Abstract

MUNOZ-CERNADA, Adriana; FERNANDEZ-CERVERA, Mirna  and  GARCIA-RODRIGUEZ, Julio César. Factors involved in the design of nasal delivery systems for peptides and proteins. Biotecnol Apl [online]. 2013, vol.30, n.2, pp.88-96. ISSN 1027-2852.

Because the nasal mucous is one of the most permeable areas, the intranasal delivery route is the most promising for proteins and peptides to reach the central nervous system (CNS). Nevertheless certain aspects of these macromolecules limit their bioavailability, such as molecular weight, the rapid mucociliary clearance mechanism and enzymatic degradation. This paper critically summarizes the factors participating in the design of systems for the nasal delivery of peptides and proteins. The physicochemical properties of the biomolecules and features of the formulation design that directly influence their bioavailablity and stability are presented. Pharmaceutical aspects include an analysis of the influence of excipients that act as stabilizers, antimicrobial preservatives, absorption enhancers, and bioadhesive polymers as well as the administration device. The use of molecules involved in endogenous neuroprotection administered intranasally is a recent proposal in the development of new drugs. Neurotrophic factors, interferon beta-1b, erithropietin (i.e.: rH-EPO, Neuro-EPO) and insulin, are among the biotechnology products administered intranasally. These new products show greater therapeutic potential as putative neuroprotectors in neurological diseases, both for treatment during the acute phase, and for the chronic stage.

Keywords : intranasal delivery; peptides; proteins; excipients; formulation; neuroprotection.

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