Sublingual drug delivery allows systemic delivery of drug without difficulties connected with the gastrointestinal pathway. We developed a new simple protocol for easy-to-use processing and storage of porcine sublingual mucosal membrane for in vitro studies using "flash freezing" in liquid nitrogen. All the dextrans used as mucosal membrane integrity and permeability markers permeated only slowly through sublingual mucosa illustrating usability both the "fresh" and "flash frozen" sublingual membranes whereas conventional cold storage "frozen" membranes have shown significantly higher permeabilities for macromolecules due to the sustained damage. The permeability values were too low to expect dextrans to be potential carriers at this context. To test albumin as a drug carrier we compared FITC-albumin permeation from solutions vs. nanofiber mats donors. To increase the amounts and prolong the transport, we manufactured nanofiber mats loaded with fluorescently marked albumin using well-scalable electrospinning technology. Nanofiber mats have allowed albumin passage through the sublingual membrane in similar amounts as from the pure artificial saliva solution. Since salivary washout strictly limits the duration of liquid dosages, nanofiber mats may thus permit prolonged sublingual administration.
- MeSH
- albuminy aplikace a dávkování MeSH
- aplikace sublinguální MeSH
- dextrany aplikace a dávkování MeSH
- fluorescein-5-isothiokyanát aplikace a dávkování analogy a deriváty MeSH
- kofein aplikace a dávkování MeSH
- nanovlákna aplikace a dávkování MeSH
- permeabilita MeSH
- prasata MeSH
- roztoky MeSH
- sliznice anatomie a histologie metabolismus MeSH
- systémy cílené aplikace léků * MeSH
- zmrazování MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
A considerable obstacle of the real nanofiber use in drug dosage forms consists in the low weight of the doses and in the content non-uniformity of medicated nanofiber products, especially of those manufactured on a large scale. The electrospinning nanofiber technology is the most promising in this context; however, no results obtained by validated production have been published so far. Here we present the results of the validation study of electrospun medicated strips intended for administration of rizatriptan as a drug medicated in milligrams per dose. The results obtained demonstrate a compliance with the good manufacturing practice and pharmacopoeial requirements on weight and content uniformity. We have concluded that the tested Nanospider™ electrospinning technology is validable and thus suitable for a wide number of drugs intended for single-dose administration of small drug quantities.
- Publikační typ
- abstrakt z konference MeSH
- MeSH
- chronická nemoc MeSH
- hojení ran * MeSH
- kočky MeSH
- koně MeSH
- nemoci nohy (od hlezna dolů) terapie veterinární MeSH
- otitis externa terapie veterinární MeSH
- plazmové plyny * terapeutické užití MeSH
- pododermatitida terapie MeSH
- psi MeSH
- výsledek terapie MeSH
- zánět terapie veterinární MeSH
- zvířata MeSH
- Check Tag
- kočky MeSH
- psi MeSH
- zvířata MeSH
- Publikační typ
- kazuistiky MeSH
- práce podpořená grantem MeSH
- Publikační typ
- abstrakt z konference MeSH
- Publikační typ
- abstrakt z konference MeSH
A nanofibrous membrane carrier for nearly water insoluble drug diosmin was formulated. The aim of this study was to evaluate the drug release and dissolution properties in an aqueous buffer of pH 7.8, and to compare the suitability of the drug carrier with the available drug forms and screen diosmin absorption extent. The membranes were produced from HPC/PVA/PEO-drug water solutions and then evaluated by SEM and DSC measurements. The results showed that diosmin was incorporated within the nanofibers in an amorphous state, and/or as a solid dispersion. The results of in vitro release experiments excerpt a very fast release of the drug, followed by the formation of an over saturated solution and partial precipitation of the drug (a "spring" effect). The enormous increases in dissolution of the drug from a nanofibrous carrier, compared to a micronized and crystalline form, was achieved. The in vivo bioavailability study carried out on rats showed higher initial drug plasma levels and higher AUC values after administration of the nanofibrous drug formulation, compared to the micronized form. The results of the study demonstrated that the improvement of the diosmin in vitro dissolution also brought the enhanced in vivo absorption extent of the drug.
- MeSH
- aplikace orální MeSH
- diosmin aplikace a dávkování krev chemie farmakokinetika MeSH
- intestinální absorpce MeSH
- nanovlákna aplikace a dávkování chemie MeSH
- nosiče léků aplikace a dávkování chemie farmakokinetika MeSH
- potkani Wistar MeSH
- příprava léků metody MeSH
- rozpustnost MeSH
- roztoky MeSH
- zvířata MeSH
- Check Tag
- mužské pohlaví MeSH
- ženské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Publikační typ
- abstrakt z konference MeSH
- Publikační typ
- abstrakt z konference MeSH