Nose-to-brain delivery: A comparative study between carboxymethyl chitosan based conjugates of dopamine

Novel Nanoparticles Based on N,O-Carboxymethyl Chitosan-Dopamine Amide Conjugate for Nose-to-Brain Delivery

“…The quantitative determination of DA was carried out by HPLC as previously reported [30] using 0.02 M potassium phosphate buffer, pH 2.8: CH 3 OH 70:30 (v:v) as mobile phase and the elution of the column in isocratic mode took place at the flow rate of 0.7 mL/min. Under such chromatographic conditions, the retention times of DA and N,O-CMCS-DA were 5.5 min and 4.9 min, respectively [30].…”

“…In order to offer several advantages including enhanced drug solubilisation, prolonged circulation and improved mucoadhesive properties, polymer-drug conjugates can be nanostructured leading to polymeric nanoparticles which may be able to cross the BBB by endocytosis [27,28]. Our interest in using chitosan and its derivatives as biopolymers for DRS by pharmacological approaches [21,22] led us to evaluate N,O-Carboxymethyl chitosan-DA conjugates where the polymeric chain is linked to the neurotransmitter moiety by a cleavable ester or amide bond [29,30].…”

“…The aim of the present work was to prepare novel nanoparticles (NPs) based on N,O-Carboxymethyl chitosan-DA amide conjugate (N,O-CMCS-DA) [30] and to evaluate their potential for nose-to-brain delivery of DA to be administered as such or formulated by using an appropriate biomaterial [1,18]. It is now recognized, indeed, that the use of biomaterials to deliver drugs for the treatment of neurological disorders, as PD, is favourable because they can allow appropriate release kinetics or prevents degradation of the therapeutic agent [1,18].…”

“…Carbohydrates, as chitosan and its derivatives, indeed, have received considerable attention for brain delivery due to their natural origin, inherent biodegradability and biocompatibility. The feasibility of using carbohydrate-based DDS in brain delivery has been demonstrated both with oligomeric as well as polymeric carbohydrates [30,34]. For the purpose mentioned, N,O-CMCS-DA NPs were successfully prepared by nanoprecipitation method starting from the N,O-CMCS-DA amide conjugate [30].…”

“…The feasibility of using carbohydrate-based DDS in brain delivery has been demonstrated both with oligomeric as well as polymeric carbohydrates [30,34]. For the purpose mentioned, N,O-CMCS-DA NPs were successfully prepared by nanoprecipitation method starting from the N,O-CMCS-DA amide conjugate [30]. These nanocarriers were characterized from a technological viewpoint including their internal structure, thermal stability, surface features, release profile and physical stability.…”