Development of Donepezil Hydrochloride Loaded Gellan Gum Based Nasal Mucoadhesive Microspheres by Spray Drying Method

Gangane, Purushottam; Kawtikwar, Pravin

doi:10.5530/ijper.54.4.187

Cited by 9 publications

(4 citation statements)

References 16 publications

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“…Gangopathyay and co-workers evaluated the permeation of DPZ gel in ex vivo nasal mucosa from sheep, resulting in an increased permeation of DPZ [ 29 ]. High permeation was also observed by Gangane et al of DPZ microspheres gel in ex vivo goat and sheep nasal mucosa [ 30 , 31 ]. Patil R.P tested a gel of cubosomes containing DPZ administered intranasally to rats, and they studied the biodistribution of DPZ in brain tissue and plasma.…”

Section: Resultsmentioning

confidence: 72%

Comparative Study of Donepezil-Loaded Formulations for the Treatment of Alzheimer’s Disease by Nasal Administration

Espinoza

Guaya

Calpena

et al. 2022

Gels

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Alzheimer’s disease is characterized by a progressive deterioration of neurons resulting in a steady loss of cognitive functions and memory. Many treatments encounter the challenge of overcoming the blood–brain barrier, thus the intranasal route is a non-invasive effective alternative that enhances the drug delivery in the target organ–the brain–and reduces the side effects associated with systemic administration. This study aimed at developing intranasal gels of donepezil as an approach to Alzheimer’s disease. Three different gels were elaborated and characterized in terms of pH, morphology, gelation temperature, rheology, and swelling. An in vitro release study and an ex vivo permeation in porcine nasal mucosa were conducted on Franz diffusion cells. The tolerability of the formulations was determined by the cytotoxicity in human nasal cells RPMI 2650. Results showed that pluronic gels exhibit the higher release rate and enhanced permeation compared to chitosan gel. Moreover, the combination of Pluronic F-127 and Transcutol® P exerted a synergic effect on the permeation of donepezil through the nasal mucosa. The resulting gels showed suitable tolerance in the RPMI 2650 cell line and physicochemical characteristics for intranasal delivery, and thus gel formulations administered by nasal mucosa could be an alternative strategy to improve the bioavailability of donepezil.

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Section: Resultsmentioning

confidence: 72%

Comparative Study of Donepezil-Loaded Formulations for the Treatment of Alzheimer’s Disease by Nasal Administration

Espinoza

Guaya

Calpena

et al. 2022

Gels

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“…Gellan gum is an anionic deacetylated exo-cellular polysaccharide that undergoes in situ gelling in the presence of cations like Ca 2+ present in biological fluids and thus forms a three-dimensional network by complexation and hydrogen bonding with water [ 50 ]. Thus, addition of gellan gum enhance the contact between the formulation and the nasal mucosa resulting in longer nasal clearance time and prolonged residence time [ 24 , 51 , 52 ].…”

Section: Resultsmentioning

confidence: 99%

Ion-Triggered In Situ Gelling Nanoemulgel as a Platform for Nose-to-Brain Delivery of Small Lipophilic Molecules

et al. 2021

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Background: Intranasal route offers a direct nose-to-brain delivery via olfactory and trigeminal nerves and minimizes the systemic exposure of the drug. Although reliable and non-invasive, intranasal administration of lipophilic neuroprotective agents for brain targeting is still challenging. Literature focuses on naturally-derived compounds as a promising therapeutics for chronic brain diseases. Naringin, a natural flavonoid obtained from citrus fruits possesses neuroprotective effects. By regulating multiple crucial cellular signaling pathways, naringin acts on several therapeutic targets that make it suitable for the treatment of neurodegenerative diseases like Alzheimer’s disease and making it a suitable candidate for nasal administration. However, the hydrophobicity of naringin is the primary challenge to formulate it in an aqueous system for nasal administration. Method: We designed a lipid-based nanoemulsifying drug delivery system of naringin using Acrysol K140 as an oil, Tween 80 as a surfactant and Transcutol HP as a cosolvent, to improve solubility and harness the benefits of nanosizing like improved cellular penetration. Intranasal instillations of therapeutic agents have limited efficacy due to drug washout and inadequate adherence to the nasal mucosa. Therefore, we reconstituted the naringin self-emulsifying system in a smart, biodegradable, ion-triggered in situ gelling hydrogel and optimized for desirable gel characteristics. The naringin-loaded composition was optimized and characterized for various physicochemical and rheological properties. Results: The formulation showed a mean droplet size 152.03 ± 4.6 nm with a polydispersity index <0.23. Ex vivo transmucosal permeation kinetics of the developed formulation through sheep nasal mucosa showed sustained diffusion and enhanced steady-state flux and permeability coefficient. Scanning and transmission electron microscopy revealed the spherical shape of emulsion droplets and entrapment of droplets in a gel structure. The formulation showed excellent biocompatibility as analyzed from the viability of L929 fibroblast cells and nasal mucosa histopathology after treatment. In vivo biodistribution studies revealed significantly higher drug transport and brain targeting efficiency. Conclusion: In situ gelling system with nanoemulsified naringin demonstrated a safe nasal delivery providing a new dimension to the treatment of chronic neurodegenerative diseases using small hydrophobic phytoconstituents with minimization of dose and related systemic adverse effects.

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“…Glipizide is a good option for colonic medication administration because of its physicochemical qualities and short half-life. [10] To study the effect of solvents and polymer composition by emulsion solvent evaporation on various physicochemical parameters and release pattern, an attempt was made to develop microspheres using various organic solvents with synthetic and natural mucoadhesive polymers like eudragitRs100 and ethyl cellulose as a carrier polymer [11].…”

Section: Introductionmentioning

confidence: 99%

Study an effect of various orgainic solvents for preparation of glipizide mucoadhesive microspheres

Verma

Kumari

2022

ijhs

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Glipizide is a potent, rapid-acting with short duration of action and well tolerated second-generation sulfonylureas effective in reducing postprandial glucose level. However, if a dosage is missed before a meal, the risk of postprandial hypoglycemia and post-meal glucose excursions is always linked with the use of glipizide for the treatment of type 2 diabetes mellitus. Type 2 diabetes mellitus is a polygenic illness that includes both insulin secretion dysfunction and peripheral insulin resistance. (1)The study an effect of organic solvents preparation of glipizide controlled released mucoadhesive microspheres. (2)The microspheres were formulated conventional tremendous technique by emulsion solvent evaporation technique. (3) Mucoadhesive microspheres were evaluation parameters Examine by their impact on mucoadhesion, drug encapsulation efficacy (EE%), and in-vitro drug release. The produced microspheres were subjected to physical characterizations such as FTIR, DSC, particle analyzer, and SEM. Using cock stomach tissue, the ex-vivo mucoadhesive properties of the various orgainic solvents microspheres were studied. When compared to the other solvents microspheres employing, such as ethanol, methanol, acetone, glipizide loaded ethanol mucoadhesive microspheres had a higher EE percent (83.63±0.17%), a more sustained release profile over 10 hours, and superior adherence to cock stomach mucosa.

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Development of Donepezil Hydrochloride Loaded Gellan Gum Based Nasal Mucoadhesive Microspheres by Spray Drying Method

Cited by 9 publications

References 16 publications

Comparative Study of Donepezil-Loaded Formulations for the Treatment of Alzheimer’s Disease by Nasal Administration

Comparative Study of Donepezil-Loaded Formulations for the Treatment of Alzheimer’s Disease by Nasal Administration

Ion-Triggered In Situ Gelling Nanoemulgel as a Platform for Nose-to-Brain Delivery of Small Lipophilic Molecules

Study an effect of various orgainic solvents for preparation of glipizide mucoadhesive microspheres

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