Abstract
The aim of this work was to design and characterize a new nanovesicular nasal delivery system (NDS) containing buspirone, and investigate its efficiency in an animal model for the treatment of hot flushes. The presence of multilamellar vesicles with a mean size distribution of 370 nm was evidenced by transition electron microscopy (TEM), cryo-scanning electron microscopy (Cryo-SEM), and dynamic light scattering (DLS) tests. Pharmacodynamic evaluation of the nasal treatment efficacy with the new system was carried out in ovariectomized (OVX) rat—an animal model for hot flushes—and compared with other treatments. We found that the nasal administration of a buspirone NDS resulted in a significant reduction in tail skin temperature (TST). This effect was not observed in the control buspirone-treated groups. Buspirone levels in the plasma and brain of nasally-treated normal rats were quantified and compared with those of rats that had received oral administration by a LC-MS/MS assay. A significantly higher bioavailability was achieved with the new treatment relative to an oral administration of the same drug dose. No pathological changes in the nasal cavity were observed following sub-chronic nasal administration of buspirone NDS. In conclusion, the data of our investigation show that buspirone in the new nanovesicular nasal carrier could be considered for further studies for the development of a treatment for the hot flushes ailment.
Highlights
Most of therapeutic products for hot flushes are based on hormone therapy (HT), involving the administration of estrogen alone or in combination with progesterone
We reported that buspirone administrated in a transdermal system has efficiently treated hot flushes in an animal model [2]
To overcome the above drawbacks, we propose here the nasal administration of buspirone incorporated in a new nanovesicular delivery system (NDS) to be tested in a hot flushes animal model
Summary
Most of therapeutic products for hot flushes are based on hormone therapy (HT), involving the administration of estrogen alone or in combination with progesterone. We reported that buspirone administrated in a transdermal system has efficiently treated hot flushes in an animal model [2]. Buspirone—a 5-HT1A agonist—is currently administered orally and indicated for the treatment of generalized anxiety disorder (GAD). Buspirone HCl belongs to biopharmaceutics classification system (BCS) class I, being highly soluble and highly permeable. Oral administration of this drug is associated with low bioavailability: ~4% due to an extensive first-pass metabolism [3]. This centrally acting drug lacks the ability to penetrate the blood–brain barrier (BBB)
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