A novel nasal almotriptan loaded solid lipid nanoparticles in mucoadhesive in situ gel formulation for brain targeting: Preparation, characterization and in vivo evaluation

Youssef, Nancy Abdel Hamid Abou; Kassem, Abeer Ahmed; Farid, Ragwa M.; Ismail, Fatma Ahmed; El-Massik, Magda A.; Boraie, Nabila

doi:10.1016/j.ijpharm.2018.07.014

Cited by 98 publications

(44 citation statements)

References 73 publications

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“…to 4.4 mg/kg of ZTP) was instilled in each nostril using micropipette. While dosing, rats were held at slant position on their back for proper instillation of dose [39]. At fixed time intervals, blood specimens were collected in EDTA-coated tubes by retro-orbital puncture under mild anesthesia and immediately brain was excised from the sacrificed (CO 2 exposure) animal.…”

Section: Animal Protocolmentioning

confidence: 99%

Intranasal Zotepine Nanosuspension: intended for improved brain distribution in rats

et al. 2019

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Background Zotepine (ZTP), an antipsychotic drug is well tolerated and particularly effective for treating negative symptoms of psychosis. But is limited by low oral bioavailability caused by substantial first pass metabolism and thereby less amount of drug reaches the brain due to blood brain barrier (BBB). Objectives Since ZTP displays dose dependent side effects, purpose of the contemporary study is to develop zotepine loaded nanosuspension (ZTP-NS) for increased brain targeting in rats at lower doses. Methods ZTP-NS is prepared by two techniques viz., sonoprecipitation (SP) and combination technique (high pressure homogenization preceded by precipitation) by employing various stabilizers. Optimized ZTP-NS was characterized for particle size, solid state, morphology and solubility. In vitro drug release of ZTP and formulations was conducted using Franz diffusion cell. Stability study was performed at different temperature conditions. Pharmacokinetic study was performed in Wistar rats to determine the bioavailability and brain distribution of ZTP after intra-nasal (IN) and intravenous (IV) administration. Histopathology of brain was done after repeated administration of IN ZTP dispersion and NS up to 14 days. Results The optimized ZTP-NS formulated with Pluronic F-127 (0.3%w/v), Hydroxypropyl methyl cellulose E15 (0.3%w/v) and soya lecithin (0.4%w/v) showed particle size of 519.26 ± 10.44 nm & 330.2 ± 12.90 nm and zeta potential of −21.7 ± 1.39 mV and − 18.26 ± 1.64 mV with sonoprecipitation and combination technique respectively. In vitro drug release was high (81.79 ± 3.23%) for ZTP-NS prepared by combination technique. Intranasal NS resulted in high brain concentrations of 8.6 fold (sonoprecipitation) and 10.79-fold hike in AUC 0-24h in contrast to intravenous ZTP solution. Histopathology results reveal no significant changes in brain microscopic images. Conclusion ZTP-NS was successfully developed, characterized and found that nanosuspension is a favorable approach for intranasal delivery of zotepine.

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Section: Animal Protocolmentioning

confidence: 99%

Intranasal Zotepine Nanosuspension: intended for improved brain distribution in rats

et al. 2019

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“…However, the low mucoadhesive activity of PLX 407 is its major disadvantage and restricts its widespread use.In the literature, some Pluronic-based preparations have been prepared by using additional mucoadhesive polymers. In the current study, NaCMC has been used to improve gel reliability, strength, and physicochemical properties due to its gelling and mucoadhesive properties [22,23].…”

Section: Resultsmentioning

confidence: 99%

Preparation and detailed characterization of fusidic acid loaded in situ gel formulations for ophthalmic application

Rençber¹,

Bulbul²,

Okur³

et al. 2021

jrp

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“…This approach used an in situ stable gel formation for IN administration [ 79 ]. For instance, polymers, almotriptan and opiorphin [ 80 , 81 ] were delivered to the brain via IN administration. The authors presented the physicochemical properties and biological effects of the nasal brain transport system using functionalized G5 PEG-PAMAM dendrimers prepared from G5 PAMAM dendrimers, bearing 128 primary amino groups, and encapsulating the poorly water soluble natural product paeonol (PAE, log P = 2.054, solubility = ∼560 mg/ml in pH 7.4 PBS) as a central neuroprotective agent [ 82 ] and protection in rat hippocampal neurons [ 83 ] with in situ gel ( Scheme 1 ).…”

Section: Nose To Brain Transport Pathways Of Drugs In Association Witmentioning

confidence: 99%

Non-invasive intranasal administration route directly to the brain using dendrimer nanoplatforms: An opportunity to develop new CNS drugs

Mignani

Shi

Karpus

et al. 2021

European Journal of Medicinal Chemistry

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There are several routes of administration to the brain, including intraparenchymal, intraventricular, and subarachnoid injections. The blood-brain barrier (BBB) impedes the permeation and access of most drugs to the central nervous system (CNS), and consequently, many neurological diseases remain undertreated. For past decades, to circumvent this effect, several nanocarriers have been developed to deliver drugs to the brain. Importantly, intranasal (IN) administration can allow direct delivery of drugs into the brain through the anatomical connection between the nasal cavity and brain without crossing the BBB. In this regard, dendrimers may possess great potential to deliver drugs to the brain by IN administration, bypassing the BBB and reducing systemic exposure and side effects, to treat diseases of the CNS. In this original concise review, we highlighted the few examples advocated regarding the use of dendrimers to deliver CNS drugs directly via IN. This review highlighed the few examples of the association of dendrimer encapsulating drugs ( e.g. , small compounds: haloperidol and paeonol; macromolecular compounds: dextran, insulin and calcitonin; and siRNA) using IN administration. Good efficiencies were observed. In addition, we will present the in vivo effects of PAMAM dendrimers after IN administration, globally, showing no general toxicity.

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A novel nasal almotriptan loaded solid lipid nanoparticles in mucoadhesive in situ gel formulation for brain targeting: Preparation, characterization and in vivo evaluation

Cited by 98 publications

References 73 publications

Intranasal Zotepine Nanosuspension: intended for improved brain distribution in rats

Intranasal Zotepine Nanosuspension: intended for improved brain distribution in rats

Preparation and detailed characterization of fusidic acid loaded in situ gel formulations for ophthalmic application

Non-invasive intranasal administration route directly to the brain using dendrimer nanoplatforms: An opportunity to develop new CNS drugs

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