Next Article in Journal
Investigations Concerning the Residence Time Distribution of Twin-Screw-Extrusion Processes as Indicator for Inherent Mixing
Next Article in Special Issue
A Tailored Thermosensitive PLGA-PEG-PLGA/Emulsomes Composite for Enhanced Oxcarbazepine Brain Delivery via the Nasal Route
Previous Article in Journal
Targeted Nanomedicine to Treat Bone Metastasis
Previous Article in Special Issue
Hydrophobic Amino Acid Tryptophan Shows Promise as a Potential Absorption Enhancer for Oral Delivery of Biopharmaceuticals
Due to scheduled maintenance work on our core network, there may be short service disruptions on this website between 16:00 and 16:30 CEST on September 25th.
Article

The Role of Combined Penetration Enhancers in Nasal Microspheres on In Vivo Drug Bioavailability

1
Department of Chemistry and Pharmacy, University of Sassari, via Muroni 23/a, 07100 Sassari, Italy
2
Department of Life Sciences and Biotechnology, University of Ferrara, via Borsari 46, 44121 Ferrara, Italy
3
Department of Biomedical and Specialist Surgical Sciences, University of Ferrara, via Borsari 46, 44121 Ferrara, Italy
4
Department of Chemical and Pharmaceutical Sciences, University of Ferrara, via Fossato di Mortara 19, 44121 Ferrara, Italy
*
Author to whom correspondence should be addressed.
Received: 21 September 2018 / Revised: 22 October 2018 / Accepted: 23 October 2018 / Published: 26 October 2018
(This article belongs to the Special Issue Transmucosal Absorption Enhancers in the Drug Delivery Field)
Microspheres based on both methyl-β-cyclodextrins and chitosan were prepared by spray-drying as nasal formulations of a model polar drug to analyze, firstly, how the composition of the carrier affects drug permeation across synthetic membranes and, secondly, how it induces systemic or brain delivery of the drug. Microparticles with different weight ratios of the two penetration enhancers (10–90, 50–50, 90–10) were characterized with respect to morphology, size, structural composition, water uptake, and the in vitro drug permeation profile. The leader formulation (weight ratio of 50–50) was then nasally administered to rats; systemic and cerebrospinal fluid (CSF) drug concentrations were analyzed by high performance liquid chromatography (HPLC) over time. Microspheres obtained with a single enhancer, methyl-β-cyclodextrins or chitosan, were administered in vivo as a comparison. The in vitro properties of combined microspheres appeared modified with regard to the polymeric matrix ratio. In vivo results suggest that the optimal drug distribution between CSF and bloodstream can be easily obtained by varying the amount of these two penetration enhancers studied in the matrix of nasal microspheres. View Full-Text
Keywords: combined microsphere; chitosan; cyclodextrin; nasal delivery; nose to brain transport; penetration enhancer; nasal formulation; in vivo studies combined microsphere; chitosan; cyclodextrin; nasal delivery; nose to brain transport; penetration enhancer; nasal formulation; in vivo studies
Show Figures

Graphical abstract

MDPI and ACS Style

Rassu, G.; Ferraro, L.; Pavan, B.; Giunchedi, P.; Gavini, E.; Dalpiaz, A. The Role of Combined Penetration Enhancers in Nasal Microspheres on In Vivo Drug Bioavailability. Pharmaceutics 2018, 10, 206. https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics10040206

AMA Style

Rassu G, Ferraro L, Pavan B, Giunchedi P, Gavini E, Dalpiaz A. The Role of Combined Penetration Enhancers in Nasal Microspheres on In Vivo Drug Bioavailability. Pharmaceutics. 2018; 10(4):206. https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics10040206

Chicago/Turabian Style

Rassu, Giovanna, Luca Ferraro, Barbara Pavan, Paolo Giunchedi, Elisabetta Gavini, and Alessandro Dalpiaz. 2018. "The Role of Combined Penetration Enhancers in Nasal Microspheres on In Vivo Drug Bioavailability" Pharmaceutics 10, no. 4: 206. https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics10040206

Find Other Styles
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop