Formulation and evaluation of nasal insert for nose-to-brain drug delivery of rivastigmine tartrate

Shaghlil, Lena; Alshishani, Anas; Sa'aleek, Asmaa Abu; Abdalkader, Hamdy; Al-ebini, Yousef

doi:10.1016/j.jddst.2022.103736

Cited by 10 publications

(5 citation statements)

References 49 publications

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“…To reveal any cytotoxic effect of the optimized ZP-loaded NLCs (NLC-OP) as any sign of alteration or pathological damage to the nasal mucosa, an ex vivo cytotoxicity study was conducted. Isolated sheep nasal mucosa is believed to have a morphology and histology almost identical to human nasal mucosa ( Shaghlil et al, 2022 ). Thus, a 2-year-old sheep's head was obtained from a nearby slaughterhouse.…”

Section: Methodsmentioning

confidence: 99%

Cod liver oil nano-structured lipid carriers (Cod-NLCs) as a promising platform for nose to brain delivery: Preparation, in vitro optimization, ex vivo cytotoxicity & in vivo biodistribution utilizing radioiodinated zopiclone

Taha

Nour

Mamdouh

et al. 2023

International Journal of Pharmaceutics: X

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Section: Methodsmentioning

confidence: 99%

Cod liver oil nano-structured lipid carriers (Cod-NLCs) as a promising platform for nose to brain delivery: Preparation, in vitro optimization, ex vivo cytotoxicity & in vivo biodistribution utilizing radioiodinated zopiclone

Taha

Nour

Mamdouh

et al. 2023

International Journal of Pharmaceutics: X

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“…To understand the dissolution mechanisms from M3, the released data were fitted also using Korsmeyer-Peppas model. Anomalous transport is characterized by a release exponent value, n, that is between 0.5 and 1.0, indicating that the drug release is controlled by both the drug diffusion and other mechanisms [80,81]. The release exponent was found to be 0.96, and 0.99 respectively for AA and CAFF which implies that the drug release from the system follow anomalous (non-Fickian transport).…”

Section: Drug Release Kineticsmentioning

confidence: 94%

Development and Evaluation of an Innovative Approach Using Niosomes Based Polymeric Microneedles to Deliver Dual Antioxidant Drugs

et al. 2023

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Ascorbic acid (AA) and caffeine (CAFF) work to protect cells from ultraviolet (UV) radiation and slow down the photoaging process of the skin. However, cosmetic application of AA and CAFF is limited due to poor penetration across the skin and rapid oxidation of AA. The aim of this study was to design and evaluate the dermal delivery of dual antioxidants utilizing microneedles (MNs) loaded with AA and CAFF niosomes. The niosomal nanovesicles were prepared using the thin film method and had particle sizes ranging from 130.6–411.2 nm and a negative Zeta potential of around −35 mV. The niosomal formulation was then combined with polyvinylpyrrolidone (PVP) and polyethylene glycol 400 (PEG 400) to create an aqueous polymer solution. The best skin deposition of AA and CAFF was achieved with the formulation containing 5% PEG 400 (M3) and PVP. Furthermore, the role of AA and CAFF as antioxidants in preventing cancer formation has been well-established. Here we validated the antioxidant properties of ascorbic acid (AA) and caffeine (CAFF) in a novel niosomal formulation referred to as M3 by testing its ability to prevent H2O2-indued cell damage and apoptosis in MCF-7 breast cancer cells. Results showed that M3 was able to shield MCF-7 cells from H2O2 induced damage at concentrations below 2.1 µg/mL for AA and 1.05 µg/mL for CAFF, and also exhibited anticancer effects at higher concentrations of 210 µg/mL for AA and 105 µg/mL. The formulations were stable for two months at room temperature in terms of moisture and drug content. The use of MNs and niosomal carriers could be a promising approach for dermal delivery of hydrophilic drugs like AA and CAFF.

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“…The PH of the obtained gel solution was measured and adjusted with tri-ethanolamine to be maintained at PH = 5.5. Gel solution containing 12 mg/mL atomoxetine base was transferred to 1.5 mL Eppendorf tubes and freeze dried for 24 h using a Virtis Advantage freeze drier (Virtis, New York, NY, USA), with pre-set cycle stages; freezing) for 8 h, reducing temperature from −30 to −60 °C in 10 °C increments), primary drying (18 h increasing temperature from 10 to 22 °C in 5 °C increments, with chamber pressure decreasing from 100 to 40 mTorr) [ 18 , 61 , 62 ].…”

Section: Methodsmentioning

confidence: 99%

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

et al. 2023

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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.

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Formulation and evaluation of nasal insert for nose-to-brain drug delivery of rivastigmine tartrate

Cited by 10 publications

References 49 publications

Cod liver oil nano-structured lipid carriers (Cod-NLCs) as a promising platform for nose to brain delivery: Preparation, in vitro optimization, ex vivo cytotoxicity & in vivo biodistribution utilizing radioiodinated zopiclone

Cod liver oil nano-structured lipid carriers (Cod-NLCs) as a promising platform for nose to brain delivery: Preparation, in vitro optimization, ex vivo cytotoxicity & in vivo biodistribution utilizing radioiodinated zopiclone

Development and Evaluation of an Innovative Approach Using Niosomes Based Polymeric Microneedles to Deliver Dual Antioxidant Drugs

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

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