Carbamazepine Mucoadhesive Nanoemulgel (MNEG)asbrain targeting delivery system via the olfactory mucosa

Abstract

Carbamazepine (CBZ) is an antiepileptic orally administered drug, but due to its low solubility in water, its gastrointestinal absorption is slow and irregular, leading to delayed brain uptake with consequent peripheral side actions. The objective of this study was the brain targeting of CBZ via the olfactory mucosa in form of an intranasal mucoadhesive o/w nanoemulgel (MNEG). CBZ was formulated in a nanoemulgel system containing oleic acid/labrasol in a ratio of 1:5 as oil/surfactant and 0.1% xanthan gum as anionic mucoadhesive polymer. The prepared MNEG was characterized with respect to oil droplet size, mucoadhesion, in-vitro release of the drug and CBZ uptake by phosphatidylcoline liposomes as an in-vitro model for olfactory cells. The anticonvulsant action of nasal MNEG was studied on chemically and electrically induced convulsive Swiss Albino mice. The in-vitro release of CBZ from MNEG was very low, however CBZ uptake via liposomal membrane reached 65% within 1 hr. Treatment of animals with MNEG significantly prolonged the onset times for convulsion of chemically convulsive mice and protected the animals from two electric shocks. One can thus spire and hope for the emergence of a new intranasal treatment of epilepsy with consequent decrease in the peripheral side actions of CBZ.

Nose to brain microemulsion-based drug delivery system of rivastigmine: formulation and ex-vivo characterization

“…From Figure 9, it was revealed that the percentage drug diffused was highest in case of CH-ME when compared to CTAB-ME, ME and DS. All formulations showed sustained release for RHT, which can be explained by the fact that the diffusion of RHT from the oily core and interface is hindered by the aqueous medium, which acts as a barrier to drug transport (Samia et al, 2012). It was concluded that the extent of RHT diffused from MMEs was greater than ME and DS.…”

“…Ingredients (% w/w) ME CH-ME CTAB-ME adsorb on the holey film grid and observed after drying (Samia et al, 2012). Contact angle measurement: An instrument called optical contact angle (15 Pro, Data Physics, Germany) with an inbuilt facility for imaging and having fixed syringe (Hamilton 500 ml) with an outer needle diameter of 0.52 mm was used to determine the contact angle between a drop of ME and MME using suitable surface mimicking nasal mucosa (flat piece of goat nasal mucosa of 0.4 mm thickness).…”

Pharmacoresistant epilepsy and nanotechnology

“…Eskandari et al (116) described that the anticonvulsant effect of valproic acid is augmented when it is applied by intranasal route using nanostructured lipid carriers. Using the maximal electroshock model, Nair et al (117) reported that the anticonvulsant effect induced by oral administration of carbamazepine is increased when the drug is loaded in solid lipid nanoparticles of chitosan. Yusuf et al (118) described that the anticonvulsant effect of β-carotene in acute experimental models of seizures is improved when it is encapsulated in nanoparticles of poly(d,l-lactide-coglycolide), an effect that is more effective when the nanoparticles are coated with polysorbate-80.…”

Nanomedicine in Central Nervous System (CNS) Disorders: A Present and Future Prospective

“…189 Carbamazepine loaded solid lipid nanoparticles of chitosan reported to be more effective than nano emulged loaded carbamazepine. 190 Similarly, poly (d,l-lactide-co-glycolide) nanoparticle loaded β-carotene anticonvulsant considered more effective when it coated with polysorbate-80. 191 …”