Vía intranasal: una alternativa para la administración de fármacos de acción central en equinos

Ferreira, Violeta; Velloso, María Inés; Vita, Mariangeles; Landoni, M. F.

doi:10.24215/15142590e033

Cited by 2 publications

(2 citation statements)

References 31 publications

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“…Brain drug delivery is reduced by blood-brain-barrier, nevertheless, intranasal administration allows to avoid it, so the drug let into brain by direct and non-invasive path. This quality is profitable for the administration of drugs whose site of action is inside the central nervous system such as butorphanol (Velloso et al, 2019). Butorphanol is used in horses to treat superficial and visceral pain (Ferreira et al, 2019).…”

Section: Discussionmentioning

confidence: 99%

Effect of two surfactants on in vitro permeation of butorphanol through horse nasal mucosa

2021

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The aim of the present study was to evaluate the effect of two surfactants on in vitro permeation of butorphanol through equine nasal mucosa. Franz diffusion cells and equine nasal mucosa were used. Three formulations were developed based on citric acid, sodium citrate, sodium chloride, and butorphanol tartrate and administered at a 24.4 g cm-3 dose. Control formulation lacked any penetration enhancer. Formulation 1 (F1) had a cationic surfactant (cetrimonium bromide) and formulation 2 (F2) had a non-ionic surfactant (Tween 80). Statistically comparing flux values at the steady state (Jss), apparent permeability coefficient (Kp), and lag-time from control, F1 and F2 for the respiratory region does not show statistically significant differences (α= 0.05). However, statistically significant differences were found on the Jss and Kp, values from control, F1, and F2 in olfactory mucosa. A statistical analysis on the latter showed significant differences between the Jss values of F1 and F2 and between control and F2. Based on this, Tween 80 proved to be a promising excipient in developing intranasal butorphanol formulations in equines since it increases its passage through the nasal mucosa. These results are very promising to continue with the development of intranasal butorphanol formulation in equines.

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Section: Discussionmentioning

confidence: 99%

Effect of two surfactants on in vitro permeation of butorphanol through horse nasal mucosa

2021

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“…Some changes have been used to improve lipophilicity and absorption through the passive diffusion pathway, such as blocking the C-terminal by cyclization, amide production, or esterification of proteins. 94 Although the octanol–water partition coefficient is a simple metric that can predict mucosal permeability, it does not necessarily correlate with peptide absorption since peptide bioavailability changes parabolically with lipophilicity. 95 …”

Section: Gridlocks To Oral Delivery Of Therapeutic Peptides and Proteinsmentioning

confidence: 99%

Recent progress in the oral delivery of therapeutic peptides and proteins: Overview of pharmaceutical strategies to overcome absorption hurdles

Mehrotra,

Kalyan BG,

Nayak

et al. 2023

Adv Pharm Bull

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Objective: This review aims to critically examine and summarize the innovations and mechanisms involved in oral delivery of peptide and protein drugs. Significance: Proteins and peptides have secured a place as excellent therapeutic moieties on account of their high selectivity and efficacy. However due to oral absorption limitations, current formulations are mostly delivered parenterally. Oral delivery of peptides and proteins can be considered the need of the hour due to the immense benefits of this route. Methods: Comprehensive literature search was undertaken, spanning the early development to the current state of the art, using online search tools (PubMed, Google Scholar, ScienceDirect and Scopus). Results: Research in oral delivery of proteins and peptides has a long and rich history and the development of biologics has encouraged additional research effort in recent decades. Enzyme hydrolysis and inadequate permeation into intestinal mucosa are the major causes that result in limited oral absorption of biologics. Pharmaceutical and technological strategies including use of absorption enhancers, enzyme inhibition, chemical modification (PEGlyation, pro-drug approach, peptidomimetics, glycosylation), particulate delivery (polymeric nanoparticles, liposomes, micelles, microspheres), site-specific delivery in the GIT, membrane transporters, novel approaches (self-nanoemulsifying drug delivery systems, Eligen technology, peptelligence, self-assembling bubble carrier approach, luminal unfolding microneedle injector, microneedles) and lymphatic targeting, are discussed. Limitations of these strategies and future innovations for improving oral bioavailability of protein and peptide drugs are also discussed. Conclusion: This review underlines the application of oral route for peptide and protein delivery, which can direct the formulation scientist for better exploitation of this route.

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Vía intranasal: una alternativa para la administración de fármacos de acción central en equinos

Cited by 2 publications

References 31 publications

Effect of two surfactants on in vitro permeation of butorphanol through horse nasal mucosa

Effect of two surfactants on in vitro permeation of butorphanol through horse nasal mucosa

Recent progress in the oral delivery of therapeutic peptides and proteins: Overview of pharmaceutical strategies to overcome absorption hurdles

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