvmalveers h[1a0v]e. Great potential in drug delivery and tissue engineering [7,8,9], in addTihteiornmtoosesnensistoivrse apnodlyvmalevress a[1re0].a subcategory of smart polymers that undergo temperatureinduTcehdermreovseernsisbitleivesol-pgoellymtraenrssitiaorne upaonsuhbecaatitnego/croyolinogf osfmtahret apquoleyomuserspolythmaet r usonlduetirogno. TDemrupgesr/faoturmreu-ilnatdiouncesdserqeuvesrtseibreled swoli-thgeinl trhaensseitciopnoulypmonerhs ebaytinsigm/pcoleolminigxinogf tahre aqdumeionuissteproedlymasear ssoolluuttiioonn. ScShcehmemataicticdiadgiargamramof othf ethsoel-sgoell-gtrealntsriatinosnitioofnBAofBBtAypBe tpyopley(lpaocltyic(laccitdic-coa-cgidly-co-lgiclyaccoidli)capcoidly)(-eptohlyyl(eentheylgelnyecogll)y-pcooll)y-(ploaclyti(clacatcicida-cciod-g-cloy-cgollyicolaiciadc)id()P(LPGLGAA-P-EPGEG-P-LPGLGAA) )ttrri-i-bblolocckk ccooppoollyymmerr aaqquueeoouuss ssoolluuttiioonn iinnrreessppoonnsseettootteemmppeerraattuurree
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