Oxidized Alginate Dopamine Conjugate: In Vitro Characterization for Nose-to-Brain Delivery Application

Abstract

Background: The blood–brain barrier (BBB) bypass of dopamine (DA) is still a challenge for supplying it to the neurons of Substantia Nigra mainly affected by Parkinson disease. DA prodrugs have been studied to cross the BBB, overcoming the limitations of DA hydrophilicity. Therefore, the aim of this work is the synthesis and preliminary characterization of an oxidized alginate-dopamine (AlgOX-DA) conjugate conceived for DA nose-to-brain delivery. Methods: A Schiff base was designed to connect oxidized polymeric backbone to DA and both AlgOX and AlgOX-DA were characterized in terms of Raman, XPS, FT-IR, and 1H- NMR spectroscopies, as well as in vitro mucoadhesive and release tests. Results: Data demonstrated that AlgOX-DA was the most mucoadhesive material among the tested ones and it released the neurotransmitter in simulated nasal fluid and in low amounts in phosphate buffer saline. Results also demonstrated the capability of scanning near-field optical microscopy to study the structural and fluorescence properties of AlgOX, fluorescently labeled with fluorescein isothiocyanate microstructures. Interestingly, in SH-SY5Y neuroblastoma cell line up to 100 μg/mL, no toxic effect was derived from AlgOX and AlgOX-DA in 24 h. Conclusions: Overall, the in vitro performances of AlgOX and AlgOX-DA conjugates seem to encourage further ex vivo and in vivo studies in view of nose-to-brain administration.

Antibacterial Biodegradable Films Based on Alginate with Silver Nanoparticles and Lemongrass Essential Oil–Innovative Packaging for Cheese

“…Mechanical properties are enhanced by adding plasticizers, glycerol being the most common choice due to its superior compatibility with the polymeric matrix [27,28]. Antibacterial activity can be bestowed to the alginate by adding various nanoparticles such as ZnO [29], Ag [30], CuO [31], natural extracts [32][33][34], or other substances of pharmaceutical interest [35][36][37].…”

Recent Advances in Mucoadhesive Interface Materials, Mucoadhesion Characterization, and Technologies

“…Note that η b may decrease with increasing shear rate hence it is recommended to measure the viscosity coefficients at high shear rates. Figure 7 shows viscosity coefficient measurements for three representative mucoadhesive polymers (bovine serum albumin, BSA, chitosan, and polyacrylic acid, PAA) against mucin at pH 1 and Chitosan-dopamine/chitosan-tyrosine Polymerization/conjugation in solvents In vitro evaluation of mucoadhesion Nose-to-brain delivery [112] Oxidized alginate/dopamine Conjugation in ethanol/water mix In vitro drug release Nose-to-brain delivery [113] Poly(vinyl alcohol) (PVA)/dopamine Polymerization/conjugation in solvents at high T…”

Alginate as a Promising Biopolymer in Drug Delivery and Wound Healing: A Review of the State-of-the-Art

“…The recent nasal formulations include SA/Polaxomer 407/gellan gum/timosaponin BII [ 231 ], SA in situ gels based on agomelatine (AGM) [ 232 ], ALG based magnetic short nanofibres 3D composite hydrogel encapsulating human olfactory mucosa stem cells [ 233 ], OA-dopamine conjugate [ 234 ], ALG nanoparticles/venlafaxine (VLF-AG-NPs) [ 235 ], Mycobacterium bovis Bacille Calmette-Guérin (BCG)-loaded microparticles using ALG/CS [ 236 ], ALG/CS/attenuated Androctonus australis hector (Aah) venom [ 237 ], CS/ALG nanoparticles/SpBMP-9 (growth factor) [ 238 ], ALG/trimethyl CS liposomes/lipopeptide subunit vaccine [ 239 ], SA microspheres/ Lactobacillus casei [ 240 ].…”