Study of excipients influence on the noopept releasing from the nasal dosage form
Keywords:noopept, releasing, nasal dosage form
The development of medicines for fast delivery is the actual direction of modern pharmacy. In this connection, the nasal route of drug administration is perspective and has some advantages. The greater permeability of nasal mucosa with large surface area affords a rapid onset of therapeutic effect. The nasal route circumvents hepatic first-pass elimination associated with oral delivery; it is easily accessible and suitable for a patient.
For the development of the new dosage form with nootropic and neuroprotective characteristics, the noopept was chosen. This substance has low toxicity, does not have any side effects, is characterized by the anti-oxidant and anti-inflammatory activity, decreases the calcium and glutamate neurotoxicity, improves rheological properties of blood.
The aim of work is the determination of excipients' influence on the noopept releasing from the nasal dosage form.
Materials and methods. For the investigation, the basic groups of excipients for the development of nasal dosage form were chosen: mucoadhesives and viscosity modifiers (polymers) and humectants (alcohols). Noopept releasing was studied using equilibrium dialysis by Kruvchinsky at 37 ± 0.5 °С through the semipermeable membrane – cellophane film “Kuprofan”. Noopept concentration after 30 minutes was determined by the U –spectrophotometry at 258 nm.
Results. According to the results of the carried out variance analysis, it was determined that for both factors Fexperim. > Ftabl., so the polymers and alcohols have a significant influence on the noopept releasing from the nasal dosage forms. After verification of average results of significant factors by the Dunkan’s multiple rank test the next preferred series was built: sodium carboxymethylcellulose (chitosan) > sodium alginate (sodium hyaluronate); glycerol > sorbit > D-panthenol (without alcohol).
Conclusions. It was determined that sort of polymer of hydrophilic bases and alcohols for moistening mucous membrane has a significant influence on noopept releasing from the nasal dosage forms. Sodium carboxymethylcellulose and chitosan with addition of glycerol provide with the optimal noopept releasing.
Bhise, S. B., Yadav, A. V., Avachat, A. M., & Malayandi, R. (2008). Bioavailability of intranasal drug delivery system. Asian Journal of Pharmaceutics, 2(4), 201-215.
Hanson, L., & Frey, W. (2007). Strategies for intranasal delivery of therapeutics for the prevention and treatment of neuroAIDS. Journal Of Neuroimmune Pharmacology, 2(1), 81-86. doi: 10.1007/s11481-006-9039-x
Kushwaha, S. K. S., Keshari, R. K., & Rai, A K. (2011). Advances in nasal trans-mucosal drug delivery. Journal of Applied Pharmaceutical Science, 1(7), 21-28.
Ostrovskaya, R. U., Gudasheva, T. A., Voronina, T. A., & Seredenin, S. B. (2002). Originalniy nootropniy i nejroprotectivniy preparat noopept [Noopept as original nootropic and neuroprotective drug]. Experimentalnaya i clinicheskaya farmakologija, 65(5), 66-72. doi: 10.30906/0869-2092-2002-65-5-66-72 [in Russian].
Pelsman, A., Hoyo-Vadillo, C., Gudasheva, T., Seredenin, S., Ostrovskaya, R., & Busciglio, J. (2003). GVS-111 prevents oxidative damage and apoptosis in normal and Down’s syndrome human cortical neurons. International Journal Of Developmental Neuroscience, 21(3). 117-141. doi: 10.1016/s0736-5748(03)00031-5
Bukanova, J., Solntseva, E., & Skrebitsky, V. (2002). Selective suppression of the slow-inactivating potassium currents by nootropics in molluscan neurons. The International Journal Of Neuropsychopharmacology, 5(03), 229-266. doi: 10.1017/s1461145702002997
Amelin, A. V., Ilyuchyna, A. U., & Shmonin, A. A. (2011). Noopept v lechenii umerennych kognitivnyh narushenij u pacientov s ishemicheskim insultom [Noopept in treating moderate cognitive impairments in ischemic stroke patients]. Zh Nevrol Psikhiatr Im SS Korsakova, 111(10), 44-46. [in Russian].
Prajapati, N., Srivastava, P., & Bhargava, S. (2012). Recent advances in nasal drug delivery using natural polymers. Current Drug Therapy, 7(3), 170-178. doi: 10.2174/157488512803988076
Hroshovyi, T. A., Martseniuk, V. P., Kucherenko, L. I., & Vronska, L. P. (2008). Matematychne planuvannia eksperymentu pry provedenni naukovykh doslidzhen v farmatsii [Mathematical planning of experiment when conducting scientific research in pharmacy]. Ternopil: TDMU. [in Ukrainian].
Antypenko, L., Burlaka, B., Belenichev, I. (2016). Noopept: development and validation of a UV-Vis spectrophotometric method for the quantification of (S)-N-phenylacetyl-L-prolylglycine ethyl ester in bulk drug substance. Pharmakeftiki, 28 (4), 161-169.
How to Cite
Authors who publish with this journal agree to the following terms:
- Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution License that allows others to share the work with an acknowledgement of the work's authorship and initial publication in this journal.
- Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgement of its initial publication in this journal.
- Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (See The Effect of Open Access)